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Scientific Article   |    
Bone Morphogenetic Protein-7 Modulates Genes that Maintain the Vascular Smooth Muscle Cell Phenotype in Culture
Haimanti Dorai, PhD; T Kuber Sampath, PhD
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Investigation performed at Creative BioMolecules Inc., Hopkinton, Massachusetts
Haimanti Dorai, PhD T. Kuber Sampath, PhD Curis Inc, 21 Erie Street, Cambridge, MA 02139. E-mail adddress for H. Dorai: hdorai@curis.comThe authors did not receive grants or outside funding in support of their research or preparation of this manuscript. One or more of the authors received payments or other benefits or a commitment or agreement to provide such benefits from a commercial entity (Creative Biomolecule) No commercial entity paid or directed, or agreed to pay or direct, any benefits to any research fund, foundation, educational institution, or other charitable or nonprofit organization with which the authors are affiliated or associated.

The Journal of Bone & Joint Surgery.  2001; 83:S70-S78 
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Abstract

Background: The vasculature is an important component in the musculoskeletal system, and vascularization is a key event in the development of normal cartilage and bone formation. Blood vessels deliver nutrients, oxygen, and precursor cells to maintain the structural and functional integrity of joints and soft and hard tissues. Therefore, agents that help to inhibit proliferation and retain the phenotype of vascular smooth muscle cells (SMCs) are of critical importance. In this study, we examined the capacity of bone morphogenetic protein-7 (BMP-7) to inhibit the proliferation of SMCs and maintain their phenotype.

Methods: A thymidine-incorporation assay was used to monitor the proliferative activity of SMCs on stimulation with platelet-derived growth factor (PDGF) and transforming growth factor-beta (TGF-ß), agents known to be stimulatory for these cells. Reverse transcriptase-polymerase chain reaction (RT-PCR), Northern blot analysis, and enzyme-linked immunosorbent assay (ELISA) were used to monitor the modulation of various genes and gene products. Immunolocalization of SMC specific markers was also performed.

Results: BMP-7 inhibited both serum-stimulated and growth factor-induced (PDGF-BB and TGF-ß1) SMC growth, as measured by 3 H-thymidine uptake and cell number, in primary human aortic smooth muscle (HASM) cell cultures. The addition of BMP-7 stimulated the expression of developmentally regulated as well as SMC-specific markers, namely, Id-1 and Id-2, a-actin, and SMC-specific heavy-chain myosin, as examined by semiquantitative and quantitative RT-PCR and by Northern blot analysis. Additionally, BMP-7 exhibited anti-inflammatory activity by downregulating intercellular adhesion molecule-1 (ICAM-1) expression. The collagen type III/I ratio that becomes lower with the transdifferentiation of SMCs into myofibroblasts is maintained in BMP-7-treated cultures compared with untreated controls. Studies on the mechanism of action indicate that BMP-7 treatment induces cyclin-dependent kinase-2 inhibitor, p21, which was inhibited during PDGF-BB-induced proliferation of SMCs. Finally, BMP-7 upregulates the expression of the inhibitory Smads, Smad6 and Smad7, which are known to inhibit TGF-ß superfamily signaling.

Conclusions: These results suggest that BMP-7 maintains the expression of the vascular SMC phenotype. Thus, BMP-7 may prevent vascular proliferative disorders and potentially could act as a palliative agent following damage to the vasculature.

Clinical Relevance: In musculoskeletal disorders in which the vasculature plays an important role, BMP-7 may be of benefit as an anti-inflammatory and anti-proliferative agent for vascular endothelium and help maintain vascular integrity.

Figures in this Article
    Vascular trauma due to metabolic, mechanical, or immunological insult is characterized by changes in the vascular endothelium, including migration and proliferation of smooth muscle cells (SMCs), loss of expression of SMC phenotype, enhanced extracellular-matrix synthesis, and cell death due to apoptosis and necrosis. These cellular changes gradually result in intimal thickening of the blood vessel and loss of elasticity in the vasculature 1 . Vasculature also plays an important role in endochondral ossification 2 , and vascularization is a key event in the development of normal cartilage and bone.
    A number of local and systemic factors participate in the maintenance of vascular integrity 3,4 . Platelet-derived growth factor (PDGF), basic fibroblast growth factor (bFGF), and insulin-like growth factor-1 (IGF-1) are known to exert strong growth-promoting activity on SMCs in vitro5 and play critical roles in the migration and proliferation of SMCs in vivo6,7 . Notably, these growth factors are detected at high concentrations within vascular proliferative lesions 8 . Conversely, systemic factors such as gamma-interferon and progesterone have been shown to exhibit growth-inhibitory activity on SMCs 9,10 . TGF-ß, a bifunctional growth-regulatory molecule for vascular SMCs, stimulates or inhibits cell growth, depending on the cell culture conditions, the presence of other growth-regulatory molecules, and the dose and frequency with which they are employed 11 . It has been shown that the injury site has high concentrations of TGF-ß, which subsequently cause an enhanced extracellular-matrix production leading to intimal thickening in blood vessels. Thus, the regulation of SMC proliferation and expression of SMC phenotype is a dynamic process, tightly governed by local and systemic factors to maintain the vascular integrity and continuous blood flow in vivo .
    Bone morphogenetic proteins (BMPs), also called osteogenic proteins (OPs), are members of the TGF-ß superfamily, originally identified by their ability to induce endochondral bone formation at an extraskeletal site 12,13 . They have been shown to regulate the migration, proliferation, and differentiation of pluripotent progenitor cells involved in the development of organ systems during embryogenesis and in adult tissue repair 14 . We have shown that systemic administration of recombinant human BMP-7 is capable of protecting heart 15 , brain 16,17 , and in particular kidney function following ischemia-reperfusion injury in rat models 18 . The tissue protective function of BMP-7 may be complex; however, we demonstrated that BMP-7 maintains the expression of vascular smooth muscle phenotype in peritubular capillaries after ischemic acute renal failure (ARF) in the rat 18 . In addition, administration of BMP-7 in norepinephrine-induced ARF in rats has been shown to improve renal function by increasing the glomeruli filtration rate, renal blood flow, and urine flow rate 19 .
    In this study, we show that BMP-7 inhibits proliferation and stimulates the expression of the SMC phenotype when it is added to human aorta-derived SMCs in culture. This BMP-7-induced growth-inhibitory effect was also observed when the SMC proliferation was stimulated by PDGF-BB and TGF-ß, suggesting that in addition to its role in the prevention of ischemic injury, BMP-7 may be a cytoprotective agent for vascular proliferative disorders.
     
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    +Fig. 1:Effect of bone morphogenetic protein-7 (BMP-7), transforming growth factor-beta (TGF-ß), and platelet-derived growth factor-BB (PDGF-BB) on human aortic smooth muscle cell proliferation. First, 4 × 10 4 cells were serum-starved for 48 hours. They were then induced to proliferate in medium containing 1% serum. At this time, various concentrations of BMP-7, TGF-ß, or PDGF-BB ( A ) or various concentrations of BMP-7 plus 1 ng/ml TGF-ß ( B ) or various concentrations of BMP-7 plus 40 ng/ml PDGF ( C ) were added. The cells were further incubated for 24 hours. They were pulsed during the last 4 hours with 3 H-thymidine at 1 µCi/ml. For cell-number studies, the PDGF-BB (40 ng/ml) and BMP-7 (100 ng/ml)-treated cultures were harvested at days 2, 3, and 4 and counted ( D ). The data are given as the mean and the standard deviation (in quadruplicates); values were normalized to counts per minute (cpm) incorporated by control cultures. *p < 0.05 and **p < 0.01 compared with 0 ng/ml growth factor. (Adapted, with permission of Wiley-Liss, a subsidiary of John Wiley and Sons, Inc., from Dorai H, Vukicevic S, Sampath TK. Bone morphogenetic protein-7 [osteogenic protein-1] inhibits smooth muscle cell proliferation and stimulates the expression of markers that are characteristic of SMC phenotype in vitro. J Cell Physiol. 2000;184:37-45.)
     
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    +Fig. 2:Effect of bone morphogenetic protein-7 (BMP-7) on p21 expression in platelet-derived growth factor (PDGF)-treated human aortic smooth muscle cultures. First, 1 × 10 6 cells were serum-starved for 48 hours before the addition of various concentrations of BMP-7 and PDGF (40 ng/ml) in medium containing 1% serum. They were further incubated for 24 hours. Subsequently, the cDNA was isolated and subjected to quantitative reverse transcriptase-polymerase chain reaction with use of the human ß-actin and p21 primers.
     
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    +Fig. 3-A:Fig. 3 Genes induced by bone morphogenetic protein-7 (BMP-7) in human aortic smooth muscle cells. A : First, 1 × 10 6 cells were treated with BMP-7 (100 ng/ml) and/or transforming growth factor-beta (TGF-ß) (1 ng/ml) and/or platelet-derived growth factor (PDGF) (40 ng/ml) for 24 hours. Subsequently, total RNA was made. Next, 1 µg of total RNA was used to prepare cDNA, which was then subjected to quantitative reverse transcriptase-polymerase chain reaction.
     
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    +Fig. 3-B:Fig. 3 Genes induced by bone morphogenetic protein-7 (BMP-7) in human aortic smooth muscle cells. B : First, 1 × 10 6 cells were treated with various concentrations of BMP-7 for 48 hours. Total RNA was then extracted, and 5 µg of each sample was subjected to a Northern blot analysis. The probe used was a HindIII-RI fragment of Smad6 cDNA 23 .
     
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    +Fig. 4-A:Fig. 4 Effect of bone morphogenetic protein-7 (BMP-7) on the endogenous and interleukin-1b (IL-1b)-induced intercellular adhesion molecule-1 (ICAM-1). A : Cells were plated in a 24-well plate (4 × 10 4 cells/well). The next day, growth medium was replaced with medium containing 0.1% serum. IL-1b (1 ng/ml) and various concentrations of BMP-7 were added. After 5 days of incubation, soluble ICAM-1 in lysed cells was measured by enzyme-linked immunosorbent assay.
     
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    +Figs. 4-B and 4-C:Fig. 4 Effect of bone morphogenetic protein-7 (BMP-7) on the endogenous and interleukin-1b (IL-1b)-induced intercellular adhesion molecule-1 (ICAM-1). B : First, 1 × 10 6 cells were treated with various concentrations of BMP-7 for 24 hours. The cells were harvested, and total RNA was made. Next, 1 g of total RNA was used to prepare cDNA, which was then subjected to semiquantitative reverse transcriptase-polymerase chain reaction with use of human glyceraldehyde-3-phosphate (GAPDH) and ICAM-1 primers. One-fifth of the reaction was subjected to agarose gel electrophoresis and photographed. M = DNA marker. C : Densitometer scan of the ICAM-1 gel photograph.
     
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    +Fig. 5-A:Fig. 5 Effect of bone morphogenetic protein-7 (BMP-7) on the expression of smooth muscle cell markers. A : First, 2 × 10 6 cells were treated with 100 ng/ml BMP-7 for various times in long-term cultures; then, they were harvested and cDNA was synthesized. Semiquantitative reverse transcriptase-polymerase chain reaction (RT-PCR) was carried out with use of the primers shown. Lanes 1-4, control, day 3, 5, 7, and 9, respectively; lanes 5-8, 100 ng/ml BMP-7, day 3, 5, 7, and 9, respectively.
     
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    +Fig. 5-B:Fig. 5 Effect of bone morphogenetic protein-7 (BMP-7) on the expression of smooth muscle cell markers. B : First, 1 × 10 6 cells were treated with various concentrations of BMP-7 for 24 hours. Cells were harvested, and total RNA was made. Then, 1 µg of total RNA was used to prepare cDNA, which was then subjected to quantitative RT-PCR.
     
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    +Fig. 5-C:Fig. 5 Effect of bone morphogenetic protein-7 (BMP-7) on the expression of smooth muscle cell markers. C : First, 1 × 10 6 cells were treated with various concentrations of BMP-7 for 24 hours. The cells were harvested, and total RNA was made. Next, 1 g of total RNA was used to prepare cDNA, which was then subjected to semiquantitative RT-PCR with use of human glyceraldehyde-3-phosphate (GAPDH) and a-actin primers. One-fifth of the reaction was subjected to agarose gel electrophoresis and photographed.
     
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    +Fig. 5-D:Fig. 5 Effect of bone morphogenetic protein-7 (BMP-7) on the expression of smooth muscle cell markers. D : First, 5 × 10 5 cells were plated in growth medium and treated with 100 ng/ml BMP-7 or vehicle for 9 days. They were then photographed. Magnification is 20 × .

    Cell Culture

    Human primary aortic smooth muscle cells (HASM) were purchased from Clonetics (San Diego, California). They were grown in growth medium provided by the same company. Cells from passages 4-9 were used for all experiments.

    3 H-Thymidine Incorporation

    HASM cells were plated into 24-well plates at a concentration of 4 × 10 4 cells/well such that they were 60-70% confluent the next day. At this time, they were rendered quiescent by changing the medium to Dulbecco's modified Eagle medium (DMEM) (Gibco BRL, Gaithersburg, Maryland) containing 0.1% serum for 60-72 hours. The medium was then replaced with DMEM containing 1% serum with or without various concentrations of a homogenous preparation of recombinant human mature BMP-7 20 , PDGF-BB, or TGF-ß (Upstate Biologicals, Syracuse, New York) for 24 hours. During the last 3 hours of culture, cells were labeled with [methyl- 3 H]-thymidine (Dupont/NEN, Boston, Massachusetts) at 1 Ci/ml/well in thymidine-free medium. At the end of the incubation period, the cells were fixed in 75% methanol/25% acetic acid (v/v) for at least 2 hours, followed by several washes with 80% methanol. Incorporated 3 H-thymidine was measured in a liquid scintillation counter. All experiments were performed multiple times employing cells from different passages (passages 4-9). The data presented are representative of one such experiment.

    Cell Counting

    HASM cells were plated into a 24-well plate at a concentration of 8 × 10 3 cells/well. After 24 hours, various concentrations of BMP-7, PDGF-BB, or TGF-ß1 were added and the cells were incubated for a total of 72 hours. The total cell number was determined at 0, 24, 48, and 72 hours with use of a hemocytometer and trypan blue staining for viable cells. Cells from four wells were combined for an average reading.

    Long-Term Cultures of HASM Cells

    Eight 100-mm dishes were plated with HASM cells at a concentration of 1.2 × 10 6 cells/dish. After 24 hours, 100 ng/ml BMP-7 was added to four plates and an equal amount of vehicle was added to the other four. The day that the cultures reached confluence was noted and marked as day 0. The medium was changed that day and every other day thereafter, and fresh BMP-7 was added. Beginning day 3 and every other day thereafter, one plate from each group was harvested and total RNA was isolated. Thus, total RNA was made from BMP-7-treated and untreated cultures on day 3, 5, 7, and 9, respectively.

    Total RNA Preparation and Semiquantitative Reverse Transcriptase-Polymerase Chain Reaction (RT-PCR) Analysis

    Total RNA from HASM cells was isolated with TRIzol as indicated (Gibco BRL). Contaminating genomic DNA was removed with RNAase-free DNAase following the manufacturer's protocol. Complementary DNA was synthesized with Superscript reverse transcriptase (Gibco BRL) as described in the same protocol. Four micrograms of DNAase-treated RNA was incubated with 2 µloligo dT at 70°C for 10 minutes. Next, 14 µlof 53 buffer, 7 µlDTT (0.1 M ), 3.5 µlof each nucleotide (10 m M ), 1.5 µlRNAase inhibitor, and 2 µlSuperscript reverse transcriptase (Gibco BRL) were added to each reaction. The samples were incubated for 10 minutes at room temperature, 50 minutes at 42°C, 10 minutes at 50°C, and 5 minutes at 90°C. RNAase-H (1 µl) (Gibco BRL) was added to the reactions, and samples were incubated for 20 minutes at 37°C. PCR was performed as indicated by the manufacturer (Perkin-Elmer, Norwalk, Connecticut) with the following primers: a-actin sense 5'GCT CAC GGA GGC ACC CCT GAA, antisense 5'CTG ATA GGA CAT TGT TAG CAT; glyceraldehyde-3-phosphate (GAPDH) senseACC ACA GTC CAT GCC ATC AC, antisense 5'TCC ACC ACC CTG TTG CTG TA; collagen III sense 5'GGT GTG GAC GTT GGC CCT GTT TGC, antisense 5'CTA AGT AAC CGT ACG GTG TCC C; collagen I sense 59TGA CTT GAG ACT CAG CCA CCC A, antisense 5'AGG TTG CCA GTC TCC TCA TCC A; and intercellular adhesion molecule-1 (ICAM-1) sense 59GGG AAT CCA GCC CCT AAT CTG A, ICAM-1 antisense 5'GAC TGT CCC AGC TTT CCC ATG T.
    Reactions included 5 µlof 103 buffer, 3 µlof 25 m M MgCl2, 1 µlof 10 m M dNTP, 1 µlof 20 M 3' primer, 1 µlof 20 M 5' primer, 0.5 µlTaq polymerase (Perkin-Elmer, Foster City, California), and 1 µlcDNA. Samples were incubated for 5 minutes at 94°C followed by 25-40 cycles of 45 seconds at 94°C, 45 seconds at 59°C, 1 minute at 72°C, and final extension at 72°C for 10 minutes in a Perkin-Elmer DNA Thermal Cycler. To compare the relative quantity of the RT-PCR reactions, the transcription level of GAPDH was used as a control. GAPDH gene expression was found to be similar at all time points examined, enabling analysis of the relative levels of gene expression for the desired genes. PCR primer sets were optimized with use of human placental and embryonic cDNA libraries purchased from Clonetech (Palo Alto, California). The PCR product was verified at least twice.

    Quantitative RT-PCR Analysis

    cDNA was generated by reverse-transcribing 1 µg of total RNA in a volume of 100 µlwith use of a kit provided by Promega (Madison, Wisconsin). This cDNA (2 µl) was then used as a template for PCR reactions. Quantitative PCR was performed with use of a PE Biosystems 5700 SDS with SYBR Green core reagents (PE Biosytems, Foster City, California). Reactions were performed in triplicate and quantitated to that of ß-actin, which remained unchanged by the addition of BMP-7. The primers used were ß-actin sense 5'CTG GAA CGG TGA AGG TGA CA, antisense 59CGG CCA CAT TGT GAA CTT TG; p21 sense 5'CCC GTT TCT CCA CCT AGA CTG T, antisense 5'TCA GCA TTG TGC GAG GAG CT; Smad6 sense 5'GCC ACT GGA TCT GTC CGA TT, antisense 5'CAC CCG GAG CAG TGA TGA G; Smad7 sense 5'CTG GGA GGG ACA TGC TTA GC, antisense 5'TCA GCC TAG GAT GGT ACC TTG G; a-actin sense 5'CCA GCA GAT GTG GAT CAG CA, antisense 5'AAG CAT TTG CGG TGG ACA AT; Id-1 sense 5'AGA ACC GCA AGG TGA GCA A, antisense 5'TCC ACC TGA AGG TCC CTG ATG; Id-2 sense 5'CCA CCC TCA ACA CGG ATA TCA, antisense 5'ACA CAG TGC TTT GCT GTC ATT TG; Id-3 sense 5'GCG GCA GAG CTG GTC TTC, antisense 5'TCA GGG CAA CAG AAC CTT TCT C; basic calponin sense 5'AGG AGC TGA GAG AGT GGA TCG A, antisense 59TCG CAA AGA ATG ATG CCA TCT; and H-chain myosin sense 5'TCA ACA TGC AGG CGC TCA, antisense 5' CGT CTC ATA CTC GTG AAG CTG TCT.

    Northern Blot Analysis

    Five micrograms of total RNA was electrophoresed in a 1.2% formaldehyde-agarose gel and blotted onto nitrocellulose filters that were hybridized with randomly primed 32 P-labeled Smad6 cDNA probe as described 21 . The hybridized filters were washed in 30 m M NaCl, 3 m M sodium citrate, and 0.1% sodium dodecyl sulfate at 55°C and autoradiographed on Kodak XAR film at -80°C on phosphor screen. To correct for differences in RNA loading, the filters were washed at 80°C in 50% formamide solution and rehybridized with a radiolabeled GAPDH probe. The GAPDH probe was generated from RT-PCR product.

    ICAM-1 Estimation by ELISA

    HASM cells were plated at 5 × 10 4 cells/well in a 24-well plate, in growth medium containing 5% fetal bovine serum (FBS). The next day, the medium was replaced with medium containing 0.1% FBS. Then, 1 ng/ml of IL-1b (R&D Systems, Minneapolis, Minnesota) and various concentrations of BMP-7 were added as indicated. Three or five days later, the medium was removed and the cell layer was washed twice with phosphate buffered saline (PBS) and lysed in 0.5 ml PBS by three freeze-thaw cycles. Finally, 20-100 µlof cell lysates was analyzed for soluble human ICAM-1 with use of ELISA kits (R&D Systems). Recombinant human ICAM-1 and IL-6 were provided by the manufacturer and used as standards.
    The results are indicated as units/mg of protein in cell lysates.

    SMCs Express BMP-7 Receptors

    Prior to evaluating the direct effect of BMP-7 on vascular SMCs, we examined cultures of HASM cells for the presence of BMP-7 and its type-I and II receptors by RT-PCR. Although there was no detectable BMP-7, BMP type-I receptors ALK-3 (ActR-IA) and ALK-6 (BMPR-IB) were abundant. The presence of several type-I receptors for BMPs [ALK-2 (ActR-I), ALK-3 (BMPR-IA), and ALK-6 (BMPR-IB)] in vascular SMC also has been reported previously 22-24 . Although we were unable to detect BMP type-II receptors (BMPR-II), we found abundant activin type-IIB receptor (ActR-IIB), which has been shown to function as a type-II receptor for BMP-7 25 . Similarly, BMP-2 has been shown to bind to ActR-II and ActR-IIB in the presence of the appropriate type-I receptors 26 .

    BMP-7 Inhibits Serum and Growth Factor-Induced Proliferation of SMCs

    We examined the effect of exogenously added BMP-7 on cell growth in HASM cell cultures by 3 H-thymidine incorporation into DNA. Prior to the addition of BMP-7, cells were synchronized by serum starvation for 60-72 hours and then induced to proliferate by providing the medium with 1% serum. Various concentrations of BMP-7 with or without PDGF-BB or TGF-ß1 were added. BMP-7 exhibits a biphasic effect on the serum-induced proliferation of HASM cells in culture ( Fig. 1-A ). At very low concentrations (0.1-1.0 ng/ml), BMP-7 had a small but reproducible stimulatory effect (about 10%) on these cells, whereas at higher concentrations (10-200 ng/ml) it inhibited the serum-induced HASM cell proliferation in a dose-dependent manner. About 60% inhibition of proliferation was obtained within 24 hours by the addition of BMP-7 (200 ng/ml). Under identical experimental conditions, TGF-ß1 (1 ng/ml) and PDGF-BB (40 ng/ml) stimulated the proliferation of HASM cells by 30% and 300%, respectively ( Fig. 1-A ). Interestingly, when BMP-7 was added in conjunction with these growth factors, the same biphasic pattern was observed as seen with BMP-7 alone ( Fig. 1-B and Fig. 1-C ). At very low concentrations (0.1-1 ng/ml), BMP-7 had either no effect or a small but reproducible stimulatory effect, whereas at higher concentrations (10-200 ng/ml), BMP-7 was able to inhibit the stimulatory activity of TGF-ß1 and PDGF-BB in a dose-dependent manner. In accordance with reduced 3 H-thymidine incorporation into DNA, the cell number was also decreased when cells were treated with BMP-7 and PDGF as compared with PDGF alone ( Fig. 1-D ).
    Several cell-cycle proteins, including cyclin-dependent kinase-2 (cdk-2) and cdk-2 kinase inhibitor, p21 (cip), mediate SMC proliferation 27,29 , and BMP-7 inhibits the proliferative activity of PDGF in HASM cells. Therefore, we examined the effect of BMP-7 on these cell-cycle-modulated genes by quantitative RT-PCR. As shown in Fig. 2 , 40 ng PDGF-BB per ml dramatically downregulated the expression of cdk-2 kinase inhibitor, p21, which was completely neutralized by BMP-7 in a dose-dependent manner. Correspondingly, the cdk-2 kinase gene expression was upregulated by PDGF and this effect was inhibited by BMP-7.

    BMP-7 Induces the Expression of Inhibitors of Helix-Loop-Helix Transcription Factors and Inhibitory Smads

    Id proteins control cell differentiation by interfering with DNA binding of transcription factors. Previously, it was shown that BMP-2 upregulated Id-1 in the process of osteoblast differentiation of myoblast cell line C2C12 29 . Investigating the mechanism of BMP-7 action, we found that the expression of inhibitors of helix-loop-helix transcription factors Id-1 and Id-2 was dramatically upregulated by BMP-7 ( Fig. 3-A ). Greater than 25-fold induction of both Id-1 and Id-2 was obtained by 100 ng/ml BMP-7. In contrast, TGF-ß and PDGF had little or no effect on the expression of Ids. This induction was rapid and was detected at the earliest time point we have examined: 15 minutes after the addition of BMP-7. When BMP-7 was added in conjunction with TGF-ß or PDGF, Id-1 and Id-2 were induced to a lesser extent.
    The inhibitory Smads, Smad6 and Smad7, have been shown to act as an inhibitor of Smad phosphorylation in the BMP and TGF-ß signaling pathway and have been implicated in the control of these pathways 21,30,32 . Both Smad6 (35-fold) and Smad7 (15-fold) were induced by 100 ng/ml BMP-7 ( Fig. 3-A ). Under identical culture conditions, PDGF had no effect on the expression of these two genes and TGF-ß induced only Smad7. A dose-dependent induction of Smad6 could be detected by Northern blot analysis of the same RNA ( Fig. 3-B ).

    BMP- 7 Downregulates Endogenous and Induced ICAM-1

    One key feature of vascular proliferative disorders is inflammation. IL-1b and other pro-inflammatory cytokines from aggregating macrophages and monocytes induce in turn the expression of ICAM-1, MCP-1, and other pro-inflammatory cytokines in SMC cells. IL-1b (1 ng/ml) dramatically induced the expression of ICAM-1, which can be inhibited to as much as 40% by 200 ng/ml BMP-7 ( Fig. 4-A ). Additionally, BMP-7 can dose-dependently downregulate the expression of endogenous ICAM-1 ( Fig. 4-B and Fig. 4-C ) and IL-6 (data not shown) as examined by semiquantitative RT-PCR.

    BMP-7 Maintains the Expression of Markers Characteristic of SMC Phenotype

    When primary HASM cells are maintained in culture for long periods, they tend to adopt a more fibroblast-like morphology with a concomitant loss of SMC markers such as a-actin and SMC-specific H-chain myosin. We found that HASM cultures containing BMP-7 (100 ng/ml) maintained the expression of a-actin beyond day 6 in confluent cultures, whereas untreated cultures started to loose a-actin expression as early as day 3 ( Fig. 5-A ). As it has been shown that in atherosclerotic lesions type-I collagen synthesis is enhanced compared with that of type-III collagen, we examined the ability of BMP-7 to maintain type-III collagen synthesis in long-term cultures by semiquantitative RT-PCR. Although the expression of collagen type I remained unaltered beyond day 3 following confluence in treated and untreated cultures ( Fig. 5-A ), the expression of collagen type III was significantly decreased over the same time period in untreated cultures ( Fig. 5-A . However, its expression remained unaltered or even enhanced in BMP-7-treated cultures. This is confirmed by densitometer scanning of the gel followed by calculations of ratios (collagen III/GAPDH). Furthermore, BMP-7 induced a dose-dependent increase in the expression of a-actin, basic calponin, and H-chain myosin as examined by quantitative and semiquantitative RT-PCR ( Fig. 5-B and Fig. 5-C ). Additionally, there was a discernable change in morphology ( Fig. 5-D ) from needle-shaped fibroblast-like cells that are stacked on top of each other to more randomly organized smaller cells at the addition of BMP-7 to these cultures. The true appearance of SMCs in culture is unclear.
    We show here that HASM cells when treated with recombinant human BMP-7 (also called osteogenic protein-l [OP-1]) inhibit serum-stimulated cell proliferation in culture over a wide range of physiologic concentrations (10-200 ng/ml). Notably, this BMP-7-mediated inhibition of SMC proliferation was more pronounced when cell growth had been stimulated with PDGF-BB or TGF-ß, suggesting for the first time a potential role for BMPs in the prevention of SMC proliferation following vascular injury. The inhibitory effect of BMP-7 was due in part to an increased expression of the inhibitor of cyclin-dependent kinase-2, p21, which was inhibited during PDGF-BB-mediated cell proliferation. BMP-7 also induced the expression of developmentally regulated genes such as Id-1 and Id-2, which are required for several key cellular differentiation pathways and inhibitory Smads. Smad6 and Smad7, which negate both the TGF-ß and TGF-ß superfamily of proteins, mediated downstream signaling. Concurrently, BMP-7-mediated inhibition of cell growth is accompanied by enhanced expression of markers that are characteristic of the SMC phenotype, a-actin, SMC-specific heavy-chain myosin, and maintenance of the type III/I collagen ratio. Finally, BMP-7 downregulated endogenous and IL-1b induced ICAM-1, a cell-surface molecule known to play a role in neutrophil adhesion and activation during inflammation. Our findings suggest that BMP-7 may provide a basis for developing therapeutic strategies to effectively suppress SMC proliferation, delay the onset of inflammation, and diminish the formation of connective tissue in and around the vascular endothelium associated with vascular proliferative disorders 4 .
    Several peptide growth factors (PDGF, FGF, IGF-1, and TGF-ß), pro-inflammatory cytokines (interleukin-1 [IL-1] and tumor necrosis factor-alpha [TNF-a]), and agents such as nitric oxide and lipids are known to regulate migration, proliferation, and differentiation of vascular SMCs 6,7,32-34 . Specifically, following injury, the migration and proliferation of SMCs are stimulated by (1) the paracrine action of PDGF-BB, released by platelets at their activation 4 , (2) the autocrine action of PDGF-AA induced by the pro-inflammatory cytokines (IL-1 and TNF-a), and (3) TGF-ß 33,34 . In addition, FGF and IGF-1 are released locally by activated SMCs 4 that act on SMC growth. Studies attempting to antagonize the activities of growth factors PDGF, FGF, and TGF-ß and their receptors using specific antibodies and antisense oligonucleotides 35,36 have provided protection against SMC proliferation following balloon angioplasty and thus help to reduce myo-intimal thickening. In addition, therapeutic modalities such as the infusion of IFN-gamma 37 and anti-ICAM 38 antibodies have been reported to diminish intimal thickening in various animal models. Since an ideal artery contains SMCs that are both contractile and quiescent with respect to proliferation, therapies that would decrease the likelihood of SMC hyperplasia and consequent luminal occlusion may provide cyto-protection against the vascular proliferative disorders and delayed dysfunction that occur after organ transplantation.
    Although BMPs were originally identified in bone, their morphogenic roles have been widely documented in a wide variety of other nonskeletal tissues 14 . BMPs are novel growth and differentiation factors constituting a large subfamily in the TGF-ß superfamily of proteins. BMPs have been shown to play inductive roles in migration and proliferation of pluripotent stem cells 39 and have a subsequent differentiation into lineage-specific cell types during morphogenesis. Furthermore, BMPs are capable of stimulating the expression of phenotypes characteristic to a specific cell type 40 and serve as maintenance factors during the repair and regeneration of adult tissue 18,41 . Therefore, when BMPs are made available in and around the vascular endothelium, they may assist in maintaining SMCs in a contractile and quiescent state rather than aid in the proliferation and loss of phenotype at vascular injury and as observed in various proliferative disorders. To support this notion, BMP-2, a related member of BMP-7, has been shown to inhibit rat vascular smooth muscle proliferation in vitro and to inhibit injury-induced intimal hyperplasia when administered locally by adenovirus-mediated gene transfer following balloon angioplasty in rats 42 . Our present study supports and extends these observations. Potentially, BMPs can be used to maintain the expression of SMC phenotype in cultures during cell expansion in order to engineer functional vascular grafts for clinical need. Since the effect of BMPs on cell growth and differentiation is dependent on the developmental stage of the responding cells, it is likely that the presence of the BMPs in the culture medium will help to differentiate the expanded cells into the more "mature" contractile quiescent SMCs.
    Among TGF-ß superfamily proteins, TGF-ß has been studied in the context of vascular integrity in vitro and in vivo43 . This morphogen is a bifunctional growth regulator of SMCs that was shown to stimulate or inhibit the growth of SMCs depending on the conditions of cell culture, the presence of other regulatory molecules, the sequence of their addition, and the concentration of TGF-ß 44 . Moreover, several studies have shown that TGF-ß is potent in stimulating the deposition of connective tissues by SMCs 43 . Under our culture conditions, TGF-ß had a proliferative effect on serum-stimulated DNA synthesis of SMCs. Thus, the beneficial effect of BMP-7 on SMCs does not appear comparable with that of TGF-ß. Although the mode of action of the BMP-7 activity is currently unknown, the results suggest that BMP-7 upregulates both Smad6 and Smad7, the two inhibitory Smads in the TGF-ß superfamily. Under these conditions, Smad7 but not Smad6 was upregulated by TGF-ß, whereas neither was induced by PDGF. Additionally, it has been shown that BMP-7 upregulates Smad7 expression in lung cancer cell lines 45 and in myoblast cell line C2C12 (unpublished observation). In vivo studies have shown that both Smad6 and Smad7 were induced in vascular endothelium at mechanical stimulus 46 , suggesting potential protection against vascular injury. The fact that Smad6 is important for the inhibition of BMP signaling 29 suggests that this molecule may in part be involved in the regulation of the effects of BMP on SMCs.
    The observed cytoprotective effect of BMPs on vascular SMC may provide a basis for developing therapeutic agents for intervention against vascular proliferative disorders.
    RossR,Glomset JA. Atherosclerosis and the arterial smooth muscle cell: proliferation of smooth muscle is a key event in the genesis of the lesions of atherosclerosis. Science,1973;180: 1332-S9. 1801332  1973  [PubMed][CrossRef]
     
    BittnerK, Vischer P, Bartholmes P,Bruckner P. Role of subchondral vascular system in endochondral ossification: endothelial cells specifically derepress late differentiation in resting chondrocytes in vitro. Exp Cell Res,1998;238: 491-S7. 238491  1998  [PubMed][CrossRef]
     
    RossR. The pathogenesis of atherosclerosis-an update. N Engl J Med,1986;314: 488-S500. 314488  1986  [PubMed][CrossRef]
     
    RossR. The pathogenesis of atherosclerosis: a perspective for the 1990s. Nature,1993;362: 801-S9. 362801  1993  [PubMed][CrossRef]
     
    BanskotaNK, Taub R, Zellner K,King G. Insulin, insulin-like growth factor I and platelet-derived growth factor interact additively in the induction of the protooncogene c-myc and cellular proliferation in cultured bovine aortic smooth muscle cells. Mol Endocrinol,1989;3: 1183-S90. 31183  1989  [PubMed][CrossRef]
     
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    KawamataT, Ren J, Chen TC, Charette M,Finkelstein SP. Intracisternal osteogenic protein-1 enhances functional recovery following focal stroke. Neuroreport,1998;9: 1441-S5. 91441  1998  [PubMed][CrossRef]
     
    RenJ, Kaplan PL, Charette MF, Speller H,Finkelstein SP. Time window of intracisternal osteogenic protein-1 in enhancing functional recovery after stroke. Neuropharmacology,2000;39: 860-S5. 39860  2000  [PubMed][CrossRef]
     
    VukicevicS, Basic V, Rogic D, Basic N, Shih MS, Shepard A, Jin D, Dattatreyamurty B, Jones W, Dorai H, Ryan S, Griffiths D, Maliakal J, Jelic M, Pastorcic M, Stavljenic A,Sampath TK. Osteogenic protein-1 (bone morphogenetic protein-7) reduces severity of injury after ischemic acute renal failure in rat. J Clin Invest,1998;102: 202-S14. 102202  1998  [PubMed][CrossRef]
     
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    SampathTK, Maliakal JC, Hauschka PV, Jones WK, Sasak H, Tucker RF, White KH, Coughlin JE, Tucker MM,Pang RH. Recombinant human osteogenic protein-1 (hOP-1) induces new bone formation in vivo with a specific activity comparable with natural bovine osteogenic protein and stimulates osteoblast proliferation and differentiation in vitro. J Biol Chem,1992;267: 20352-S62. 26720352  1992  [PubMed]
     
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    +Fig. 5-B:Fig. 5 Effect of bone morphogenetic protein-7 (BMP-7) on the expression of smooth muscle cell markers. B : First, 1 × 10 6 cells were treated with various concentrations of BMP-7 for 24 hours. Cells were harvested, and total RNA was made. Then, 1 µg of total RNA was used to prepare cDNA, which was then subjected to quantitative RT-PCR.
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    +Fig. 5-C:Fig. 5 Effect of bone morphogenetic protein-7 (BMP-7) on the expression of smooth muscle cell markers. C : First, 1 × 10 6 cells were treated with various concentrations of BMP-7 for 24 hours. The cells were harvested, and total RNA was made. Next, 1 g of total RNA was used to prepare cDNA, which was then subjected to semiquantitative RT-PCR with use of human glyceraldehyde-3-phosphate (GAPDH) and a-actin primers. One-fifth of the reaction was subjected to agarose gel electrophoresis and photographed.
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    +Fig. 5-D:Fig. 5 Effect of bone morphogenetic protein-7 (BMP-7) on the expression of smooth muscle cell markers. D : First, 5 × 10 5 cells were plated in growth medium and treated with 100 ng/ml BMP-7 or vehicle for 9 days. They were then photographed. Magnification is 20 × .
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    +Fig. 5-A:Fig. 5 Effect of bone morphogenetic protein-7 (BMP-7) on the expression of smooth muscle cell markers. A : First, 2 × 10 6 cells were treated with 100 ng/ml BMP-7 for various times in long-term cultures; then, they were harvested and cDNA was synthesized. Semiquantitative reverse transcriptase-polymerase chain reaction (RT-PCR) was carried out with use of the primers shown. Lanes 1-4, control, day 3, 5, 7, and 9, respectively; lanes 5-8, 100 ng/ml BMP-7, day 3, 5, 7, and 9, respectively.
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    +Figs. 4-B and 4-C:Fig. 4 Effect of bone morphogenetic protein-7 (BMP-7) on the endogenous and interleukin-1b (IL-1b)-induced intercellular adhesion molecule-1 (ICAM-1). B : First, 1 × 10 6 cells were treated with various concentrations of BMP-7 for 24 hours. The cells were harvested, and total RNA was made. Next, 1 g of total RNA was used to prepare cDNA, which was then subjected to semiquantitative reverse transcriptase-polymerase chain reaction with use of human glyceraldehyde-3-phosphate (GAPDH) and ICAM-1 primers. One-fifth of the reaction was subjected to agarose gel electrophoresis and photographed. M = DNA marker. C : Densitometer scan of the ICAM-1 gel photograph.
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    +Fig. 4-A:Fig. 4 Effect of bone morphogenetic protein-7 (BMP-7) on the endogenous and interleukin-1b (IL-1b)-induced intercellular adhesion molecule-1 (ICAM-1). A : Cells were plated in a 24-well plate (4 × 10 4 cells/well). The next day, growth medium was replaced with medium containing 0.1% serum. IL-1b (1 ng/ml) and various concentrations of BMP-7 were added. After 5 days of incubation, soluble ICAM-1 in lysed cells was measured by enzyme-linked immunosorbent assay.
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    +Fig. 3-B:Fig. 3 Genes induced by bone morphogenetic protein-7 (BMP-7) in human aortic smooth muscle cells. B : First, 1 × 10 6 cells were treated with various concentrations of BMP-7 for 48 hours. Total RNA was then extracted, and 5 µg of each sample was subjected to a Northern blot analysis. The probe used was a HindIII-RI fragment of Smad6 cDNA 23 .
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    +Fig. 3-A:Fig. 3 Genes induced by bone morphogenetic protein-7 (BMP-7) in human aortic smooth muscle cells. A : First, 1 × 10 6 cells were treated with BMP-7 (100 ng/ml) and/or transforming growth factor-beta (TGF-ß) (1 ng/ml) and/or platelet-derived growth factor (PDGF) (40 ng/ml) for 24 hours. Subsequently, total RNA was made. Next, 1 µg of total RNA was used to prepare cDNA, which was then subjected to quantitative reverse transcriptase-polymerase chain reaction.
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    +Fig. 2:Effect of bone morphogenetic protein-7 (BMP-7) on p21 expression in platelet-derived growth factor (PDGF)-treated human aortic smooth muscle cultures. First, 1 × 10 6 cells were serum-starved for 48 hours before the addition of various concentrations of BMP-7 and PDGF (40 ng/ml) in medium containing 1% serum. They were further incubated for 24 hours. Subsequently, the cDNA was isolated and subjected to quantitative reverse transcriptase-polymerase chain reaction with use of the human ß-actin and p21 primers.
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    +Fig. 1:Effect of bone morphogenetic protein-7 (BMP-7), transforming growth factor-beta (TGF-ß), and platelet-derived growth factor-BB (PDGF-BB) on human aortic smooth muscle cell proliferation. First, 4 × 10 4 cells were serum-starved for 48 hours. They were then induced to proliferate in medium containing 1% serum. At this time, various concentrations of BMP-7, TGF-ß, or PDGF-BB ( A ) or various concentrations of BMP-7 plus 1 ng/ml TGF-ß ( B ) or various concentrations of BMP-7 plus 40 ng/ml PDGF ( C ) were added. The cells were further incubated for 24 hours. They were pulsed during the last 4 hours with 3 H-thymidine at 1 µCi/ml. For cell-number studies, the PDGF-BB (40 ng/ml) and BMP-7 (100 ng/ml)-treated cultures were harvested at days 2, 3, and 4 and counted ( D ). The data are given as the mean and the standard deviation (in quadruplicates); values were normalized to counts per minute (cpm) incorporated by control cultures. *p < 0.05 and **p < 0.01 compared with 0 ng/ml growth factor. (Adapted, with permission of Wiley-Liss, a subsidiary of John Wiley and Sons, Inc., from Dorai H, Vukicevic S, Sampath TK. Bone morphogenetic protein-7 [osteogenic protein-1] inhibits smooth muscle cell proliferation and stimulates the expression of markers that are characteristic of SMC phenotype in vitro. J Cell Physiol. 2000;184:37-45.)
    RossR,Glomset JA. Atherosclerosis and the arterial smooth muscle cell: proliferation of smooth muscle is a key event in the genesis of the lesions of atherosclerosis. Science,1973;180: 1332-S9. 1801332  1973  [PubMed][CrossRef]
     
    BittnerK, Vischer P, Bartholmes P,Bruckner P. Role of subchondral vascular system in endochondral ossification: endothelial cells specifically derepress late differentiation in resting chondrocytes in vitro. Exp Cell Res,1998;238: 491-S7. 238491  1998  [PubMed][CrossRef]
     
    RossR. The pathogenesis of atherosclerosis-an update. N Engl J Med,1986;314: 488-S500. 314488  1986  [PubMed][CrossRef]
     
    RossR. The pathogenesis of atherosclerosis: a perspective for the 1990s. Nature,1993;362: 801-S9. 362801  1993  [PubMed][CrossRef]
     
    BanskotaNK, Taub R, Zellner K,King G. Insulin, insulin-like growth factor I and platelet-derived growth factor interact additively in the induction of the protooncogene c-myc and cellular proliferation in cultured bovine aortic smooth muscle cells. Mol Endocrinol,1989;3: 1183-S90. 31183  1989  [PubMed][CrossRef]
     
    HeldinCH,Westermark B. Platelet-derived growth factor: mechanism of action and possible in vivo function. Cell Regul,1990;1: 555-S66. 1555  1990  [PubMed]
     
    BurgessWH,Maciag T. The heparin-binding (fibroblast) growth factor family of proteins. Annu Rev Biochem,1989;58: 575-S606. 58575  1989  [PubMed][CrossRef]
     
    RossR, Masuda J, Raines HW, Gown AM, Katsuda S, Sasahara M, Malden LT, Masuko H,Sato H. Localization of PDGF-BB protein in macrophages in all phases of atherogenesis. Science,1990;248: 1009-S12. 2481009  1990  [PubMed][CrossRef]
     
    HanssonGK, Hellstrand L, Rymo L, Rubbia L,Gabbiani G. Interferon gamma inhibits both proliferation and expression of differentiation-specific alpha-smooth muscle actin in arterial smooth muscle cells. J Exp Med,1989;170: 1595-S1608. 1701595  1989  [PubMed][CrossRef]
     
    LeeWS, Harder JA, Yoshizumi M, Lee ME,Haber E. Progesterone inhibits arterial smooth muscle cell proliferation. Nat Med,1997;3: 1005-S8. 31005  1997  [PubMed][CrossRef]
     
    BattegayEJ, Raines EW, Seifert RA, Bowen-Pope DF,Ross R. TGF-beta induces bimodal proliferation of connective tissue cells via complex control of an autocrine PDGF loop. Cell,1990;63: 515-S24. 63515  1990  [PubMed][CrossRef]
     
    UristMR. Bone: formation by autoinduction. Science,1965;150: 893-S9. 150893  1965  [PubMed][CrossRef]
     
    SampathTK,Reddi AH. Dissociative extraction and reconstitution of extra-cellular matrix components involved in local bone differentiation. Proc Natl Acad Sci U S A,1981;78: 7599-S603. 787599  1981  [PubMed][CrossRef]
     
    HoganBL. Bone morphogenetic proteins in development. Curr Opin Genet Dev,1996;6: 432-S8. 6432  1996  [PubMed][CrossRef]
     
    LeferAM, Tsao PS, Ma XL,Sampath TK. Anti-ischemic and endothelial protective actions of recombinant human osteogenic protein (hOP-1). J Mol Cell Cardiol,1992;24: 585-S93. 24585  1992  [PubMed][CrossRef]
     
    KawamataT, Ren J, Chen TC, Charette M,Finkelstein SP. Intracisternal osteogenic protein-1 enhances functional recovery following focal stroke. Neuroreport,1998;9: 1441-S5. 91441  1998  [PubMed][CrossRef]
     
    RenJ, Kaplan PL, Charette MF, Speller H,Finkelstein SP. Time window of intracisternal osteogenic protein-1 in enhancing functional recovery after stroke. Neuropharmacology,2000;39: 860-S5. 39860  2000  [PubMed][CrossRef]
     
    VukicevicS, Basic V, Rogic D, Basic N, Shih MS, Shepard A, Jin D, Dattatreyamurty B, Jones W, Dorai H, Ryan S, Griffiths D, Maliakal J, Jelic M, Pastorcic M, Stavljenic A,Sampath TK. Osteogenic protein-1 (bone morphogenetic protein-7) reduces severity of injury after ischemic acute renal failure in rat. J Clin Invest,1998;102: 202-S14. 102202  1998  [PubMed][CrossRef]
     
    ChanT, Falk S,Conger J. Effect of osteogenic protein-1 on the course of norepinephrine induced acute renal failure. J Am Soc Nephrol,1997;8: 2721A. 82721  1997 
     
    SampathTK, Maliakal JC, Hauschka PV, Jones WK, Sasak H, Tucker RF, White KH, Coughlin JE, Tucker MM,Pang RH. Recombinant human osteogenic protein-1 (hOP-1) induces new bone formation in vivo with a specific activity comparable with natural bovine osteogenic protein and stimulates osteoblast proliferation and differentiation in vitro. J Biol Chem,1992;267: 20352-S62. 26720352  1992  [PubMed]
     
    TakaseM, Imamura T, Sampath TK, Takeda K, Ichijo H, Miyazono K,Kawabata M. Induction of Smad6 mRNA by bone morphogenetic protein. Biochem Biophys Res Commun,1998;244: 26-S9. 24426  1998  [PubMed][CrossRef]
     
    AgrotisA, Samuel M, Prapas G,Bobik A. Vascular smooth muscle cells express multiple type I receptors for TGF-beta, activin, and bone morphogenic proteins. Biochem Biophys Res Commun,1996;219: 613-S8. 219613  1996  [PubMed][CrossRef]
     
    DoraiH, Shepard A, Maliakal J, Oppermann H, Vukicevic S,Sampath TK. Osteogenic protein-1 (OP-1/BMP-7) modulates smooth muscle growth and maintains the expression of cell phenotype and protects against cell injury mediated by nephrotoxic and inflammatory agents in vitro. J Am Soc Nephrol,1997;8: 136A. 8136  1997 
     
    DoraiH, Vukicevic S,Sampath TK. Bone morphogenetic protein-7 (osteogenic protein-1) inhibits smooth muscle cell proliferation and stimulates the expression of markers that are characteristic of SMC phenotype in vitro. J Cell Physiol,2000;184: 37-S45. 18437  2000  [PubMed][CrossRef]
     
    Macias-Silva M, Hoodless PA, Tang SJ, Buchwald M,Wrana JL. Specific activation of Smad1 signaling pathways by the BMP7 type I receptor, ALK2. J Biol Chem,1998;273: 25628-S36. 27325628  1998  [PubMed][CrossRef]
     
    LetsouA, Arora K, Wrana JL, Simin K, Twombly V, Jamal J, Staehling-Hampton K, Hoffmann FM, Gelbart WM, Massague J,O'Connor MB. Drosophila Dpp signaling is mediated by the punt gene product: a dual ligand-binding type II receptor of the TGF beta receptor family. Cell,1995;80: 899-S908. 80899  1995  [PubMed][CrossRef]
     
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