PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 27306340-2 2016 The objective of this study was to investigate the effects of SD-208, TGF-beta-RI kinase inhibitor, on the expression of some miRNAs including a miR-17/92 cluster in retinoblastoma cells. SD-208 62-68 miR-17-92a-1 cluster host gene Homo sapiens 145-154 27464628-0 2016 [Effects of transforming growth factor beta1 receptor inhibitor SD-208 on human hypertrophic scar]. SD-208 64-70 transforming growth factor beta 1 Homo sapiens 12-44 27464628-1 2016 OBJECTIVE: To investigate the effects of transforming growth factor beta1 (TGF-beta1) receptor inhibitor SD-208 on human hypertrophic scar and its mechanisms. SD-208 105-111 transforming growth factor beta 1 Homo sapiens 41-73 27464628-1 2016 OBJECTIVE: To investigate the effects of transforming growth factor beta1 (TGF-beta1) receptor inhibitor SD-208 on human hypertrophic scar and its mechanisms. SD-208 105-111 transforming growth factor beta 1 Homo sapiens 75-84 27464628-25 2016 CONCLUSIONS: SD-208 has significant inhibition effect on human hypertrophic scars, and the mechanism is correlated to the inhibition of protein expression of endogenous TGF-beta1. SD-208 13-19 transforming growth factor beta 1 Homo sapiens 169-178 25333263-5 2014 SD-208, a TGF-beta receptor 1 specific inhibitor, blocks this TGF-beta induced biology. SD-208 0-6 transforming growth factor beta 1 Homo sapiens 10-18 27383203-11 2016 Inhibition of TGF-beta-Smad2/3 signaling with SD-208 significantly attenuated the upregulation of miRNA-181b. SD-208 46-52 transforming growth factor beta 1 Homo sapiens 14-22 27383203-11 2016 Inhibition of TGF-beta-Smad2/3 signaling with SD-208 significantly attenuated the upregulation of miRNA-181b. SD-208 46-52 SMAD family member 3 Homo sapiens 23-30 25747583-0 2015 SD-208, a novel protein kinase D inhibitor, blocks prostate cancer cell proliferation and tumor growth in vivo by inducing G2/M cell cycle arrest. SD-208 0-6 protein kinase D1 Homo sapiens 16-32 25747583-3 2015 In this study, we describe the discovery of a novel PKD small molecule inhibitor, SD-208, from a targeted kinase inhibitor library screen, and the synthesis of a series of analogs to probe the structure-activity relationship (SAR) vs. PKD1. SD-208 82-88 protein kinase D1 Homo sapiens 52-55 25747583-3 2015 In this study, we describe the discovery of a novel PKD small molecule inhibitor, SD-208, from a targeted kinase inhibitor library screen, and the synthesis of a series of analogs to probe the structure-activity relationship (SAR) vs. PKD1. SD-208 82-88 polycystin 1, transient receptor potential channel interacting Homo sapiens 235-239 25747583-4 2015 SD-208 displayed a narrow SAR profile, was an ATP-competitive pan-PKD inhibitor with low nanomolar potency and was cell active. SD-208 0-6 protein kinase D1 Homo sapiens 66-69 25747583-5 2015 Targeted inhibition of PKD by SD-208 resulted in potent inhibition of cell proliferation, an effect that could be reversed by overexpressed PKD1 or PKD3. SD-208 30-36 protein kinase D1 Homo sapiens 23-26 25747583-5 2015 Targeted inhibition of PKD by SD-208 resulted in potent inhibition of cell proliferation, an effect that could be reversed by overexpressed PKD1 or PKD3. SD-208 30-36 polycystin 1, transient receptor potential channel interacting Homo sapiens 140-144 25747583-5 2015 Targeted inhibition of PKD by SD-208 resulted in potent inhibition of cell proliferation, an effect that could be reversed by overexpressed PKD1 or PKD3. SD-208 30-36 PKD3 Homo sapiens 148-152 25747583-7 2015 Mechanistically, SD-208-induced G2/M arrest was accompanied by an increase in levels of p21 in DU145 and PC3 cells as well as elevated phosphorylation of Cdc2 and Cdc25C in DU145 cells. SD-208 17-23 H3 histone pseudogene 16 Homo sapiens 88-91 25747583-7 2015 Mechanistically, SD-208-induced G2/M arrest was accompanied by an increase in levels of p21 in DU145 and PC3 cells as well as elevated phosphorylation of Cdc2 and Cdc25C in DU145 cells. SD-208 17-23 proprotein convertase subtilisin/kexin type 1 Homo sapiens 105-108 25747583-7 2015 Mechanistically, SD-208-induced G2/M arrest was accompanied by an increase in levels of p21 in DU145 and PC3 cells as well as elevated phosphorylation of Cdc2 and Cdc25C in DU145 cells. SD-208 17-23 cyclin dependent kinase 1 Homo sapiens 154-158 25747583-7 2015 Mechanistically, SD-208-induced G2/M arrest was accompanied by an increase in levels of p21 in DU145 and PC3 cells as well as elevated phosphorylation of Cdc2 and Cdc25C in DU145 cells. SD-208 17-23 cell division cycle 25C Homo sapiens 163-169 25747583-8 2015 Most importantly, SD-208 given orally for 24 days significantly abrogated the growth of PC3 subcutaneous tumor xenografts in nude mice, which was accompanied by reduced proliferation and increased apoptosis and decreased expression of PKD biomarkers including survivin and Bcl-xL. SD-208 18-24 proprotein convertase subtilisin/kexin type 1 Mus musculus 88-91 25747583-8 2015 Most importantly, SD-208 given orally for 24 days significantly abrogated the growth of PC3 subcutaneous tumor xenografts in nude mice, which was accompanied by reduced proliferation and increased apoptosis and decreased expression of PKD biomarkers including survivin and Bcl-xL. SD-208 18-24 protein kinase D1 Mus musculus 235-238 25747583-8 2015 Most importantly, SD-208 given orally for 24 days significantly abrogated the growth of PC3 subcutaneous tumor xenografts in nude mice, which was accompanied by reduced proliferation and increased apoptosis and decreased expression of PKD biomarkers including survivin and Bcl-xL. SD-208 18-24 baculoviral IAP repeat-containing 5 Mus musculus 260-268 25747583-8 2015 Most importantly, SD-208 given orally for 24 days significantly abrogated the growth of PC3 subcutaneous tumor xenografts in nude mice, which was accompanied by reduced proliferation and increased apoptosis and decreased expression of PKD biomarkers including survivin and Bcl-xL. SD-208 18-24 BCL2-like 1 Mus musculus 273-279 25747583-9 2015 Our study has identified SD-208 as a novel efficacious PKD small molecule inhibitor, demonstrating the therapeutic potential of targeted inhibition of PKD for prostate cancer treatment. SD-208 25-31 protein kinase D1 Homo sapiens 55-58 25747583-9 2015 Our study has identified SD-208 as a novel efficacious PKD small molecule inhibitor, demonstrating the therapeutic potential of targeted inhibition of PKD for prostate cancer treatment. SD-208 25-31 protein kinase D1 Homo sapiens 151-154 26523217-0 2015 Down-regulation of miR-135b in colon adenocarcinoma induced by a TGF-beta receptor I kinase inhibitor (SD-208). SD-208 103-109 microRNA 135b Homo sapiens 19-27 26523217-0 2015 Down-regulation of miR-135b in colon adenocarcinoma induced by a TGF-beta receptor I kinase inhibitor (SD-208). SD-208 103-109 transforming growth factor beta 1 Homo sapiens 65-73 26523217-11 2015 Our in silico study also predicted that SD-208 could modulate the expression of potential downstream tumor suppressor targets of the miR135b. SD-208 40-46 microRNA 135b Homo sapiens 133-140 26523217-12 2015 CONCLUSION: Our data provide novel evidence that anticancer effects of SD-208 (and likely other TGF-beta inhibitors) may be owing to their ability to regulate miRNAs expression. SD-208 71-77 transforming growth factor beta 1 Homo sapiens 96-104 25982816-2 2015 Our study reveals that the TGFBR1 inhibitor SD208 effectively reduces prostate cancer bone metastases. SD-208 44-49 transforming growth factor beta receptor 1 Homo sapiens 27-33 25333263-5 2014 SD-208, a TGF-beta receptor 1 specific inhibitor, blocks this TGF-beta induced biology. SD-208 0-6 transforming growth factor beta 1 Homo sapiens 62-70 24515103-7 2014 Western blot and morphological analyses indicated that TGF-beta signaling manipulated primordial follicle growth through tuberous sclerosis complex/mTORC1 signaling in oocytes, and the mTORC1-specific inhibitor rapamycin could partially reverse the stimulated effect of SD208 on the oocyte growth and decreased the numbers of growing follicles. SD-208 270-275 transforming growth factor, beta 1 Mus musculus 55-63 24758301-8 2014 Treatment with a TGF-beta type I receptor kinase inhibitor, SD208, recovered AGE3-induced decreases in osterix (P < .001) and osteocalcin (P < .05) and antagonized the AGE3-induced increase in Runx2 mRNA expression in ST2 cells (P < .001). SD-208 60-65 transforming growth factor beta 1 Homo sapiens 17-25 24758301-8 2014 Treatment with a TGF-beta type I receptor kinase inhibitor, SD208, recovered AGE3-induced decreases in osterix (P < .001) and osteocalcin (P < .05) and antagonized the AGE3-induced increase in Runx2 mRNA expression in ST2 cells (P < .001). SD-208 60-65 RUNX family transcription factor 2 Homo sapiens 199-204 24685405-8 2014 SD-208 also abolished the promoting effect of TGF-beta on SMLC proliferation and migration but did not affect TGF-beta inhibition of VSMCs in vitro. SD-208 0-6 transforming growth factor, beta 1 Mus musculus 46-54 24685405-9 2014 CTGF, a protein downstream of TGF-beta, was downregulated with the inhibition of Smad3 phosphorylation by SD-208, both in vitro and in vivo. SD-208 106-112 cellular communication network factor 2 Mus musculus 0-4 24685405-9 2014 CTGF, a protein downstream of TGF-beta, was downregulated with the inhibition of Smad3 phosphorylation by SD-208, both in vitro and in vivo. SD-208 106-112 transforming growth factor, beta 1 Mus musculus 30-38 24685405-9 2014 CTGF, a protein downstream of TGF-beta, was downregulated with the inhibition of Smad3 phosphorylation by SD-208, both in vitro and in vivo. SD-208 106-112 SMAD family member 3 Mus musculus 81-86 24515103-7 2014 Western blot and morphological analyses indicated that TGF-beta signaling manipulated primordial follicle growth through tuberous sclerosis complex/mTORC1 signaling in oocytes, and the mTORC1-specific inhibitor rapamycin could partially reverse the stimulated effect of SD208 on the oocyte growth and decreased the numbers of growing follicles. SD-208 270-275 CREB regulated transcription coactivator 1 Mus musculus 185-191 24368833-6 2014 SD-208, a TGF-beta-receptor-I (TGF-beta-RI) kinase blocker, inhibited p-MyoFb differentiation as shown by stress fibre absence, low alpha-SMA expression, and high proliferation levels. SD-208 0-6 actin gamma 2, smooth muscle Rattus norvegicus 132-141 24425124-6 2014 The effects of GMH and SD208 on the TGF-beta pathway were evaluated by Western blot at day 3. SD-208 23-28 transforming growth factor, beta 1 Rattus norvegicus 36-44 24425124-14 2014 SD208 inhibits GMH-induced activation of the TGF-beta pathway and leads to an improved developmental profile, partial recovery of cognitive and motor functions, and attenuation of GMH-induced brain atrophy and hydrocephalus. SD-208 0-5 transforming growth factor, beta 1 Rattus norvegicus 45-53 22268139-10 2012 A 30-minute pretreatment of SD 208, a TGF-beta receptor-1 kinase inhibitor, prevented Ca(2+) waves from being evoked by TGF-beta. SD-208 28-34 transforming growth factor beta 1 Homo sapiens 38-46 24305807-5 2013 The blockade of TGF-beta receptors by the TGFbetaRI antagonist SD-208 robustly suppressed bone cancer-induced thermal hyperalgesia on post-tumor day 14 (PTD 14). SD-208 63-69 transforming growth factor, beta 1 Rattus norvegicus 16-24 23703870-9 2013 As an in vivo proof of principle, we demonstrate that administration of the TGF-beta receptor 1 (TbetaRI) kinase inhibitor, SD-208, can rescue bone mass deficits and prevent tibial fracture nonunion in Nf1(flox/-) ;Col2.3Cre mice. SD-208 124-130 neurofibromin 1 Mus musculus 202-205 23703870-9 2013 As an in vivo proof of principle, we demonstrate that administration of the TGF-beta receptor 1 (TbetaRI) kinase inhibitor, SD-208, can rescue bone mass deficits and prevent tibial fracture nonunion in Nf1(flox/-) ;Col2.3Cre mice. SD-208 124-130 collagen, type II, alpha 1 Mus musculus 215-219 23725749-7 2013 Moreover, hypoxia induced the phosphorylation of Smad2 and additional treatment with SD-208, an inhibitor of the TGF-beta receptor I kinase, resulted in a dose-dependent downregulation of CD133 and Oct4 in the K562/DOX cells. SD-208 85-91 SMAD family member 2 Homo sapiens 49-54 23725749-7 2013 Moreover, hypoxia induced the phosphorylation of Smad2 and additional treatment with SD-208, an inhibitor of the TGF-beta receptor I kinase, resulted in a dose-dependent downregulation of CD133 and Oct4 in the K562/DOX cells. SD-208 85-91 transforming growth factor beta 1 Homo sapiens 113-121 23725749-7 2013 Moreover, hypoxia induced the phosphorylation of Smad2 and additional treatment with SD-208, an inhibitor of the TGF-beta receptor I kinase, resulted in a dose-dependent downregulation of CD133 and Oct4 in the K562/DOX cells. SD-208 85-91 prominin 1 Homo sapiens 188-193 23725749-7 2013 Moreover, hypoxia induced the phosphorylation of Smad2 and additional treatment with SD-208, an inhibitor of the TGF-beta receptor I kinase, resulted in a dose-dependent downregulation of CD133 and Oct4 in the K562/DOX cells. SD-208 85-91 POU class 5 homeobox 1 Homo sapiens 198-202 22985514-4 2012 The TGF-beta 1 receptor kinase inhibitor SD208 enhances microglial proliferation by IL-34 and suppresses the neuroprotective effect of IL-34-treated microglia. SD-208 41-46 transforming growth factor beta 1 Homo sapiens 4-12 22985514-4 2012 The TGF-beta 1 receptor kinase inhibitor SD208 enhances microglial proliferation by IL-34 and suppresses the neuroprotective effect of IL-34-treated microglia. SD-208 41-46 interleukin 34 Homo sapiens 84-89 22985514-4 2012 The TGF-beta 1 receptor kinase inhibitor SD208 enhances microglial proliferation by IL-34 and suppresses the neuroprotective effect of IL-34-treated microglia. SD-208 41-46 interleukin 34 Homo sapiens 135-140 22542888-4 2012 We found that treatment of pulmonary artery smooth muscle cells with TGF-beta1 significantly increased the expression of 15-LO and levels of 15-hydroxyeicosatetraenoic acid, product of 15-LO, which were inhibited by transforming growth factor-beta receptor I (TGFbetaRI) inhibitor, SD-208 and siRNA targeted to knockdown rat TGFbetaRI. SD-208 282-288 transforming growth factor, beta 1 Rattus norvegicus 69-78 22542888-4 2012 We found that treatment of pulmonary artery smooth muscle cells with TGF-beta1 significantly increased the expression of 15-LO and levels of 15-hydroxyeicosatetraenoic acid, product of 15-LO, which were inhibited by transforming growth factor-beta receptor I (TGFbetaRI) inhibitor, SD-208 and siRNA targeted to knockdown rat TGFbetaRI. SD-208 282-288 transforming growth factor, beta receptor 1 Rattus norvegicus 216-258 22268139-10 2012 A 30-minute pretreatment of SD 208, a TGF-beta receptor-1 kinase inhibitor, prevented Ca(2+) waves from being evoked by TGF-beta. SD-208 28-34 transforming growth factor beta 1 Homo sapiens 120-128 21692070-8 2011 This effect was proportional to the total levels of TGF-beta1 and TGF-beta2 and was blocked by SB-431542 and SD-208, TGF-beta receptor I inhibitors. SD-208 109-115 transforming growth factor beta 1 Homo sapiens 52-61 22844446-9 2012 SD208, a potent TGFbeta Receptor 1 (TGFbetaR1) kinase inhibitor, can efficiently block TGFbeta1/Smad signaling and attenuate EMT induction. SD-208 0-5 transforming growth factor beta 1 Homo sapiens 87-95 21692070-8 2011 This effect was proportional to the total levels of TGF-beta1 and TGF-beta2 and was blocked by SB-431542 and SD-208, TGF-beta receptor I inhibitors. SD-208 109-115 transforming growth factor beta 2 Homo sapiens 66-75 21692070-8 2011 This effect was proportional to the total levels of TGF-beta1 and TGF-beta2 and was blocked by SB-431542 and SD-208, TGF-beta receptor I inhibitors. SD-208 109-115 transforming growth factor beta 1 Homo sapiens 52-60 21880834-6 2011 Use of a TGF-beta(1)-blocking antibody or blockage of TGF-beta(1) receptor kinase activity with SD208 prevented the CsA- and CsA/SRL-induced increase in TER. SD-208 96-101 transforming growth factor beta 1 Homo sapiens 54-64 21880834-6 2011 Use of a TGF-beta(1)-blocking antibody or blockage of TGF-beta(1) receptor kinase activity with SD208 prevented the CsA- and CsA/SRL-induced increase in TER. SD-208 96-101 chorionic somatomammotropin hormone 1 Homo sapiens 116-128 21465486-4 2011 Therefore, we assessed the effect of the disruption of TGF-beta/ALK5/Smad signalling by an ALK5 inhibitor (SD-208) in two experimental animal models of intestinal fibrosis: anaerobic bacteria- and trinitrobenzensulphonic acid-induced colitis. SD-208 107-113 transforming growth factor beta 1 Homo sapiens 55-63 21465486-4 2011 Therefore, we assessed the effect of the disruption of TGF-beta/ALK5/Smad signalling by an ALK5 inhibitor (SD-208) in two experimental animal models of intestinal fibrosis: anaerobic bacteria- and trinitrobenzensulphonic acid-induced colitis. SD-208 107-113 transforming growth factor beta receptor 1 Homo sapiens 64-68 21465486-4 2011 Therefore, we assessed the effect of the disruption of TGF-beta/ALK5/Smad signalling by an ALK5 inhibitor (SD-208) in two experimental animal models of intestinal fibrosis: anaerobic bacteria- and trinitrobenzensulphonic acid-induced colitis. SD-208 107-113 transforming growth factor beta receptor 1 Homo sapiens 91-95 21084275-0 2011 TGF-beta-RI kinase inhibitor SD-208 reduces the development and progression of melanoma bone metastases. SD-208 29-35 transforming growth factor, beta 1 Mus musculus 0-8 21084275-4 2011 In this study, we tested the effect of a small molecule inhibitor of TGF-beta receptor I kinase (TbetaRI), SD-208, on various parameters affecting the development and progression of melanoma, both in vitro and in a mouse model of human melanoma bone metastasis. SD-208 107-113 transforming growth factor, beta receptor I Mus musculus 69-95 21084275-4 2011 In this study, we tested the effect of a small molecule inhibitor of TGF-beta receptor I kinase (TbetaRI), SD-208, on various parameters affecting the development and progression of melanoma, both in vitro and in a mouse model of human melanoma bone metastasis. SD-208 107-113 transforming growth factor, beta receptor I Mus musculus 97-104 18653707-6 2008 SD-208 treatment after MI resulted in a trend for reduced ventricular and renal gene expression of TGF-beta-activated kinase-1 (a downstream modulator of TGF-beta signaling) and a significant decrease in collagen 1, in association with a marked decrease in cardiac mass. SD-208 0-6 mitogen-activated protein kinase kinase kinase 7 Mus musculus 99-126 20858897-7 2010 Furthermore, inhibition of TGFbeta signaling by TGFbeta receptor I inhibitor SD208 significantly reduced tumor area in K14cre/R26SmoM2 mice. SD-208 77-82 transforming growth factor, beta 1 Mus musculus 27-34 20858897-7 2010 Furthermore, inhibition of TGFbeta signaling by TGFbeta receptor I inhibitor SD208 significantly reduced tumor area in K14cre/R26SmoM2 mice. SD-208 77-82 transforming growth factor, beta 1 Mus musculus 48-55 18202349-5 2008 METHODS: We have used an orally active small-molecule TGF-beta receptor I inhibitor, SD-208, to determine the functional role of this pathway in MCT-PH. SD-208 85-91 transforming growth factor beta 1 Homo sapiens 54-62 18474728-5 2008 Pharmacologic inhibition of TBRI (alk5) kinase by a small molecule inhibitor, SD-208, inhibits smad2 activation in hematopoietic progenitors, suppresses TGF-beta-mediated gene activation in BM stromal cells, and reverses TGF-beta-mediated cell-cycle arrest in BM CD34(+) cells. SD-208 78-84 SMAD family member 2 Mus musculus 95-100 18474728-5 2008 Pharmacologic inhibition of TBRI (alk5) kinase by a small molecule inhibitor, SD-208, inhibits smad2 activation in hematopoietic progenitors, suppresses TGF-beta-mediated gene activation in BM stromal cells, and reverses TGF-beta-mediated cell-cycle arrest in BM CD34(+) cells. SD-208 78-84 transforming growth factor, beta 1 Mus musculus 153-161 18474728-5 2008 Pharmacologic inhibition of TBRI (alk5) kinase by a small molecule inhibitor, SD-208, inhibits smad2 activation in hematopoietic progenitors, suppresses TGF-beta-mediated gene activation in BM stromal cells, and reverses TGF-beta-mediated cell-cycle arrest in BM CD34(+) cells. SD-208 78-84 transforming growth factor, beta 1 Mus musculus 221-229 18474728-5 2008 Pharmacologic inhibition of TBRI (alk5) kinase by a small molecule inhibitor, SD-208, inhibits smad2 activation in hematopoietic progenitors, suppresses TGF-beta-mediated gene activation in BM stromal cells, and reverses TGF-beta-mediated cell-cycle arrest in BM CD34(+) cells. SD-208 78-84 CD34 antigen Mus musculus 263-267 18474728-6 2008 Furthermore, SD-208 treatment alleviates anemia and stimulates hematopoiesis in vivo in a novel murine model of bone marrow failure generated by constitutive hepatic expression of TGF-beta1. SD-208 13-19 transforming growth factor, beta 1 Mus musculus 180-189 18202349-9 2008 Inhibition of TGF-beta signaling with SD-208 in established MCT-PH resulted in a small but significant improvement in hemodynamic parameters and medial remodeling. SD-208 38-44 transforming growth factor beta 1 Homo sapiens 14-22 18202349-7 2008 Inhibition of TGF-beta signaling with SD-208 significantly attenuated the development of the PH and reduced pulmonary vascular remodeling. SD-208 38-44 transforming growth factor beta 1 Homo sapiens 14-22 17381068-7 2006 rhTGFbeta1/rhTGFbeta3 induced ALK6 up-regulation was inhibited by SD-208, a TGFbeta type I receptor inhibitor. SD-208 66-72 bone morphogenetic protein receptor type 1B Homo sapiens 30-34 18229422-3 2007 Previously, we reported that treatment of pancreatic cancer cells in vitro with SD-208, a small molecule inhibitor of the TGF-beta receptor I kinase (TGF-betaRI), inhibited expression of genes associated with tumor progression and inhibited invasiveness in a cell-based assay. SD-208 80-86 transforming growth factor beta receptor 1 Homo sapiens 122-148 18229422-3 2007 Previously, we reported that treatment of pancreatic cancer cells in vitro with SD-208, a small molecule inhibitor of the TGF-beta receptor I kinase (TGF-betaRI), inhibited expression of genes associated with tumor progression and inhibited invasiveness in a cell-based assay. SD-208 80-86 transforming growth factor beta receptor 1 Homo sapiens 150-160 17400764-3 2007 In the present study, SD-208, a 2,4-disubstituted pteridine, ATP-competitive inhibitor of the TGFbeta receptor I kinase (TGFbetaRI), was used to inhibit cellular activities and tumor progression of PANC-1, a human pancreatic tumor line. SD-208 22-28 transforming growth factor beta 1 Homo sapiens 94-101 17400764-7 2007 Using a Boyden chamber motility assay, we demonstrated that SD-208 inhibited TGFbeta-stimulated invasion in vitro. SD-208 60-66 transforming growth factor beta 1 Homo sapiens 77-84 17381068-10 2006 The rhGDF5 stimulated SMAD1/5/8 phosphorylation was enhanced by rhTGFbetal/rhTGFbeta3 but inhibited by SD-208. SD-208 103-109 SMAD family member 1 Homo sapiens 22-29 16888081-2 2006 We used an inhibitor of TGF-beta receptor I (TGF-betaRI) kinase, SD-208 (2,4-disubstituted pteridine, a ATP-competitive inhibitor of TGF-betaRI kinase), to determine the role of TGF-beta in airway allergic inflammation and remodeling. SD-208 65-71 transforming growth factor, beta 1 Rattus norvegicus 24-32 16575856-1 2006 OBJECTIVE: To use a specific transforming growth factor beta receptor type I (TGFbetaRI; activin receptor-like kinase 5 [ALK-5]) kinase inhibitor (SD208) to determine the role of activation of the TGFbetaRI kinase (ALK-5) in maintaining the profibrotic phenotype of dermal fibroblasts in systemic sclerosis (SSc). SD-208 147-152 transforming growth factor beta receptor 1 Homo sapiens 29-119 16707625-4 2006 We demonstrated that SD-208, but not SD-282, inhibited TGFbeta-induced SMAD signaling, myofibroblast transformation, and collagen gel contraction. SD-208 21-27 transforming growth factor beta 1 Homo sapiens 55-62 16575856-1 2006 OBJECTIVE: To use a specific transforming growth factor beta receptor type I (TGFbetaRI; activin receptor-like kinase 5 [ALK-5]) kinase inhibitor (SD208) to determine the role of activation of the TGFbetaRI kinase (ALK-5) in maintaining the profibrotic phenotype of dermal fibroblasts in systemic sclerosis (SSc). SD-208 147-152 transforming growth factor beta receptor 1 Homo sapiens 78-87 15708853-5 2005 Using a specific inhibitor (SD-208) we demonstrate that the abnormal phenotype of these cells is dependent upon TbetaRI kinase (ALK5) activity, and that transgenic fibroblasts show enhanced expression and activation of TGFbeta together with increased levels of wild type TbetaRII. SD-208 28-34 transforming growth factor, beta receptor I Mus musculus 128-132 15708853-5 2005 Using a specific inhibitor (SD-208) we demonstrate that the abnormal phenotype of these cells is dependent upon TbetaRI kinase (ALK5) activity, and that transgenic fibroblasts show enhanced expression and activation of TGFbeta together with increased levels of wild type TbetaRII. SD-208 28-34 transforming growth factor, beta 1 Mus musculus 219-226 15708853-5 2005 Using a specific inhibitor (SD-208) we demonstrate that the abnormal phenotype of these cells is dependent upon TbetaRI kinase (ALK5) activity, and that transgenic fibroblasts show enhanced expression and activation of TGFbeta together with increased levels of wild type TbetaRII. SD-208 28-34 transforming growth factor, beta receptor II Mus musculus 271-279 15569984-6 2004 RESULTS: SD-208 significantly inhibits not only transcription but also secretion of both IL-6 and VEGF from BMSCs triggered by either TGF-beta1 or adhesion of MM cells to BMSCs. SD-208 9-15 transforming growth factor beta 1 Homo sapiens 134-143 35050457-14 2022 Compared to the 10 nM DHT + 5 pM E2 group, the expressions of collagen I and fibronectin were decreased; the expression of elastin was increased in WPMY-1 cells after the supplement of TGF-beta/Smad pathway inhibitor SD208 group (p < 0.05, p < 0.01). SD-208 217-222 elastin Homo sapiens 123-130 15569984-3 2004 We show here that the TGF-beta receptor I kinase inhibitor SD-208 significantly decreases secretion of both IL-6 and vascular endothelial growth factor (VEGF) from BMSCs, as well as tumor cell growth triggered by MM cell adhesion to BMSCs. SD-208 59-65 interleukin 6 Homo sapiens 108-112 15569984-3 2004 We show here that the TGF-beta receptor I kinase inhibitor SD-208 significantly decreases secretion of both IL-6 and vascular endothelial growth factor (VEGF) from BMSCs, as well as tumor cell growth triggered by MM cell adhesion to BMSCs. SD-208 59-65 vascular endothelial growth factor A Homo sapiens 117-151 15569984-3 2004 We show here that the TGF-beta receptor I kinase inhibitor SD-208 significantly decreases secretion of both IL-6 and vascular endothelial growth factor (VEGF) from BMSCs, as well as tumor cell growth triggered by MM cell adhesion to BMSCs. SD-208 59-65 vascular endothelial growth factor A Homo sapiens 153-157 15569984-5 2004 Effects of SD-208 on TGF-beta1-induced signaling pathways triggering IL-6 and VEGF transcription in BMSCs were also delineated. SD-208 11-17 transforming growth factor beta 1 Homo sapiens 21-30 15569984-5 2004 Effects of SD-208 on TGF-beta1-induced signaling pathways triggering IL-6 and VEGF transcription in BMSCs were also delineated. SD-208 11-17 interleukin 6 Homo sapiens 69-73 15569984-6 2004 RESULTS: SD-208 significantly inhibits not only transcription but also secretion of both IL-6 and VEGF from BMSCs triggered by either TGF-beta1 or adhesion of MM cells to BMSCs. SD-208 9-15 interleukin 6 Homo sapiens 89-93 15569984-6 2004 RESULTS: SD-208 significantly inhibits not only transcription but also secretion of both IL-6 and VEGF from BMSCs triggered by either TGF-beta1 or adhesion of MM cells to BMSCs. SD-208 9-15 vascular endothelial growth factor A Homo sapiens 98-102 15520202-2 2004 Here we characterize the effects of a novel TGF-beta receptor (TGF-betaR) I kinase inhibitor, SD-208, on the growth and immunogenicity of murine SMA-560 and human LN-308 glioma cells in vitro and the growth of and immune response to intracranial SMA-560 gliomas in syngeneic VM/Dk mice in vivo. SD-208 94-100 transforming growth factor beta 1 Homo sapiens 44-52 15520202-5 2004 Peripheral blood lymphocytes or purified T cells, cocultured with TGF-beta-releasing LN-308 glioma cells in the presence of SD-208, exhibit enhanced lytic activity against LN-308 targets. SD-208 124-130 transforming growth factor beta 1 Homo sapiens 66-74 15520202-7 2004 SD-208 restores the lytic activity of polyclonal natural killer cells against glioma cells in the presence of recombinant TGF-beta or of TGF-beta-containing glioma cell supernatant. SD-208 0-6 transforming growth factor beta 1 Homo sapiens 122-130 15520202-7 2004 SD-208 restores the lytic activity of polyclonal natural killer cells against glioma cells in the presence of recombinant TGF-beta or of TGF-beta-containing glioma cell supernatant. SD-208 0-6 transforming growth factor beta 1 Homo sapiens 137-145 15520202-8 2004 The oral bioavailability of SD-208 was verified by demonstrating the inhibition of TGF-beta-induced Smad phosphorylation in spleen and brain. SD-208 28-34 transforming growth factor beta 1 Homo sapiens 83-91 15520202-12 2004 These data define TGF-beta receptor I kinase inhibitors such as SD-208 as promising novel agents for the treatment of human malignant glioma and other conditions associated with pathological TGF-beta activity. SD-208 64-70 transforming growth factor beta 1 Homo sapiens 18-26 15520202-12 2004 These data define TGF-beta receptor I kinase inhibitors such as SD-208 as promising novel agents for the treatment of human malignant glioma and other conditions associated with pathological TGF-beta activity. SD-208 64-70 transforming growth factor beta 1 Homo sapiens 191-199 34373217-6 2021 Importantly, inhibition of the TGF-beta signaling through ectopic expression of dominant-negative Tgfbr2 (Tgfbr2-DN) or treatment with Tgfbr1 inhibitor SD-208 consistently abrogated tumor metastasis in nude mouse allograft assays. SD-208 152-158 transforming growth factor alpha Mus musculus 31-39 34373217-6 2021 Importantly, inhibition of the TGF-beta signaling through ectopic expression of dominant-negative Tgfbr2 (Tgfbr2-DN) or treatment with Tgfbr1 inhibitor SD-208 consistently abrogated tumor metastasis in nude mouse allograft assays. SD-208 152-158 transforming growth factor, beta receptor I Mus musculus 135-141 34504485-9 2021 Pharmacological blockade of the TGF-beta signalling pathway with SD208 (TGF-beta receptor type I inhibitor), SIS3 (Smad3 inhibitor) or (5Z)-7-oxozeaenol (TGF-beta-activated kinase 1 inhibitor) ameliorated fibronectin levels and type I collagen secretion. SD-208 65-70 transforming growth factor alpha Homo sapiens 32-40 34504485-9 2021 Pharmacological blockade of the TGF-beta signalling pathway with SD208 (TGF-beta receptor type I inhibitor), SIS3 (Smad3 inhibitor) or (5Z)-7-oxozeaenol (TGF-beta-activated kinase 1 inhibitor) ameliorated fibronectin levels and type I collagen secretion. SD-208 65-70 fibronectin 1 Homo sapiens 205-216 35050457-14 2022 Compared to the 10 nM DHT + 5 pM E2 group, the expressions of collagen I and fibronectin were decreased; the expression of elastin was increased in WPMY-1 cells after the supplement of TGF-beta/Smad pathway inhibitor SD208 group (p < 0.05, p < 0.01). SD-208 217-222 transforming growth factor alpha Homo sapiens 185-193 35050457-14 2022 Compared to the 10 nM DHT + 5 pM E2 group, the expressions of collagen I and fibronectin were decreased; the expression of elastin was increased in WPMY-1 cells after the supplement of TGF-beta/Smad pathway inhibitor SD208 group (p < 0.05, p < 0.01). SD-208 217-222 SMAD family member 7 Homo sapiens 194-198 33427061-3 2021 TGFB1-receptor antagonist SD-208 prevents increases of beta6-integrin, TGFB1-SMAD signaling and PDGFB/CTGF expression after IRI, and ameliorates fibrosis (Am J Pathol 174:1291, 2009; Am J Pathol 181:1236, 2012). SD-208 26-32 transforming growth factor beta 1 Homo sapiens 0-5 34013984-7 2021 This inhibitory effect of TGFbeta1 on healthy hematopoiesis was functionally corrobated and could be pharmacologically reverted by SD208, an inhibitor of TGFbeta receptor 1 signaling. SD-208 131-136 transforming growth factor beta 1 Homo sapiens 26-34 33427061-3 2021 TGFB1-receptor antagonist SD-208 prevents increases of beta6-integrin, TGFB1-SMAD signaling and PDGFB/CTGF expression after IRI, and ameliorates fibrosis (Am J Pathol 174:1291, 2009; Am J Pathol 181:1236, 2012). SD-208 26-32 transforming growth factor beta 1 Homo sapiens 71-76 33427061-3 2021 TGFB1-receptor antagonist SD-208 prevents increases of beta6-integrin, TGFB1-SMAD signaling and PDGFB/CTGF expression after IRI, and ameliorates fibrosis (Am J Pathol 174:1291, 2009; Am J Pathol 181:1236, 2012). SD-208 26-32 platelet derived growth factor subunit B Homo sapiens 96-101 33427061-3 2021 TGFB1-receptor antagonist SD-208 prevents increases of beta6-integrin, TGFB1-SMAD signaling and PDGFB/CTGF expression after IRI, and ameliorates fibrosis (Am J Pathol 174:1291, 2009; Am J Pathol 181:1236, 2012). SD-208 26-32 cellular communication network factor 2 Homo sapiens 102-106 33427061-8 2021 Remarkably, TGFB1 receptor antagonist SD-208 prevented all of these abnormalities excepting increased LPA2. SD-208 38-44 transforming growth factor beta 1 Homo sapiens 12-17 33427061-8 2021 Remarkably, TGFB1 receptor antagonist SD-208 prevented all of these abnormalities excepting increased LPA2. SD-208 38-44 lysophosphatidic acid receptor 2 Homo sapiens 102-106 33427061-9 2021 SD208 inhibits only one arm of LPA signaling: LPA2-Galphaq-alphavbeta6-integrin dependent production of active TGFB1 and its receptor-bound downstream effects. SD-208 0-5 lysophosphatidic acid receptor 2 Homo sapiens 46-50 33427061-9 2021 SD208 inhibits only one arm of LPA signaling: LPA2-Galphaq-alphavbeta6-integrin dependent production of active TGFB1 and its receptor-bound downstream effects. SD-208 0-5 transforming growth factor beta 1 Homo sapiens 111-116 33427061-12 2021 SD208 effects may also involve mitigation of injury caused by IRI-induced TGFB1 signaling in endothelial cells and monocytes. SD-208 0-5 transforming growth factor beta 1 Homo sapiens 74-79 31829243-9 2019 RESULTS: TGFbeta-1 was induced in cultures expressing Nef at 24 h followed by CCL2 induction which was prevented by blocking TGFbetaRI with SD208 (competitive inhibitor). SD-208 140-145 transforming growth factor, beta 1 Rattus norvegicus 9-18 32443848-6 2020 Fibrotic phenotype of cardiac microtissues was inhibited by treatment with TGF-beta-receptor type 1 inhibitor SD208 in a dose-dependent manner. SD-208 110-115 transforming growth factor beta receptor 1 Homo sapiens 75-99 32317146-11 2021 Smad signal transduction activation was significantly down-regulated by Bindarit (300 muM) and/or SD208 (1 muM) with TGF-beta1 compared to vehicle control with TGF-beta1. SD-208 98-103 transforming growth factor beta 1 Homo sapiens 117-126 32317146-11 2021 Smad signal transduction activation was significantly down-regulated by Bindarit (300 muM) and/or SD208 (1 muM) with TGF-beta1 compared to vehicle control with TGF-beta1. SD-208 98-103 transforming growth factor beta 1 Homo sapiens 160-169 32303620-9 2020 Blockade of TGF-beta-receptor signaling with the specific kinase inhibitor SD-208 was able to protect CD8+ and CD4+ ROR1-CAR T-cells from the inhibitory effect of TGF-beta, and sustained their antitumor function in vitro and in the microphysiologic 3D tumor model. SD-208 75-81 CD8a molecule Homo sapiens 102-105 32303620-9 2020 Blockade of TGF-beta-receptor signaling with the specific kinase inhibitor SD-208 was able to protect CD8+ and CD4+ ROR1-CAR T-cells from the inhibitory effect of TGF-beta, and sustained their antitumor function in vitro and in the microphysiologic 3D tumor model. SD-208 75-81 CD4 molecule Homo sapiens 111-114 32303620-9 2020 Blockade of TGF-beta-receptor signaling with the specific kinase inhibitor SD-208 was able to protect CD8+ and CD4+ ROR1-CAR T-cells from the inhibitory effect of TGF-beta, and sustained their antitumor function in vitro and in the microphysiologic 3D tumor model. SD-208 75-81 receptor tyrosine kinase like orphan receptor 1 Homo sapiens 116-120 32303620-9 2020 Blockade of TGF-beta-receptor signaling with the specific kinase inhibitor SD-208 was able to protect CD8+ and CD4+ ROR1-CAR T-cells from the inhibitory effect of TGF-beta, and sustained their antitumor function in vitro and in the microphysiologic 3D tumor model. SD-208 75-81 nuclear receptor subfamily 1 group I member 3 Homo sapiens 121-124 32303620-9 2020 Blockade of TGF-beta-receptor signaling with the specific kinase inhibitor SD-208 was able to protect CD8+ and CD4+ ROR1-CAR T-cells from the inhibitory effect of TGF-beta, and sustained their antitumor function in vitro and in the microphysiologic 3D tumor model. SD-208 75-81 transforming growth factor alpha Homo sapiens 12-20 32303620-10 2020 Combination treatment with SD-208 also led to increased viability and lower expression of PD-1 on ROR1-CAR T-cells at the end of the antitumor response. SD-208 27-33 MHC class I antigen 1 Sus scrofa 90-94 32303620-10 2020 Combination treatment with SD-208 also led to increased viability and lower expression of PD-1 on ROR1-CAR T-cells at the end of the antitumor response. SD-208 27-33 receptor tyrosine kinase like orphan receptor 1 Sus scrofa 98-102 32303620-10 2020 Combination treatment with SD-208 also led to increased viability and lower expression of PD-1 on ROR1-CAR T-cells at the end of the antitumor response. SD-208 27-33 CXADR Ig-like cell adhesion molecule Sus scrofa 103-106 32303620-12 2020 Our study supports the continued preclinical development and the clinical evaluation of combination treatments that shield CAR T-cells from TGF-beta, as exemplified by the TGF-beta-receptor kinase inhibitor SD-208 in this study. SD-208 207-213 CXADR Ig-like cell adhesion molecule Sus scrofa 123-126 32303620-12 2020 Our study supports the continued preclinical development and the clinical evaluation of combination treatments that shield CAR T-cells from TGF-beta, as exemplified by the TGF-beta-receptor kinase inhibitor SD-208 in this study. SD-208 207-213 transforming growth factor alpha Sus scrofa 140-148 32303620-12 2020 Our study supports the continued preclinical development and the clinical evaluation of combination treatments that shield CAR T-cells from TGF-beta, as exemplified by the TGF-beta-receptor kinase inhibitor SD-208 in this study. SD-208 207-213 transforming growth factor alpha Sus scrofa 172-180 31829243-9 2019 RESULTS: TGFbeta-1 was induced in cultures expressing Nef at 24 h followed by CCL2 induction which was prevented by blocking TGFbetaRI with SD208 (competitive inhibitor). SD-208 140-145 C-C motif chemokine ligand 2 Rattus norvegicus 78-82 31829243-12 2019 Brain tissue from Nef-treated rats given SD208 showed reduced CCL2, phospho-SMAD2, cluster of differentiation 163 (CD163), and GFAP immunoreactivity compared to the placebo group. SD-208 41-46 C-C motif chemokine ligand 2 Rattus norvegicus 62-66 31829243-12 2019 Brain tissue from Nef-treated rats given SD208 showed reduced CCL2, phospho-SMAD2, cluster of differentiation 163 (CD163), and GFAP immunoreactivity compared to the placebo group. SD-208 41-46 SMAD family member 2 Rattus norvegicus 76-81 31829243-12 2019 Brain tissue from Nef-treated rats given SD208 showed reduced CCL2, phospho-SMAD2, cluster of differentiation 163 (CD163), and GFAP immunoreactivity compared to the placebo group. SD-208 41-46 glial fibrillary acidic protein Rattus norvegicus 127-131 31829243-14 2019 In contrast, rats treated with Nef + SD208 showed better spatial learning suggesting that Nef disrupts memory formation in a TGFbeta-1-dependent manner. SD-208 37-42 transforming growth factor, beta 1 Rattus norvegicus 125-134 31442332-8 2019 We also discovered that SD-208 promoted osteoblastic differentiation (and overcame the TGFbeta-induced block in osteoblastogenesis) in myeloma patient bone marrow stromal cells in vitro, comparable to normal donors. SD-208 24-30 transforming growth factor beta 1 Homo sapiens 87-94 29773599-6 2018 These suppressive effects of transforming growth factor beta1 on stromal cell functionality were abrogated by SD-208, an established inhibitor of transforming growth factor beta receptor signaling. SD-208 110-116 potassium calcium-activated channel subfamily M regulatory beta subunit 1 Homo sapiens 56-61 31240740-6 2019 This sustained enhancement by TGF-beta1 could be blocked by extracellular treatment of selective TGF-beta receptor I antagonist SD-208, and abolished by blockade of intracellular several non-Smad-signaling pathways. SD-208 128-134 transforming growth factor, beta 1 Rattus norvegicus 30-39 29773599-8 2018 Our findings establish transforming growth factor beta1 as a relevant trigger causing functional inhibition of mesenchymal stromal cells in myelodysplastic syndromes and acute myeloid leukemia and identify SD-208 as a candidate to revert these effects. SD-208 206-212 potassium calcium-activated channel subfamily M regulatory beta subunit 1 Homo sapiens 50-55 28229177-7 2017 To block TGF-beta signaling, we used SD208, a TGF-beta type I receptor kinase inhibitor. SD-208 37-42 transforming growth factor, beta 1 Mus musculus 9-17 28229177-7 2017 To block TGF-beta signaling, we used SD208, a TGF-beta type I receptor kinase inhibitor. SD-208 37-42 transforming growth factor, beta 1 Mus musculus 46-54