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Items: 1 to 20 of 131

1.

SM16, an orally active TGF-beta type I receptor inhibitor prevents myofibroblast induction and vascular fibrosis in the rat carotid injury model.

Fu K, Corbley MJ, Sun L, Friedman JE, Shan F, Papadatos JL, Costa D, Lutterodt F, Sweigard H, Bowes S, Choi M, Boriack-Sjodin PA, Arduini RM, Sun D, Newman MN, Zhang X, Mead JN, Chuaqui CE, Cheung HK, Zhang X, Cornebise M, Carter MB, Josiah S, Singh J, Lee WC, Gill A, Ling LE.

Arterioscler Thromb Vasc Biol. 2008 Apr;28(4):665-71. doi: 10.1161/ATVBAHA.107.158030. Epub 2008 Jan 17.

2.

Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis.

Grygielko ET, Martin WM, Tweed C, Thornton P, Harling J, Brooks DP, Laping NJ.

J Pharmacol Exp Ther. 2005 Jun;313(3):943-51. Epub 2005 Mar 15.

3.

Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis.

Higashiyama H, Yoshimoto D, Kaise T, Matsubara S, Fujiwara M, Kikkawa H, Asano S, Kinoshita M.

Exp Mol Pathol. 2007 Aug;83(1):39-46. Epub 2006 Dec 24.

PMID:
17274978
4.
5.

Attenuated development of cardiac fibrosis in left ventricular pressure overload by SM16, an orally active inhibitor of ALK5.

Engebretsen KV, Skårdal K, Bjørnstad S, Marstein HS, Skrbic B, Sjaastad I, Christensen G, Bjørnstad JL, Tønnessen T.

J Mol Cell Cardiol. 2014 Nov;76:148-57. doi: 10.1016/j.yjmcc.2014.08.008. Epub 2014 Aug 26.

PMID:
25169971
6.

SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7.

DaCosta Byfield S, Major C, Laping NJ, Roberts AB.

Mol Pharmacol. 2004 Mar;65(3):744-52.

7.

Progressive transforming growth factor beta1-induced lung fibrosis is blocked by an orally active ALK5 kinase inhibitor.

Bonniaud P, Margetts PJ, Kolb M, Schroeder JA, Kapoun AM, Damm D, Murphy A, Chakravarty S, Dugar S, Higgins L, Protter AA, Gauldie J.

Am J Respir Crit Care Med. 2005 Apr 15;171(8):889-98. Epub 2004 Nov 24.

PMID:
15563636
8.

An orally active small molecule TGF-beta receptor I antagonist inhibits the growth of metastatic murine breast cancer.

Rausch MP, Hahn T, Ramanathapuram L, Bradley-Dunlop D, Mahadevan D, Mercado-Pimentel ME, Runyan RB, Besselsen DG, Zhang X, Cheung HK, Lee WC, Ling LE, Akporiaye ET.

Anticancer Res. 2009 Jun;29(6):2099-109.

9.
10.

Cell-specific delivery of a transforming growth factor-beta type I receptor kinase inhibitor to proximal tubular cells for the treatment of renal fibrosis.

Prakash J, de Borst MH, van Loenen-Weemaes AM, Lacombe M, Opdam F, van Goor H, Meijer DK, Moolenaar F, Poelstra K, Kok RJ.

Pharm Res. 2008 Oct;25(10):2427-39. doi: 10.1007/s11095-007-9515-x. Epub 2008 Jan 9.

PMID:
18183478
11.

Small molecular inhibitor of transforming growth factor-beta protects against development of radiation-induced lung injury.

Anscher MS, Thrasher B, Zgonjanin L, Rabbani ZN, Corbley MJ, Fu K, Sun L, Lee WC, Ling LE, Vujaskovic Z.

Int J Radiat Oncol Biol Phys. 2008 Jul 1;71(3):829-37. doi: 10.1016/j.ijrobp.2008.02.046. Epub 2008 Apr 12.

PMID:
18411002
12.

Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.

Gellibert F, de Gouville AC, Woolven J, Mathews N, Nguyen VL, Bertho-Ruault C, Patikis A, Grygielko ET, Laping NJ, Huet S.

J Med Chem. 2006 Apr 6;49(7):2210-21.

PMID:
16570917
13.

The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta.

Tojo M, Hamashima Y, Hanyu A, Kajimoto T, Saitoh M, Miyazono K, Node M, Imamura T.

Cancer Sci. 2005 Nov;96(11):791-800.

14.

Transforming growth factor-beta receptor type 1 (TGFbetaRI) kinase activity but not p38 activation is required for TGFbetaRI-induced myofibroblast differentiation and profibrotic gene expression.

Kapoun AM, Gaspar NJ, Wang Y, Damm D, Liu YW, O'young G, Quon D, Lam A, Munson K, Tran TT, Ma JY, Murphy A, Dugar S, Chakravarty S, Protter AA, Wen FQ, Liu X, Rennard SI, Higgins LS.

Mol Pharmacol. 2006 Aug;70(2):518-31. Epub 2006 May 17.

15.

The expression of CSRP2 encoding the LIM domain protein CRP2 is mediated by TGF-beta in smooth muscle and hepatic stellate cells.

Herrmann J, Borkham-Kamphorst E, Haas U, Van de Leur E, Fraga MF, Esteller M, Gressner AM, Weiskirchen R.

Biochem Biophys Res Commun. 2006 Jul 14;345(4):1526-35. Epub 2006 May 22.

PMID:
16735029
16.

Perivascular gene transfer of dominant-negative N19RhoA attenuates neointimal formation via inhibition of TGF-beta1-Smad2 signaling in rats after carotid artery balloon injury.

Chen W, Chu Y, Zhu D, Yan C, Liu J, Ji K, Gao P.

Biochem Biophys Res Commun. 2009 Nov 13;389(2):217-23. doi: 10.1016/j.bbrc.2009.08.104. Epub 2009 Aug 23.

PMID:
19706289
17.

Inhibition of ALK5 as a new approach to treat liver fibrotic diseases.

de Gouville AC, Huet S.

Drug News Perspect. 2006 Mar;19(2):85-90. Review.

PMID:
16628263
18.

Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).

Li X, Wang L, Long L, Xiao J, Hu Y, Li S.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4868-72. doi: 10.1016/j.bmcl.2009.04.066. Epub 2009 Apr 20.

PMID:
19616940
19.

Antitumor activity of TGF-beta inhibitor is dependent on the microenvironment.

Medicherla S, Li L, Ma JY, Kapoun AM, Gaspar NJ, Liu YW, Mangadu R, O'Young G, Protter AA, Schreiner GF, Wong DH, Higgins LS.

Anticancer Res. 2007 Nov-Dec;27(6B):4149-57. Erratum in: Anticancer Res. 2008 Jan-Feb;28(1b):567, 4152-3.

20.

Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5).

Goldberg FW, Ward RA, Powell SJ, Debreczeni JE, Norman RA, Roberts NJ, Dishington AP, Gingell HJ, Wickson KF, Roberts AL.

J Med Chem. 2009 Dec 10;52(23):7901-5. doi: 10.1021/jm900807w.

PMID:
19736928

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