SB-431542 Is a Potent and Specific Inhibitor of Transforming Growth Factor-β Superfamily Type I Activin Receptor-Like Kinase (ALK) Receptors ALK4, ALK5, and ALK7

Molecular Pharmacology - Tập 62 Số 1 - Trang 65-74 - 2002
Gareth J. Inman1,2,3,4,5, Francisco José Nicolás1,2,3,4,5, James F. Callahan1,2,3,4,5, John D. Harling1,2,3,4,5, Laramie M. Gaster1,2,3,4,5, Alastair D. Reith1,2,3,4,5, Nicholas J. Laping1,2,3,4,5, Caroline S. Hill1,2,3,4,5
11Laboratory of Developmental Signalling, Cancer Research UK London Research Institute, Lincoln's Inn Fields Laboratories, London, UK (G.J.I., F.J.N., C.S.H.)
22Department of Medicinal Chemistry, GlaxoSmithKline Pharmaceuticals, Collegeville, Pennsylvania (J.F.C.)
33Department of Medicinal Chemistry, GlaxoSmithKline Pharmaceuticals, Stevenage, Hertfordshire, UK (J.D.H.)
44Department of High-Throughput Chemistry (L.M.G.) and 5High-Throughput Biology (A.D.R.), GlaxoSmithKline Pharmaceuticals, Harlow, Essex, UK
56Renal and Urology Research, GlaxoSmithKline Pharmaceuticals, King of Prussia, Pennsylvania (N.J.L.)

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Tài liệu tham khảo

Armes, 1997, The ALK-2 and ALK-4 activin receptors transduce distinct mesoderm-inducing signals during early Xenopus development but do not cooperate to establish thresholds., Development, 124, 3797, 10.1242/dev.124.19.3797

Attisano, 1996, Activation of signalling by the activin receptor complex., Mol Cell Biol, 16, 1066, 10.1128/MCB.16.3.1066

10.1101/gad.8.14.1664

10.1128/MCB.20.23.9018-9027.2000

10.1056/NEJM200005043421807

10.1016/S0960-9822(01)00167-1

10.1021/jm010493y

10.1074/jbc.M010768200

10.1016/S0092-8674(00)00116-1

10.1093/emboj/17.11.3091

10.1016/0092-8674(94)90380-8

Faure, 2000, Endogenous patterns of TGFβ superfamily signaling during early Xenopus development., Development, 127, 2917, 10.1242/dev.127.13.2917

10.1074/jbc.273.29.18623

Germain, 2000, Homeodomain and winged-helix transcription factors recruit activated Smads to distinct promoter elements via a common Smad interaction motif., Genes Dev, 14, 435, 10.1101/gad.14.4.435

10.1074/jbc.M102678200

10.1074/jbc.M002704200

10.1074/jbc.274.38.27161

10.1016/0092-8674(93)90238-L

10.1016/S0092-8674(05)80020-0

10.1074/jbc.M005200200

10.1074/jbc.273.30.18793

10.1124/mol.62.1.58

10.1074/jbc.273.40.25628

10.1016/0092-8674(93)90237-K

10.1016/S0092-8674(00)00121-5

10.1101/gad.14.6.627

10.1093/emboj/19.8.1745

Mohun, 1987, Xenopus cytoskeletal actin and human c-fos gene promoters share a conserved protein-binding site., EMBO (Eur Mol Biol Organ) J, 6, 667, 10.1002/j.1460-2075.1987.tb04806.x

10.1093/emboj/16.17.5353

10.1016/S0968-0004(00)01595-4

10.1073/pnas.97.6.2626

Piek, 1999, Specificity, diversity and regulation in TGF-β superfamily signaling., FASEB J, 13, 2105, 10.1096/fasebj.13.15.2105

10.1128/MCB.20.23.9041-9054.2000

Price, 1996, The p38 and ERK MAP kinase pathways cooperate to activate ternary complex factors and c-fos transcription in response to UV light., EMBO (Eur Mol Biol Organ) J, 15, 6552, 10.1002/j.1460-2075.1996.tb01046.x

Price, 1995, Comparative analysis of the ternary complex factors Elk-1, SAP-1a and SAP-2 (ERP/NET)., EMBO (Eur Mol Biol Organ) J, 14, 2589, 10.1002/j.1460-2075.1995.tb07257.x

Raingeaud, 1996, MKK3- and MKK6-regulated gene expression is mediated by the p38 mitogen-activated protein kinase signal transduction pathway., Mol Cell Biol, 16, 1247, 10.1128/MCB.16.3.1247

10.1101/gad.201801

10.3109/08977199309029129

10.1016/S0092-8674(00)81011-9

10.1126/science.8140412

10.1101/gad.12.16.2445

Wieser, 1995, GS domain mutations that constitutively activate TβR-I, the downstream signaling component in the TGF-β receptor complex., EMBO (Eur Mol Biol Organ) J, 14, 2199, 10.1002/j.1460-2075.1995.tb07214.x