Detalhe da pesquisa
1.
Defining a therapeutic window for the novel TGF-ß inhibitor LY2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model.
Br J Clin Pharmacol
; 77(5): 796-807, 2014 May.
Artigo
em Inglês
| MEDLINE | ID: mdl-24868575
2.
Targeting the Transforming Growth Factor-beta pathway inhibits human basal-like breast cancer metastasis.
Mol Cancer
; 9: 122, 2010 May 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-20504320
3.
Developing and applying a gene functional association network for anti-angiogenic kinase inhibitor activity assessment in an angiogenesis co-culture model.
BMC Genomics
; 9: 264, 2008 Jun 02.
Artigo
em Inglês
| MEDLINE | ID: mdl-18518970
4.
Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice.
Eur J Cancer
; 44(1): 142-50, 2008 Jan.
Artigo
em Inglês
| MEDLINE | ID: mdl-18039567
5.
Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.
J Med Chem
; 51(7): 2302-6, 2008 Apr 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-18314943
6.
Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-ß receptor type I inhibitor.
Oncotarget
; 9(6): 6659-6677, 2018 Jan 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-29467918
7.
Analysis of pathway activity in primary tumors and NCI60 cell lines using gene expression profiling data.
Genomics Proteomics Bioinformatics
; 5(1): 15-24, 2007 Feb.
Artigo
em Inglês
| MEDLINE | ID: mdl-17572360
8.
Development of TGF-beta signalling inhibitors for cancer therapy.
Nat Rev Drug Discov
; 3(12): 1011-22, 2004 Dec.
Artigo
em Inglês
| MEDLINE | ID: mdl-15573100
9.
Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
J Med Chem
; 49(6): 2138-42, 2006 Mar 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-16539403
10.
Transforming the TGFbeta pathway: convergence of distinct lead generation strategies on a novel kinase pharmacophore for TbetaRI (ALK5).
Curr Opin Drug Discov Devel
; 7(4): 437-45, 2004 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-15338953
11.
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
J Med Chem
; 46(19): 3953-6, 2003 Sep 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-12954047
12.
Effect of transforming growth factor beta (TGF-ß) receptor I kinase inhibitor on prostate cancer bone growth.
Bone
; 50(3): 695-703, 2012 Mar.
Artigo
em Inglês
| MEDLINE | ID: mdl-22173053
13.
LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-ß and BMP-associated proinflammatory and proangiogenic signals.
Clin Cancer Res
; 18(13): 3616-27, 2012 Jul 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-22547771
14.
Outgrowth of drug-resistant carcinomas expressing markers of tumor aggression after long-term TßRI/II kinase inhibition with LY2109761.
Cancer Res
; 71(6): 2339-49, 2011 Mar 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-21282335
15.
Therapeutic inhibition of MAP kinase interacting kinase blocks eukaryotic initiation factor 4E phosphorylation and suppresses outgrowth of experimental lung metastases.
Cancer Res
; 71(5): 1849-57, 2011 Mar 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-21233335
16.
Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase.
Cancer Res
; 71(3): 955-63, 2011 Feb 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-21189329
17.
Smad7 regulates the adult neural stem/progenitor cell pool in a transforming growth factor beta- and bone morphogenetic protein-independent manner.
Mol Cell Biol
; 30(14): 3685-94, 2010 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-20479122
18.
TGF-ß Receptor Inhibitors Target the CD44(high)/Id1(high) Glioma-Initiating Cell Population in Human Glioblastoma.
Cancer Cell
; 18(6): 655-68, 2010 Dec 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-21156287
19.
Cancer-associated transforming growth factor beta type II receptor gene mutant causes activation of bone morphogenic protein-Smads and invasive phenotype.
Cancer Res
; 68(6): 1656-66, 2008 Mar 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-18339844
20.
Analysis and variability of TGFbeta measurements in cancer patients with skeletal metastases.
Biologics
; 2(3): 563-9, 2008 Sep.
Artigo
em Inglês
| MEDLINE | ID: mdl-19707386