Literature DB >> 16134929

Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.

Mark Wittman1, Joan Carboni, Ricardo Attar, Balu Balasubramanian, Praveen Balimane, Patrick Brassil, Francis Beaulieu, Chiehying Chang, Wendy Clarke, Janet Dell, Jeffrey Eummer, David Frennesson, Marco Gottardis, Ann Greer, Steven Hansel, Warren Hurlburt, Bruce Jacobson, Subramaniam Krishnananthan, Francis Y Lee, Aixin Li, Tai-An Lin, Peiying Liu, Carl Ouellet, Xiaopeng Sang, Mark G Saulnier, Karen Stoffan, Yax Sun, Upender Velaparthi, Henry Wong, Zheng Yang, Kurt Zimmermann, Mary Zoeckler, Dolatrai Vyas.   

Abstract

Compound 3 (BMS-536924), a novel small-molecule inhibitor of the insulin-like growth factor receptor kinase with equal potency against the insulin receptor is described. The in vitro and in vivo biological activity of this interesting compound is also reported.

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Year:  2005        PMID: 16134929     DOI: 10.1021/jm050392q

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  36 in total

1.  A monoclonal antibody against alphaVbeta3 integrin inhibits development of atherosclerotic lesions in diabetic pigs.

Authors:  Laura A Maile; Walker H Busby; Timothy C Nichols; Dwight A Bellinger; Elizabeth P Merricks; Michael Rowland; Umadevi Veluvolu; David R Clemmons
Journal:  Sci Transl Med       Date:  2010-02-10       Impact factor: 17.956

2.  The effect of IGF-I receptor blockade for human esophageal squamous cell carcinoma and adenocarcinoma.

Authors:  Yasushi Adachi; Hirokazu Ohashi; Arisa Imsumran; Hiroyuki Yamamoto; Yasutaka Matsunaga; Hiroaki Taniguchi; Katsuhiko Nosho; Hiromu Suzuki; Yasushi Sasaki; Yoshiaki Arimura; David P Carbone; Kohzoh Imai; Yasuhisa Shinomura
Journal:  Tumour Biol       Date:  2013-09-13

Review 3.  Insulin receptor (IR) and insulin-like growth factor receptor 1 (IGF-1R) signaling systems: novel treatment strategies for cancer.

Authors:  Pushpendra Singh; Jimi Marin Alex; Felix Bast
Journal:  Med Oncol       Date:  2013-12-14       Impact factor: 3.064

Review 4.  Inhibitors of insulin-like growth factor signaling: a therapeutic approach for breast cancer.

Authors:  Deepali Sachdev; Douglas Yee
Journal:  J Mammary Gland Biol Neoplasia       Date:  2006-01       Impact factor: 2.673

5.  Drug efflux by breast cancer resistance protein is a mechanism of resistance to the benzimidazole insulin-like growth factor receptor/insulin receptor inhibitor, BMS-536924.

Authors:  Xiaonan Hou; Fei Huang; Joan M Carboni; Karen Flatten; Yan W Asmann; Cynthia Ten Eyck; Takeo Nakanishi; Jennifer D Tibodeau; Douglas D Ross; Marco M Gottardis; Charles Erlichman; Scott H Kaufmann; Paul Haluska
Journal:  Mol Cancer Ther       Date:  2011-01       Impact factor: 6.261

Review 6.  Targeting the insulin-like growth factor receptor: developing biomarkers from gene expression profiling.

Authors:  David N Boone; Adrian V Lee
Journal:  Crit Rev Oncog       Date:  2012

7.  Small-molecule inhibition and activation-loop trans-phosphorylation of the IGF1 receptor.

Authors:  Jinhua Wu; Wanqing Li; Barbara P Craddock; Kenneth W Foreman; Mark J Mulvihill; Qun-sheng Ji; W Todd Miller; Stevan R Hubbard
Journal:  EMBO J       Date:  2008-06-19       Impact factor: 11.598

8.  Insulin-like growth factor 1 receptor stabilizes the ETV6-NTRK3 chimeric oncoprotein by blocking its KPC1/Rnf123-mediated proteasomal degradation.

Authors:  Cristina E Tognon; Bo Rafn; Naniye Malli Cetinbas; Takumi Kamura; Genny Trigo; Barak Rotblat; Fumihiko Okumura; Masaki Matsumoto; Christine Chow; Monika Davare; Michael Pollak; Thibault Mayor; Poul H Sorensen
Journal:  J Biol Chem       Date:  2018-06-14       Impact factor: 5.157

Review 9.  Reactivation of the insulin-like growth factor-II signaling pathway in human hepatocellular carcinoma.

Authors:  Kai Breuhahn; Peter Schirmacher
Journal:  World J Gastroenterol       Date:  2008-03-21       Impact factor: 5.742

10.  HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924.

Authors:  Paul Haluska; Joan M Carboni; Cynthia TenEyck; Ricardo M Attar; Xiaonan Hou; Chunrong Yu; Malvika Sagar; Tai W Wong; Marco M Gottardis; Charles Erlichman
Journal:  Mol Cancer Ther       Date:  2008-09-02       Impact factor: 6.261

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