Literature DB >> 21310613

Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer.

Qing Dong1, Douglas R Dougan, Xianchang Gong, Petro Halkowycz, Bohan Jin, Toufike Kanouni, Shawn M O'Connell, Nicholas Scorah, Lihong Shi, Michael B Wallace, Feng Zhou.   

Abstract

A novel 5-phenylamino-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione series of MEK inhibitors has been developed using structure-based drug design. Lead optimization of this series led to the discovery of TAK-733. This was advanced to Phase I clinical studies for cancer treatment.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21310613     DOI： 10.1016/j.bmcl.2011.01.071

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  33 in total

1.  Structure-based reassessment of the caveolin signaling model: do caveolae regulate signaling through caveolin-protein interactions?

Authors:  Brett M Collins; Melissa J Davis; John F Hancock; Robert G Parton
Journal:  Dev Cell       Date:  2012-07-17       Impact factor: 12.270

2.  A novel mechanism by which small molecule inhibitors induce the DFG flip in Aurora A.

Authors:  Mathew P Martin; Jin-Yi Zhu; Harshani R Lawrence; Roberta Pireddu; Yunting Luo; Riazul Alam; Sevil Ozcan; Said M Sebti; Nicholas J Lawrence; Ernst Schönbrunn
Journal:  ACS Chem Biol       Date:  2012-01-27       Impact factor: 5.100

Review 3.  Signaling pathways as therapeutic targets in biliary tract cancer.

Authors:  Jennifer Yang; Matthew R Farren; Daniel Ahn; Tanios Bekaii-Saab; Gregory B Lesinski
Journal:  Expert Opin Ther Targets       Date:  2017-03-17       Impact factor: 6.902

Review 4.  Targeting mutant NRAS signaling pathways in melanoma.

Authors:  Ha Linh Vu; Andrew E Aplin
Journal:  Pharmacol Res       Date:  2016-03-15       Impact factor: 7.658

Review 5.  Targeting RAS-ERK signalling in cancer: promises and challenges.

Authors:  Ahmed A Samatar; Poulikos I Poulikakos
Journal:  Nat Rev Drug Discov       Date:  2014-12       Impact factor: 84.694

6.  Antitumor activity of the MEK inhibitor TAK-733 against melanoma cell lines and patient-derived tumor explants.

Authors:  Lindsey N Micel; John J Tentler; Aik-Choon Tan; Heather M Selby; Kelsey L Brunkow; Kelli M Robertson; S Lindsey Davis; Peter J Klauck; Todd M Pitts; Esha Gangolli; Robyn Fabrey; Shawn M O'Connell; Patrick W Vincent; S Gail Eckhardt
Journal:  Mol Cancer Ther       Date:  2014-11-05       Impact factor: 6.261

Review 7.  MEK1/2 Inhibitors: Molecular Activity and Resistance Mechanisms.

Authors:  Pui-Kei Wu; Jong-In Park
Journal:  Semin Oncol       Date:  2015-09-24       Impact factor: 4.929

Review 8.  Targeting the RAS oncogene.

Authors:  Asami Takashima; Douglas V Faller
Journal:  Expert Opin Ther Targets       Date:  2013-01-30       Impact factor: 6.902

9.  BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors.

Authors:  Kimberly Brown Dahlman; Junfeng Xia; Katherine Hutchinson; Charles Ng; Donald Hucks; Peilin Jia; Mohammad Atefi; Zengliu Su; Suzanne Branch; Pamela L Lyle; Donna J Hicks; Viviana Bozon; John A Glaspy; Neal Rosen; David B Solit; James L Netterville; Cindy L Vnencak-Jones; Jeffrey A Sosman; Antoni Ribas; Zhongming Zhao; William Pao
Journal:  Cancer Discov       Date:  2012-07-13       Impact factor: 39.397

10.  Generation of highly potent DYRK1A-dependent inducers of human β-Cell replication via Multi-Dimensional compound optimization.

Authors:  Paul A Allegretti; Timothy M Horton; Yassan Abdolazimi; Hannah P Moeller; Benjamin Yeh; Matthew Caffet; Guillermina Michel; Mark Smith; Justin P Annes
Journal:  Bioorg Med Chem       Date:  2019-11-11       Impact factor: 3.641
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