Timofeevski S - Search Results

1

Pharmacological characterization of a small molecule inhibitor of c-Jun kinase.

Cho H, Black SC, Looper D, Shi M, Kelly-Sullivan D, Timofeevski S, Siegel K, Yu XH, McDonnell SR, Chen P, Yie J, Ogilvie KM, Fraser J, Briscoe CP. Cho H, et al. Among authors: timofeevski s. Am J Physiol Endocrinol Metab. 2008 Nov;295(5):E1142-51. doi: 10.1152/ajpendo.90298.2008. Epub 2008 Aug 26. Am J Physiol Endocrinol Metab. 2008. PMID: 18728225 Free article.

2

Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.

Humphries PS, Lafontaine JA, Agree CS, Alexander D, Chen P, Do QQ, Li LY, Lunney EA, Rajapakse RJ, Siegel K, Timofeevski SL, Wang T, Wilhite DM. Humphries PS, et al. Among authors: timofeevski sl. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2099-102. doi: 10.1016/j.bmcl.2009.03.023. Epub 2009 Mar 13. Bioorg Med Chem Lett. 2009. PMID: 19327989

3

Identification of small-molecule inhibitors of the JIP-JNK interaction.

Chen T, Kablaoui N, Little J, Timofeevski S, Tschantz WR, Chen P, Feng J, Charlton M, Stanton R, Bauer P. Chen T, et al. Among authors: timofeevski s. Biochem J. 2009 May 13;420(2):283-94. doi: 10.1042/BJ20081899. Biochem J. 2009. PMID: 19243309

4

Engineering of an isolated p110α subunit of PI3Kα permits crystallization and provides a platform for structure-based drug design.

Chen P, Deng YL, Bergqvist S, Falk MD, Liu W, Timofeevski S, Brooun A. Chen P, et al. Among authors: timofeevski s. Protein Sci. 2014 Oct;23(10):1332-40. doi: 10.1002/pro.2517. Epub 2014 Aug 7. Protein Sci. 2014. PMID: 25043846 Free PMC article.

5

PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.

Zou HY, Li Q, Engstrom LD, West M, Appleman V, Wong KA, McTigue M, Deng YL, Liu W, Brooun A, Timofeevski S, McDonnell SR, Jiang P, Falk MD, Lappin PB, Affolter T, Nichols T, Hu W, Lam J, Johnson TW, Smeal T, Charest A, Fantin VR. Zou HY, et al. Among authors: timofeevski s. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8. doi: 10.1073/pnas.1420785112. Epub 2015 Mar 2. Proc Natl Acad Sci U S A. 2015. PMID: 25733882 Free PMC article.

6

Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors.

Timofeevski SL, McTigue MA, Ryan K, Cui J, Zou HY, Zhu JX, Chau F, Alton G, Karlicek S, Christensen JG, Murray BW. Timofeevski SL, et al. Biochemistry. 2009 Jun 16;48(23):5339-49. doi: 10.1021/bi900438w. Biochemistry. 2009. PMID: 19459657

7

Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor.

Zou HY, Li Q, Lee JH, Arango ME, Burgess K, Qiu M, Engstrom LD, Yamazaki S, Parker M, Timofeevski S, Cui JJ, McTigue M, Los G, Bender SL, Smeal T, Christensen JG. Zou HY, et al. Among authors: timofeevski s. Mol Cancer Ther. 2012 Apr;11(4):1036-47. doi: 10.1158/1535-7163.MCT-11-0839. Epub 2012 Mar 2. Mol Cancer Ther. 2012. PMID: 22389468

8

Enzyme kinetics and distinct modulation of the protein kinase N family of kinases by lipid activators and small molecule inhibitors.

Falk MD, Liu W, Bolaños B, Unsal-Kacmaz K, Klippel A, Grant S, Brooun A, Timofeevski S. Falk MD, et al. Among authors: timofeevski s. Biosci Rep. 2014 Apr 1;34(2):e00097. doi: 10.1042/BSR20140010. Print 2014 Apr 1. Biosci Rep. 2014. PMID: 27919031 Free PMC article.

9

The Axl kinase domain in complex with a macrocyclic inhibitor offers first structural insights into an active TAM receptor kinase.

Gajiwala KS, Grodsky N, Bolaños B, Feng J, Ferre R, Timofeevski S, Xu M, Murray BW, Johnson TW, Stewart A. Gajiwala KS, et al. Among authors: timofeevski s. J Biol Chem. 2017 Sep 22;292(38):15705-15716. doi: 10.1074/jbc.M116.771485. Epub 2017 Jul 19. J Biol Chem. 2017. PMID: 28724631 Free PMC article.

10

Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.

Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP. Johnson TW, et al. Among authors: timofeevski s. J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q. Epub 2014 Jun 3. J Med Chem. 2014. PMID: 24819116

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