Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 26

1.

Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound ALK Mutations in ALK-Positive Lung Cancer.

Yoda S, Lin JJ, Lawrence MS, Burke BJ, Friboulet L, Langenbucher A, Dardaei L, Prutisto-Chang K, Dagogo-Jack I, Timofeevski S, Hubbeling H, Gainor JF, Ferris LA, Riley AK, Kattermann KE, Timonina D, Heist RS, Iafrate AJ, Benes CH, Lennerz JK, Mino-Kenudson M, Engelman JA, Johnson TW, Hata AN, Shaw AT.

Cancer Discov. 2018 Apr 12. pii: CD-17-1256. doi: 10.1158/2159-8290.CD-17-1256. [Epub ahead of print]

PMID:
29650534
2.

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.

J Biol Chem. 2017 Sep 22;292(38):15705-15716. doi: 10.1074/jbc.M116.771485. Epub 2017 Jul 19.

PMID:
28724631
3.

Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.

Shaw AT, Friboulet L, Leshchiner I, Gainor JF, Bergqvist S, Brooun A, Burke BJ, Deng YL, Liu W, Dardaei L, Frias RL, Schultz KR, Logan J, James LP, Smeal T, Timofeevski S, Katayama R, Iafrate AJ, Le L, McTigue M, Getz G, Johnson TW, Engelman JA.

N Engl J Med. 2016 Jan 7;374(1):54-61. doi: 10.1056/NEJMoa1508887. Epub 2015 Dec 23.

4.

Mitotic Checkpoint Kinase Mps1 Has a Role in Normal Physiology which Impacts Clinical Utility.

Martinez R, Blasina A, Hallin JF, Hu W, Rymer I, Fan J, Hoffman RL, Murphy S, Marx M, Yanochko G, Trajkovic D, Dinh D, Timofeevski S, Zhu Z, Sun P, Lappin PB, Murray BW.

PLoS One. 2015 Sep 23;10(9):e0138616. doi: 10.1371/journal.pone.0138616. eCollection 2015.

5.

PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models.

Zou HY, Friboulet L, Kodack DP, Engstrom LD, Li Q, West M, Tang RW, Wang H, Tsaparikos K, Wang J, Timofeevski S, Katayama R, Dinh DM, Lam H, Lam JL, Yamazaki S, Hu W, Patel B, Bezwada D, Frias RL, Lifshits E, Mahmood S, Gainor JF, Affolter T, Lappin PB, Gukasyan H, Lee N, Deng S, Jain RK, Johnson TW, Shaw AT, Fantin VR, Smeal T.

Cancer Cell. 2015 Jul 13;28(1):70-81. doi: 10.1016/j.ccell.2015.05.010. Epub 2015 Jul 2.

6.

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.

Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8. doi: 10.1073/pnas.1420785112. Epub 2015 Mar 2.

7.

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.

Protein Sci. 2014 Oct;23(10):1332-40. doi: 10.1002/pro.2517. Epub 2014 Aug 7.

8.

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.

J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q. Epub 2014 Jun 3.

PMID:
24819116
9.

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.

Biosci Rep. 2014 Apr 1;34(2). pii: e00097. Print 2014 Apr 1.

10.

Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.

Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Johnson PS, Kania RS, Lam H, Lam JL, Le PT, Li Q, Lingardo L, Liu W, Lu MW, McTigue M, Palmer CL, Richardson PF, Sach NW, Shen H, Smeal T, Smith GL, Stewart AE, Timofeevski S, Tsaparikos K, Wang H, Zhu H, Zhu J, Zou HY, Edwards MP.

J Med Chem. 2014 Feb 27;57(4):1170-87. doi: 10.1021/jm401805h. Epub 2014 Feb 6.

11.

Acquired resistance to crizotinib from a mutation in CD74-ROS1.

Awad MM, Katayama R, McTigue M, Liu W, Deng YL, Brooun A, Friboulet L, Huang D, Falk MD, Timofeevski S, Wilner KD, Lockerman EL, Khan TM, Mahmood S, Gainor JF, Digumarthy SR, Stone JR, Mino-Kenudson M, Christensen JG, Iafrate AJ, Engelman JA, Shaw AT.

N Engl J Med. 2013 Jun 20;368(25):2395-401. doi: 10.1056/NEJMoa1215530. Epub 2013 Jun 1.

12.

Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer.

Cui JJ, McTigue M, Nambu M, Tran-Dubé M, Pairish M, Shen H, Jia L, Cheng H, Hoffman J, Le P, Jalaie M, Goetz GH, Ryan K, Grodsky N, Deng YL, Parker M, Timofeevski S, Murray BW, Yamazaki S, Aguirre S, Li Q, Zou H, Christensen J.

J Med Chem. 2012 Sep 27;55(18):8091-109. Epub 2012 Sep 10. Erratum in: J Med Chem. 2012 Nov 26;55(22):10314.

PMID:
22924734
13.

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.

Mol Cancer Ther. 2012 Apr;11(4):1036-47. doi: 10.1158/1535-7163.MCT-11-0839. Epub 2012 Mar 2.

14.

Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).

Cui JJ, Tran-Dubé M, Shen H, Nambu M, Kung PP, Pairish M, Jia L, Meng J, Funk L, Botrous I, McTigue M, Grodsky N, Ryan K, Padrique E, Alton G, Timofeevski S, Yamazaki S, Li Q, Zou H, Christensen J, Mroczkowski B, Bender S, Kania RS, Edwards MP.

J Med Chem. 2011 Sep 22;54(18):6342-63. doi: 10.1021/jm2007613. Epub 2011 Aug 18.

PMID:
21812414
15.

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.

Biochemistry. 2009 Jun 16;48(23):5339-49. doi: 10.1021/bi900438w.

PMID:
19459657
16.

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.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2099-102. doi: 10.1016/j.bmcl.2009.03.023. Epub 2009 Mar 13.

PMID:
19327989
17.

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.

Biochem J. 2009 May 13;420(2):283-94. doi: 10.1042/BJ20081899.

PMID:
19243309
18.

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.

Am J Physiol Endocrinol Metab. 2008 Nov;295(5):E1142-51. doi: 10.1152/ajpendo.90298.2008. Epub 2008 Aug 26.

19.
20.

Enzymology of Phanerochaete chrysosporium with respect to the degradation of recalcitrant compounds and xenobiotics.

Cameron MD, Timofeevski S, Aust SD.

Appl Microbiol Biotechnol. 2000 Dec;54(6):751-8. Review.

PMID:
11152065
21.

Substrate specificity of lignin peroxidase and a S168W variant of manganese peroxidase.

Timofeevski SL, Nie G, Reading NS, Aust SD.

Arch Biochem Biophys. 2000 Jan 1;373(1):147-53.

PMID:
10620333
22.

Addition of veratryl alcohol oxidase activity to manganese peroxidase by site-directed mutagenesis.

Timofeevski SL, Nie G, Reading NS, Aust SD.

Biochem Biophys Res Commun. 1999 Mar 24;256(3):500-4.

PMID:
10080927
23.

Mechanisms for protection against inactivation of manganese peroxidase by hydrogen peroxide.

Timofeevski SL, Reading NS, Aust SD.

Arch Biochem Biophys. 1998 Aug 15;356(2):287-95.

PMID:
9705219
24.

Effects of Mn2+ and oxalate on the catalatic activity of manganese peroxidase.

Timofeevski SL, Aust SD.

Biochem Biophys Res Commun. 1997 Oct 29;239(3):645-9.

PMID:
9367821
25.

Kinetics of calcium release from manganese peroxidase during thermal inactivation.

Timofeevski SL, Aust SD.

Arch Biochem Biophys. 1997 Jun 1;342(1):169-75.

PMID:
9185626
26.

Anti-inflammatory and antishock water-soluble polyesters of glucocorticoids with low level systemic toxicity.

Timofeevski SL, Panarin EF, Vinogradov OL, Nezhentsev MV.

Pharm Res. 1996 Mar;13(3):476-80.

PMID:
8692745

Supplemental Content

Loading ...
Support Center