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Items: 1 to 20 of 126

1.

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
2.

Crizotinib, a small-molecule dual inhibitor of the c-Met and ALK receptor tyrosine kinases.

Rodig SJ, Shapiro GI.

Curr Opin Investig Drugs. 2010 Dec;11(12):1477-90. Review.

PMID:
21154129
3.

Pharmacokinetic/pharmacodynamic modeling of crizotinib for anaplastic lymphoma kinase inhibition and antitumor efficacy in human tumor xenograft mouse models.

Yamazaki S, Vicini P, Shen Z, Zou HY, Lee J, Li Q, Christensen JG, Smith BJ, Shetty B.

J Pharmacol Exp Ther. 2012 Mar;340(3):549-57. doi: 10.1124/jpet.111.188870. Epub 2011 Nov 30.

4.

A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo.

Christensen JG, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R, Lipson KE, Ramphal J, Do S, Cui JJ, Cherrington JM, Mendel DB.

Cancer Res. 2003 Nov 1;63(21):7345-55.

5.

Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.

Liu L, Norman MH, Lee M, Xi N, Siegmund A, Boezio AA, Booker S, Choquette D, D'Angelo ND, Germain J, Yang K, Yang Y, Zhang Y, Bellon SF, Whittington DA, Harmange JC, Dominguez C, Kim TS, Dussault I.

J Med Chem. 2012 Mar 8;55(5):1868-97. doi: 10.1021/jm201331s. Epub 2012 Feb 24.

PMID:
22320327
6.

The preclinical profile of crizotinib for the treatment of non-small-cell lung cancer and other neoplastic disorders.

Roskoski R Jr.

Expert Opin Drug Discov. 2013 Sep;8(9):1165-79. doi: 10.1517/17460441.2013.813015. Epub 2013 Jun 28. Review.

PMID:
23805942
7.

Crizotinib reduces the rate of dark adaptation in the rat retina independent of ALK inhibition.

Liu CN, Mathialagan N, Lappin P, Fortner J, Somps C, Seitis G, Johnson TR, Hu W, Matsumoto D.

Toxicol Sci. 2015 Jan;143(1):116-25. doi: 10.1093/toxsci/kfu213. Epub 2014 Oct 16.

PMID:
25326243
8.

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.

9.

Identification of MET genomic amplification, protein expression and alternative splice isoforms in neuroblastomas.

Yan B, Lim M, Zhou L, Kuick CH, Leong MY, Yong KJ, Aung L, Salto-Tellez M, Chang KT.

J Clin Pathol. 2013 Nov;66(11):985-91. doi: 10.1136/jclinpath-2012-201375. Epub 2013 Jun 25.

PMID:
23801497
10.

Rapid development of piperidine carboxamides as potent and selective anaplastic lymphoma kinase inhibitors.

Bryan MC, Whittington DA, Doherty EM, Falsey JR, Cheng AC, Emkey R, Brake RL, Lewis RT.

J Med Chem. 2012 Feb 23;55(4):1698-705. doi: 10.1021/jm201565s. Epub 2012 Feb 9.

PMID:
22263917
11.

Crizotinib-resistant mutants of EML4-ALK identified through an accelerated mutagenesis screen.

Zhang S, Wang F, Keats J, Zhu X, Ning Y, Wardwell SD, Moran L, Mohemmad QK, Anjum R, Wang Y, Narasimhan NI, Dalgarno D, Shakespeare WC, Miret JJ, Clackson T, Rivera VM.

Chem Biol Drug Des. 2011 Dec;78(6):999-1005. doi: 10.1111/j.1747-0285.2011.01239.x. Epub 2011 Oct 31.

12.

A selective c-met inhibitor blocks an autocrine hepatocyte growth factor growth loop in ANBL-6 cells and prevents migration and adhesion of myeloma cells.

Hov H, Holt RU, Rø TB, Fagerli UM, Hjorth-Hansen H, Baykov V, Christensen JG, Waage A, Sundan A, Børset M.

Clin Cancer Res. 2004 Oct 1;10(19):6686-94.

13.

Antibody targeting of anaplastic lymphoma kinase induces cytotoxicity of human neuroblastoma.

Carpenter EL, Haglund EA, Mace EM, Deng D, Martinez D, Wood AC, Chow AK, Weiser DA, Belcastro LT, Winter C, Bresler SC, Vigny M, Mazot P, Asgharzadeh S, Seeger RC, Zhao H, Guo R, Christensen JG, Orange JS, Pawel BR, Lemmon MA, Mossé YP.

Oncogene. 2012 Nov 15;31(46):4859-67. doi: 10.1038/onc.2011.647. Epub 2012 Jan 23. Erratum in: Oncogene. 2012 Nov 15;31(46):4888. Vigny, M [added]; Mazot, P [added].

14.

Differential inhibitor sensitivity of anaplastic lymphoma kinase variants found in neuroblastoma.

Bresler SC, Wood AC, Haglund EA, Courtright J, Belcastro LT, Plegaria JS, Cole K, Toporovskaya Y, Zhao H, Carpenter EL, Christensen JG, Maris JM, Lemmon MA, Mossé YP.

Sci Transl Med. 2011 Nov 9;3(108):108ra114. doi: 10.1126/scitranslmed.3002950.

15.

Crizotinib exhibits antitumor activity by targeting ALK signaling not c-MET in pancreatic cancer.

Yan HH, Jung KH, Son MK, Fang Z, Kim SJ, Ryu YL, Kim J, Kim MH, Hong SS.

Oncotarget. 2014 Oct 15;5(19):9150-68.

16.

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.

17.

Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.

Zhang P, Dong J, Zhong B, Zhang D, Yuan H, Jin C, Xu X, Li H, Zhou Y, Liang Z, Ji M, Xu T, Song G, Zhang L, Chen G, Meng X, Sun D, Shih J, Zhang R, Hou G, Wang C, Jin Y, Yang Q.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):1910-8. doi: 10.1016/j.bmcl.2016.03.017. Epub 2016 Mar 7.

PMID:
26979157
18.

Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors.

Matsumoto S, Miyamoto N, Hirayama T, Oki H, Okada K, Tawada M, Iwata H, Nakamura K, Yamasaki S, Miki H, Hori A, Imamura S.

Bioorg Med Chem. 2013 Dec 15;21(24):7686-98. doi: 10.1016/j.bmc.2013.10.028. Epub 2013 Oct 30.

PMID:
24216091
19.

c-Met inhibitors with novel binding mode show activity against several hereditary papillary renal cell carcinoma-related mutations.

Bellon SF, Kaplan-Lefko P, Yang Y, Zhang Y, Moriguchi J, Rex K, Johnson CW, Rose PE, Long AM, O'Connor AB, Gu Y, Coxon A, Kim TS, Tasker A, Burgess TL, Dussault I.

J Biol Chem. 2008 Feb 1;283(5):2675-83. Epub 2007 Nov 30.

20.

Design, synthesis, and biological evaluation of potent c-Met inhibitors.

D'Angelo ND, Bellon SF, Booker SK, Cheng Y, Coxon A, Dominguez C, Fellows I, Hoffman D, Hungate R, Kaplan-Lefko P, Lee MR, Li C, Liu L, Rainbeau E, Reider PJ, Rex K, Siegmund A, Sun Y, Tasker AS, Xi N, Xu S, Yang Y, Zhang Y, Burgess TL, Dussault I, Kim TS.

J Med Chem. 2008 Sep 25;51(18):5766-79. doi: 10.1021/jm8006189.

PMID:
18763753

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