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Page 1
Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy.
Jin M, Kleinberg A, Cooke A, Gokhale PC, Foreman K, Dong H, Siu KW, Bittner MA, Mulvihill KM, Yao Y, Landfair D, O'Connor M, Mak G, Pachter JA, Wild R, Rosenfeld-Franklin M, Ji Q, Mulvihill MJ. Jin M, et al. Among authors: pachter ja. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1176-80. doi: 10.1016/j.bmcl.2010.12.094. Epub 2010 Dec 23. Bioorg Med Chem Lett. 2011. PMID: 21251824
Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases.
Steinig AG, Li AH, Wang J, Chen X, Dong H, Ferraro C, Jin M, Kadalbajoo M, Kleinberg A, Stolz KM, Tavares-Greco PA, Wang T, Albertella MR, Peng Y, Crew L, Kahler J, Kan J, Schulz R, Cooke A, Bittner M, Turton RW, Franklin M, Gokhale P, Landfair D, Mantis C, Workman J, Wild R, Pachter J, Epstein D, Mulvihill MJ. Steinig AG, et al. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4381-7. doi: 10.1016/j.bmcl.2013.05.074. Epub 2013 May 30. Bioorg Med Chem Lett. 2013. PMID: 23773865
A novel, potent, and selective insulin-like growth factor-I receptor kinase inhibitor blocks insulin-like growth factor-I receptor signaling in vitro and inhibits insulin-like growth factor-I receptor dependent tumor growth in vivo.
Ji QS, Mulvihill MJ, Rosenfeld-Franklin M, Cooke A, Feng L, Mak G, O'Connor M, Yao Y, Pirritt C, Buck E, Eyzaguirre A, Arnold LD, Gibson NW, Pachter JA. Ji QS, et al. Among authors: pachter ja. Mol Cancer Ther. 2007 Aug;6(8):2158-67. doi: 10.1158/1535-7163.MCT-07-0070. Epub 2007 Aug 1. Mol Cancer Ther. 2007. PMID: 17671083
Compensatory insulin receptor (IR) activation on inhibition of insulin-like growth factor-1 receptor (IGF-1R): rationale for cotargeting IGF-1R and IR in cancer.
Buck E, Gokhale PC, Koujak S, Brown E, Eyzaguirre A, Tao N, Rosenfeld-Franklin M, Lerner L, Chiu MI, Wild R, Epstein D, Pachter JA, Miglarese MR. Buck E, et al. Among authors: pachter ja. Mol Cancer Ther. 2010 Oct;9(10):2652-64. doi: 10.1158/1535-7163.MCT-10-0318. Epub 2010 Oct 5. Mol Cancer Ther. 2010. PMID: 20924128
Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.
Crew AP, Bhagwat SV, Dong H, Bittner MA, Chan A, Chen X, Coate H, Cooke A, Gokhale PC, Honda A, Jin M, Kahler J, Mantis C, Mulvihill MJ, Tavares-Greco PA, Volk B, Wang J, Werner DS, Arnold LD, Pachter JA, Wild R, Gibson NW. Crew AP, et al. Among authors: pachter ja. Bioorg Med Chem Lett. 2011 Apr 1;21(7):2092-7. doi: 10.1016/j.bmcl.2011.01.139. Epub 2011 Feb 3. Bioorg Med Chem Lett. 2011. PMID: 21353551
Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors.
Jin M, Wang J, Kleinberg A, Kadalbajoo M, Siu KW, Cooke A, Bittner MA, Yao Y, Thelemann A, Ji Q, Bhagwat S, Mulvihill KM, Rechka JA, Pachter JA, Crew AP, Epstein D, Mulvihill MJ. Jin M, et al. Among authors: pachter ja. Bioorg Med Chem Lett. 2013 Feb 15;23(4):979-84. doi: 10.1016/j.bmcl.2012.12.042. Epub 2012 Dec 21. Bioorg Med Chem Lett. 2013. PMID: 23317569
Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR.
Jin M, Gokhale PC, Cooke A, Foreman K, Buck E, May EW, Feng L, Bittner MA, Kadalbajoo M, Landfair D, Siu KW, Stolz KM, Werner DS, Laufer RS, Li AH, Dong H, Steinig AG, Kleinberg A, Yao Y, Pachter JA, Wild R, Mulvihill MJ. Jin M, et al. Among authors: pachter ja. ACS Med Chem Lett. 2010 Aug 30;1(9):510-5. doi: 10.1021/ml100178g. eCollection 2010 Dec 9. ACS Med Chem Lett. 2010. PMID: 24900240 Free PMC article.
Discovery of novel insulin-like growth factor-1 receptor inhibitors with unique time-dependent binding kinetics.
Jin M, Petronella BA, Cooke A, Kadalbajoo M, Siu KW, Kleinberg A, May EW, Gokhale PC, Schulz R, Kahler J, Bittner MA, Foreman K, Pachter JA, Wild R, Epstein D, Mulvihill MJ. Jin M, et al. Among authors: pachter ja. ACS Med Chem Lett. 2013 May 23;4(7):627-31. doi: 10.1021/ml400160a. eCollection 2013 Jul 11. ACS Med Chem Lett. 2013. PMID: 24900721 Free PMC article.
Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin.
Bhagwat SV, Gokhale PC, Crew AP, Cooke A, Yao Y, Mantis C, Kahler J, Workman J, Bittner M, Dudkin L, Epstein DM, Gibson NW, Wild R, Arnold LD, Houghton PJ, Pachter JA. Bhagwat SV, et al. Among authors: pachter ja. Mol Cancer Ther. 2011 Aug;10(8):1394-406. doi: 10.1158/1535-7163.MCT-10-1099. Epub 2011 Jun 14. Mol Cancer Ther. 2011. PMID: 21673091
82 results