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Results: 1 to 20 of 99

1.

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.

ACS Med Chem Lett. 2010 Aug 30;1(9):510-5. doi: 10.1021/ml100178g. eCollection 2010 Dec 9.

PMID:
24900240
[PubMed]
Free PMC Article
2.

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.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1176-80. doi: 10.1016/j.bmcl.2010.12.094. Epub 2010 Dec 23.

PMID:
21251824
[PubMed - indexed for MEDLINE]
3.

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.

Mol Cancer Ther. 2010 Oct;9(10):2652-64. doi: 10.1158/1535-7163.MCT-10-0318. Epub 2010 Oct 5.

PMID:
20924128
[PubMed - indexed for MEDLINE]
Free Article
4.

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.

Mol Cancer Ther. 2007 Aug;6(8):2158-67. Epub 2007 Aug 1.

PMID:
17671083
[PubMed - indexed for MEDLINE]
Free Article
5.

Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.

Wittman MD, Carboni JM, Yang Z, Lee FY, Antman M, Attar R, Balimane P, Chang C, Chen C, Discenza L, Frennesson D, Gottardis MM, Greer A, Hurlburt W, Johnson W, Langley DR, Li A, Li J, Liu P, Mastalerz H, Mathur A, Menard K, Patel K, Sack J, Sang X, Saulnier M, Smith D, Stefanski K, Trainor G, Velaparthi U, Zhang G, Zimmermann K, Vyas DM.

J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r.

PMID:
19778024
[PubMed - indexed for MEDLINE]
6.

Dual IGF-I/II-neutralizing antibody MEDI-573 potently inhibits IGF signaling and tumor growth.

Gao J, Chesebrough JW, Cartlidge SA, Ricketts SA, Incognito L, Veldman-Jones M, Blakey DC, Tabrizi M, Jallal B, Trail PA, Coats S, Bosslet K, Chang YS.

Cancer Res. 2011 Feb 1;71(3):1029-40. doi: 10.1158/0008-5472.CAN-10-2274. Epub 2011 Jan 18.

PMID:
21245093
[PubMed - indexed for MEDLINE]
Free Article
7.

Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).

Emmitte KA, Wilson BJ, Baum EW, Emerson HK, Kuntz KW, Nailor KE, Salovich JM, Smith SC, Cheung M, Gerding RM, Stevens KL, Uehling DE, Mook RA Jr, Moorthy GS, Dickerson SH, Hassell AM, Leesnitzer MA, Shewchuk LM, Groy A, Rowand JL, Anderson K, Atkins CL, Yang J, Sabbatini P, Kumar R.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):1004-8. doi: 10.1016/j.bmcl.2008.11.058. Epub 2008 Nov 20.

PMID:
19101143
[PubMed - indexed for MEDLINE]
8.

Discovery of an inhibitor of insulin-like growth factor 1 receptor activation: implications for cellular potency and selectivity over insulin receptor.

Wood ER, Shewchuk L, Hassel A, Nichols J, Truesdale AT, Smith D, Carter HL, Weaver K, Barrett G, Leesnitzer T, Alvarez E, Bardera AI, Alamillo A, Cantizani J, Martin J, Smith GK, Jensen DE, Xie H, Mook R, Kumar R, Kuntz K.

Biochem Pharmacol. 2009 Dec 15;78(12):1438-47. doi: 10.1016/j.bcp.2009.07.022. Epub 2009 Aug 7.

PMID:
19665448
[PubMed - indexed for MEDLINE]
9.

A stable IgG-like bispecific antibody targeting the epidermal growth factor receptor and the type I insulin-like growth factor receptor demonstrates superior anti-tumor activity.

Dong J, Sereno A, Aivazian D, Langley E, Miller BR, Snyder WB, Chan E, Cantele M, Morena R, Joseph IB, Boccia A, Virata C, Gamez J, Yco G, Favis M, Wu X, Graff CP, Wang Q, Rohde E, Rennard R, Berquist L, Huang F, Zhang Y, Gao SX, Ho SN, Demarest SJ, Reff ME, Hariharan K, Glaser SM.

MAbs. 2011 May-Jun;3(3):273-88. Epub 2011 May 1.

PMID:
21393993
[PubMed - indexed for MEDLINE]
Free PMC Article
10.

Functional responses and in vivo anti-tumour activity of h7C10: a humanised monoclonal antibody with neutralising activity against the insulin-like growth factor-1 (IGF-1) receptor and insulin/IGF-1 hybrid receptors.

Pandini G, Wurch T, Akla B, Corvaia N, Belfiore A, Goetsch L.

Eur J Cancer. 2007 May;43(8):1318-27. Epub 2007 Apr 23.

PMID:
17451939
[PubMed - indexed for MEDLINE]
11.

In vitro and in vivo antitumor effects of the dual insulin-like growth factor-I/insulin receptor inhibitor, BMS-554417.

Haluska P, Carboni JM, Loegering DA, Lee FY, Wittman M, Saulnier MG, Frennesson DB, Kalli KR, Conover CA, Attar RM, Kaufmann SH, Gottardis M, Erlichman C.

Cancer Res. 2006 Jan 1;66(1):362-71.

PMID:
16397250
[PubMed - indexed for MEDLINE]
Free Article
12.

Epithelial-mesenchymal transition predicts sensitivity to the dual IGF-1R/IR inhibitor OSI-906 in hepatocellular carcinoma cell lines.

Zhao H, Desai V, Wang J, Epstein DM, Miglarese M, Buck E.

Mol Cancer Ther. 2012 Feb;11(2):503-13. doi: 10.1158/1535-7163.MCT-11-0327. Epub 2011 Dec 9.

PMID:
22161861
[PubMed - indexed for MEDLINE]
Free Article
13.

Plasma and tissue insulin-like growth factor-I receptor (IGF-IR) as a prognostic marker for prostate cancer and anti-IGF-IR agents as novel therapeutic strategy for refractory cases: a review.

Ozkan EE.

Mol Cell Endocrinol. 2011 Sep 15;344(1-2):1-24. doi: 10.1016/j.mce.2011.07.002. Epub 2011 Jul 18. Review.

PMID:
21782884
[PubMed - indexed for MEDLINE]
14.

Small-molecule ATP-competitive dual IGF-1R and insulin receptor inhibitors: structural insights, chemical diversity and molecular evolution.

Jin M, Wang J, Buck E, Mulvihill MJ.

Future Med Chem. 2012 Mar;4(3):315-28. doi: 10.4155/fmc.11.180. Review.

PMID:
22393939
[PubMed - indexed for MEDLINE]
15.

Microarray analysis of insulin and insulin-like growth factor-1 (IGF-1) receptor signaling reveals the selective up-regulation of the mitogen heparin-binding EGF-like growth factor by IGF-1.

Mulligan C, Rochford J, Denyer G, Stephens R, Yeo G, Freeman T, Siddle K, O'Rahilly S.

J Biol Chem. 2002 Nov 8;277(45):42480-7. Epub 2002 Sep 3.

PMID:
12213819
[PubMed - indexed for MEDLINE]
Free Article
16.

Small molecule inhibitors of the IGF-1R/IR axis for the treatment of cancer.

Buck E, Mulvihill M.

Expert Opin Investig Drugs. 2011 May;20(5):605-21. doi: 10.1517/13543784.2011.558501. Epub 2011 Mar 30. Review.

PMID:
21446886
[PubMed - indexed for MEDLINE]
17.

Combined Inhibition of IGF-1R/IR and Src family kinases enhances antitumor effects in prostate cancer by decreasing activated survival pathways.

Dayyani F, Parikh NU, Varkaris AS, Song JH, Moorthy S, Chatterji T, Maity SN, Wolfe AR, Carboni JM, Gottardis MM, Logothetis CJ, Gallick GE.

PLoS One. 2012;7(12):e51189. doi: 10.1371/journal.pone.0051189. Epub 2012 Dec 26.

PMID:
23300537
[PubMed - indexed for MEDLINE]
Free PMC Article
18.

Insulin receptor functionally enhances multistage tumor progression and conveys intrinsic resistance to IGF-1R targeted therapy.

Ulanet DB, Ludwig DL, Kahn CR, Hanahan D.

Proc Natl Acad Sci U S A. 2010 Jun 15;107(24):10791-8. doi: 10.1073/pnas.0914076107. Epub 2010 May 10.

PMID:
20457905
[PubMed - indexed for MEDLINE]
Free PMC Article
19.

Epidermal growth factor receptor and K-Ras mutations and resistance of lung cancer to insulin-like growth factor 1 receptor tyrosine kinase inhibitors.

Kim WY, Prudkin L, Feng L, Kim ES, Hennessy B, Lee JS, Lee JJ, Glisson B, Lippman SM, Wistuba II, Hong WK, Lee HY.

Cancer. 2012 Aug 15;118(16):3993-4003. doi: 10.1002/cncr.26656. Epub 2012 Feb 22. Erratum in: Cancer. 2012 Dec 15;118(24):6301.

PMID:
22359227
[PubMed - indexed for MEDLINE]
Free PMC Article
20.

Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase.

Sampognaro AJ, Wittman MD, Carboni JM, Chang C, Greer AF, Hurlburt WW, Sack JS, Vyas DM.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5027-30. doi: 10.1016/j.bmcl.2010.07.045. Epub 2010 Jul 15.

PMID:
20675137
[PubMed - indexed for MEDLINE]

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