Insulin-like growth factor-I receptor

The insulin-like growth factor I receptor is closely related to the insulin receptor. The RTK activity of the IGF-I receptor is regulated by intermolecular autophosphorylation at three sites within the activation loop. The crystal structure of the trisphosphorylated form of IGF-I RTK domain with an ATP analog and a specific peptide substrate showed that autophosphorylation stabilizes the activation loop in a conformation that facilitates catalysis. Furthermore, the structure revealed how... 

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Nguyen TT, Cao N, Short JL, White PJ. 2006. Intravenous insulin-like growth factor-I receptor antisense treatment reduces angiotensin receptor expression and function in spontaneously hypertensive rats. J Pharmacol Exp Ther 318 1171-1177. 

B9. Baxter, R. C., and Williams, P. F., Reciprocal modulation of insulin and insulin-like growth factor-I receptor affinity by calcium. Biochem. Biophys. Res. Cammun. 116,62-... 

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Dunn, S. E., Ehrlich, M., et al. (1998). A dominant negative mutant of the insulin-like growth factor-I receptor inhibits the adhesion, invasion, and metastasis of breast cancer. 

Papa, V., Gliozzo, B., et al. (1993). Insulin-like growth factor-I receptors are overexpressed and predict a low risk in human breast cancer. Cancer Res 53(16) 3736-40. 

Remacle-Bonnet, M., Garrouste, F., et al. (2005). Membrane rafts segregate pro- from anti-apoptotic insulin-like growth factor-I receptor signaling in colon carcinoma cells stimulated by members of the tumor necrosis factor superfamily. Am J Pathol 167(3) 761-73. 

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Wittman M, Carboni J, Attar R, et al. Discovery of a lH-benzoimidazol-2-yl-lH-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. Journal of Medicinal Chemistry 48(18), 5639, 2005. 

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Tollefsen, S., et al. (1987). Separation of the High-affinity Insulin-like Growth Factor I Receptor from Low-affinity Binding Sites by Affinity Chromatography, J. Biol. Chem. 262 16461-16469. 

Li, W., Favelyukis, S., Yang, J., Zeng, Y., Yu, J., Gangjee, A., and Miller, W. T. (2004). Inhibition of insulin-like growth factor I receptor autophosphorylation by novel 6-5 ring-fused compounds. Biochem. Pharmacol. 68,145-154. 

Lee CT, Wu S, Gabrilovich D, et al. Antitumor effects of an adenovirus expressing antisense insulin-like growth factor I receptor on human lung cancer cell lines. Cancer Res 1996 56 3038-3041. 

Rodon J, DeSantos V, Ferry RJ Jr., Kurzrock R. Early drug development of inhibitors of the insulin-like growth factor-I receptor pathway Lessons from the first clinical trials. Molecular Cancer Therapeutics 2008 7 2575—2588. 

Attias-Geva Z, Bentov I, Ludwig DL, Fishman A, Bruchim 1, Werner H. Insulin-like growth factor-I receptor (IGF-IR) targeting with monoclonal antibody cixutumumab (IMC-A12) inhibits IGF-I action in endometrial cancer cells. Eur J Cancer. 2011 47 1717-26. 

Mao Y, Shang Y, Pham VC, Ernst JA, Lill JAR, Scales SJ, Zha J. Polyubiqitination of insulin-like growth factor I receptor (IGF-IR) activation loop promotes antibody-induced receptor internalization and down-regulation. J Biol Chem. 2011 286 41852-61. 

Sarfstein R, Laron Z, Werner H. Long-acting insulin analogues elicit atypical signalling events mediated by the insulin receptor and insulin-like growth factor-I receptor. Diabetologia 2010 53(12) ... 

Bauer TW, Somcio RJ, Fan F, Liu W, Johnson M, Lesslie DP, et al. Regulatory role of c-Met in insulin-like growth factor-I receptor-mediated migration and invasion of human pancreatic carcinoma cells. Mol Cancer Ther 2006 5 1676-82. 

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