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Overview
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Background
The multifunctional cytokine transforming growth factor-β (TGF-β) is a member of a large family of growth factors involved in the regulation of a diverse array of biological processes including cell growth and differentiation, matrix modulation, and embryonic development. LY364947 is a inhibitor of the transforming growth factor-β type I receptor kinase domain.
In vitro: LY364947 was quickly identified as a potent inhibitor (IC50= 51 nM) and was chosen as a platform for SAR development. Compounds were further evaluated as inhibitors of TGF-β-dependent luciferase production in mink lung cells (p3TP Lux) and growth in mouse fibroblasts (NIH 3T3) [1].
In vivo: In a rat model of NMDA-induced retinal degeneration, simultaneous injection of NMDA and the TGF-β inhibitor LY364947 slightly but significantly attenuated the reduction in number of cells in the ganglion cell layer and almost completely prevented the enhancement of capillary degeneration. [3].
Clinical trial: Up to now, LY364947 is still in the preclinical development stage.[1] Sawyer JS, Anderson BD, Beight DW, Campbell RM, Jones ML, Herron DK, Lampe JW, McCowan JR, McMillen WT, Mort N, Parsons S, Smith EC, Vieth M, Weir LC, Yan L, Zhang F, Yingling JM. Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain. J Med Chem. 2003 Sep 11;46(19):3953-6.
[2] Ueda K, Nakahara T, Mori A, Sakamoto K, Ishii K. Protective effects of TGF-β inhibitors in a rat model of NMDA-induced retinal degeneration. Eur J Pharmacol. 2013 Jan 15;699(1-3):188-93.
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