Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells

…, DJ Meyers, K Tenney, JS Shim, P Crews…

Index: Zhang, Feiran; Bhat, Shridhar; Gabelli, Sandra B.; Chen, Xiaochun; Miller, Michelle S.; Nacev, Benjamin A.; Cheng, Yim Ling; Meyers, David J.; Tenney, Karen; Shim, Joong Sup; Crews, Phillip; Amzel, L. Mario; Ma, Dawei; Liu, Jun O. Journal of Medicinal Chemistry, 2013 , vol. 56, # 10 p. 3996 - 4016

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Citation Number: 5

Abstract

Methionine aminopeptidases (MetAPs), which remove the initiator methionine from nascent peptides, are essential in all organisms. While MetAP2 has been demonstrated to be a therapeutic target for inhibiting angiogenesis in mammals, MetAP1 seems to be vital for cell proliferation. Our earlier efforts identified two structural classes of human MetAP1 (Hs MetAP1)-selective inhibitors (1–4), but all of them failed to inhibit cellular Hs MetAP1. ...