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Open AccessMedicineChemistryBiology

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.

B. Vu, P. Wovkulich, G. Pizzolato, A. Lovey, Qing-jie Ding, Nan Jiang, Jin-jun Liu, Chunlin Zhao, Kelli J. Glenn, Yang Wen, C. Tovar, K. Packman, L. Vassilev, B. Graves

2013.4.4ACS Medicinal Chemistry Letters

DOI: 10.1021/ml4000657

tlooto Summary

RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket ofMDM2, which stabilizes p53 and activates the p 53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts.

Abstract

Abstract is not available.

Citation format

VU, B., et al. Discovery of RG7112: A small-molecule MDM2 inhibitor in clinical development. ACS Medicinal Chemistry Letters, 2013, 4 5: 466–9.