HIV-1 maturation inhibitors: An update
HIV-1 maturation inhibitors are compounds other than HIV-1 protease inhibitors that inhibit HIV-1 maturation. This review focuses on triterpene derivatives, as their preclinical and clinical pharmacological profiles have been relatively well studied. Among the triterpene anti-HIV-1 maturation inhibitors, the betulinic acid derivative bevirimat dimeglumine (MPC-4326, formerly PA-457) is at the most advanced stage of drug development. Myriad Pharmaceuticals acquired all rights to bevirimat from Panacos Pharmaceuticals and continues to develop it under the new name MPC-4326. Although bevirimat is a potent HIV-1 maturation inhibitor, the results from phase II clinical trials indicate that it is less effective in a subset (30-40%) of HIV-1-positive individuals due to Gag polymorphisms in the glutamine-valine-threonine (QVT) motif of spacer peptide SP1. In addition to clinical development, recent medicinal chemistry approaches to obtain HIV-1 maturation inhibitors that are more potent than bevirimat are summarized. Copyright © 2009 Prous Science, S.A.U. or its licensors. All rights reserved.
Dang, Z; Huang, L; Chen, C
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