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HIV-1 maturation inhibitors: An update

Publication ,  Journal Article
Dang, Z; Huang, L; Chen, C
Published in: Drugs of the Future
October 1, 2009

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.

Duke Scholars

Published In

Drugs of the Future

DOI

ISSN

0377-8282

Publication Date

October 1, 2009

Volume

34

Issue

10

Start / End Page

797 / 802

Related Subject Headings

  • Medicinal & Biomolecular Chemistry
  • 3214 Pharmacology and pharmaceutical sciences
  • 1115 Pharmacology and Pharmaceutical Sciences
 

Citation

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Dang, Z., Huang, L., & Chen, C. (2009). HIV-1 maturation inhibitors: An update. Drugs of the Future, 34(10), 797–802. https://doi.org/10.1358/dof.2009.34.10.1428207
Dang, Z., L. Huang, and C. Chen. “HIV-1 maturation inhibitors: An update.” Drugs of the Future 34, no. 10 (October 1, 2009): 797–802. https://doi.org/10.1358/dof.2009.34.10.1428207.
Dang Z, Huang L, Chen C. HIV-1 maturation inhibitors: An update. Drugs of the Future. 2009 Oct 1;34(10):797–802.
Dang, Z., et al. “HIV-1 maturation inhibitors: An update.” Drugs of the Future, vol. 34, no. 10, Oct. 2009, pp. 797–802. Scopus, doi:10.1358/dof.2009.34.10.1428207.
Dang Z, Huang L, Chen C. HIV-1 maturation inhibitors: An update. Drugs of the Future. 2009 Oct 1;34(10):797–802.

Published In

Drugs of the Future

DOI

ISSN

0377-8282

Publication Date

October 1, 2009

Volume

34

Issue

10

Start / End Page

797 / 802

Related Subject Headings

  • Medicinal & Biomolecular Chemistry
  • 3214 Pharmacology and pharmaceutical sciences
  • 1115 Pharmacology and Pharmaceutical Sciences