Darunavir, a Conceptually New HIV-1 Protease Inhibitor for the Treatment of Drug-resistant HIV

Overview

Journal Bioorg Med Chem

Specialties Biochemistry
Chemistry

Date 2007 Sep 29

PMID 17900913

Citations 81

Authors

Arun K Ghosh

Zachary L Dawson

Hiroaki Mitsuya

Affiliations

Soon will be listed here.

Abstract

Our structure-based design strategies which specifically target the HIV-1 protease backbone, resulted in a number of exceedingly potent nonpeptidyl inhibitors. One of these inhibitors, darunavir (TMC114), contains a privileged, structure-based designed high-affinity P2 ligand, 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane (bis-THF). Darunavir has recently been approved for the treatment of HIV/AIDS patients harboring multidrug-resistant HIV-1 variants that do not respond to previously existing HAART regimens.

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