Highly Potent HIV Entry Inhibitors

University of California System: University of California, Merced
posted on 06/17/2011

A potentially valuable therapeutic strategy for preventing HIV infection or preventing the spread of the virus within an infected individual is to inhibit viral entry into human cells. Since HIV entry requires interactions between human cell surface proteins (notably CD4, CCR5, and CXCR4) and HIV envelope proteins (gp120 and gp41), compounds that bind to one or more of these proteins are being explored as candidates for blocking HIV entry. However, many of the compounds tested so far are active only against particular HIV strains, can be expensive and difficult to produce, or require exceedingly high concentrations to be efficacious in practical microbiocidal formulations. Thus, there is a pressing need to find new HIV entry inhibitors that can overcome these problems.

Suggested Uses

The UCM HIV entry inhibitors are strong candidates for use in topical microbiocidal formulations for preventing HIV infection, and possibly also in therapeutic formulations for controlling the spread of the virus in HIV-positive individuals.


As compared to other candidates for inhibiting HIV entry, the UCM compounds are:

  • more potent, being efficacious in the picomolar range;
  • effective against the X4 strain as well as R5 strain of HIV, with a high likelihood of retaining efficacy against a broad spectrum of possible viral mutations and diminishing the likelihood of drug resistance emerging; and
  • particularly well-suited for microbiocidal formulations, particularly in avoiding the need for excessively high dose levels.

Innovation Details

Detailed Description

University of California, Merced (UCM) researchers have invented greatly improved chimeric HIV entry inhibitors that target both a particular human cell surface protein and a particular HIV envelope protein. The UCM compounds are able to block distinct steps in the HIV entry process and therefore achieve a very high potency. In vitro HIV assays show that UCM compounds can inhibit HIV entry at picomolar concentrations and are effective against both the R5 and the X4 strains of HIV.

File Number: 21757 

Disease: Blood and Lymphatic System

IP Protection

Patent Number(s): WO12122216
Copyright: ©2011, The Regents of the University of California

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This innovation currently is not available for online licensing. Please contact David Cepoi at University of California System: University of California, Merced for more information.

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