AI Article Synopsis
- Developing a method to convert noncontinuous active regions of proteins into small molecules is key for creating new drug therapies that target protein-protein interactions.
- The technique involves backbone cyclization to create macrocyclic molecules from the active region of CD4.
- The lead compound, CG-1, was successfully shown to be orally bioavailable in rats, indicating its potential for treating HIV infection.
Article Abstract
Rational conversion of noncontinuous active regions of proteins into a small orally bioavailable molecule is crucial for the discovery of new drugs based on inhibition of protein-protein interactions. We developed a method that utilizes backbone cyclization as an intermediate step for conversion of the CD4 noncontinuous active region into small macrocyclic molecules. We demonstrate that this method is feasible by preparing small inhibitor for human immunodeficiency virus infection. The lead compound, CG-1, proved orally available in the rat model.
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| http://dx.doi.org/10.1016/j.bmc.2010.04.053 | DOI Listing |
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