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Small Molecule Blocks Entry of HIV-1 into Cells

Studies indicate that BMS-378806, a newly synthesized small molecule HIV-1 inhibitor, blocks the first step of the infection process - the binding of the HIV-1 envelope glycoprotein gp120 to its cell surface receptor, CD4.

"[Our] studies establish the feasibility of targeting the HIV-1 gp120 envelope with a small molecule compound and support the envelope protein as a viable target for a new drug class," Dr. Pin-Fang Lin and colleagues from Bristol-Myers Squibb in Wallingford, Connecticut write in the August 18th PNAS Early Online Edition.

Of particular importance, they say, is that BMS-378806 is effective against HIV strains resistant to existing HIV-1 protease and reverse transcriptase inhibitors.

Preclinical studies indicate that BMS-378806 exhibits "potent inhibitory activity" against a panel of R5-, X4-, and R5/X4 HIV-1 laboratory and clinical isolates of the B subtype at low concentrations, the scientists report. The compound is selective for HIV-1, showing no activity against HIV-2, SIV, and a panel of other viruses.

In initial studies in dogs, rats, and monkeys, BMS-378806 shows "good oral bioavailability and a clean safety profile," according to Dr. Lin and colleagues.

"Together, the data show that BMS-378806 is a representative of a new class of HIV inhibitors that has the potential to become a valued addition to our current armamentarium of antiretroviral drugs," they write.

In an editorial, Drs. Aine McKnight and Robin A. Weiss from University College London note that while "anti-HIV compounds that block coreceptors and membrane fusion are in preliminary clinical trials, BMS-378806 is the first small molecule to block the gp120-CD4 binding event."

hmily

哦为什么是英语的？