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Biotech / Medical : Agouron Pharmaceuticals (AGPH)
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To: Peter Singleton who wrote (2922)11/21/1997 8:32:00 PM
From: james  Read Replies (1) of 6136
 
Peter, were you awared of this paper

ncbi.nlm.nih.gov

<G48V and L90M/G48V proteases had catalytic efficiency (kcat/Km) values with TLNF-PISP, RKIL-FLDG, and AETF-YVDG that were 1/10 to 1/20 the value of WT protease. The decreased catalytic efficiencies were primarily the result of increased Km values. Thus, mutations in the protease decrease the affinity of the enzyme for saquinavir and the catalytic efficiency with peptide substrates.>

Even though these mutations decrease viracept efficacy, but they also DECREASE HIV-PROTEASE'S FUNCTION IN MAKING THE VIRUS by over 10-folds. Cheers!!!!!!!

regards
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