Hydrophobicity versus activity in crosslinked interfacial peptide inhibitors of HIV-1 protease
作者:Michael D. Shultz、Jean Chmielewski
DOI:10.1016/s0957-4166(97)00572-7
日期:1997.12
Crosslinked peptides with amino functionality incorporated within the tethering moiety 2a-c, 3a-c were synthesized and tested as interfacial inhibitors of HIV-1 protease. As part of a strategy to develop the novel method of dissociative inhibition as a viable pharmacological approach, compounds were made to test hydrophobicity and size requirements of the tethering moiety. In the case of crosslinked interfacial peptide inhibitors of HIV-1 protease, hydrophilic 2a-c and bulky hydrophobic 3a-c tethers decreased effectiveness by approximately 10- and 2-fold, respectively. (C) 1997 Published by Elsevier Science Ltd. All rights reserved.