Design of tight-binding human immunodeficiency virus type 1 protease inhibitors.

摘要: Publisher Summary Most potent inhibitors of HIV-1 protease reported are peptidomimetics and based on the transition-state mimic concept. The study is a relatively new field less than decade. Despite this short period, discovery has proceeded at rapid pace, partly due to experience designing tight-binding other aspartic acid proteases. relied heavily use X-ray structures in optimizing old series inhibitors. Advances have been made toward design totally novel enzyme–inhibitor interactions. Although great progress developing enzyme inhibitors, it remains be seen whether or not these compounds will effective altering course disease. serve as way expand usefulness computer modeling improving de novo drug design.