Article
Lack of synergy for inhibitors targeting a multi-drug-resistant HIV-1 protease.
Protein science : a publication of the Protein Society - 1 Feb 2002
King Nancy M, Melnick Laurence, Prabu-Jeyabalan Moses, Nalivaika Ellen A, Yang Shiow-Shong, Gao Yun, Nie Xiaoyi, Zepp Charles, Heefner Donald L, Schiffer Celia A
Abstract excerpt
The three-dimensional structures of indinavir and three newly synthesized indinavir analogs in complex with a multi-drug-resistant variant (L63P, V82T, I84V) of HIV-1 protease were determined to approximately 2.2 A resolution. Two of the three analogs have only a single modification of indinavir, and their binding affinities to the variant HIV-1 protease are enhanced over that of indinavir. However, when both...
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