HIV-1 PROTEASE INHIBITORY ACTIVITY OF L-694,746, A NOVEL METABOLITE OF L-689,502

被引：9

作者：

LINGHAM, RB ^{[1
]}

ARISON, BH ^{[1
]}

COLWELL, LF ^{[1
]}

HSU, A ^{[1
]}

DEZENY, G ^{[1
]}

THOMPSON, WJ ^{[1
]}

GARRITY, GM ^{[1
]}

GAGLIARDI, MM ^{[1
]}

HARTNER, FW ^{[1
]}

DARKE, PL ^{[1
]}

BALANI, SK ^{[1
]}

PITZENBERGER, SM ^{[1
]}

MURPHY, JS ^{[1
]}

RAMJIT, HG ^{[1
]}

INAMINE, ES ^{[1
]}

TREIBER, LR ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD,W POINT,PA 19486

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1991年 / 181卷 / 03期

关键词：

D O I：

10.1016/0006-291X(91)92103-Q

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

L-689,502 is a potent inhibitor of HIV-1 protease activity in vitro. Microbial biotransformations of L-689,502 by cultures belonging to the genus Streptomyces sp. were performed. Extracts of culture broths were examined for the production of metabolites of L-689,502 that could inhibit HIV-1 protease activity. One culture, MA 6804 (Streptomyces lavendulae, ATCC 55095), produced L-694,746 that, while being structurally related to L-689,502, is a novel metabolite and a potent inhibitor of HIV-1 protease. © 1991.

引用

页码：1456 / 1461

页数：6

共 21 条

[1]

DARKE PL, 1989, J BIOL CHEM, V264, P2307

[2] HUMAN-IMMUNODEFICIENCY-VIRUS PROTEASE - A TARGET FOR AIDS THERAPY [J].