Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library

被引：71

作者：

Carroll, CD ^{[1
]}

Patel, H

Johnson, TO

Guo, T

Orlowski, M

He, ZM

Cavallaro, CL

Guo, J

Oksman, A

Gluzman, IY

Connelly, J

Chelsky, D

Goldberg, DE

Dolle, RE

机构：

[1] Pharmacopeia Inc, Dept Biol, Princeton, NJ 08540 USA

[2] Pharmacopeia Inc, Dept Chem, Princeton, NJ 08540 USA

[3] Pharmacopeia Inc, Dept Analyt Chem, Princeton, NJ 08540 USA

[4] Washington Univ, Howard Hughes Med Inst, Dept Med, St Louis, MO 63110 USA

[5] Washington Univ, Howard Hughes Med Inst, Dept Mol Microbiol, St Louis, MO 63110 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(98)00419-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An encoded 13,020-member combinatorial library was synthesized containing a statine core. Evaluation of this library with plasmepsin II, an aspartyl protease required for hemoglobin metabolism in the malaria parasite, led to the identification of potent and selective inhibitors as well as novel structure-activity relationships. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2315 / 2320

页数：6

共 18 条

[1] INHIBITORS OF ASPARTYL PROTEINASES
ABDELMEGUID, SS
[J]. MEDICINAL RESEARCH REVIEWS, 1993, 13 (06) : 731 - 778
[2] APELL KC, 1996, J BIOMOL SCREEN, V1, P27
[3] SYNTHESIS OF A SMALL-MOLECULE COMBINATORIAL LIBRARY ENCODED WITH MOLECULAR TAGS
BALDWIN, JJ
BURBAUM, JJ
HENDERSON, I
OHLMEYER, MHJ
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1995, 117 (20) : 5588 - 5589
[4] ON THE RATIONAL DESIGN OF RENIN INHIBITORS - X-RAY STUDIES OF ASPARTIC PROTEINASES COMPLEXED WITH TRANSITION-STATE ANALOGS
BLUNDELL, TL
COOPER, J
FOUNDLING, SI
JONES, DM
ATRASH, B
SZELKE, M
[J]. BIOCHEMISTRY, 1987, 26 (18) : 5585 - 5590
[5] A PARADIGM FOR DRUG DISCOVERY EMPLOYING ENCODED COMBINATORIAL LIBRARIES
BURBAUM, JJ
OHLMEYER, MHJ
READER, JC
HENDERSON, I
DILLARD, LW
LI, G
RANDLE, TL
SIGAL, NH
CHELSKY, D
BALDWIN, JJ
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1995, 92 (13) : 6027 - 6031
[6] MOLECULAR CHARACTERIZATION AND INHIBITION OF A PLASMODIUM-FALCIPARUM ASPARTIC HEMOGLOBINASE
FRANCIS, SE
GLUZMAN, IY
OKSMAN, A
KNICKERBOCKER, A
MUELLER, R
BRYANT, ML
SHERMAN, DR
RUSSELL, DG
GOLDBERG, DE
[J]. EMBO JOURNAL, 1994, 13 (02) : 306 - 317
[7] Hemoglobin metabolism in the malaria parasite Plasmodium falciparum
Francis, SE
Sullivan, DJ
Goldberg, DE
[J]. ANNUAL REVIEW OF MICROBIOLOGY, 1997, 51 : 97 - 123
[8] ORDER AND SPECIFICITY OF THE PLASMODIUM-FALCIPARUM HEMOGLOBIN DEGRADATION PATHWAY
GLUZMAN, IY
FRANCIS, SE
OKSMAN, A
SMITH, CE
DUFFIN, KL
GOLDBERG, DE
[J]. JOURNAL OF CLINICAL INVESTIGATION, 1994, 93 (04) : 1602 - 1608
[9] HEMOGLOBIN DEGRADATION IN THE HUMAN MALARIA PATHOGEN PLASMODIUM-FALCIPARUM - A CATABOLIC PATHWAY INITIATED BY A SPECIFIC ASPARTIC PROTEASE
GOLDBERG, DE
SLATER, AFG
BEAVIS, R
CHAIT, B
CERAMI, A
HENDERSON, GB
[J]. JOURNAL OF EXPERIMENTAL MEDICINE, 1991, 173 (04) : 961 - 969
[10] Kinetic analysis of plasmepsins I and II, aspartic proteases of the Plasmodium falciparum digestive vacuole
Luker, KE
Francis, SE
Gluzman, IY
Goldberg, DE
[J]. MOLECULAR AND BIOCHEMICAL PARASITOLOGY, 1996, 79 (01) : 71 - 78

← 1 2 →