ESTIMATING K-I VALUES FOR TIGHT-BINDING INHIBITORS FROM DOSE-RESPONSE PLOTS

被引：89

作者：

COPELAND, RA

LOMBARDO, D

GIANNARAS, J

DECICCO, CP

机构：

[1] The DuPont Merck Research Laboratories, Wilmington, DE 19880-0400

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 17期

关键词：

D O I：

10.1016/0960-894X(95)00330-V

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A simple method is described by which the K-i value of tight binding inhibitors of enzymes can be calculated directly from the IC50 value determined from graphical analysis of dose-response curves. Experimental verification of this method is provided by study of 15 inhibitors of the enzyme stromelysis which span a broad range of K-i values.

引用

页码：1947 / 1952

页数：6

共 7 条

[1] TIGHT-BINDING INHIBITORS .2. NON-STEADY STATE NATURE OF INHIBITION OF MILK XANTHINE-OXIDASE BY ALLOPURINOL AND ALLOXANTHINE AND OF HUMAN ERYTHROCYTIC ADENOSINE DEAMINASE BY COFORMYCIN
CHA, S
AGARWAL, RP
PARKS, RE
[J]. BIOCHEMICAL PHARMACOLOGY, 1975, 24 (23) : 2187 - 2197
[2] CHENG Y, 1973, BIOCHEM PHARMACOL, V22, P3099
[3] GRECO WR, 1979, J BIOL CHEM, V254, P2104
[4] LINEAR EQUATION THAT DESCRIBES STEADY-STATE KINETICS OF ENZYMES AND SUBCELLULAR PARTICLES INTERACTING WITH TIGHTLY BOUND INHIBITORS
HENDERSON, PJ
[J]. BIOCHEMICAL JOURNAL, 1972, 127 (02) : 321 - +
[5] KNIGHT CG, 1982, FEBS LETT, V296, P263
[6] HUMAN FIBROBLAST STROMELYSIN CATALYTIC DOMAIN - EXPRESSION, PURIFICATION, AND CHARACTERIZATION OF A C-TERMINALLY TRUNCATED FORM
MARCY, AI
EIBERGER, LL
HARRISON, R
CHAN, HK
HUTCHINSON, NI
HAGMANN, WK
CAMERON, PM
BOULTON, DA
HERMES, JD
[J]. BIOCHEMISTRY, 1991, 30 (26) : 6476 - 6483
[7] MYERS DK, 1952, BIOCHEM J, V51, P301

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