Fluorine NMR studies of the human carbonic anhydrase-3,5-difluorobenzenesulfonamide complex

被引：0

作者：

Veenstra, DL ^{[1
]}

Gerig, JT ^{[1
]}

机构：

[1] Univ Calif Santa Barbara, Dept Chem, Santa Barbara, CA 93106 USA

来源：

MAGNETIC RESONANCE IN CHEMISTRY | 1998年 / 36卷

关键词：

NMR; F-19; carbonic anhydrase; enzyme inhibition; protein dynamics; sulfonamide; aromatic ring rotation; nuclear Overhauser effect; relaxation;

D O I：

10.1002/(SICI)1097-458X(199806)36:13<S169::AID-OMR320>3.3.CO;2-R

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Fluorine and nitrogen-15 NMR experiments are described which show that 3,5-difluorobenzenesulfonamide binds to human carbonic anhydrase I in a 1:1 complex, that the bound inhibitor is present as an anion and that the aromatic ring of the inhibitor undergoes rapid rotation in the complex in spite of likely interactions with the aromatic ring of Phe-91 which are strong enough to give an appreciable F-19{H-1} NOE. A previously predicted enhancement of binding by fluorination of the inhibitor was confirmed. (C) 1998 John Wiley & Sons, Ltd.

引用

页码：S169 / S178

页数：10

共 32 条

[1] [Anonymous], 1989, NUCL OVERHAUSER EFFE, DOI DOI 10.1002/MRC.1260280819
[2] ARMSTRONG JM, 1966, J BIOL CHEM, V241, P5137
[3] Berliner L., 1989, BIOL MAGN RESON, V8, P1
[4] A NMR-STUDY OF THE BINDING OF NOVEL N-HYDROXYBENZENESULFONAMIDE CARBONIC-ANHYDRASE INHIBITORS TO NATIVE AND CADMIUM-111-SUBSTITUTED CARBONIC-ANHYDRASE
BLACKBURN, GM
MANN, BE
TAYLOR, BF
WORRALL, AF
[J]. EUROPEAN JOURNAL OF BIOCHEMISTRY, 1985, 153 (03): : 553 - 558
[5] CHANG A, UNPUB
[6] Tritium NMR studies of the human carbonic anhydrase I-benzenesulfonamide complex
Culf, AS
Gerig, JT
Williams, PG
[J]. JOURNAL OF BIOMOLECULAR NMR, 1997, 10 (03) : 293 - 299
[7] Use of F-19 NMR to probe protein structure and conformational changes
Danielson, MA
Falke, JJ
[J]. ANNUAL REVIEW OF BIOPHYSICS AND BIOMOLECULAR STRUCTURE, 1996, 25 : 163 - 195
[8] Dodgson S.J., 1991, CARBONIC ANHYDRASES
[9] RO GEOMETRIES OF FLUOROBENZENES AND DISTORTIONS IN BENZENE-RING STRUCTURE ON SUBSTITUTION
DORAISWAMY, S
SHARMA, SD
[J]. JOURNAL OF MOLECULAR STRUCTURE, 1983, 102 (1-2) : 81 - 92
[10] NMR-STUDIES OF CARBONIC ANHYDRASE-FLUORINATED BENZENESULFONAMIDE COMPLEXES
DUGAD, LB
COOLEY, CR
GERIG, JT
[J]. BIOCHEMISTRY, 1989, 28 (09) : 3955 - 3960

← 1 2 3 4 →