Carbonic anhydrase activators: Human isozyme II is strongly activated by oligopeptides incorporating the carboxyterminal sequence of the bicarbonate anion exchanger AE1

被引：50

作者：

Scozzafava, A ^{[1
]}

Supuran, CT ^{[1
]}

机构：

[1] Univ Florence, Dipartimento Chim, Lab Chim Bioinorgan, I-50019 Florence, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(02)00121-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Di-/tri- and especially tetrapeptides incorporating the sequence DADD present in the carboxyterminal region of the bicarbonate, chloride anion exchanger AE1 strongly activate human carbonic anhydrase (CA) isozyme II, whereas they act as more inefficient activators of isozymes I and IV. This discovery suggests that in the metabolon hCA II-AE1. the last protein plans a role both as a CA activator as well as a bicarbonate transporter. A synthesis of the tripeptide DAD and the tetrapeptide DADD is also presented together with the possible explanation why such highly acidic oligopeptides efficiently bind to hCA II but not to the closely related isozymes I and IV. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1177 / 1180

页数：4

共 30 条

[1]

Briganti F, 1998, INORG CHIM ACTA, V276, P295

[2] Carbonic anhydrase activators: X-ray crystallographic and spectroscopic investigations for the interaction of isozymes I and II with histamine [J].

Briganti, F ;

Mangani, S ;

Orioli, P ;

Scozzafava, A ;

Vernaglione, G ;

Supuran, CT .

BIOCHEMISTRY, 1997, 36 (34) :10384-10392

[3] Novel carbonic anhydrase isozymes I, II and IV activators incorporating sulfonyl-histamino moieties [J].

Briganti, F ;

Scozzafava, A ;

Supuran, CT .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (14) :2043-2048

[4] CARBONIC-ANHYDRASE ACTIVATORS .3. STRUCTURE-ACTIVITY CORRELATIONS OF A SERIES OF ISOZYME-II ACTIVATORS [J].

CLARE, BW ;

SUPURAN, CT .

JOURNAL OF PHARMACEUTICAL SCIENCES, 1994, 83 (06) :768-773

[5] A RE-INVESTIGATION OF THE QUESTION OF ACTIVATORS OF CARBONIC ANHYDRASE [J].

CLARK, AM ;

PERRIN, DD .

BIOCHEMICAL JOURNAL, 1951, 48 (04) :495-503

[6] Activity of carbonic anhydrase in relation to gastric secretion [J].

Feldberg, W ;

Keilin, D ;

Mann, T .

NATURE, 1940, 146 :651-652

[7] Carbonic anhydrase activators: Design of high affinity isozymes I, II, and IV activators, incorporating tri-/tetrasubstituted-pyridinium-azole moieties [J].

Ilies, M ;

Banciu, MD ;

Ilies, MA ;

Scozzafava, A ;

Caproiu, MT ;

Supuran, CT .

JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (02) :504-510

[8]

ITOH M, 1975, TETRAHEDRON LETT, P4393

[9] The activation of carbonic acid hydrasis [J].

Kiese, M .

NATURWISSENSCHAFTEN, 1941, 29 :116-117

[10] The activators of carbonic acid anhydratase [J].

Leiner, M ;

Leiner, G .

NATURWISSENSCHAFTEN, 1941, 29 :195-197

← 1 2 3 →