Keynote review: Allosterism in membrane receptors

被引：46

作者：

Gao, ZG ^{[1
]}

Jacobson, KA ^{[1
]}

机构：

[1] Natl Inst Diabet & Digest & Kidney Dis, Lab Bioorgan Chem, Mol Recognit Sect, NIH, Bethesda, MD 20892 USA

来源：

DRUG DISCOVERY TODAY | 2006年 / 11卷 / 5-6期

关键词：

D O I：

10.1016/S1359-6446(05)03689-5

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Allosteric modulation of membrane receptors has been intensively studied in the past three decades and is now considered to be an important indirect mechanism for the control of receptor function. The allosteric site on the GABA(A) receptor is the target for the most widely prescribed sleep medicines, the benzodiazepines. Cinacalcet, an allosteric enhancer of the calcium-sensing receptor, is used to treat secondary hyperparathyroidism. Allosteric ligands might be especially valuable to control receptors for which the design of selective orthosteric agonists or antagonists has been elusive, such as muscarinic acetylcholine receptors.

引用

页码：191 / 202

页数：12

共 148 条

[1] A novel family of mammalian taste receptors [J].

Adler, E ;

Hoon, MA ;

Mueller, KL ;

Chandrashekar, J ;

Ryba, NJP ;

Zuker, CS .

CELL, 2000, 100 (06) :693-702

[2]

Alexander K, 1999, J PHARMACOL EXP THER, V291, P1135

[3] A novel calcium-sensing receptor antagonist transiently stimulates parathyroid hormone secretion in vivo [J].

Arey, BJ ;

Seethala, R ;

Ma, ZP ;

Fura, A ;

Morin, J ;

Swartz, J ;

Vyas, V ;

Yang, W ;

Dickson, JK ;

Feyen, JHM .

ENDOCRINOLOGY, 2005, 146 (04) :2015-2022

[4] The benzodiazepine site of the GABAA receptor:: an old target with new potential? [J].

Bateson, AN .

SLEEP MEDICINE, 2004, 5 :S9-S15

[5]

Bendall L, 2005, HISTOL HISTOPATHOL, V20, P907, DOI 10.14670/HH-20.907

[6] Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: Prevention of reperfusion injury [J].

Bertini, R ;

Allegretti, M ;

Bizzarri, C ;

Moriconi, A ;

Locati, M ;

Zampella, G ;

Cervellera, MN ;

Di Cioccio, V ;

Cesta, MC ;

Galliera, E ;

Martinez, FO ;

Di Bitondo, R ;

Troiani, G ;

Sabbatini, V ;

D'Anniballe, G ;

Anacardio, R ;

Cutrin, JC ;

Cavalieri, B ;

Mainiero, F ;

Strippoli, R ;

Villa, P ;

Di Girolamo, M ;

Martin, F ;

Gentile, M ;

Santoni, A ;

Corda, D ;

Poli, G ;

Mantovani, A ;

Ghezzi, P ;

Colotta, F .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2004, 101 (32) :11791-11796

[7] Positive allosteric modulator of the human 5-HT2C receptor [J].

Bin Im, W ;

Chio, CL ;

Alberts, GL ;

Dinh, DM .

MOLECULAR PHARMACOLOGY, 2003, 64 (01) :78-84

[8] Molecular mechanisms of GABAB receptor activation:: new insights from the mechanism of action of CGP7930, a positive allosteric modulator [J].

Binet, V ;

Goudet, C ;

Brajon, C ;

Le Corre, L ;

Acher, F ;

Pin, JP ;

Prézeau, L .

BIOCHEMICAL SOCIETY TRANSACTIONS, 2004, 32 :871-872

[9] Allosterism at muscarinic receptors: Ligands and mechanisms [J].

Birdsall, NJM ;

Lazareno, S .

MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2005, 5 (06) :523-543

[10]

Birdsall NJM, 1999, MOL PHARMACOL, V55, P778

← 1 2 3 4 5 6 7 8 9 10 →