Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays

被引：80
作者：
Charlton, Steven J. [1 ]
Vauquelin, Georges [2 ]
机构：
[1] Novartis Inst Biomed Res, Horsham RH12 5AB, W Sussex, England
[2] Vrije Univ Brussel, Dept Mol & Biochem Pharmacol, Brussels, Belgium
来源：
BRITISH JOURNAL OF PHARMACOLOGY | 2010年 / 161卷 / 06期
关键词：
calcium assay; equilibrium; hemi-equilibrium; antagonist; agonist; modelling and simulation; receptor theory; drug discovery; PROTEIN; MECHANISM; CELLS; DISSOCIATION; TRAFFICKING; ANTAGONISTS; EFFICACY; POTENCY; MODELS;
D O I：
10.1111/j.1476-5381.2010.00863.x
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
LINKED ARTICLES This article is part of a themed section on Analytical Receptor Pharmacology in Drug Discovery. To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2010.161.issue-6.
引用
收藏
页码：1250 / 1265
页数：16
相关论文
共 61 条
[1]  
ARIENS EJ, 1954, ARCH INT PHARMACOD T, V99, P32
[2]   SOME QUANTITATIVE USES OF DRUG ANTAGONISTS [J].
ARUNLAKSHANA, O ;
SCHILD, HO .
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY, 1959, 14 (01) :48-58
[3]   How does calcium trigger neurotransmitter release? [J].
Augustine, GJ .
CURRENT OPINION IN NEUROBIOLOGY, 2001, 11 (03) :320-326
[4]   Circular permutation and receptor insertion within green fluorescent proteins [J].
Baird, GS ;
Zacharias, DA ;
Tsien, RY .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1999, 96 (20) :11241-11246
[5]   Calcium signalling: Dynamics, homeostasis and remodelling [J].
Berridge, MJ ;
Bootman, MD ;
Roderick, HL .
NATURE REVIEWS MOLECULAR CELL BIOLOGY, 2003, 4 (07) :517-529
[6]  
BERRIDGE MJ, 1990, J BIOL CHEM, V265, P9583
[7]   CALCIUM SIGNALING AND CELL-PROLIFERATION [J].
BERRIDGE, MJ .
BIOESSAYS, 1995, 17 (06) :491-500
[8]   OPERATIONAL MODELS OF PHARMACOLOGICAL AGONISM [J].
BLACK, JW ;
LEFF, P .
PROCEEDINGS OF THE ROYAL SOCIETY SERIES B-BIOLOGICAL SCIENCES, 1983, 220 (1219) :141-162
[9]  
BLINKS JR, 1989, METHOD ENZYMOL, V172, P164
[10]   Development of a Ca2+-Activated photoprotein, Photina®, and its application to high-throughput screening [J].
Bovolenta, Silvia ;
Foti, Maria ;
Lohmer, Stefan ;
Corazza, Sabrina .
JOURNAL OF BIOMOLECULAR SCREENING, 2007, 12 (05) :694-704
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