Differences between natural and recombinant G protein-coupled receptor systems with varying receptor G protein stoichiometry

被引:139
作者
Kenakin, T [1 ]
机构
[1] Glaxo Wellcome Inc, Res & Dev, Dept Receptor Biochem, Res Triangle Pk, NC 27709 USA
关键词
D O I
10.1016/S0165-6147(97)90683-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The increasing accessibility of genetically engineered receptor systems for the study of drug-receptor interaction has led to a corresponding increase in the testing of new drug entities in recombinant receptor systems. In this article Terry Kenakin illustrates some possible conditions within these recombinant systems where the relative stoichiometry of the receptors to other cellular components may differ from that found in natural systems and where this difference may lead to anomalies in drug testing.
引用
收藏
页码:456 / 464
页数:9
相关论文
共 19 条
[1]   Do recombinant receptor assays provide affinity and potency estimates? [J].
Bockaert, J ;
Brand, C ;
Journot, L .
RECEPTOR CLASSIFICATION: THE INTEGRATION OF OPERATIONAL, STRUCTURAL, AND TRANSDUCTIONAL INFORMATION, 1997, 812 :55-70
[2]   Expression cloning and receptor pharmacology of human calcitonin receptors from MCF-7 cells and their relationship to amylin receptors [J].
Chen, WJ ;
Armour, S ;
Way, J ;
Chen, G ;
Watson, C ;
Irving, P ;
Cobb, J ;
Kadwell, S ;
Beaumont, K ;
Rimele, T ;
Kenakin, T .
MOLECULAR PHARMACOLOGY, 1997, 52 (06) :1164-1175
[3]  
Chidiac P, 1996, MOL PHARMACOL, V50, P662
[4]   IMPRECISION IN PRESENTATION OF BINDING-STUDIES [J].
COLQUHOUN, D .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1985, 6 (05) :197-197
[5]   MOLECULAR-CLONING AND EXPRESSION OF A CDNA-ENCODING THE SECRETIN RECEPTOR [J].
ISHIHARA, T ;
NAKAMURA, S ;
KAZIRO, Y ;
TAKAHASHI, T ;
TAKAHASHI, K ;
NAGATA, S .
EMBO JOURNAL, 1991, 10 (07) :1635-1641
[7]   AGONIST-RECEPTOR EFFICACY .2. AGONIST TRAFFICKING OF RECEPTOR SIGNALS [J].
KENAKIN, T .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1995, 16 (07) :232-238
[8]   Protean agonists - Keys to receptor active states? [J].
Kenakin, T .
RECEPTOR CLASSIFICATION: THE INTEGRATION OF OPERATIONAL, STRUCTURAL, AND TRANSDUCTIONAL INFORMATION, 1997, 812 :116-125
[9]  
Kenakin T., 1997, PHARM ANAL DRUG RECE, V3rd, P1
[10]   The stability of the agonist beta(2)-adrenergic receptor-G(s) complex: Evidence for agonist-specific states [J].
Krumins, AM ;
Barber, R .
MOLECULAR PHARMACOLOGY, 1997, 52 (01) :144-154