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Endothelin receptors: what's new and what do we need to know?

ingrid_86 添加于 2010-6-26 22:06 | 1867 次阅读 | 0 个评论

作者
Watts SW
摘要
Receptors are at the heart of how a molecule transmits a signal to a cell. Two receptor classes for endothelin (ET) are recognized, the ET(A) and ET(B) receptors. Intriguing questions have arisen in the field of ET receptor pharmacology, physiology, and function. For example, a host of pharmacological studies support the interaction of the ET(A) and ET(B) receptor in tissues (veins, arteries, bronchus, arterioles, esophagus), but yet few have been able to demonstrate direct ET(A)/ET(B) receptor interaction. Have we modeled this interaction wrong? Do we have a truly selective ET(A) receptor agonist such that we could selectively stimulate this important receptor? What can we learn from the recent phylogenic studies of the ET receptor family? Have we adequately addressed the number of biological molecules with which ET can interact to exert a biological effect? Recent mass spectrometry studies in our laboratory suggest that ET-1 interacts with other hereto unrecognized proteins. Biased ligands (ligands at the same receptor that elicit distinct signaling responses) have been discovered for other receptors. Do these exist for ET receptors and can we take advantage of this possibility in drug design? These and other questions will be posed in this minireview on topics on ET receptors.
详细资料
- 关键词: Animals; Endothelin-1/metabolism/pharmacology; Endothelins/metabolism/pharmacology; Humans; Ligands; Receptor, Endothelin A/agonists/drug effects/physiology; Receptor, Endothelin B/drug effects/physiology; Receptors, Endothelin/classification/drug effects/*physiology
- 文献种类:期刊
- 期刊名称: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
- 期刊缩写: Am J Physiol Regul Integr Comp Physiol
- 期卷页: 2010年第298卷第2期 R254-60页
- 地址: Dept. of Pharmacology and Toxicology, B445 Life Sciences Bldg., East Lansing, MI 48824-1317, USA. wattss@msu.edu
- ISBN: 0363-6119
- 备注:PMID:19907001
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