期刊
EUROPEAN JOURNAL OF PHARMACOLOGY
卷 763, 期 -, 页码 206-213出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejphar.2015.05.012
关键词
GPCRs; Opioid binding; Receptor; Molecular dynamics; Allosteric modulators; Virtual screening; Functional selectivity; Dimerization
资金
- National Institutes of Health [DA026434, DA034049]
- National Science Foundation [OCI-1053575]
Opioid receptors are important drug targets for pain management, addiction, and mood disorders. Although substantial research on these important subtypes of G protein-coupled receptors has been conducted over the past two decades to discover ligands with higher specificity and diminished side effects, currently used opioid therapeutics remain suboptimal. Luckily, recent advances in structural biology of opioid receptors provide unprecedented insights into opioid receptor pharmacology and signaling. We review here a few recent studies that have used the crystal structures of opioid receptors as a basis for revealing mechanistic details of signal transduction mediated by these receptors, and for the purpose of drug discovery. (C) 2015 Elsevier B.V. All rights reserved.
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