期刊
TRENDS IN PHARMACOLOGICAL SCIENCES
卷 40, 期 1, 页码 71-83出版社
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2018.11.005
关键词
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资金
- James Cook Research Fellowship of the Royal Society of New Zealand
- Barbara Basham Doctoral Scholarship
- Marsden Fund, Royal Society of New Zealand
The calcitonin gene-related peptide (CGRP) receptor system has emerged as an important drug target for migraine. This is highlighted by the recent regulatory approval of the first drug targeting the CGRP signalling pathway, the CGRP receptor antibody erenumab. The cellular compartments in which receptors are found affects drug access and whether they can exert their effects. G protein-coupled receptors (GPCRs) were thought to signal only at the cell surface, but it is now recognised that some GPCRs, including the CGRP receptor, undergo sustained signalling from endosomes, once internalised in response to ligand. What does this mean for drugs like erenumab? This review covers recent insights into the regulation of CGRP family receptors and examines what implications this may have on drug activity.
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