Pepducin-mediated G Protein-Coupled Receptor Signaling in the Cardiovascular System.
Pepducin-mediated G Protein-Coupled Receptor Signaling in the Cardiovascular System.
复制标题
DOI：
10.1097/fjc.0000000000001236
复制
发表时间：
2022-09-01
影响因子：
3
通讯作者：
Tilley, Douglas G.
中科院分区：
文献类型：
--
作者：
Xu, Heli;Tilley, Douglas G.
Pepducins are small-lipidated peptides designed from the intracellular loops (iLs) of G protein-coupled receptors (GPCRs) that act in an allosteric manner to modulate the activity of GPCRs. Over the last two decades, pepducins have progressed initially from pharmacologic tools used to manipulate GPCR activity in an orthosteric site-independent manner to compounds with therapeutic potential that have even been used safely in Phase 1 and 2 clinical trials in human subjects. The effect of pepducins at their cognate receptors has been shown to vary between antagonist, partial agonist or biased agonist outcomes in various primary and clonal cell systems, with even small changes in amino acid sequence altering these properties and their receptor selectivity. To date, pepducins designed from numerous GPCRs have been studied for their impact on pathologic conditions, including cardiovascular diseases such as thrombosis, myocardial infarction and atherosclerosis. This review will focus in particular on pepducins designed from protease-activated receptors (PARs), C-X-C motif chemokine receptors (CXCRs), formyl peptide receptors and the β2-adrenergic receptor. We will discuss the historic context of pepducin development for each receptor, as well as the structural, signaling, pathophysiologic consequences and therapeutic potential for each pepducin class.
DOI：
10.1016/j.jbc.2021.101057
发表时间：
2021-09
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Nassour H;Hoang TA;Martin RD;Dallagnol JCC;Billard É;Létourneau M;Novellino E;Carotenuto A;Allen BG;Tanny JC;Fournier A;Hébert TE;Chatenet D
通讯作者：
Chatenet D
影响因子：
3.7
作者：
Winther M;Holdfeldt A;Sundqvist M;Rajabkhani Z;Gabl M;Bylund J;Dahlgren C;Forsman H
通讯作者：
Forsman H