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Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Annu+Rev+Biophys 2017 ; 46 (ä): 175-98 Nephropedia Template TP
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What do structures tell us about chemokine receptor function and antagonism? #MMPMID28532213
Kufareva I; Gustavsson M; Zheng Y; Stephens BS; Handel TM
Annu Rev Biophys 2017[May]; 46 (ä): 175-98 PMID28532213show ga
Chemokines and their cell surface G protein-coupled receptors are critical for cell migration not only in many fundamental biological processes but also in inflammatory diseases and cancer. Recent X-ray structures of two chemokines complexed with full-length receptors provide unprecedented insight into the atomic details of chemokine recognition and receptor activation, and computational modeling informed by new experiments leverages these insights to gain understanding of many more receptor:chemokine pairs. In parallel, chemokine receptor structures with small molecules reveal complicated and diverse structural foundations of small molecule antagonism and allostery, highlight inherent physicochemical challenges of receptor:chemokine interfaces, and suggest novel epitopes that can be exploited to overcome these challenges. The structures and models promote unique understanding of chemokine receptor biology, including the interpretation of two decades of experimental studies, and will undoubtedly assist future drug discovery endeavors.