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Solution structures and molecular interactions of selective melanocortin receptor antagonists.

Authors
 Chul-Jin Lee  ;  Ji-Hye Yun  ;  Sung-Kil Lim  ;  Weontae Lee 
Citation
 Molecules and Cells, Vol.30(6) : 551-556, 2010 
Journal Title
 Molecules and Cells 
ISSN
 1016-8478 
Issue Date
2010
Abstract
The solution structures and inter-molecular interaction of the cyclic melanocortin antagonists SHU9119, JKC363, HS014, and HS024 with receptor molecules have been determined by NMR spectroscopy and molecular modeling. While SHU9119 is known as a nonselective antagonist, JKC363, HS014, and HS024 are selective for the melanocortin subtype-4 receptor (MC4R) involved in modulation of food intake. Data from NMR and molecular dynamics suggest that the conformation of the Trp9 sidechain in the three MC4R-selective antagonists is quite different from that of SHU9119. This result strongly supports the concept that the spatial orientation of the hydrophobic aromatic residue is more important for determining selectivity than the presence of a basic, "arginine-like" moiety responsible for biological activity. We propose that the conformation of hydrophobic residues of MCR antagonists is critical for receptor-specific selectivity
Full Text
http://link.springer.com/article/10.1007%2Fs10059-010-0152-6
DOI
10.1007/s10059-010-0152-6
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Internal Medicine (내과학교실) > 1. Journal Papers
Yonsei Authors
Lim, Sung Kil(임승길)
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URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/101635
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