Structure and receptor binding of PYY analogs

被引:95
作者
Keire, DA [1 ]
Bowers, CW
Solomon, TE
Reeve, JR
机构
[1] Greter Los Angeles Vet Hlth Care Syst, CURE Digest Dis Res Ctr, Los Angeles, CA 90073 USA
[2] Univ Calif Los Angeles, Sch Med, Div Digest Dis, Los Angeles, CA 90095 USA
关键词
PYY; NPY; PP; Y-1; Y-2; Y-4; Y-5; receptor binding; tertiary structure; conformation; structure-activity-relationships;
D O I
10.1016/S0196-9781(01)00602-7
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Differences in the structure of PYY and two important analogs, PYY [3-36] and [Pro(34)]PYY, are evaluated. Y-receptor subtype ligand binding data are used in conjunction with structural data to develop a model for receptor subtype selective agonists. For PYY it is proposed that potent binding to Y-1, Y-4 and Y-5 receptors requires the juxtaposition of the two termini while Y-2 binding only requires the C-terminal helix. Further experiments that delineate between primary and tertiary structure contributions for receptor binding and activation are required to support the hypothesis that tertiary structure is stable enough to influence the expression of PYY's bioactivity. (C) 2002 Elsevier Science Inc. All rights reserved.
引用
收藏
页码:305 / 321
页数:17
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