Structure-activity studies on prolactin-releasing peptide (PrRP). Analogues of PrRP-(19-31)-peptide

被引:26
作者
Boyle, RG
Downham, R
Ganguly, T
Humphries, J
Smith, J
Travers, S
机构
[1] Millennium Pharmaceut Ltd, Cambridge CB1 6ET, England
[2] Millennium Pharmaceut Ltd, Cambridge, MA 02139 USA
[3] Sareum Ltd, Cambridge CB2 4EE, England
关键词
agonist; orphan receptor; oGPCR10/hGR3; prolactin releasing peptide (PrRP);
D O I
10.1002/psc.612
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
An investigation of a series of single replacement analogues of PrRP-(19-31)-peptide has shown that good functional activity was retained when Phe(31) was replaced with His(Bzl), Phe(4Cl), Nle, Trp, Cys(Bzl) or Glu(OBzl); when Val(28) or Ile(25) was replaced with Phg; when Gly(24) was replaced with D-Ala, L-Ala, Pro or Sar; when Ser(22) was replaced with Gly and when Ala(21) was replaced with Thr or MeAla. The results confirm that the functionally important residues are located within the carboxyl terminal segment, -Ile-Arg-Pro-Val-Gly-Arg-Phe-NH2. Copyright (c) 2004 European Peptide Society and John Wiley & Sons, Ltd.
引用
收藏
页码:161 / 165
页数:5
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