Structure-activity studies on prolactin-releasing peptide (PrRP). Analogues of PrRP-(19-31)-peptide. |
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| Authors: | Robert G Boyle Robert Downham Tanmoy Ganguly John Humphries Jeff Smith Stuart Travers |
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| Institution: | Millennium Pharmaceuticals Limited, Granta Park, Great Abingdon, Cambridge CB1 6ET, UK. |
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| Abstract: | An investigation of a series of single replacement analogues of PrRP-(19-31)-peptide has shown that good functional activity was retained when Phe31 was replaced with His(Bzl), Phe(4Cl), Nle, Trp, Cys(Bzl) or Glu(OBzl); when Val28 or Ile25 was replaced with Phg; when Gly24 was replaced with D-Ala, L-Ala, Pro or Sar; when Ser22 was replaced with Gly and when Ala21 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. |
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| Keywords: | agonist orphan receptor oGPCR10/hGR3 prolactin releasing peptide (PrRP) |
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