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Structure-Activity Relationships of Glucose-Dependent Insulinotropic Polypeptide (GIP)
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S.A. Hinke
Published/Copyright:
June 1, 2005
Abstract
Six GIP1-30NH2 analogs were synthesized with modifications (de-protonation, N-methylation, reversed chirality, and substitution) at positions 1, 3, and 4 of the N-terminus, and additionally, a cyclized GIP derivative was synthesized. The relationship between altered structure to biological activity was assessed by measuring receptor binding affinity and ability to stimulate adenylyl cyclase in CHO-K1 cells transfected with the wild-type GIP receptor (wtGIPR). These structureactivity relationship studies demonstrate the importance of the GIP N-terminus and highlight structural constraints that can be introduced in GIP analogs. These analogs may be useful starting points for design of peptides with enhanced in vivo bioactivity.
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Published Online: 2005-06-01
Published in Print: 2003-03-14
Copyright © 2003 by Walter de Gruyter GmbH & Co. KG
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