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Biological Chemistry

Editor-in-Chief: Brüne, Bernhard

Editorial Board: Buchner, Johannes / Lei, Ming / Ludwig, Stephan / Thomas, Douglas D. / Turk, Boris / Wittinghofer, Alfred


IMPACT FACTOR 2017: 3.022

CiteScore 2017: 2.81

SCImago Journal Rank (SJR) 2017: 1.562
Source Normalized Impact per Paper (SNIP) 2017: 0.705

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ISSN
1437-4315
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Volume 384, Issue 3

Issues

Structure-Activity Relationships of Glucose-Dependent Insulinotropic Polypeptide (GIP)

S.A. Hinke / R. Gelling / S. Manhart / F. Lynn / R.A. Pederson / K. Kühn-Wache / F. Rosche / H.-U. Demuth / D. Coy / C.H.S. McIntosh
Published Online: 2005-06-01 | DOI: https://doi.org/10.1515/BC.2003.046

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.

About the article

Published Online: 2005-06-01

Published in Print: 2003-03-14


Citation Information: Biological Chemistry, Volume 384, Issue 3, Pages 403–407, ISSN (Print) 1431-6730, DOI: https://doi.org/10.1515/BC.2003.046.

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