Journal article

Retro-inverso forms of gastrin(5-12) are as biologically active as glycine-extended gastrin in vitro but not in vivo

Kathryn M Marshall, Marie Laval, Ioulia Sims, Arthur Shulkes, Graham S Baldwin

PEPTIDES | ELSEVIER SCIENCE INC | Published : 2015

Abstract

Non-amidated gastrin peptides such as glycine-extended gastrin (Ggly) are biologically active in vitro and in vivo and have been implicated in the development of gastric and colonic cancers. Previous studies have shown that the truncated form of Ggly, the octapeptide LE5AY, was still biologically active in vitro, and that activity was dependent on ferric ion binding but independent of binding to the cholecystokinin 2 (CCK2) receptor. The present work was aimed at creating more stable gastrin-derived 'super agonists' using retro-inverso technology. The truncated LE5AY peptide was synthesized using end protecting groups in three forms with l-amino acids (GL), d-amino acids (GD) or retro-invers..

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