Premium
Cover Picture: Development of Potent and Metabolically Stable APJ Ligands with High Therapeutic Potential (ChemMedChem 21/2016)
Author(s) -
Juhl Cathleen,
ElsHeindl Sylvia,
Schönauer Ria,
Redlich Gorden,
Haaf Erik,
Wunder Frank,
Riedl Bernd,
Burkhardt Nils,
BeckSickinger Annette G.,
Bierer Donald
Publication year - 2016
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201600531
Subject(s) - apelin , in vivo , chemistry , g protein coupled receptor , ligand (biochemistry) , pharmacology , drug discovery , front cover , receptor , stereochemistry , combinatorial chemistry , biochemistry , cover (algebra) , biology , mechanical engineering , engineering , microbiology and biotechnology
The front cover picture shows the stabilized apelin‐13 peptide illustrated by a knight sitting on a horse, protected by lance and shield. The shortest known endogenous apelin receptor ligand was modified by unnatural amino acids, cyclization, and palmitoylation to increase the metabolic stability. In vitro and in vivo stability tests revealed a very active and stable apelin analog, which will be beneficial to facilitate in vivo investigation of apelin effects and progress drug development. More information can be found in the Full Paper by Donald Bierer et al. on page 2378 in Issue 21, 2016 (DOI: 10.1002/cmdc.201600307). Artwork by Stefanie Wittrisch.