Ontology highlight
ABSTRACT:
SUBMITTER: Durek T
PROVIDER: S-EPMC5999400 | biostudies-literature | 2018 Apr
REPOSITORIES: biostudies-literature
Durek Thomas T Cromm Philipp M PM White Andrew M AM Schroeder Christina I CI Kaas Quentin Q Weidmann Joachim J Ahmad Fuaad Abdullah A Cheneval Olivier O Harvey Peta J PJ Daly Norelle L NL Zhou Yang Y Dellsén Anita A Österlund Torben T Larsson Niklas N Knerr Laurent L Bauer Udo U Kessler Horst H Cai Minying M Hruby Victor J VJ Plowright Alleyn T AT Craik David J DJ
Journal of medicinal chemistry 20180411 8
Ultrastable cyclic peptide frameworks offer great potential for drug design due to their improved bioavailability compared to their linear analogues. Using the sunflower trypsin inhibitor-1 (SFTI-1) peptide scaffold in combination with systematic N-methylation of the grafted pharmacophore led to the identification of novel subtype selective melanocortin receptor (MCR) agonists. Multiple bicyclic peptides were synthesized and tested toward their activity at MC1R and MC3-5R. Double N-methylated co ...[more]