Ontology highlight
ABSTRACT:
SUBMITTER: Ding Y
PROVIDER: S-EPMC4538441 | biostudies-literature | 2015 Aug
REPOSITORIES: biostudies-literature
Ding Yun Y O'Keefe Heather H DeLorey Jennifer L JL Israel David I DI Messer Jeffrey A JA Chiu Cynthia H CH Skinner Steven R SR Matico Rosalie E RE Murray-Thompson Monique F MF Li Fan F Clark Matthew A MA Cuozzo John W JW Arico-Muendel Christopher C Morgan Barry A BA
ACS medicinal chemistry letters 20150707 8
The aggrecan degrading metalloprotease ADAMTS-4 has been identified as a novel therapeutic target for osteoarthritis. Here, we use DNA-encoded Library Technology (ELT) to identify novel ADAMTS-4 inhibitors from a DNA-encoded triazine library by affinity selection. Structure-activity relationship studies based on the selection information led to the identification of potent and highly selective inhibitors. For example, 4-(((4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-6-(((4-methylpiperazin- ...[more]