Ontology highlight
ABSTRACT:
SUBMITTER: Clark JM
PROVIDER: S-EPMC9059126 | biostudies-literature | 2022 Apr
REPOSITORIES: biostudies-literature
Clark Jennifer M JM Salgado-Polo Fernando F Macdonald Simon J F SJF Barrett Tim N TN Perrakis Anastassis A Jamieson Craig C
Journal of medicinal chemistry 20220420 8
Autotaxin (ATX) facilitates the hydrolysis of lysophosphatidylcholine to lysophosphatidic acid (LPA), a bioactive phospholipid, which facilitates a diverse range of cellular effects in multiple tissue types. Abnormal LPA expression can lead to the progression of diseases such as cancer and fibrosis. Previously, we identified a potent ATX steroid-derived hybrid (partially orthosteric and allosteric) inhibitor which did not form interactions with the catalytic site. Herein, we describe the design, ...[more]