Ontology highlight
ABSTRACT:
SUBMITTER: Friberg A
PROVIDER: S-EPMC7288559 | biostudies-literature | 2020 Jun
REPOSITORIES: biostudies-literature
Friberg Anders A Rehwinkel Hartmut H Nguyen Duy D Pütter Vera V Quanz Maria M Weiske Jörg J Eberspächer Uwe U Heisler Iring I Langer Gernot G
ACS omega 20200527 22
Lactate dehydrogenase A (LDHA) is frequently overexpressed in tumors, thereby sustaining high glycolysis rates, tumor growth, and chemoresistance. High-throughput screening resulted in the identification of phthalimide and dibenzofuran derivatives as novel lactate dehydrogenase inhibitors, selectively inhibiting the activity of the LDHA isoenzyme. Cocrystallization experiments confirmed target engagement in addition to demonstrating binding to a novel allosteric binding site present in all four ...[more]