Ontology highlight
ABSTRACT:
SUBMITTER: Di Bussolo V
PROVIDER: S-EPMC4497792 | biostudies-literature | 2015
REPOSITORIES: biostudies-literature
Di Bussolo Valeria V Calvaresi Emilia C EC Granchi Carlotta C Del Bino Linda L Frau Ileana I Lang Maria Chiara Dasso MC Tuccinardi Tiziano T Macchia Marco M Martinelli Adriano A Hergenrother Paul J PJ Minutolo Filippo F
RSC advances 20150101 26
Inhibitors of human lactate dehydrogenase A (LDH-A) are promising therapeutic agents against cancer. The development of LDH-A inhibitors that possess cellular activities has so far proved to be particularly challenging, since the enzyme's active site is narrow and highly polar. In the recent past, we were able to develop a glucose-conjugated <i>N</i>-hydroxyindole-based LDH-A inhibitor designed to exploit the sugar avidity expressed by cancer cells (the Warburg effect). Herein we describe a stru ...[more]