Ontology highlight
ABSTRACT:
SUBMITTER: Prabhu VV
PROVIDER: S-EPMC7588802 | biostudies-literature | 2020 Oct
REPOSITORIES: biostudies-literature
Prabhu Varun Vijay VV Morrow Sara S Rahman Kawakibi Abed A Zhou Lanlan L Ralff Marie M Ray Jocelyn J Jhaveri Aakash A Ferrarini Isacco I Lee Young Y Parker Cassandra C Zhang Yiqun Y Borsuk Robyn R Chang Wen-I WI Honeyman Joshua N JN Tavora Fabio F Carneiro Benedito B Raufi Alexander A Huntington Kelsey K Carlsen Lindsey L Louie Anna A Safran Howard H Seyhan Attila A AA Tarapore Rohinton S RS Schalop Lee L Stogniew Martin M Allen Joshua E JE Oster Wolfgang W El-Deiry Wafik S WS
Neoplasia (New York, N.Y.) 20201023 12
ONC201 was originally discovered as TNF-Related Apoptosis Inducing Ligand (TRAIL)-inducing compound TIC10. ONC201 appears to act as a selective antagonist of the G protein coupled receptor (GPCR) dopamine receptor D2 (DRD2), and as an allosteric agonist of mitochondrial protease caseinolytic protease P (ClpP). Downstream of target engagement, ONC201 activates the ATF4/CHOP-mediated integrated stress response leading to TRAIL/Death Receptor 5 (DR5) activation, inhibits oxidative phosphorylation v ...[more]