Preferred Label : HDAC Inhibitor MPT0E028;
NCIt synonyms : 3-(1-Benzenesulfonyl-2,3-dihydro-1H-indol-5-yl)-N-hydroxy-acrylamide; (E)-N-hydroxy-3-(1-(phenylsulfonyl)indolin-5-yl)acrylamide;
NCIt definition : An orally bioavailable N-hydroxyacrylamide-derived inhibitor of both human pan-histone
deacetylase (HDAC) enzymes and the serine/threonine protein kinase Akt (protein kinase
B), with potential antineoplastic activity. Upon administration, HDAC inhibitor MPT0E028
selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins
and leads to the accumulation of highly acetylated histones. This may result in both
an induction of chromatin remodeling, and the selective transcription of tumor suppressor
genes. This prevents cell division and induces both cell cycle arrest and apoptosis,
which may inhibit the proliferation of susceptible tumor cells. In addition, MPT0E028
inhibits the phosphorylation and activation of Akt, which prevents the activation
of downstream signaling pathways, independent of its HDAC inhibitory activity. HDACs,
upregulated in many tumor cell types, are a family of enzymes that deacetylate histone
proteins. Akt, overexpressed in many tumor cell types, plays a key role in tumor cell
proliferation and survival.;
CAS number : 1338320-94-7;
Molecule name : MPT-0E028; MPT 0E028;
Origin ID : C120312;
UMLS CUI : C3661262;
Automatic exact mappings (from CISMeF team)
- Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
