Preferred Label : RSK1-4 Inhibitor PMD-026;
NCIt synonyms : RSK Inhibitor PMD-026;
NCIt definition : An orally bioavailable inhibitor of the serine/threonine kinase p90 ribosomal S6 kinase
(p90RSK; RSK) subtypes 1-4, with high selectivity for RSK subtype 2 (RSK2), with potential
antineoplastic activity. Upon administration of the RSK1-4 inhibitor PMD-026, this
agent targets and inhibits the RSK subtypes, thereby inhibiting RSK-mediated signaling.
This prevents the phosphorylation and activation of the transcription factor Y-box
binding protein-1 (YB-1) and leads to cell cycle arrest, an induction of apoptosis,
and an inhibition of tumor cell proliferation in RSK-expressing tumor cells. RSK is
overexpressed in a variety of cancers, especially in triple negative breast cancer
(TNBC). It plays a key role in tumor cell proliferation, differentiation, survival,
and metastasis.;
Molecule name : PMD 026; PMD-026;
NCI Metathesaurus CUI : CL979208;
Origin ID : C166135;
UMLS CUI : C5237722;
Semantic type(s)
- concept_is_in_subset
- has_target
