Preferred Label : Rogocekib;
NCIt synonyms : Splicing Modulator CTX-712; CLK Inhibitor CTX-712;
NCIt definition : An orally bioavailable inhibitor of CLK family kinases, with potential antineoplastic
activity. Upon oral administration, rogocekib binds to and inhibits the activity of
CLK family kinases, thereby inhibiting the phosphorylation of serine/arginine-rich
(SR) domain-containing splicing factors (SFs). This modulates RNA splicing, prevents
the expression of certain tumor-associated genes, and inhibits tumor cell proliferation.
In many cancer cells, core spliceosome proteins, including SF3B1, U2 small nuclear
ribonucleoprotein auxiliary factor 1 (U2AF1), serine/arginine-rich splicing factor
2 (SRSF2) and U2 small nuclear ribonucleoprotein auxiliary factor subunit-related
protein 2 (ZRSR2), are mutated and aberrantly activated leading to a dysregulation
of mRNA splicing. CLK family kinases, an evolutionarily conserved group of kinases,
phosphorylates various SR proteins including SR domain-containing SFs.;
UNII : XE88VQP94E;
CAS number : 2144751-78-8;
Molecule name : CTX 712; CTX-712;
NCI Metathesaurus CUI : CL1929091;
Origin ID : C206982;
concept_is_in_subset
