Preferred Label : CLK Inhibitor CTX-712;
NCIt synonyms : Splicing Modulator CTX-712;
NCIt definition : An orally bioavailable inhibitor of CLK family kinases, with potential antineoplastic
activity. Upon oral administration, CLK inhibitor CTX-712 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.;
Molecule name : CTX-712; CTX 712;
NCI Metathesaurus CUI : CL1906855;
Origin ID : C199490;
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