Preferred Label : CLK Inhibitor BH-30236;
NCIt synonyms : CLK1/2/4 Inhibitor BH-30236;
NCIt definition : An orally bioavailable macrocyclic ATP-competitive inhibitor of CDC2-like kinase (CLK)
family kinases, including CLK1, CLK2 and CLK4, with potential antineoplastic activity.
Upon oral administration, CLK inhibitor BH-30236 targets, binds to and inhibits the
activity of CLK1/2/4, 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 : BH-30236; BH 30236;
Origin ID : C208220;
concept_is_in_subset
- has_target
