Identification of a novel and potent small molecule inhibitor of SRPK1: mechanism of dual inhibition of SRPK1 for the inhibition of cancer progression

• DOI: 10.18632/aging.202301
• Publication Date: 2020-12-03T14:44:23Z
• Authors: Anshuman Chandra; Hanumappa Ananda; Nagendra Singh; Imteyaz Qamar
• Keywords: Identification

Protein kinases are the family of attractive enzyme targets for drug design with relevance to cancer biology. Serine arginine protein kinase 1 (SRPK1) is responsible phosphorylation serine/arginine (SR)-rich proteins. Alternative Splicing Factor/Splicing Factor 2 (ASF/SF2) involved in mRNA editing. ASF/SF2 over expressed many cancers and plays crucial roles cell survival. Phosphorylation decisive its functions cancer. In search potential anticancer therapeutic agents attenuating ASF/SF2, we have explored specific inhibitors SRPK1 from natural like compounds databases using in-silico methods. Compound ZINC02154892 (C02) was found be most potent inhibitor SRPK1. In-vitro molecular biology studies shown C02 as a survival leukemic line. Structural analysis compound revealed unique pattern binding targeting ATP site along inhibiting recruitment by The possibilities used lead paving way development designing novel inferred current studies.