SRPK inhibitor

Description

Serine/arginine-rich protein kinase 1 (SRPK1) targets proteins that contain multiple serine/arginine (SR) dipeptides, including SR-rich splicing factor 1, SRSF1. SRPIN340 is an isonicotinamide compound that inhibits SRPK1 (K_i = 0.89 μM). It is about 10-fold less effective against SRPK2 and does not inhibit the related SRPKs, Clk1 and Clk4. SRPIN340 suppresses the propagation of Sindbis virus in Vero cells and the replication of hepatitis C virus in Huh7/Rep-Feo-2a cells. By blocking SRPK1-mediated phosphorylation of SRSF1, SRPIN340 modulates alternative splicing of VEGF, reducing neovascularization both in cells and in animals.

The Uses of SRPK inhibitor

SRPIN340 is a SRPK1 kinase inhibitor, which shows potential novel targeted therapeutic strategy in prostate cancer.

What are the applications of Application

SRPIN 340 is an SRPK1 inhibitor

References

1) Fukuhara?et al.?(2006),?Utilization of host SR protein kinases and RNA-splicing machinery during viral replication; Proc. Natl. Acad. Sci. USA,?103?11329 2) Gammons?et al.?(2013),?SRPK1 inhibition modulates VEGF splicing to reduce pathological neovascularization in a rat model of retinopathy of prematurity; Invest. Ophthalmol. Vis. Sci.,?54?5797 3) Gammons?et al.?(2014),?Targeting SRPK1 to control VEGF-mediated tumour angiogenesis in metastatic melanoma; Br. J. Cancer,?111?477