One of the most recent additions to the Ximbio website is a protein kinase D inhibitor CRT5 (CRT0066051) small molecule. CRT5 is a novel pyrazine benzamide PKD inhibitor developed internally at the Cancer Research Technology Discovery Laboratories (CRT-DL).
Structure of CRT5
It was developed as previous studies showed that VEGF (vascular endothelial growth factor) activated PKD in endothelial cells in order to regulate a variety of cellular functions including signalling events, proliferation, migration and angiogenesis. The effects of CRT5 were measured in HUVECs (human umbilical vein endothelial cells). CRT5 blocked the activity of both PKD isoforms; PKD1 and PKD2 after stimulation with VEGF.
Many studies investigating the role of PKD have been hampered by the lack of specific inhibitors to PKD. CRT5 has been shown, by it's IC50 number,to be 100-fold more effective at PKD1 inhibition than CID755673. CRT5 can also inhibit PKD activity in vitro and in intact endothelial cells. Due to this it is thought that CRT5 and/or its derivatives may have great potential, both as a biochemical tool and as a starting point for novel anti-angiogenic therapeutic drug development.
CRT-DLis a small molecule drug discovery organisation which works in partnership with the best minds from industry and academia. Theirexpertise spans cancer target validation and disease positioning, assay development and HTS, protein crystallography, medicinal chemistry, PK-PD and cancer models.
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