Development of Irreversible Inhibitors of MELK Kinase

Abstract

We have performed 3 rounds of in silico docking combined with in vitro MELK kinase activity assays. We have identified 5 independent scaffolds capable of MELK inhibition in the range of 100nm-Ium. These compounds are capable to tightly bind MELK catalytic domain as measured by OCS ruling out the protein aggregation and other non-specific inhibitory modalities. These leads are now being developed into potent anti-MELK drugs.

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Document Details

Document Type
Technical Report
Publication Date
Aug 01, 2007
Accession Number
ADA487036

Entities

People

  • Alexey V. Terskikh

Organizations

  • Sanford Burnham Prebys Medical Discovery Institute

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  • Molecular and Cellular Biochemistry