Development of Irreversible Inhibitors of MELK Kinase

reportActive / Technical Report | Accession Number: ADA492687 | Open PDF

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-1um. These compounds are capable to tightly bind MELK catalytic domain as measured by DCS, ruling out the protein aggregation and other non-specific inhibiotry modalities. These leads are now being developed into potent anti-MELK drugs.

Author(s):
Terskikh, Alexey V.
Author Organization(s):
BURNHAM INST LA JOLLA CA
Descriptive Note:
Final rept. 15 Jul 2006-14 Jul 2008
Supplementary Note:
DOI: 10.21236/ADA492687
Pagination:
0008

Security Markings

DOCUMENT & CONTEXTUAL SUMMARY

Distribution:
Approved For Public Release
Distribution Statement:
Approved For Public Release; Distribution Is Unlimited.

RECORD

Collection: TR
Identifying Numbers
Contract/Grant Number(s):
W81XWH-06-1-0606
Monitor Series:
USAMRMC
 Subject Terms
Joint Capability Areas:
JCA_5_Command and Control; JCA_5.5.2_Task; JCA_5.5_Direct
Communities of Interest:
No COI(s) Identified
Descriptor(s):
*BREAST CANCER, *MAMMARY GLANDS, *INHIBITORS, BIOASSAY, PHOSPHORUS TRANSFERASES, CATALYSIS, IN VITRO ANALYSIS, PROTEINS, IRREVERSIBLE PROCESSES
Field(s)/Group(s):
Anatomy and Physiology, Medicine and Medical Research
Report Date:
2008 Aug 01
Creation Date:
2009 Feb 04