Bicoll and the European Molecular Biology Laboratory (EMBL) identify aurora kinase inhibitors

24-Jun-2010 - Germany

Bicoll GmbH and EMBL announced the successful completion of a joint research project on the identification of active compounds as inhibitors of aurora kinases.

Aurora kinases have gained a great deal of attention as possible anticancer drug targets as these serine/threonine kinases are frequently over expressed in human tumours. For a research project on genetic instability and cellular proliferation caused by aurora kinase expression in several cancer entities, including multiple myeloma, the group of Dr. Joe Lewis, Head of Chemical Biology Core Facility at EMBL Heidelberg, has been searching for novel aurora kinase inhibitors supplementing already known clinical aurora kinase inhibitors such as VX680. The search for promising compounds was based on the screening of BICOLL’s library of plant metabolites.

“We were looking for a cost- and resource-efficient way to expand our chemical structural variety on the search of novel aurora kinase inhibitors without the need for expensive virtual screening or access to hundreds of thousands of structures,” explains Dr. Joe Lewis. ”Bicoll’s idea of using pooled and fractionated small molecule collections, derived from endemic Asian plants has already successfully led to the identification of hit compounds in various high-throughput-screening processes in other cooperations. We were curious to find out, whether natural products could also demonstrate their proof-of-concept for our biochemical screening methods.” he continues.

BICOLL provided a set of 1,000 Profiles™ (equals around 3-10.000 different small molecules) from its proprietary small molecule natural product library to EMBL's robust biochemical screening program, which resulted in 18 hit clusters showing specific kinase activity. Because of the unexpected high hit rate of 2%, the group of EMBL researchers elected to focus on 4 hit clusters for isolation and structure elucidation.

“Within only three months and a second round of screening, BICOLL identified and structurally elucidated two pure compounds with interesting structural motifs for our client’s further development programs,” comments Dr. Kai Lamottke, Managing Director of BICOLL. “Subsequent investigation of our pure natural compound database, using the newly found structural motifs, additionally led to the testing in EMBL's protein-protein interaction test. Additional compounds for further structure-activity-relationship could be identified.” he announces.

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