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 ProfilesTM from BICOLL’s highly diversified 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.
About BICOLL:
BICOLL is a biopharmaceutical company, offering pre-clinical support in the area of Drug Discovery from Natural Products and Medicinal Chemistry. Dedicated to the discovery and optimization of the highest quality lead compounds, BICOLL provides an efficient, multi-disciplinary approach to drug discovery. With outstanding expertise in high tech natural product chemistry and validated experience in medicinal chemistry, BICOLL increases quality and quantity of the drug discovery pipeline of its partner's candidates portfolio. The BICOLL Group provides its services to a number of international clients of various fields of interest, e.g. pharmaceutical and agrochemical industry.
The BICOLL Group comprises two legal entities:
BICOLL GmbH in Munich, Germany and BICOLL Biotechnology (Shanghai) Co. Ltd., P.R. China. Technology development, cooperation management and marketing are functions in Munich, while facilities for research and development are located in Shanghai. BICOLL currently employs 40 people at both locations. About EMBL: The European Molecular Biology Laboratory is a basic research institute funded by public research monies from 20 member states (Austria, Belgium, Croatia, Denmark, Finland, France, Germany, Greece, Iceland, Ireland, Israel, Italy, Luxembourg, the Netherlands, Norway, Portugal, Spain, Sweden, Switzerland and the United Kingdom) and associate member state Australia.
Research at EMBL is conducted by approximately 85 independent groups covering the spectrum of molecular biology. The Laboratory has five units: the main Laboratory in Heidelberg, and Outstations in Hinxton (the European Bioinformatics Institute), Grenoble, Hamburg, and Monterotondo near Rome. The cornerstones of EMBL’s mission are: to perform basic research in molecular biology; to train scientists, students and visitors at all levels; to offer vital services to scientists in the member states; to develop new instruments and methods in the life sciences and to actively engage in technology transfer activities. Around 190 students are enrolled in EMBL’s International PhD programme. Additionally, the Laboratory offers a platform for dialogue with the general public through various science communication activities such as lecture series, visitor programmes and the dissemination of scientific achievements.
For further information about BICOLL please contact:
Dr. Nicole Feling, Public Relations Management, BICOLL Tel: +49 (0) 89 / 82010630, nicole.feling@ bicoll-group.com www.bicoll-group.com
For further information about EMBL please contact:
Sonia Furtado – Press Officer, EMBL +49 (0) 6221 / 387 8263 sonia.furtado@embl.de www.embl.org Press Release / Story Bicoll and EMBL announce identification of aurora kinase inhibitors URL http://www.bicoll-group.com/index.php?page=6100 Nicole Feling Email nicole.feling@bicoll-group.com
