Astex
Encyclopedia
Astex Therapeutics is a biotechnology
Biotechnology
Biotechnology is a field of applied biology that involves the use of living organisms and bioprocesses in engineering, technology, medicine and other fields requiring bioproducts. Biotechnology also utilizes these products for manufacturing purpose...

 company focused on the discovery and development of drugs in oncology
Oncology
Oncology is a branch of medicine that deals with cancer...

 and other areas. Astex was founded in 1999 by Sir Tom Blundell
Tom Blundell
Sir Tom Leon Blundell, FRS, FMedSci is a British biochemist and science administrator. Up until 2009, he was the Sir William Dunn Professor of Biochemistry and head of the Department of Biochemistry at the University of Cambridge....

, Chris Abell
Chris Abell
Christopher Abell, MA, PhD is a British biological chemist. As of 2009, he is a professor of biological chemistry at the Department of Chemistry of the University of Cambridge and Todd-Hamied Fellow of Christ's College....

 & Harren Jhoti, and is located in Cambridge
Cambridge
The city of Cambridge is a university town and the administrative centre of the county of Cambridgeshire, England. It lies in East Anglia about north of London. Cambridge is at the heart of the high-technology centre known as Silicon Fen – a play on Silicon Valley and the fens surrounding the...

, UK.

The company's research efforts focus on utilization of a proprietary "drug discovery engine" dubbed Pyramid. Astex has also solved the structure of two key cytochrome P450
Cytochrome P450 oxidase
The cytochrome P450 superfamily is a large and diverse group of enzymes. The function of most CYP enzymes is to catalyze the oxidation of organic substances. The substrates of CYP enzymes include metabolic intermediates such as lipids and steroidal hormones, as well as xenobiotic substances...

 isoenzymes involved in drug metabolism
Drug metabolism
Drug metabolism is the biochemical modification of pharmaceutical substances by living organisms, usually through specialized enzymatic systems. This is a form of xenobiotic metabolism. Drug metabolism often converts lipophilic chemical compounds into more readily excreted polar products...

, 2C9
CYP2C9
Cytochrome P450 2C9 is a protein that in humans is encoded by the CYP2C9 gene.- Function :CYP2C9 is an important cytochrome P450 enzyme with a major role in the oxidation of both xenobiotic and endogenous compounds. CYP2C9 makes up about 18% of the cytochrome P450 protein in liver microsomes...

 & 3A4
CYP3A4
Cytochrome P450 3A4 , a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body. CYP3A4 is involved in the oxidation of the largest range of substrates of all the CYPs. As a result, CYP3A4 is present in...

, which the company hopes will help in optimizing the pharmacokinetic properties and safety of their lead compounds.

Astex's first drug candidate, a cell cycle
Cell cycle
The cell cycle, or cell-division cycle, is the series of events that takes place in a cell leading to its division and duplication . In cells without a nucleus , the cell cycle occurs via a process termed binary fission...

 inhibitor, entered Phase I clinical trials in 2005, and two other candidates are in pre-clinical development
Pre-clinical development
In drug development, pre-clinical development is a stage of research that begins before clinical trials can begin, and during which important feasibility, iterative testing and drug safety data is collected....

.

Further reading

  • Carr RA, Congreve M, Murray CW, Rees DC (2005) Fragment-based lead discovery: leads by design. Drug Discov Today 10: 987-92.
  • Congreve M, Murray CW, Blundell TL (2005) Structural biology and drug discovery. Drug Discov Today 10: 895-907.
  • Williams PA, Cosme J, Vinkovic DM, et al. (2004) Crystal structures of human cytochrome P450 3A4 bound to metyrapone and progesterone Science 305: 683-86 (available online by registration at Science website)
  • Astex Technology: Pioneering Fragment-based Lead Discovery
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