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SUMMARY:"Chemical Biology and Chemogenomics in Drug Discovery" - Professor
  Hugo Kubinyi\, Weisenheim am Sand
DTSTART:20100302T141500Z
DTEND:20100302T151500Z
UID:TALK22774@talks.cam.ac.uk
CONTACT:Susan Begg
DESCRIPTION:Chemical Biology and Chemogenomics in Drug Discovery\n\nHugo K
 ubinyi\, BASF SE and University of Heidelberg (retired)\, Germany\, URL  w
 ww.kubinyi.de\n\nChemical biology [1] and chemogenomics [2-4] are recent s
 trategies in the systematic search for new lead structures. Chemical biolo
 gy studies the influence of chemical libraries on simple biological system
 s\, e.g. stem cells\, yeast and other cellular systems\, parasites\, or sm
 all animals\, like Caenorhabditis elegans\, Drosophila or the zebrafish\, 
 Danio rerio. If a new phenotype is discovered by the action of a certain s
 ubstance\, the next step is the identification of the respective target. \
 nChemogenomics aims to discover selective ligands of a certain target with
 in a family of proteins or to shift biological activity and/or selectivity
  from one target to a related one. This is achieved by testing libraries o
 f chemically related compounds in classes of evolutionary related targets 
 (GPCRs\, integrins\, nuclear hormone receptors\, aspartyl\, metallo-\, ser
 ine and cysteine proteases\, kinases\, phosphatases\, ion channels\, etc.)
 . In lead optimization\, one should cover the chemical space around the cu
 rrent lead as completely as possible\, in order not to loose any interesti
 ng candidate and to obtain a solid intellectual property position. Know-ho
 w from lead optimization at one target can be transferred to another targe
 t\; in addition\, several analogs of non-specific compounds may show signi
 ficantly different selectivities. Another systematic method for the discov
 ery of new leads is the SOSA (selective opimization of side activities) ap
 proach\, recently proposed by Camille Wermuth [5]. \nTypical chemogenomics
  applications will be presented and the advantages of these approaches\, a
 s compared to classical screening\, will be highlighted. \n\nReferences\n\
 n[1]	Schreiber\, S. L.\, Kapoor\, T. and Wess\, G.\, Eds.\, Chemical Biolo
 gy. From Small Molecules to System Biology and Drug Design\, Wiley-VCH\, W
 einheim\, 2007.\n[2]	Kubinyi\, H. and Müller\, G.\, Eds.\, Chemogenomics 
 in Drug Discovery - A Medicinal Chemistry Perspective (Volume 22 of Method
 s and Principles in Medicinal Chemistry\, Mannhold\, R.\, Kubinyi\, H. and
  Folkers\, G.\, Eds.)\, Wiley-VCH\, Weinheim\, 2004.\n[3]	Jacoby\, E.\, Ed
 .\, Chemogenomics. Knowledge-based Approaches to Drug Discovery\, Imperial
  College Press\, London\, 2006.\n[4]	Kubinyi\, H.\, Ernst Schering Researc
 h Foundation Workshop 58\, "Chemical Genomics. Small Molecule Probes to St
 udy Cellular Function"\, Jaroch\, S. and Weinmann\, H.\, Eds.\, Springer\,
  Berlin 2006\, pp. 1-19 (www.kubinyi.de/ schering58-2006.pdf).\n[5]	Wermut
 h\, C. G.\, J. Med. Chem. 47\, 1303-1314 (2004).\n\n\n
LOCATION:Unilever Lecture Theatre\, Unilever Centre for Molecular Informat
 ics\, Dept. of Chemistry
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