Trends in Drug Research III: Proceedings of the 13th Noordwijkerhout-Caminero Symposium, the Netherlands, 6-11 May 2001 (Pharmacochemistry Library)

The tradition of setting new trends in medicinal chemistry continued at the 13th Symposium where topics included chemical and biological diversity, new paradigms in drug action, and new insights in receptor mechanisms. Other topics of great interest discussed, and included in these proceedings, are the discoveries in green chemistry, the interface between organic synthesis and biosynthesis, the growing problem of resistant micro-organisms and the possibilities to identify new, and better, antibiotics. And finally, in recent developments, the discovery of small molecules with insulin sensitizing properties. Content: Preface Page ix H. Timmerman Towards rational design of AMPA receptor ligands: An integrated medicinal, computational, biostructural and molecular pharmacological approach Original Research Article Pages 1-12 Anders Hogner, Jette S. Kastrup, Jeremy Greenwood, Stine B. Vogensen, Eva H. Møller, Tine B. Stensbøl, Jan Egebjerg, Povl Krogsgaard-Larsen From heparin to synthetic antithrombotics: The pentasaccharide story and follow-up Original Research Article Pages 13-19 C.A.A. van Boeckel A new future for synthesis? Original Research Article Pages 21-26 Alle Bruggink Directed evolution of enantioselective enzymes as catalysts in the production of chiral pharmaceuticals Original Research Article Pages 27-37 Manfred T. Reetz At the interface of organic synthesis and biosynthesis Original Research Article Pages 39-51 Rob Schoevaart, Tom Kieboom What can structure tell us about function in the estrogen receptors? Original Research Article Pages 53-56 Roderick E. Hubbard Molecular docking and dynamics simulations in the ligand binding domain of steroid hormone receptors Original Research Article Pages 57-66 Milou Kouwijzer, Jordi Mestres Peroxisome proliferator-activated receptors and reverse endocrinology Original Research Article Pages 67-79 Steven Kliewer, Glaxo Smith Kline Biomolecular mass spectrometry related to drug research Original Research Article Pages 81-94 Albert J.R. Heck, Claudia S. Maier Chemical and biological diversity in drug discovery Pages 95-96 P. Angeli, G. Gaviraghi Muscarinic acetylcholine receptor knockout mice: Phenotypical analysis and clinical implications Original Research Article Pages 97-113 J. Gomeza, M. Yamada, A. Duttaroy, W. Zhang, R. Makita, T. Miyakawa, J. Crawley, L. Zhang, H. Shannon, F.P. Bymaster, C.C. Felder, C. Deng, J. Wess Changes in expression of the orphan G-protein coupled receptor GPR7 in human painful peripheral neuropathies Original Research Article Pages 115-124 P.F. Zaratin, A. Quattrini, S. Previtali, G. Hervieu, M.A. Scheideler Computational methods for the analysis of molecular diversity Original Research Article Pages 125-133 Valerie J. Gillet, Peter Willett Enhancing drug discovery by acquisition of chemical diversity Original Research Article Pages 135-146 David Langley Chemical diversity as a driving force to design and put in practice synthetic strategies leading to combinatorial libraries for lead discovery and lead optimization Original Research Article Pages 147-160 Pierfausto Seneci Beyond G proteins: The role of accessory proteins in G protein-coupled receptor signalling Original Research Article Pages 161-173 Herwig Just, Eduard Stefan, Cornelia Czupalla, Bernd Nürnberg, Christian Nanoff, Michael Freissmuth Mechanisms of action of antipsychotic drugs: the role of inverse agonism at the D 2 dopamine receptor Original Research Article Pages 175-180 Philip G. Strange Agonist channeling of α 2 -adrenoceptor function Original Research Article Pages 181-192 Karl E.O. Åkerman, Johnny Näsman, Tomas Holmqvist, Jyrki P. Kukkonen Antibacterials as wonder drugs and how their effectiveness is being compromised Original Research Article Pages 193-205 Dasantila Golemi, Laurent Maveyraud, Jalal Haddad, Wenlin Lee, Akihiro Ishiwata, Kazuyuki Miyashita, Lionel Mourey, Sergei Vakulenko, Lakshmi Kotra, Jean-Pierre Samama, Shahriar Mobashery Pseudomonas aeruginosa quorum sensing: A target for antipa thogenic drug discovery Original Research Article Pages 207-212 Everett P. Greenberg Discovery and development of new anti-bacterial drugs Original Research Article Pages 213-225 Ian Chopra, Lars Hesse, Alexander O'Neill Discovery of small molecule insulin mimetics as potential novel antidiabetic agents Original Research Article Pages 227-236 Bei B. Zhang Expression databases for pharmaceutical lead optimisation Original Research Article Pages 237-247 L. Mike Furness New developments in the pharmacology of cannabinoids Original Research Article Pages 249-258 Roger G. Pertwee Author index Page 259 Subject index Pages 261-262