By Stefan Jaroch (Editor), Hilmar Weinmann (Editor)
Chemical genomics is a hugely interdisciplinary and intensely fascinating box of analysis either in lecturers and within the lifestyles sciences undefined. The Ernst Schering examine origin Workshop fifty eight was once equipped to compile medical leaders within the box to debate the results of chemical genomics for drug discovery. numerous facets of the interface among chemistry and biology are lined during this quantity, resembling chemogenomics efforts within the pharmaceutical undefined, diversity-oriented synthesis, chemogenomic ways to the research of cellphone functionality, screening applied sciences, and usual items as instruments in chemical biology.
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Extra resources for Chemical Genomics: Small Molecule Probes to Study Cellular Function (Ernst Schering Research Foundation Workshop 58)
5 Chemogenomics Strategy for G-Protein Coupled Receptor Hit Finding The most challenging scenario in a Lead Generation project is to target a receptor without any information about small molecule ligands. In the case of GPCRs, the ﬁrst step is to identify phylogenetically related receptors for which lead-like compounds with pharmacological activity are known. These molecules will be called seeds. , topological or pharmacophore descriptors) would be applied to identify a focused screening subset from the corporate compound depository containing compounds that are similar to the seeds.
4 Synthetic Chemist’s Strategies . 6 Technology Aspects . . . . 7 Conclusion . . . . . . . References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 48 50 52 53 56 58 59 59 Abstract. This article covers the diversity-oriented synthesis (DOS) of small molecules in order to generate a collection of pure compounds that are attractive for lead generation in a phenotypic, high-throughput screening approach useful for chemical genetics and drug discovery programmes.
Activated by binding of their physiological ligand an extracellular signal is transformed by conformational changes of the receptor into an intracellular response. GPCR ligands are of diverse nature: these can be small molecules such as biogenic amines, amino acids, lipids, nucleosides, and nucleotides, small peptides, but also proteins such as chemokines. Excluding olfactory receptors, the current estimate of GPCRs in the human genome is about 400 (Venter et al. 2001; Wise et al. 2002). Among the 100 top-selling drugs, 25 act on GPCRs (Klabunde and Hessler 2002).
Chemical Genomics: Small Molecule Probes to Study Cellular Function (Ernst Schering Research Foundation Workshop 58) by Stefan Jaroch (Editor), Hilmar Weinmann (Editor)