By Stefan Jaroch (Editor), Hilmar Weinmann (Editor)
Chemical genomics is a hugely interdisciplinary and extremely fascinating box of analysis either in lecturers and within the existence sciences undefined. The Ernst Schering learn beginning Workshop fifty eight used to be prepared to assemble medical leaders within the box to debate the results of chemical genomics for drug discovery. a number of facets of the interface among chemistry and biology are lined during this quantity, similar to chemogenomics efforts within the pharmaceutical undefined, diversity-oriented synthesis, chemogenomic techniques to the examine of mobilephone functionality, screening applied sciences, and ordinary 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)
Kluwer/ESCOM, Dordrecht, 1998, pp 225–252; also published in Persp Drug Design Discov 1998, 9–11:225–252 Kubinyi H (2004) Drug discovery from side effects. In: Kubinyi H, Müller G, (eds) Chemogenomics in drug discovery – a medicinal chemistry perspective, vol. 22 of Methods and principles in medicinal chemistry. Mannhold R, Kubinyi H, Folkers G (eds) Wiley-VCH, Weinheim, pp 43–67 Kubinyi H, Müller G (eds) (2004) Chemogenomics in drug discovery – a medicinal chemistry perspective, vol. 22, Methods and principles in medicinal chemistry.
3b, validating the design principle for (a subset of) peptide receptors: (a) binding is mainly seen for the peptide receptors with ﬁve out of ten peptide-binding GPCRs (vasopressin V1, µ opiate, melanocortin MC3, neurokinin NK1, and angiotensin AT1 receptor), showing afﬁnity toward these library subsets; (b) no activities are seen for the purinergic GPCRs and some unexpected afﬁnity is found for some of the lipid-binding GPCRs; (c) two novel series with submicromolar binding afﬁnities for the NK1 and the µ opiate receptor, and (d) one novel series with micromolar binding afﬁnity toward the V1 receptor could be identiﬁed.
3 Nature’s Strategies . . . . . 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.
Chemical Genomics: Small Molecule Probes to Study Cellular Function (Ernst Schering Research Foundation Workshop 58) by Stefan Jaroch (Editor), Hilmar Weinmann (Editor)