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• W1523205249 abstract "Publisher Summary This chapter describes a systematic approach for designing potent and selective agonists for GPCRs. Sufficient and detailed experiments are provided in the chapter as a model to synthesize the peptide agonists successfully. The design of peptides resulting in potent and selective agonist activities is difficult because of several factors, but success can be normally obtained with a systematic approach. This approach requires highly interdisciplinary considerations that combine knowledge gathered from structure–biological activity relationships, conformational analysis, computer-assisted calculations and molecular design, biophysical analysis of structures (spectroscopy, crystallography, etc.), and in vivo and in vitro assays. In addition, new asymmetric syntheses and other synthetic methodologies are often important in preparing the designed compounds. Once a lead compound (whether from nature or from a peptide library prepared by combinatorial chemistry) has been defined based on the desired agonist activity, it is often desirable to determine the minimal structural requirements for bioactivity." @default.
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• W1523205249 date "2002-01-01" @default.
• W1523205249 modified "2023-09-22" @default.
• W1523205249 title "Design of peptide agonists" @default.
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• W1523205249 doi "https://doi.org/10.1016/s0076-6879(02)43128-x" @default.
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