Design of peptide agonists.

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