Abstract
Many peptide hormones and neurotransmitters exert their various biological effects through interaction with several distinct receptor types. The design and synthesis of peptide analogs with high specificity for a particular receptor class and with altered “efficacy” (antagonists or superagonists) represent major goals in peptide drug development. The classical approach based on amino acid substitutions, deletions or additions has been used for more than three decades in peptide analog design and in many cases has permitted the development of antagonists or of more specific receptor ligands. It still represents the method of choice for determining initial structure-activity relationships with a newly discovered peptide hormone or neurotransmitter. In recent years our increasing knowledge of the receptors interacting with biologically active peptides has led to new design principles. In particular, new design concepts based on the distinct conformational requirements, proposed different membrane environment and putative proximity relationships of the different receptor classes interacting with a given peptide hormone or neurotransmitter have been developed.
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© 1988 Plenum Press, New York
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Schiller, P.W. (1988). New Concepts in Peptide Analog Design. In: Chrétien, M., McKerns, K.W. (eds) Molecular Biology of Brain and Endocrine Peptidergic Systems. Biochemical Endocrinology. Springer, Boston, MA. https://doi.org/10.1007/978-1-4684-8801-2_4
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DOI: https://doi.org/10.1007/978-1-4684-8801-2_4
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