Journal
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 53, 2013
Volume 53, Issue -, Pages 557-+Publisher
ANNUAL REVIEWS
DOI: 10.1146/annurev-pharmtox-010510-100456
Keywords
peptide pharmacophores; peptide hormones; peptide neurotransmitters; blood-brain barrier; topographical structures; conformation and biological activity; peptide stability
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Funding
- NIDA NIH HHS [R01 DA013449] Funding Source: Medline
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Peptide hormones and neurotransmitters are of central importance in most aspects of intercellular communication and are involved in virtually all degenerative diseases. In this review, we discuss physicochemical approaches to the design of novel peptide and peptidomimetic agonists, antagonists, inverse agonists, and related compounds that have unique biological activity profiles, reduced toxic side effects, and, if desired, the ability to cross the blood-brain barrier. Designing ligands for specific biological and medical needs is emphasized, as is the close collaboration of chemists and biologists to maximize the chances for success. Special emphasis is placed on the use of conformational (phi-psi space) and topographical (chi space) considerations in design.
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