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Design of peptide and peptidomimetic ligands with novel pharmacological activity profiles.

ABSTRACT: 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 (?-? space) and topographical (? space) considerations in design.

SUBMITTER: Hruby VJ

PROVIDER: S-EPMC5079645 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature

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Design of peptide and peptidomimetic ligands with novel pharmacological activity profiles.

Hruby Victor J VJ Cai Minying M

Annual review of pharmacology and toxicology 20130101

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 spec ...[more]

PMID: 23294313

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