Molecular recognition at kappa opioid receptors

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Structure - activity relationships are rarely straightforward, and often are more complicated than they appear. For this reason, the use of site-directed mutagenesis as a complementary tool to analyze structure - activity relationships has been invaluable. Here, we illustrate how site-directed mutagenesis has led to greater insight into the molecular basis for molecular recognition of norbinaltorphimine and to the design of novel kappa antagonists. Given the paucity of high-resolution crystal structures for membrane-bound receptors, the use of a coordinated "two-dimensional" paradigm that involves molecular modification of both the ligand and the receptor, affords a useful approach to the study of molecular recognition. This paradigm has led to the design of highly potent and selective kappa opioid receptor antagonists that are derivatives of the delta opioid receptor antagonist, naltrindole.

Original languageEnglish (US)
Pages (from-to)1387-1391
Number of pages5
JournalPure and Applied Chemistry
Volume73
Issue number9
DOIs
StatePublished - Jan 1 2001

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Molecular recognition
kappa Opioid Receptor
Mutagenesis
naltrindole
Narcotic Antagonists
delta Opioid Receptor
Crystal structure
Ligands
Derivatives
Membranes
norbinaltorphimine

Cite this

Molecular recognition at kappa opioid receptors. / Portoghese, Philip S.

In: Pure and Applied Chemistry, Vol. 73, No. 9, 01.01.2001, p. 1387-1391.

Research output: Contribution to journalArticle

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