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Pure Appl. Chem. Vol.
73, No. 9, pp. 1387-1391 (2001)
Pure and Applied Chemistry
Vol. 73, Issue 9
Molecular recognition at kappa opioid receptors*
Philip S. Portoghese
Department of Medicinal Chemistry, College of Pharmacy,
University of Minnesota, Minneapolis, USA
Abstract: Structureactivity 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
structureactivity 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.
*Plenary lecture presented at the Hungarian-German-Italian-Polish
Joint Meeting on Medicinal Chemistry, Budapest, Hungary, 2 6 September
2001. Other presentations are published in this issue, pp.
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