Nitric oxide synthases activation and inhibition by metallacarborane- cluster-based isoform-specific affectors

Robert Kaplánek, Pavel Martásek, Bohumír Grüner, Satya Panda, Jakub Rak, Bettie Sue Siler Masters, Vladimír Král, Linda J. Roman

Research output: Contribution to journalArticle

11 Scopus citations

Abstract

A small library of boron-cluster- and metallacarborane-cluster-based ligands was designed, prepared, and tested for isoform-selective activation or inhibition of the three nitric oxide synthase isoforms. On the basis of the concept of creating a hydrophobic analogue of a natural substrate, a stable and nontoxic basic boron cluster system, previously used for boron neutron capture therapy, was modified by the addition of positively charged moieties to its periphery, providing hydrophobic and nonclassical hydrogen bonding interactions with the protein. Several of these compounds show efficacy for inhibition of NO synthesis with differential effects on the various nitric oxide synthase isoforms.

Original languageEnglish (US)
Pages (from-to)9541-9548
Number of pages8
JournalJournal of Medicinal Chemistry
Volume55
Issue number22
DOIs
StatePublished - Nov 26 2012

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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