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

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.

journal_name

J Med Chem

authors

Kaplánek R,Martásek P,Grüner B,Panda S,Rak J,Masters BS,Král V,Roman LJ

doi

10.1021/jm300805x

subject

Has Abstract

pub_date

2012-11-26 00:00:00

pages

9541-8

issue

22

eissn

0022-2623

issn

1520-4804

journal_volume

55

pub_type

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