Nitric Oxide Synthases Activation and Inhibition by Metallacarborane-Cluster-Based Isoform-Specific Affectors
Year: 2012
Type: article
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.
Source: Journal of Medicinal Chemistry
DOI: 10.1021/jm300805x
Institutions: University of Chemistry and Technology, Prague, Charles University, General University Hospital in Prague, Czech Academy of Sciences, Czech Academy of Sciences, Institute of Inorganic Chemistry, The University of Texas at San Antonio Health Science Center, Sanofi (France), Sanofi (Czechia)
Language: English
Topic: Boron Compounds in Chemistry
Subfield: Radiology, Nuclear Medicine and Imaging
Field: Medicine
Domain: Health Sciences
Open Access status: green
OpenAlex ID: W2097928666