The inhibitory activity of an omega-alkoxy analogue of the HDAC inhibitor, Vorinostat (SAHA), against the 11 isoforms of HDAC is described and evaluated with regard to structural biology information retrieved through computational methods. Preliminary absorption and metabolism studies were performed, which positioned this compound as a potential candidate for further preclinical studies and delineated measures for improving its pharmacokinetic profile.

Vorinostat-Like Molecules as Structural, Stereochemical, and Pharmacological Tools

Auzzas L;
2010

Abstract

The inhibitory activity of an omega-alkoxy analogue of the HDAC inhibitor, Vorinostat (SAHA), against the 11 isoforms of HDAC is described and evaluated with regard to structural biology information retrieved through computational methods. Preliminary absorption and metabolism studies were performed, which positioned this compound as a potential candidate for further preclinical studies and delineated measures for improving its pharmacokinetic profile.
2010
Istituto di Chimica Biomolecolare - ICB - Sede Pozzuoli
HDAC promiscuous inhibitors
SAHA analogues
HDAC1-11 profile
class IIa-specific profile
absorption and metabolism
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.14243/162077
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