NADPH oxidase inhibitors: a patent review.

Abstract

INTRODUCTION:

NADPH oxidases, a family of multi-subunit enzyme complexes, catalyze the production of reactive oxygen species (ROS), which may contribute to the pathogenesis of a variety of diseases. In addition to the first NADPH oxidase found in phagocytes, four non-phagocytic NADPH oxidase isoforms have been identified, which all differ in their catalytic subunit (Nox1-5) and tissue distribution.

AREAS COVERED:

This paper provides a comprehensive review of the patent literature on NADPH oxidase inhibitors, small molecule Nox inhibitors, peptides and siRNAs.

EXPERT OPINION:

Since each member of the NADPH oxidase family has great potential as a therapeutic target, several different compounds have been registered as NADPH oxidase inhibitors in the patent literature. As yet, none have gone through clinical trials, and some have not completed preclinical trials, including safety and specificity evaluation. Recently, small molecule pyrazolopyridine and triazolopyrimidine derivatives have been submitted as potent NADPH oxidase inhibitors and reported as first-in-class inhibitors for idiopathic pulmonary fibrosis and acute stroke, respectively. Further clinical efficacy and safety data are warranted to prove their actual clinical utility.

• Authors: Jung-Ae Kim, Ganesh Prasad Neupane, Eung Seok Lee, Byeong-Seon Jeong, Byung Chul Park, Pritam Thapa
• Journal: Expert opinion on therapeutic patents (Expert Opin Ther Pat) Vol. 21 Issue 8 Pg. 1147-58 (Aug 2011) ISSN: 1744-7674 [Electronic] England
• PMID: 21554154 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Enzyme Inhibitors
• Peptides
• RNA, Small Interfering
• Reactive Oxygen Species
• NADPH Oxidases

Topics

• Animals
• Enzyme Inhibitors (chemistry, pharmacology)
• Genetic Therapy (methods)
• Humans
• Idiopathic Pulmonary Fibrosis (drug therapy)
• NADPH Oxidases (antagonists & inhibitors, genetics, metabolism)
• Patents as Topic
• Peptides (chemistry, pharmacology)
• RNA Interference
• RNA, Small Interfering (metabolism)
• Reactive Oxygen Species (metabolism)
• Stroke (drug therapy)
• Structure-Activity Relationship