Abstract:
:Nitric Oxide (NO) is widely recognized as an important messenger and effector molecule in a variety of biological systems. There is strong evidence from animal models that elevated or lowered NO levels are associated with a variety of pathological states. In nature, NO is synthesised from the amino acid l-arginine by a small family of closely related oxygenase enzymes: the nitric oxide synthases (NOS). A number of studies in animals have associated excessive NO production by one of these enzymes--the inducible NOS isoform (iNOS or NOS-II)--with acute and chronic inflammation in model systems and have also demonstrated that administration of NOS inhibitors can produce beneficial effects. Regrettably, however, the relatively poor potency, selectivity and pharmacokinetic (ADME) profiles of the available inhibitors have so far precluded a convincing demonstration of their efficacy in the clinic. This review will describe the current state of knowledge of the structure and function of NOS and the various approaches that are being followed in the search for truly selective NOS inhibitors as therapeutic agents for inflammatory diseases.
journal_name
Curr Top Med Chemjournal_title
Current topics in medicinal chemistryauthors
Tinker AC,Wallace AVdoi
10.2174/156802606775270297keywords:
subject
Has Abstractpub_date
2006-01-01 00:00:00pages
77-92issue
2eissn
1568-0266issn
1873-4294journal_volume
6pub_type
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journal_title:Current topics in medicinal chemistry
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