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Selective COX-1 Inhibition: A Therapeutic Target to be Reconsidered

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Since cyclooxygenase (COX) isozymes discovery, many papers and reviews have been published to describe the structural bases of COX inhibition, and to debate on the therapeutic and adverse effects of worldwide clinically used nonsteroidal anti-inflammatory drugs (NSAIDs), included COX-2 selective inhibitors (well known as Coxibs). COX-2 inhibition has been widely investigated, whereas the role of COX-1 in human pathophysiology is mostly not yet well ascertained. As time goes on, the cliche that the constitutively expressed isoform COX-1 is only involved in normal physiological functions, such as platelet aggregation, gastric mucosa protection and renal electrolyte homeostasis is going to be shattered. Low-dose aspirin, behaving as a preferential inhibitor of platelet COX-1, allowed to enlighten the role exerted by this isoenzyme in many mammalian cell types. This review would elucidate the most recent findings on selective COX-1 inhibition and their relevance to human pathology such as cancer, neuro-inflammation, cardioprotection, fever and pain. It would also focus on the design and development of new highly selective COX-1 inhibitors, useful tools in pharmacological studies aimed at gaining a deeper insight of the role of COX-1 in human health and disease. Among the traditional NSAIDs, other then aspirin and indomethacin, only few examples of selective COX-1 inhibitors (SC-560, FR122047, mofezolac, P6 and TFAP) have been so far identified. This review has also the scope to stimulate the development of novel drugs, which activity is COX-1 mediated.

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Keywords: Alzheimer's disease (AD); Arylpropionic Acids; Benzenesulfonanilide; COX-1 inhibition; Creutzfeldt-Jacob disease; Curcumin; Cyclooxygenase; Diarylheterocycles; Dipyrone; Nephrotoxic syndromes; Neuropathic pain; Oxicams; Parkinson's disease (PD); Pyrazolones; Salicylic acid; Stilbenes; Sulindac Derivatives; acetaminophen; adenocarcinoma; arachidonic acid; aspirin; atherosclerotic plaque; atherothrombosis; blood-brain barrier (BBB); celecoxib; cyclooxygenase; cyclooxygenase (COX); enzyme immunoassay; epileptogenesis; hippocampus; homeostasis; housekeeping gene; hydroperoxide; indomethacin; interleukin; isozymes; leptomeninges; lipopolysaccha-ride; lipopolysaccharide; microglia; mofezolac; mutagenesis; neoplasias; neuro-inflammation; neurodegenerative disorders; neuroinflammation; nociceptors; nonsteroidal anti-inflammatory drugs; phorbol myristate acetate; po-larographic oxygen electrode; prostacyclin; prostaglandin; prostanoids; radioimmunological assay; renal electrolyte; rofecoxib; selective inhibitors; structure-activity relationships; thromboxane; traumatic brain injury; tumor necrosis factor; tumorigenesis; tumorigenicity; ventrolateral medulla (VLM); ventromedial preoptic nucleus (VMPO)

Document Type: Research Article

Publication date: 01 November 2010

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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