关键词: Serine proteases gastrointestinal inflammation inflammation kallikreins lung inflammation neutrophil elastase plasmin skin inflammation therapeutical inhibitors

Mesh : Animals Anti-Inflammatory Agents / pharmacology Drug Design Humans Inflammation / drug therapy enzymology physiopathology Inflammation Mediators / metabolism Patents as Topic Serine Proteases / drug effects metabolism Serine Proteinase Inhibitors / pharmacology

来  源:   DOI:10.1080/13543776.2018.1406478   PDF(Sci-hub)

Abstract:
Inflammation is a physiological part of the complex biological response of tissues to counteract various harmful signals. This process involves diverse actors such as immune cells, blood vessels, and nerves as sources of mediators for inflammation control. Among them serine proteases are key elements in both physiological and pathological inflammation.
Serine protease inhibitors to treat inflammatory diseases are being actively investigated by various industrial and academic institutions. The present review covers patent literature on serine protease inhibitors for the therapy of inflammatory diseases patented between 2011 and 2016.
Serine proteases regulating inflammation are versatile enzymes, usually involved in proinflammatory cytokine production and activation of immune cells. Their dysregulation during inflammation can have devastating consequences, promoting various diseases including skin and lung inflammation, neuroinflammation, and inflammatory arthritis. Several serine proteases were selected for their contribution to inflammatory diseases and significant efforts that are spread to develop inhibitors. Strategies developed for inhibitor identification consist on either peptide-based inhibitor derived from endogenous protein inhibitors or small-organic molecules. It is also worth noting that among the recent patents on serine protease inhibitors related to inflammation a significant number are related to retinal vascular dysfunction and skin diseases.
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