Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0033774 (pruritus)
 14,546 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Little is known about the role of the kallikrein-kinin system in chronic spontaneous urticaria (CSU). Kallikrein 5 (KLK5), a trypsin-like enzyme, is the most abundant in the skin and plays a role in itching and inflammatory reaction. In this study, we determined plasma KLK5 concentration, and its associations with acute phase response in CSU patients. Concentrations of KLK5 in plasma and CRP in serum were measured in patients with CSU of varying severity and in the healthy subjects. Plasma KLK5 concentrations were significantly lower in CSU (all) and moderate-severe CSU patients, as compared with the controls. There were no significant differences in KLK5 concentration in mild CSU patients as compared with the healthy subjects and moderate-severe CSU patients. No correlation was observed between KLK5 and CRP concentrations in the patients. It may be considered that circulating kallikrein 5 is down-regulated in CSU patients, however its potential role and the possible underlying mechanism are unknown.
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PMID:Decreased plasma kallikrein 5 concentrations in patients with chronic spontaneous urticaria. 2868 45

The connection between Netherton syndrome and overactivation of epidermal/dermal proteases, particularly Kallikrein 5 (KLK5) has been well established and it is expected that a KLK5 inhibitor would improve the dermal barrier and also reduce the pain and itch that afflict Netherton syndrome patients. One of the challenges of covalent protease inhibitors has been achieving selectivity over closely related targets. In this paper we describe the use of structural insight to design and develop a selective and highly potent reversibly covalent KLK5 inhibitor from an initial weakly binding fragment.
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PMID:Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors. 3185 61