Proteinase 3 phosphonic inhibitors

Renata Grzywa , Adam Lesner , Brice Korkmaz , Marcin Sieńczyk

Abstract

Neutrophils are one of the most important military services of the armed forces of the immune system, a crucial line of defense against bacterial or fungal onslaughts. One of their mechanisms of action relies on the production of serine proteases. One of these enzymes is proteinase 3 (PR3), which is engaged in the processing of pro-inflammatory cytokines, receptors, heat shock proteins and in the generation of antibacterial peptides. Despite its protective function, uncontrolled activity of PR3 has been associated with the progression of inflammation and tissue injury. Although PR3 was characterized at the beginning of 90's of the last century for the first time, the research on the development of its inhibitors is barely noticeable. Here we present the recent findings on the design, synthesis and the activity of phosphonic PR3 inhibitors together with the historical perspective.
Publication typeIn press (online first, early view)
Author Renata Grzywa
Renata Grzywa,,
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, Adam Lesner (FCh / DET / LBAN)
Adam Lesner,,
- Laboratory of Biochemical Analytics and Nanodiagnostics
, Brice Korkmaz
Brice Korkmaz,,
-
, Marcin Sieńczyk
Marcin Sieńczyk,,
-
Journal seriesBiochimie, ISSN 0300-9084, (A 25 pkt)
Issue year2019
Noonline first
Pages1-8
Publication size in sheets0.5
Keywords in EnglishActivity-based probes, aminophosphonates, inhibitors, neutrophil serine proteases, proteinase 3
ASJC Classification2700 General Medicine; 1303 Biochemistry
DOIDOI:10.1016/j.biochi.2019.03.005
URL https://doi.org/10.1016/j.biochi.2019.03.005
Languageen angielski
Score (nominal)25
ScoreMinisterial score = 25.0, 24-07-2019, ArticleFromJournal
Publication indicators Scopus SNIP (Source Normalised Impact per Paper): 2016 = 0.975; WoS Impact Factor: 2017 = 3.188 (2) - 2017=3.058 (5)
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