ArticleJournal of medicinal chemistry2008
X-ray snapshot of the mechanism of inactivation of human neutrophil elastase by 1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives.
Article in Journal of medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
11 citing papers in PubMed, 30 citations in OpenAlex.
- The role of neutrophil elastase in aortic valve calcification.Journal of translational medicine · 2022Article
- Sequence preference and scaffolding requirement for the inhibition of human neutrophil elastase by ecotin peptide.Protein science : a publication of the Protein Society · 2022Article
- Neutrophil elastase inhibitory effects of pentacyclic triterpenoids from Eriobotrya japonica (loquat leaves).Journal of ethnopharmacology · 2019Article
- Crystal structure of highly glycosylated human leukocyte elastase in complex with an S2' site binding inhibitor.Acta crystallographica. Section F, Structural biology communications · 2018Article
- Paucimannose-RichMolecular & cellular proteomics : MCP · 2017Article
- Article
- Dual function inhibitors of relevance to chronic obstructive pulmonary disease.Bioorganic & medicinal chemistry letters · 2011Article
- Design, synthesis, and in vitro evaluation of potential West Nile virus protease inhibitors based on the 1-oxo-1,2,3,4-tetrahydroisoquinoline and 1-oxo-1,2-dihydroisoquinoline scaffolds.Journal of combinatorial chemistry · 2010Article
- Effects of structure on inhibitory activity in a series of mechanism-based inhibitors of human neutrophil elastase.Bioorganic & medicinal chemistry · 2010Article
- Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold.European journal of medicinal chemistry · 2010Article
- Mechanism-based inhibitors of serine proteases with high selectivity through optimization of S' subsite binding.Bioorganic & medicinal chemistry · 2009Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
The mechanism of action of a general class of mechanism-based inhibitors of serine proteases, including human neutrophil elastase (HNE), has been elucidated by determining the X-ray crystal structure of an enzyme-inhibitor complex. The captured intermediate indicates that processing of inhibitor by the enzyme generates an N-sulfonyl imine functionality that is tethered to Ser195, in accordance with the postulated mechanism of action of this class of inhibitors. The identity of the HNE-N-sulfonyl imine species was further corroborated using electrospray ionization mass spectrometry.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.