{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["9(4)"],"submitter":["Schulz-Fincke AC"],"pubmed_abstract":["Human leukocyte elastase plays a crucial role in a variety of inflammatory disorders and represents an important subject of biomedical studies. The chemotype of peptidic phosphonates was employed for the design of a new activity-based probe for human leukocyte elastase. Its structure combines the phosphonate warhead with an adequate peptide portion and a BODIPY fluorophore with a clickable ethinylphenyl moiety at meso position. The probe 6 was assembled by copper-catalyzed alkyne-azide 1,3-dipolar cycloaddition. It was characterized as an active site-directed elastase inhibitor exhibiting a second-order rate constant of inactivation of 88400 M-1s-1. The suitability of 6 as a fluorescent probe for human leukocyte elastase was demonstrated by in-gel fluorescence analysis. Labeling experiment"],"journal":["ACS medicinal chemistry letters"],"pagination":["345-350"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC5900331"],"repository":["biostudies-literature"],"pubmed_title":["A BODIPY-Tagged Phosphono Peptide as Activity-Based Probe for Human Leukocyte Elastase."],"pmcid":["PMC5900331"],"pubmed_authors":["Gutschow M","Braune A","Schulz-Fincke AC","Blaut M"],"additional_accession":[]},"is_claimable":false,"name":"A BODIPY-Tagged Phosphono Peptide as Activity-Based Probe for Human Leukocyte Elastase.","description":"Human leukocyte elastase plays a crucial role in a variety of inflammatory disorders and represents an important subject of biomedical studies. The chemotype of peptidic phosphonates was employed for the design of a new activity-based probe for human leukocyte elastase. Its structure combines the phosphonate warhead with an adequate peptide portion and a BODIPY fluorophore with a clickable ethinylphenyl moiety at meso position. The probe 6 was assembled by copper-catalyzed alkyne-azide 1,3-dipolar cycloaddition. It was characterized as an active site-directed elastase inhibitor exhibiting a second-order rate constant of inactivation of 88400 M-1s-1. The suitability of 6 as a fluorescent probe for human leukocyte elastase was demonstrated by in-gel fluorescence analysis. Labeling experiment","dates":{"release":"2018-01-01T00:00:00Z","publication":"2018 Apr","modification":"2025-05-29T22:16:47.821Z","creation":"2025-05-29T22:16:47.821Z"},"accession":"S-EPMC5900331","cross_references":{"pubmed":["29670698"],"doi":["10.1021/acsmedchemlett.7b00533"]}}