Activity-based probes (ABPs) are valuable chemical tools for profiling enzymes. They have been particularly useful in the study of proteases. ABPs rely on electrophilic scaffolds that covalently modify the target enzymes. Ideally, they can be made in a fast and uncomplicated manner. Here, we explore alkyne-substituted benzoxazin-4-ones as ABPs for serine proteases, because they inhibitserine proteases covalently and their synthesis is very straightforward. We show that alkyne-tagged benzoxazin-4-ones can be used in two-step bioorthogonal tandem labeling procedures or pre-functionalized with a biotin or fluorophore. We demonstrate that these reagents can be used to label and identify various serine proteases. Therefore, we expect that tagged benzoxazin-4-ones will offer easily synthesizable tools for profiling of serine proteases.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1002/cbic.202000848 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Prospective validation study of a combined urine and plasma test for predicting high-grade prostate cancer in biopsy naïve men.
Scand J Urol
January 2025
Department of Urology, Odense University Hospital, Odense, Denmark; Academy of Geriatric Cancer Research (AgeCare), Odense University Hospital, Odense, Denmark; Department of Clinical Research, University of Southern Denmark, Odense, Denmark.
Objective: Early and accurate diagnosis of prostate cancer (PC) is crucial for effective treatment. Diagnosing clinically insignificant cancers can lead to overdiagnosis and overtreatment, highlighting the importance of accurately selecting patients for further evaluation based on improved risk prediction tools. Novel biomarkers offer promise for enhancing this diagnostic process.
View Article and Find Full Text PDFCCN1 is a matricellular protein highly expressed in esophageal squamous cell carcinoma (ESCC) but hardly detectable in esophageal adenocarcinoma (EAC). Expression of CCN1 in EAC cells leads to TRAIL-mediated apoptosis. Unlike TRAIL, which primarily triggers cell death, APRIL and BAFF promote cell growth via NFκB signaling.
View Article and Find Full Text PDFMALDI-TOF MS analysis for detection of bovine coronavirus with tryptic peptides from viral proteins.
J Microorg Control
January 2025
Division of Microbiology, National Institute of Health Sciences.
Bovine coronavirus (BCoV）, a significant cattle pathogen causing enteric and respiratory diseases, is primarily detected using reverse transcription-polymerase chain reaction. Our objective was to develop a novel detection method for BCoV by matrix-assisted laser desorption/ionization‒time-of-flight mass spectrometry (MALDI-TOF MS）. Peptide mass fingerprint analysis revealed that nucleocapsid (N）, membrane (M）, and hemagglutinin-esterase (HE) were three main BCoV proteins.
View Article and Find Full Text PDFTenecteplase for the Treatment of Pediatric Arterial Ischemic Stroke: A Safety Surveillance Report.
Neurology
February 2025
Department of Neurology, Washington University School of Medicine, St. Louis, MO.
Objectives: Intravenous tenecteplase (TNK) is increasingly used to treat adult patients with acute arterial ischemic stroke, but the risk profile of TNK in childhood stroke is unknown. This study aims to prospectively gather safety data regarding TNK administration in children.
Methods: Since December 2023, a monthly email survey was sent to participants recruited from the International Pediatric Stroke Study and Pediatric Neurocritical Care Research Group querying recent experience with TNK in childhood stroke.
Safe Implementation of Treatments in Stroke: a study on intravenous thrombolysis in patients over 80 years of age with acute ischaemic stroke.
BMJ Open
January 2025
Department of Neurology, Karolinska University Hospital, Stockholm, Sweden.
Objectives: To investigate the safety and efficacy outcomes of intravenous thrombolysis (IVT) in patients aged >80 years with acute ischaemic stroke (AIS) after IVT was approved in this patient population in several European and non-European countries during 2018-2019.
Design: This is an observational registry study using prospectively collected data from the Safe Implementation of Treatment in Stroke (SITS) registry. Comparisons will be performed between patients treated post-approval (July 2018 to December 2021) period with those treated pre-approval (June 2015 to June 2018) period using propensity score matching (PSM).
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!