A5019623740- Coagulation, Bradykinin, Polyphosphates, and Angioedema
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Catalytic Alkyne Reactions
- Chemical Synthesis and Analysis
- Peptidase Inhibition and Analysis
- Blood Coagulation and Thrombosis Mechanisms
- Gold and Silver Nanoparticles Synthesis and Applications
- Advanced biosensing and bioanalysis techniques
- Metalloenzymes and iron-sulfur proteins
- Cell death mechanisms and regulation
- Endoplasmic Reticulum Stress and Disease
- Machine Learning in Bioinformatics
- Catalytic C–H Functionalization Methods
- Radical Photochemical Reactions
- Protease and Inhibitor Mechanisms
- Ocular Diseases and Behçet’s Syndrome
- Beetle Biology and Toxicology Studies
- Otitis Media and Relapsing Polychondritis
- Neurobiology and Insect Physiology Research
- Phytochemical compounds biological activities
- Click Chemistry and Applications
- Enzyme function and inhibition
- Protein Interaction Studies and Fluorescence Analysis
- Alzheimer's disease research and treatments
Sorbonne Université
2014-2025
Centre National de la Recherche Scientifique
2014-2025
Inserm
2016-2025
Microbiologie de l’alimentation au service de la santé
2020-2025
AgroParisTech
2020-2025
Institut National de Recherche pour l'Agriculture, l'Alimentation et l'Environnement
2020-2025
Université Paris-Saclay
2020-2025
Adaptation Biologique et Vieillissement
2014-2024
Université Paris Cité
2015
Institut de Biologie Paris-Seine
2014
The inhibition of kallikreins 5 and 7, possibly kallikrein 14 matriptase, (that initiates the proteolytic cascade) constitutes an innovative way to treat some skin diseases such as Netherton syndrome. We present here inhibitory properties coumarin-3-carboxylate derivatives against these enzymes. Our small collection versatile organic compounds was enriched by newly synthesized in order obtain molecules selective one, two, three enzymes or acting on four ones. evidenced a series with IC50...
ABSTRACT The gastrointestinal (GI) tract is a site of replication severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and GI symptoms are often reported by patients. SARS-CoV-2 cell entry depends upon heparan sulfate (HS) proteoglycans, which commensal bacteria that bathe the human mucosa known to modify. To explore gut HS-modifying bacterial abundances how their presence may impact infection, we developed task-based analysis proteoglycan degradation on large-scale shotgun...
N-Propargyl tryptamine and tryptophan derivatives that are readily available from both synthetic biocatalytic approaches undergo gold-catalyzed dearomative cyclizations in aqueous media to the corresponding spirocyclic derivatives. In addition efficiency of method, operating affords a selective entry C2-unsubstituted spiroindolenines have long remained unattainable by Au(I) catalysis. Moderate excellent yields desired products bearing various substituents were obtained.
Kallikrein-related peptidases (KLKs) are implicated in many cancer-related processes. KLK6, one of the 15 KLK family members, is a promising biomarker for diagnosis cancers and has been associated with poor prognosis colorectal cancer (CRC) patients. Herein, we evaluated expression cellular functions KLK6 colon cancer-derived cell lines clinical samples from CRC We showed that, although KLKs transcripts upregulated lines, KLK10, KLK11 most highly secreted proteins. induced calcium flux HT29...
Members of the tissue kallikrein-related peptidase (KLK) family not only regulate several important physiological functions, but aberrant expression has also been associated with various malignancies. Clinically, KLKs have suggested as promising biomarkers for diagnosis and prognosis in many types cancer. As yet, their role skin cancers are, however, poorly addressed. Malignant melanoma is an aggressive disease poor prognosis. Hence, diagnostic to monitor progression are needed. Herein, we...
Abstract Caspase-2 (Casp2) is a promising therapeutic target in several human diseases, including nonalcoholic steatohepatitis (NASH) and Alzheimer’s disease (AD). However, the design of an active-site-directed inhibitor selective to individual caspase family members challenging because caspases have extremely similar active sites. Here we present new peptidomimetics derived from VDVAD pentapeptide structure, harboring non-natural modifications at P2 position irreversible warhead. Enzyme...
B12 -dependent radical SAM enzymes are an emerging enzyme family with approximately 200,000 proteins. These have been shown to catalyze chemically challenging reactions such as methyl transfer sp2- and sp3-hybridized carbon atoms. However, date we little information regarding their complex mechanisms biosynthetic potential. Here show, using X-ray absorption spectroscopy, mutagenesis synthetic probes that the vitamin TsrM catalyzes not only C- but also N-methyl further expanding its...
Proteases are found deregulated in many diseases including cancer and neurodegenerative diseases. They thus represent good therapeutical targets for the development of inhibitors mainly small organic molecules. Peptide substrates containing fluorogenic groups constitute central tools monitoring protease activities inhibitor screening platforms. Amino‐methyl coumarin (AMC) is a well‐known group that functionalized huge number peptide used kinetics vitro but also vivo . However, either...
PylB is a radical
Abstract The activity of kallikrein-related peptidase 6 (KLK6) is deregulated in various diseases such as cancer and neurodegenerative diseases. KLK6 thus considered an attractive therapeutical target. In this short report, we depict some novel findings on the regulation activity. Namely, identified mechanism-based inhibitors (suicide substrates) from in-house library 6-substituted coumarin-3-carboxylate derivatives. addition, a molecular dynamics study evidenced allosteric behavior similar...
We took advantage of the powerful adenine SERS (Surface Enhanced Raman Spectroscopy) probe to design peptide–adenine conjugates as candidates for use serine protease substrates. Whereas direct introduction peptide sequence on exocyclic N6 amine gave an imidazopurinone derivative, aminoethyl linker between group and chain led expected candidate probes. These potential substrates were then evaluated monitoring hydrolytic activity trypsin, used a model protease, by HPLC SERS. demonstrated that...
Multiple sclerosis (MS) is an autoimmune demyelinating disease of the central nervous system (CNS) that causes severe motor, sensory, and cognitive impairments. Kallikrein-related peptidase (KLK)6 most abundant serine protease secreted in CNS, mainly by oligodendrocytes, myelin-producing cells KLK6 assumed to be a robust biomarker MS, since it highly increased cerebrospinal fluid (CSF) MS patients. Here, we report design biological evaluation KLK6's low-molecular-weight inhibitors,...
N-Propargyl tryptamine and tryptophan derivatives that are readily available from both synthetic biocatalytic approaches, undergo gold-catalyzed dearomative cyclizations in aqueous media to the corresponding spirocyclic derivatives. In addition efficiency of method, operating affords a selective entry C2-unsubstituted spiroindolenines have long remained unattainable by Au(I)-catalysis. Moderate excellent yields desired products bearing various substituents were obtained.
N-Propargyl tryptamine and tryptophan derivatives that are readily available from both synthetic biocatalytic approaches, undergo gold-catalyzed dearomative cyclizations in aqueous media to the corresponding spirocyclic derivatives. In addition efficiency of method, operating affords a selective entry C2-unsubstituted spiroindolenines have long remained unattainable by Au(I)-catalysis. Moderate excellent yields desired products bearing various substituents were obtained. <br>