A5031359497- Protease and Inhibitor Mechanisms
- Peptidase Inhibition and Analysis
- Trypanosoma species research and implications
- Coagulation, Bradykinin, Polyphosphates, and Angioedema
- Cell Adhesion Molecules Research
- Antimicrobial Peptides and Activities
- Research on Leishmaniasis Studies
- Signaling Pathways in Disease
- Coccidia and coccidiosis research
- Lysosomal Storage Disorders Research
- Interstitial Lung Diseases and Idiopathic Pulmonary Fibrosis
- Pulmonary Hypertension Research and Treatments
- Bone Metabolism and Diseases
- Cellular transport and secretion
- Trace Elements in Health
- Chronic Obstructive Pulmonary Disease (COPD) Research
- S100 Proteins and Annexins
- Animal Nutrition and Physiology
- Bone and Dental Protein Studies
- Calpain Protease Function and Regulation
- Malaria Research and Control
- Neonatal Respiratory Health Research
- Biochemical and Structural Characterization
- Enzyme Production and Characterization
- Parasitic Infections and Diagnostics
Inserm
2015-2024
Centre d'Étude des Pathologies Respiratoires
2015-2024
Université de Tours
2015-2024
Clinical Investigation Center Plurithematic Tours
2005-2024
Thion Medical (France)
2022
Center for Economic and Policy Research
2018-2020
Centre National de la Recherche Scientifique
1990-2019
Institut National de Recherche en Santé Publique
2005-2015
Serine Proteases and Pathophysiology of the neurovascular Unit
2008-2012
Children's Hospital Agia Sophia
2009
Voltage-gated sodium channels (Na(V)) are functionally expressed in highly metastatic cancer cells derived from nonexcitable epithelial tissues (breast, prostate, lung, and cervix). MDA-MB-231 breast express functional channel complexes, consisting of Na(V)1.5 associated auxiliary beta-subunits, that responsible for a sustained inward current at the membrane potential. Although these do not regulate cellular multiplication or migration, their inhibition by specific blocker tetrodotoxin...
Studies using inhibitors that reportedly discriminate between cathepsin B and related lysosomal cysteine proteinases have implicated the enzyme in a wide range of physiological pathological processes. The most popular substance to selectively inhibit vivo is CA-074Me, methyl ester E-64 derivative CA-074. However, we now found CA-074Me inactivates both L within murine fibroblasts. In contrast, exposure these cells parental compound CA 074 leads selective inhibition endogenous B, while...
In mammalian ovaries, terminal follicular growth is accompanied by a decrease in levels of intrafollicular insulin-like factor binding protein-2 (IGFBP-2) and IGFBP-4. The IGFBP-4 essentially due to an increase proteolytic degradation pregnancy-associated plasma protein-A (PAPP-A) growing healthy follicles. contrast, the IGFBP-2 partly mRNA expression cells also degradation, as previously shown ewes sows. present work we show that bovine porcine preovulatory fluid contains activity degrades...
"Click" protein: CuI-catalyzed cycloaddition of azides and terminal alkynes has been applied to the successive ligations three unprotected peptide fragments. Peptidomimetic triazole ligation (PTL, see scheme) as a new method for chemical production bioactive proteins is synthesis triazole-containing analogue 97 amino acid protein cystatin A. Detailed facts importance specialist readers are published "Supporting Information". Such documents peer-reviewed, but not copy-edited or typeset. They...
Hepatocellular carcinoma is the most frequent primary liver cancer. Macroautophagy/autophagy inhibitors have been extensively studied in cancer but, to date, none has reached efficacy clinical trials. In this study, we demonstrated that GNS561, a new autophagy inhibitor, whose anticancer activity was previously linked lysosomal cell death, displayed high tropism and potent antitumor against panel of human lines two hepatocellular vivo models. We showed due its lysosomotropic properties,...
Up-regulation of nitric oxide (NO) production by activated murine macrophages was observed during infection Trypanosoma cruzi, the etiological agent Chagas' disease. Cell T. cruzi depends at least in part on cruzipain, a membrane-associated papain-related proteinase which is sensitive to inhibition synthetic inhibitors cysteine proteinases. Using natural inhibitor chicken cystatin, representative member cystatin family 2, investigate effect cruzipain macrophage and NO release, we found that...
Human cysteine cathepsin S (catS) participates in distinct physiological and pathophysiological cellular processes is considered as a valuable therapeutic target autoimmune diseases, cancer, atherosclerosis, asthma. We evaluated the capacity of negatively charged glycosaminoglycans (heparin, heparan sulfate, chondroitin 4/6-sulfates, dermatan hyaluronic acid) to modulate activity catS. Chondroitin 4-sulfate (C4-S) impaired collagenolytic (type IV collagen) inhibited peptidase (Z-Phe-Arg-AMC)...
The aspartic protease cathepsin D, a poor prognostic indicator of breast cancer, is abundantly secreted as procathepsin D by human cancer cells and self-activates at low pH in vitro, giving rise to catalytically active D. Due lower extracellular tumor microenvironments compared normal tissues, may cleave pathophysiological substrates contributing progression. Here, we show yeast 2-hybrid degradomics analyses that cystatin C, the most potent natural inhibitor cysteine cathepsins, both binds...
Lung matrix homeostasis partly depends on the fine regulation of proteolytic activities. We examined expression human cysteine cathepsins (Cats) and their relative contribution to TGF-β1-induced fibroblast differentiation into myofibroblasts. Assays were conducted using both primary fibroblasts obtained from patients with idiopathic pulmonary fibrosis lung CCD-19Lu fibroblasts. Pharmacological inhibition genetic silencing Cat B diminished α-smooth muscle actin expression, delayed...
Abstract Pulmonary fibrosis is a progressive disease characterized by widespread accumulation of myofibroblasts and extracellular matrix components. Growing evidences support that cysteine cathepsins, embracing cathepsin B (CatB) affects TGF-β1-driven Smad pathway, along with their inhibitor cystatin C, participate in myofibrogenesis. Here we established curcumin, potent antifibrotic drug used traditional Asian medicine, impaired the expression both α-smooth muscle actin mature TGF-β1...
Lung cysteine cathepsins B, K, L, and S contribute to physiological pathological processes including degradation of antimicrobial peptides/proteins (AMPs) such as surfactant protein SP-A, lactoferrin, secretory leukocyte peptidase inhibitor, beta-defensins-2 -3. Substantial amounts uncleaved LL-37, a 37-mer cationic AMP, were observed in the sputum patients with cystic fibrosis (CF). Nevertheless LL-37 was degraded after prolonged incubation CF sputum, hydrolysis blocked by E-64, selective...
Cigarette smoking has marked effects on lung tissue, including induction of oxidative stress, inflammatory cell recruitment, and a protease/antiprotease imbalance. These contribute to tissue remodeling destruction resulting in loss function chronic obstructive pulmonary disease (COPD) patients. Cathepsin S (CatS) is cysteine protease that involved the remodeling/degradation connective basement membrane. Aberrant expression or activity CatS been implicated variety diseases, arthritis, cancer,...
Cystatins are natural tight‐binding, reversible inhibitors of cysteine proteases. We have shown that cystatins also stimulate nitric oxide (NO) production by interferon‐γ‐activated mouse peritoneal macrophages [Verdot, L., Lalmanach, G., Vercruysse, V., Hartman, S., Lucius, R., Hoebeke, J., Gauthier F. & Vray, B. (1996) J. Biol. Chem . 271 , 28077–28081]. The present study was undertaken to further document this new function. Macrophages activated with interferon‐γ and then stimulated...