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View article: Biarylacetamides: a novel class of late-stage autophagy inhibitors
Biarylacetamides: a novel class of late-stage autophagy inhibitors Open
Targeting autophagy is believed to hold great promise for the treatment of various diseases, including cancer. However, since the therapeutic efficacy of currently available autophagy-modulating drugs is limited by off-target effects and t…
View article: Dipeptidyl Peptidase 9 in Human Leukocytes: Novel Inhibitors Induce Caspase‐1‐ and Gasdermin‐Dependent Cell Death
Dipeptidyl Peptidase 9 in Human Leukocytes: Novel Inhibitors Induce Caspase‐1‐ and Gasdermin‐Dependent Cell Death Open
Dipeptidyl peptidase 9 (DPP9) is an intracellular serine protease with key roles in the immune response. In human leukocytes, DPP9 interacts with caspase recruitment domain‐containing protein 8 (CARD8) to form an inhibitory complex that pr…
View article: Human Transmembrane Serine Protease 2 (TMPRSS2) on Human Seminal Fluid Extracellular Vesicles Is Proteolytically Active
Human Transmembrane Serine Protease 2 (TMPRSS2) on Human Seminal Fluid Extracellular Vesicles Is Proteolytically Active Open
Human transmembrane serine protease 2 (TMPRSS2) has garnered substantial interest due to its clinical significance in various pathologies, notably its pivotal role in viral entry into host cells. The development of effective strategies to …
View article: Oxazole-Based Ferroptosis Inhibitors with Promising Properties to Treat Central Nervous System Diseases
Oxazole-Based Ferroptosis Inhibitors with Promising Properties to Treat Central Nervous System Diseases Open
Ferroptosis plays an important role in the occurrence and development of many diseases, including neurodegenerative diseases. Thus, ferroptosis inhibitors able to cross the blood-brain barrier may have therapeutic potential. The best ferro…
View article: Chemically diverse activity-based probes with unexpected inhibitory mechanisms targeting trypsin-like serine proteases
Chemically diverse activity-based probes with unexpected inhibitory mechanisms targeting trypsin-like serine proteases Open
Activity-based probes (ABP) are molecules that bind covalently to the active form of an enzyme family, making them an attractive tool for target and biomarker identification and drug discovery. The present study describes the synthesis and…
View article: ATG4B Inhibitor UAMC-2526 Potentiates the Chemotherapeutic Effect of Gemcitabine in a Panc02 Mouse Model of Pancreatic Ductal Adenocarcinoma
ATG4B Inhibitor UAMC-2526 Potentiates the Chemotherapeutic Effect of Gemcitabine in a Panc02 Mouse Model of Pancreatic Ductal Adenocarcinoma Open
Resistance against anti-cancer therapy is one of the major challenges during treatment of multiple cancers. Gemcitabine is a standard first-line chemotherapeutic drug, yet autophagy is highly activated in the hypoxic microenvironment of so…
View article: Proteolytic Cleavage of Bioactive Peptides and Protease-Activated Receptors in Acute and Post-Colitis
Proteolytic Cleavage of Bioactive Peptides and Protease-Activated Receptors in Acute and Post-Colitis Open
The protease activity in inflammatory bowel disease (IBD) and irritable bowel syndrome has been studied extensively using synthetic fluorogenic substrates targeting specific sets of proteases. We explored activities in colonic tissue from …
View article: The Effect of a Novel Serine Protease Inhibitor on Inflammation and Intestinal Permeability in a Murine Colitis Transfer Model
The Effect of a Novel Serine Protease Inhibitor on Inflammation and Intestinal Permeability in a Murine Colitis Transfer Model Open
Background: A protease/antiprotease disbalance is observed in inflammatory bowel diseases (IBD). We therefore studied the effect of the novel serine protease inhibitor UAMC-00050 on intestinal inflammation and permeability in a chronic col…
View article: Local Colonic Administration of a Serine Protease Inhibitor Improves Post-Inflammatory Visceral Hypersensitivity in Rats
Local Colonic Administration of a Serine Protease Inhibitor Improves Post-Inflammatory Visceral Hypersensitivity in Rats Open
Dysregulation of the protease–antiprotease balance in the gastrointestinal tract has been suggested as a mechanism underlying visceral hypersensitivity in conditions such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IB…
View article: Macromolecular biosynthetic parameters and metabolic profile in different life stages of Leishmania braziliensis: Amastigotes as a functionally less active stage
Macromolecular biosynthetic parameters and metabolic profile in different life stages of Leishmania braziliensis: Amastigotes as a functionally less active stage Open
It was recently hypothesized that Leishmania amastigotes could constitute a semi-quiescent stage characterized by low replication and reduced metabolic activity. This concept developed with Leishmania (Leishmania) mexicana and Leishmania (…
View article: Evolutionary genomics of epidemic visceral leishmaniasis in the Indian subcontinent
Evolutionary genomics of epidemic visceral leishmaniasis in the Indian subcontinent Open
Leishmania donovani causes visceral leishmaniasis (VL), the second most deadly vector-borne parasitic disease. A recent epidemic in the Indian subcontinent (ISC) caused up to 80% of global VL and over 30,000 deaths per year. Resistance aga…
View article: Highlights from the 11th ISCB Student Council Symposium 2015
Highlights from the 11th ISCB Student Council Symposium 2015 Open
Table of contents A1 Highlights from the eleventh ISCB Student Council Symposium 2015 Katie Wilkins, Mehedi Hassan, Margherita Francescatto, Jakob Jespersen, R. Gonzalo Parra, Bart Cuypers, Dan DeBlasio, Alexander Junge, Anupama Jigisha, F…
View article: Author response: Evolutionary genomics of epidemic visceral leishmaniasis in the Indian subcontinent
Author response: Evolutionary genomics of epidemic visceral leishmaniasis in the Indian subcontinent Open
Full text Figures and data Side by side Abstract eLife digest Introduction Results Discussion Materials and methods Appendix 1 - SNP detection procedure using the COCALL algorithm Appendix 2 - Somy, CNV, indel and episome detection Data av…
View article: Experimental Resistance to Drug Combinations in Leishmania donovani: Metabolic and Phenotypic Adaptations
Experimental Resistance to Drug Combinations in Leishmania donovani: Metabolic and Phenotypic Adaptations Open
Together with vector control, chemotherapy is an essential tool for the control of visceral leishmaniasis (VL), but its efficacy is jeopardized by growing resistance and treatment failure against first-line drugs. To delay the emergence of…
View article: Understanding leishmania development and drug resistance using an integrative ‘omics compendium
Understanding leishmania development and drug resistance using an integrative ‘omics compendium Open
1Department of Mathematics and Computer Sciences, University of Antwerp; 2Biomedical informatics research center Antwerpen (biomina), University of Antwerp / Antwerp University Hospital; 3Molecular Parasitology Unit, Department of Biomedic…