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Article ; Online: Proteases and Their Potential Role as Biomarkers and Drug Targets in Dry Eye Disease and Ocular Surface Dysfunction.

Ramos-Llorca, Alba / Scarpellini, Camilla / Augustyns, Koen

International journal of molecular sciences

2022 Volume 23, Issue 17

Abstract: Dry eye disease (DED) is a multifactorial disorder that leads to ocular discomfort, visual disturbance, and tear film instability. DED is accompanied by an increase in tear osmolarity and ocular surface inflammation. The diagnosis and treatment of DED ... ...

Abstract	Dry eye disease (DED) is a multifactorial disorder that leads to ocular discomfort, visual disturbance, and tear film instability. DED is accompanied by an increase in tear osmolarity and ocular surface inflammation. The diagnosis and treatment of DED still present significant challenges. Therefore, novel biomarkers and treatments are of great interest. Proteases are present in different tissues on the ocular surface. In a healthy eye, proteases are highly regulated. However, dysregulation occurs in various pathologies, including DED. With this review, we provide an overview of the implications of different families of proteases in the development and severity of DED, along with studies involving protease inhibitors as potential therapeutic tools. Even though further research is needed, this review aims to give suggestions for identifying novel biomarkers and developing new protease inhibitors.
MeSH term(s)	Biomarkers ; Dry Eye Syndromes/diagnosis ; Endopeptidases ; Humans ; Inflammation/drug therapy ; Peptide Hydrolases/therapeutic use ; Protease Inhibitors/therapeutic use ; Tears
Chemical Substances	Biomarkers ; Protease Inhibitors ; Endopeptidases (EC 3.4.-) ; Peptide Hydrolases (EC 3.4.-)
Language	English
Publishing date	2022-08-29
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms23179795
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: The Potential Role of Regulated Cell Death in Dry Eye Diseases and Ocular Surface Dysfunction.

Scarpellini, Camilla / Ramos Llorca, Alba / Lanthier, Caroline / Klejborowska, Greta / Augustyns, Koen

International journal of molecular sciences

2023 Volume 24, Issue 1

Abstract: The research on new treatments for dry eye diseases (DED) has exponentially grown over the past decades. The increased prevalence of dry eye conditions, particularly in the younger population, has received much attention. Therefore, it is of utmost ... ...

Abstract	The research on new treatments for dry eye diseases (DED) has exponentially grown over the past decades. The increased prevalence of dry eye conditions, particularly in the younger population, has received much attention. Therefore, it is of utmost importance to identify novel therapeutical targets. Regulated cell death (RCD) is an essential process to control the biological homeostasis of tissues and organisms. The identification of different mechanisms of RCD stimulated the research on their involvement in different human pathologies. Whereas apoptosis has been widely studied in DED and included in the DED vicious cycle, the role of RCD still needs to be completely elucidated. In this review, we will explore the potential roles of different types of RCD in DED and ocular surface dysfunction. Starting from the evidence of oxidative stress and inflammation in dry eye pathology, we will analyse the potential therapeutic applications of the following principal RCD mechanisms: ferroptosis, necroptosis, and pyroptosis.
MeSH term(s)	Humans ; Dry Eye Syndromes/metabolism ; Inflammation ; Regulated Cell Death ; Apoptosis ; Oxidative Stress
Language	English
Publishing date	2023-01-01
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms24010731
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Article ; Online: Beyond ferrostatin-1: a comprehensive review of ferroptosis inhibitors.

Scarpellini, Camilla / Klejborowska, Greta / Lanthier, Caroline / Hassannia, Behrouz / Vanden Berghe, Tom / Augustyns, Koen

Trends in pharmacological sciences

2023 Volume 44, Issue 12, Page(s) 902–916

Abstract: Ferroptosis is an iron-catalysed form of regulated cell death, which is critically dependent on phospholipid peroxidation of cellular membranes. Ferrostatin 1 was one of the first synthetic radical-trapping antioxidants (RTAs) reported to block ... ...

Abstract	Ferroptosis is an iron-catalysed form of regulated cell death, which is critically dependent on phospholipid peroxidation of cellular membranes. Ferrostatin 1 was one of the first synthetic radical-trapping antioxidants (RTAs) reported to block ferroptosis and it is widely used as reference compound. Ferroptosis has been linked to multiple diseases and the use of its inhibitors could have therapeutic potential. Although, novel biochemical pathways provide insights for different pharmacological targets, the use of lipophilic RTAs to block ferroptosis remains superior. In this Review, we provide a comprehensive overview of the different classes of ferroptosis inhibitors, focusing on endogenous and synthetic RTAs. A thorough analysis of their chemical, pharmacokinetic, and pharmacological properties and potential for in vivo use is provided.
MeSH term(s)	Humans ; Ferroptosis ; Lipid Peroxidation ; Cyclohexylamines/metabolism ; Cyclohexylamines/pharmacology ; Antioxidants/pharmacology
Chemical Substances	ferrostatin-1 ; Cyclohexylamines ; Antioxidants
Language	English
Publishing date	2023-09-26
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	282846-7
ISSN	1873-3735 ; 0165-6147
ISSN (online)	1873-3735
ISSN	0165-6147
DOI	10.1016/j.tips.2023.08.012
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Article ; Online: Characterization of Structurally Diverse

Adhikari, Karuna / Dewulf, Jonatan / Vangestel, Christel / Van der Veken, Pieter / Stroobants, Sigrid / Elvas, Filipe / Augustyns, Koen

ACS omega

2023 Volume 8, Issue 41, Page(s) 38252–38262

Abstract: ... ...

Abstract	Background
Language	English
Publishing date	2023-10-08
Publishing country	United States
Document type	Journal Article
ISSN	2470-1343
ISSN (online)	2470-1343
DOI	10.1021/acsomega.3c04597
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Article ; Online: A high-throughput target-based screening approach for the identification and assessment of

Smiejkowska, Natalia / Oorts, Lauren / Van Calster, Kevin / De Vooght, Linda / Geens, Rob / Mattelaer, Henri-Philippe / Augustyns, Koen / Strelkov, Sergei V / Lamprecht, Dirk / Temmerman, Koen / Sterckx, Yann G-J / Cappoen, Davie / Cos, Paul

Microbiology spectrum

2024 Volume 12, Issue 3, Page(s) e0372323

Abstract: The World Health Organization's goal to combat tuberculosis (TB) is hindered by the emergence of anti-microbial resistance, therefore necessitating the exploration of new drug targets. Multidrug regimens are indispensable in TB therapy as they provide ... ...

Abstract	The World Health Organization's goal to combat tuberculosis (TB) is hindered by the emergence of anti-microbial resistance, therefore necessitating the exploration of new drug targets. Multidrug regimens are indispensable in TB therapy as they provide synergetic bactericidal effects, shorten treatment duration, and reduce the risk of resistance development. The research within our European RespiriTB consortium explores Importance: The growing anti-microbial resistance poses a global public health threat, impeding progress toward eradicating tuberculosis. Despite decades of active research, there is still a dire need for the discovery of drugs with novel modes of action and exploration of combination drug regimens. Within the European RespiriTB consortium, we explore
MeSH term(s)	Humans ; Mycobacterium tuberculosis ; Antitubercular Agents/chemistry ; High-Throughput Screening Assays ; Drug Design ; Tuberculosis/drug therapy ; Oxidoreductases
Chemical Substances	mycothione reductase (EC 1.3.-) ; Antitubercular Agents ; Oxidoreductases (EC 1.-)
Language	English
Publishing date	2024-02-05
Publishing country	United States
Document type	Journal Article
ZDB-ID	2807133-5
ISSN	2165-0497 ; 2165-0497
ISSN (online)	2165-0497
ISSN	2165-0497
DOI	10.1128/spectrum.03723-23
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Article ; Online: Design and Synthesis of 1,3-Diarylpyrazoles and Investigation of Their Cytotoxicity and Antiparasitic Profile.

Bozdag, Murat / Mertens, Freke / Matheeussen, An / Van Pelt, Natascha / Foubert, Kenn / Hermans, Nina / De Meyer, Guido R Y / Augustyns, Koen / Martinet, Wim / Caljon, Guy / Van der Veken, Pieter

International journal of molecular sciences

2024 Volume 25, Issue 9

Abstract: Herein, we report a series of 1,3-diarylpyrazoles that are analogues of ... ...

Abstract	Herein, we report a series of 1,3-diarylpyrazoles that are analogues of compound
MeSH term(s)	Pyrazoles/pharmacology ; Pyrazoles/chemistry ; Pyrazoles/chemical synthesis ; Humans ; Trypanosoma cruzi/drug effects ; Antiparasitic Agents/pharmacology ; Antiparasitic Agents/chemical synthesis ; Antiparasitic Agents/chemistry ; Drug Design ; Leishmania infantum/drug effects ; Structure-Activity Relationship ; Trypanosoma brucei rhodesiense/drug effects ; Antiprotozoal Agents/pharmacology ; Antiprotozoal Agents/chemical synthesis ; Antiprotozoal Agents/chemistry
Chemical Substances	Pyrazoles ; Antiparasitic Agents ; Antiprotozoal Agents
Language	English
Publishing date	2024-04-25
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms25094693
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Article ; Online: Active site-directed probes targeting dipeptidyl peptidases 8 and 9.

Espadinha, Margarida / De Loose, Joni / Corthaut, Sam / Thys, Sofie / Van Rymenant, Yentl / Verhulst, Emile / Benramdane, Siham / Filippi, Nicolò / Augustyns, Koen / Van Wielendaele, Pieter / Pintelon, Isabel / De Meester, Ingrid / Van der Veken, Pieter

European journal of medicinal chemistry

2024 Volume 270, Page(s) 116389

Abstract: Dipeptidyl peptidases (DPP) 8 and 9 are intracellular serine proteases that play key roles in various biological processes and recent findings highlight DPP8 and DPP9 as potential therapeutic targets for hematological and inflammasome-related diseases. ... ...

Abstract	Dipeptidyl peptidases (DPP) 8 and 9 are intracellular serine proteases that play key roles in various biological processes and recent findings highlight DPP8 and DPP9 as potential therapeutic targets for hematological and inflammasome-related diseases. Despite the substantial progress, the precise biological functions of these proteases remain elusive, and the lack of selective chemical tools hampers ongoing research. In this paper, we describe the synthesis and biochemical evaluation of the first active site-directed DPP8/9 probes which are derived from DPP8/9 inhibitors developed in-house. Specifically, we synthesized fluorescent inhibitors containing nitrobenzoxadiazole (NBD), dansyl (DNS) and cyanine-3 (Cy3) reporters to visualize intracellular DPP8/9. We demonstrate that the fluorescent inhibitors have high affinity and selectivity towards DPP8/9 over related S9 family members. The NBD-labeled DPP8/9 inhibitors were nominated as the best in class compounds to visualize DPP8/9 in human cells. Furthermore, a method has been developed for selective labeling and visualization of active DPP8/9 in vitro by fluorescence microscopy. A collection of potent and selective biotinylated DPP8/9-targeting probes was also prepared by replacing the fluorescent reporter with a biotin group. The present work provides the first DPP8/9-targeting fluorescent compounds as useful chemical tools for the study of DPP8 and DPP9's biological functions.
MeSH term(s)	Humans ; Dipeptidyl Peptidase 4/metabolism ; Dipeptidyl-Peptidases and Tripeptidyl-Peptidases ; Catalytic Domain ; Serine Endopeptidases ; Serine Proteases ; Dipeptidases/metabolism
Chemical Substances	Dipeptidyl Peptidase 4 (EC 3.4.14.5) ; Dipeptidyl-Peptidases and Tripeptidyl-Peptidases (EC 3.4.14.-) ; Serine Endopeptidases (EC 3.4.21.-) ; Serine Proteases (EC 3.4.-) ; Dipeptidases (EC 3.4.13.-)
Language	English
Publishing date	2024-04-03
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2024.116389
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Article ; Online: Inhibitors Targeting RIPK1/RIPK3: Old and New Drugs.

Martens, Sofie / Hofmans, Sam / Declercq, Wim / Augustyns, Koen / Vandenabeele, Peter

Trends in pharmacological sciences

2020 Volume 41, Issue 3, Page(s) 209–224

Abstract: The scaffolding function of receptor-interacting protein kinase 1 (RIPK1) regulates prosurvival signaling and inflammatory gene expression, while its kinase activity mediates both apoptosis and necroptosis; the latter involving RIPK3 kinase activity. The ...

Abstract	The scaffolding function of receptor-interacting protein kinase 1 (RIPK1) regulates prosurvival signaling and inflammatory gene expression, while its kinase activity mediates both apoptosis and necroptosis; the latter involving RIPK3 kinase activity. The mutual transition between the scaffold and kinase functions of RIPK1 is regulated by (de)ubiquitylation and (de)phosphorylation. RIPK1-mediated cell death leads to disruption of epithelial barriers and/or release of damage-associated molecular patterns (DAMPs), cytokines, and chemokines, propagating inflammatory and degenerative diseases. Many drug development programs have pursued targeting RIPK1, and to a lesser extent RIPK3 kinase activity. In this review, we classify existing and novel small-molecule drugs based on their pharmacodynamic (PD) type I, II, and III binding mode. Finally, we discuss their applicability and therapeutic potential in inflammatory and degenerative experimental disease models.
MeSH term(s)	Apoptosis ; Cell Death ; Humans ; Necrosis ; Pharmaceutical Preparations ; Phosphorylation ; Receptor-Interacting Protein Serine-Threonine Kinases/metabolism
Chemical Substances	Pharmaceutical Preparations ; RIPK1 protein, human (EC 2.7.11.1) ; RIPK3 protein, human (EC 2.7.11.1) ; Receptor-Interacting Protein Serine-Threonine Kinases (EC 2.7.11.1)
Language	English
Publishing date	2020-02-05
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	282846-7
ISSN	1873-3735 ; 0165-6147
ISSN (online)	1873-3735
ISSN	0165-6147
DOI	10.1016/j.tips.2020.01.002
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Article: A Novel Ferroptosis Inhibitor UAMC-3203, a Potential Treatment for Corneal Epithelial Wound.

Balla, Anusha / Tran, Bao / Valtari, Annika / Steven, Philipp / Scarpellini, Camilla / Augustyns, Koen / Urtti, Arto / Vellonen, Kati-Sisko / Ruponen, Marika

Pharmaceutics

2022 Volume 15, Issue 1

Abstract: Corneal wound, associated with pain, impaired vision, and even blindness, is the most common ocular injury. In this study, we investigated the effect of a novel ferroptosis inhibitor, UAMC-3203 (10 nM-50 µM), in corneal epithelial wound healing in vitro ... ...

Abstract	Corneal wound, associated with pain, impaired vision, and even blindness, is the most common ocular injury. In this study, we investigated the effect of a novel ferroptosis inhibitor, UAMC-3203 (10 nM-50 µM), in corneal epithelial wound healing in vitro in human corneal epithelial (HCE) cells and ex vivo using alkali-induced corneal wounded mice eye model. We evaluated in vivo acute tolerability of the compound by visual inspection, optical coherence tomography (OCT), and stereomicroscope imaging in rats after its application (100 µM drug solution in phosphate buffer pH 7.4) twice a day for 5 days. In addition, we studied the partitioning of UAMC-3203 in corneal epithelium and corneal stroma using excised porcine cornea. Our study demonstrated that UAMC-3203 had a positive corneal epithelial wound healing effect at the optimal concentration of 10 nM (IC
Language	English
Publishing date	2022-12-29
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics15010118
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Article ; Online: Druglike,

Tanc, Muhammet / Filippi, Nicolò / Van Rymenant, Yentl / Grintsevich, Sergei / Pintelon, Isabel / Verschuuren, Marlies / De Loose, Joni / Verhulst, Emile / Moon, Euy Sung / Cianni, Lorenzo / Stroobants, Sigrid / Augustyns, Koen / Roesch, Frank / De Meester, Ingrid / Elvas, Filipe / Van der Veken, Pieter

Journal of medicinal chemistry

2024 Volume 67, Issue 9, Page(s) 7068–7087

Abstract: Fibroblast activation protein (FAP) is a very reliable biomarker for tissue remodeling. FAP has so far mainly been studied in oncology, but there is growing interest in the enzyme in other diseases like fibrosis. Recently, FAP-targeting diagnostics and ... ...

Abstract	Fibroblast activation protein (FAP) is a very reliable biomarker for tissue remodeling. FAP has so far mainly been studied in oncology, but there is growing interest in the enzyme in other diseases like fibrosis. Recently, FAP-targeting diagnostics and therapeutics have emerged, of which the so-called FAPIs are among the most promising representatives. FAPIs typically have a relatively high molecular weight and contain very polar, multicharged chelator moieties. While this is not limiting the application of FAPIs in oncology, more druglike FAPIs could be required to optimally study diseases characterized by denser, less permeable tissue. In response, we designed the first druglike
MeSH term(s)	Animals ; Positron-Emission Tomography/methods ; Endopeptidases/metabolism ; Fluorine Radioisotopes/chemistry ; Gelatinases/metabolism ; Gelatinases/antagonists & inhibitors ; Membrane Proteins/metabolism ; Membrane Proteins/antagonists & inhibitors ; Humans ; Mice ; Tissue Distribution ; Serine Endopeptidases/metabolism ; Radiopharmaceuticals/chemistry ; Radiopharmaceuticals/pharmacokinetics ; Radiopharmaceuticals/chemical synthesis ; Radiopharmaceuticals/pharmacology ; Cell Line, Tumor ; Female
Chemical Substances	fibroblast activation protein alpha (EC 3.4.21.-) ; Endopeptidases (EC 3.4.-) ; Fluorine Radioisotopes ; Gelatinases (EC 3.4.24.-) ; Membrane Proteins ; Serine Endopeptidases (EC 3.4.21.-) ; Fluorine-18 (GZ5I74KB8G) ; Radiopharmaceuticals
Language	English
Publishing date	2024-04-24
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.3c02402
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