ArticleCell death and differentiation2019
Potent and selective caspase-2 inhibitor prevents MDM-2 cleavage in reversine-treated colon cancer cells.
Article in Cell death and differentiation, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 35 citations in OpenAlex.
- The PIDDosome controls cardiomyocyte polyploidization during postnatal heart development.Cell death and differentiation · 2026Article
- The concealed side of caspases: beyond a killer of cells.Cellular and molecular life sciences : CMLS · 2024Review
- Dissecting caspase-2-mediated cell death: from intrinsic PIDDosome activation to chemical modulation.Protein & cell · 2024Article
- Caspase-2 is essential for proliferation and self-renewal of nucleophosmin-mutated acute myeloid leukemia.Science advances · 2024Article
- Chemoproteomics Identifies State-Dependent and Proteoform-Selective Caspase-2 Inhibitors.Journal of the American Chemical Society · 2024Article
- An electrophilic fragment screening for the development of small molecules targeting caspase-2.European journal of medicinal chemistry · 2023Article
- Targeting caspase-2 interactions with tau in Alzheimer's disease and related dementias.Translational research : the journal of laboratory and clinical medicine · 2023Review
- Selective chemical reagents to investigate the role of caspase 6 in apoptosis in acute leukemia T cells.Chemical science · 2023Article
- Role of microRNA-494 in tumor progression.American journal of translational research · 2023Review
- Genuine selective caspase-2 inhibition with new irreversible small peptidomimetics.Cell death & disease · 2022Article
- Characterization of caspase-2 inhibitors based on specific sites of caspase-2-mediated proteolysis.Archiv der Pharmazie · 2022Article
- Non-Canonical Programmed Cell Death in Colon Cancer.Cancers · 2022Review
- Caspase-2 Inhibitor Blocks Tau Truncation and Restores Excitatory Neurotransmission in Neurons Modeling FTDP-17 Tauopathy.ACS chemical neuroscience · 2022Article
- Structure-Based Design and Biological Evaluation of Novel Caspase-2 Inhibitors Based on the Peptide AcVDVAD-CHO and the Caspase-2-Mediated Tau Cleavage Sequence YKPVD314.ACS pharmacology & translational science · 2022Article
- A long way to go: caspase inhibitors in clinical use.Cell death & disease · 2021Review
- Multiple functions of reversine on the biological characteristics of sheep fibroblasts.Scientific reports · 2021Article
- Centriolar distal appendages activate the centrosome-PIDDosome-p53 signalling axis via ANKRD26.The EMBO journal · 2021Article
- SARS-CoV-2 MNature chemical biology · 2021Article
- A Switch in p53 Dynamics Marks Cells That Escape from DSB-Induced Cell Cycle Arrest.Cell reports · 2020Article
- Noninvasive optical detection of granzyme B from natural killer cells with enzyme-activated fluorogenic probes.The Journal of biological chemistry · 2020Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
Most caspases can be positioned unambiguously within the regulated cell death networks of apoptosis and pyroptosis, but the role of caspase-2, a highly conserved protease within the family, remains enigmatic. This is mainly due to lack of selective chemical and biochemical tools for the investigation of this protease. In this study, we used our hybrid combinatorial substrate library (HyCoSuL) approach to broadly profile caspase-2 substrate specificity using peptide scanning libraries. This screen uncovered previously unknown caspase-2 peptidyl substrate preferences, which were further used to develop caspase-2 selective fluorogenic substrates and covalent, irreversible AOMK inhibitors. Finally, we used the champion inhibitor (NH-23-C2) in reversine-treated HCT-116 colon cancer cells to selectively block caspase-2 activity and caspase-2-mediated MDM-2 cleavage. In addition, we showed that NH-23-C2 does not block caspase-3 or caspase-8, which makes it a powerful chemical tool to dissect the true role of caspase-2 in various biological setups.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.