ArticleThe Biochemical journal2009
A constitutively active and uninhibitable caspase-3 zymogen efficiently induces apoptosis.
Article in The Biochemical journal, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 73 papers.
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Who cites it
73 citing papers in PubMed, 162 citations in OpenAlex.
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- Pharmacologic Modulation of the PAR-2-ERK Axis by Statins Converts Inflammatory Survival Signalling into Apoptosis in Colorectal Cancer Cells.International journal of molecular sciences · 2026Article
- Artemisinin protected human bronchial epithelial cells from amiodarone-induced oxidative damage via 5'-AMP-activated protein kinase (AMPK) activation.Redox report : communications in free radical research · 2025Article
- Inosine Treatment Attenuates White Matter Injury in Neonatal Rats Exposed to Maternal Inflammation.Neurochemical research · 2025Article
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- Phenotypical, genotypical and pathological characterization of the moonwalker mouse, a model of ataxia.Neurobiology of disease · 2024Article
- An Overview of Ischemia-Reperfusion Injury: Review on Oxidative Stress and Inflammatory Response.The Eurasian journal of medicine · 2022Article
- Upregulated miR-322-5p regulates cell cycle and promotes cell proliferation and apoptosis by directly targeting Wee1 in mice liver injury.Cell cycle (Georgetown, Tex.) · 2022Article
- Dimethyl Sulfoxide: A Bio-Friendly or Bio-Hazard Chemical? The Effect of DMSO in Human Fibroblast-like Synoviocytes.Molecules (Basel, Switzerland) · 2022Article
- Developmental deltamethrin: Sex-specific hippocampal effects in Sprague Dawley rats.Current research in toxicology · 2022Article
- The role of microRNAs in cell death pathways.Yeungnam University journal of medicine · 2021Article
- DNA double-strand breaks in the Toxoplasma gondii-infected cells by the action of reactive oxygen species.Parasites & vectors · 2020Article
- Prdx2 Upregulation Promotes the Growth and Survival of Gastric Cancer Cells.Pathology oncology research : POR · 2020Article
- Anticancer Effect of Radix Astragali on Cholangiocarcinoma In Vitro and Its Mechanism via Network Pharmacology.Medical science monitor : international medical journal of experimental and clinical research · 2020Article
- Inhibition of PHLPP1 ameliorates cardiac dysfunction via activation of the PI3K/Akt/mTOR signalling pathway in diabetic cardiomyopathy.Journal of cellular and molecular medicine · 2020Article
- Radiolabelled Peptides for Positron Emission Tomography and Endoradiotherapy in Oncology.Pharmaceuticals (Basel, Switzerland) · 2020Review
13 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
The caspase-3 zymogen has essentially zero activity until it is cleaved by initiator caspases during apoptosis. However, a mutation of V266E in the dimer interface activates the protease in the absence of chain cleavage. We show that low concentrations of the pseudo-activated procaspase-3 kill mammalian cells rapidly and, importantly, this protein is not cleaved nor is it inhibited efficiently by the endogenous regulator XIAP (X-linked inhibitor of apoptosis). The 1.63 A (1 A = 0.1 nm) structure of the variant demonstrates that the mutation is accommodated at the dimer interface to generate an enzyme with substantially the same activity and specificity as wild-type caspase-3. Structural modelling predicts that the interface mutation prevents the intersubunit linker from binding in the dimer interface, allowing the active sites to form in the procaspase in the absence of cleavage. The direct activation of procaspase-3 through a conformational switch rather than by chain cleavage may lead to novel therapeutic strategies for inducing cell death.
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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.