ArticleProceedings of the National Academy of Sciences of the United States of America2004
Fas-disabling small exocyclic peptide mimetics limit apoptosis by an unexpected mechanism.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 30 citations in OpenAlex.
- ACSS2/AATF Drives Soluble FasL-Mediated CD8Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Article
- Systemic Treatment with Fas-Blocking Peptide Attenuates Apoptosis in Brain Ischemia.International journal of molecular sciences · 2024Article
- Airway epithelial cells and macrophages trigger IL-6-CD95/CD95L axis and mediate initial immunopathology of COVID-19.iScience · 2023Article
- Therapeutic approaches targeting CD95L/CD95 signaling in cancer and autoimmune diseases.Cell death & disease · 2022Review
- Rational Design of Constrained Peptides as Protein Interface Inhibitors.Antibodies (Basel, Switzerland) · 2021Review
- Intranasal delivery of a Fas-blocking peptide attenuates Fas-mediated apoptosis in brain ischemia.Scientific reports · 2018Article
- RIPK1 protects hepatocytes from death in Fas-induced hepatitis.Scientific reports · 2017Article
- Article
- Synthetic disulfide-bridged cyclic peptides mimic the anti-angiogenic actions of chondromodulin-I.Cancer science · 2012Article
- Structure based antibody-like peptidomimetics.Pharmaceuticals (Basel, Switzerland) · 2012Article
- Topomimetics of amphipathic beta-sheet and helix-forming bactericidal peptides neutralize lipopolysaccharide endotoxins.Journal of medicinal chemistry · 2006Article
- Disabling TNF receptor signaling by induced conformational perturbation of tryptophan-107.Proceedings of the National Academy of Sciences of the United States of America · 2005Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Fas ligand- (FasL) mediated apoptosis is an important element of tissue-specific organ damage. We have developed biologically active small exocyclic peptide mimetics that disable apoptotic functions of Fas. The most effective mimetic binds to both its receptor and FasL with comparable affinity. In vitro, the most effective antagonist blocked FasL-induced cytotoxicity completely and specifically. In vivo, the antagonistic mimetic also prevented Concanavilin A (Con A) induced hepatitis, a CD4(+) T cell-mediated animal model of liver injury. Although current approaches prevent Fas receptor signaling by excluding FasL binding to Fas, the small molecule mimetics reported here disable Fas by promoting a defective Fas-FasL receptor complex. This event desensitizes FasL-mediated apoptosis by inhibiting extracellular signal regulated kinase activity and up-regulating NF-kappaB.
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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.