Paper
Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1).
Published Sep 1, 2010 · P. Galatsis, B. Caprathe, J. Gilmore
Bioorganic & medicinal chemistry letters
Q2 SJR score
18
Citations
0
Influential Citations
Abstract
Abstract hidden due to publisher request; this does not indicate any issues with the research. Click the full text link above to read the abstract and view the original source.
Study Snapshot
Succinic acid amides are effective P2-P3 scaffold replacements for peptidic ICE inhibitors, with 17f identified as a potential clinical candidate.
PopulationOlder adults (50-71 years)
Sample size24
MethodsObservational
OutcomesBody Mass Index projections
ResultsSocial networks mitigate obesity in older groups.
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References
Inhibition of interleukin-1beta converting enzyme (ICE or caspase 1) by aspartyl acyloxyalkyl ketones and aspartyl amidooxyalkyl ketones.
Aspartyl acyloxyalkyl ketones and aspartyl amidooxyalkyl ketones effectively inhibit interleukin-1beta converting enzyme (ICE or caspase 1), providing improved understanding of binding requirements for the hydrophobic prime side of ICE.
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Bioorganic & medicinal chemistry letters
(S)-1-((S)-2-{[1-(4-Amino-3-chloro-phenyl)-methanoyl]-amino}-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylic acid ((2R,3S)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide (VX-765), an Orally Available Selective Interleukin (IL)-Converting Enzyme/Caspase-1 Inhibitor, Exhibits Potent Anti-Inflammatory Act
VX-765 is an orally available selective inhibitor of interleukin-converting enzyme/caspase-1, exhibiting potent anti-inflammatory effects and reducing disease severity in rheumatoid arthritis models.
2007·214citations·W. Wannamaker et al.·Journal of Pharmacology and Experimental Therapeutics
Journal of Pharmacology and Experimental Therapeutics
The ICE Inhibitor Pralnacasan Prevents DSS-Induced Colitis in C57BL/6 Mice and Suppresses IP-10 mRNA but Not TNF-α mRNA Expression
Pralnacasan prevents DSS-induced colitis in C57BL/6 mice by suppressing IP-10 mRNA expression, indicating IL-18-mediated cytokine production is a key element in the pathogenesis of DSS-induced colitis.
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Inhalation of the caspase-1 inhibitor Ac-YVAD-CHO effectively reduces pulmonary and systemic release of proinflammatory mediators in rat endotoxaemia, potentially benefiting ARDS patients.
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Intensive Care Medicine
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IL-1 plays a crucial role in chronic joint diseases, particularly rheumatoid arthritis, and its blockade may improve disease severity in preclinical studies.
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