Lazaroids U83836E and U74389G are Potent, Time-Dependent Inhibitors of Caspase-1

Autor:	Thomas K. Hagerman, Caitlin E. Karver, Margaret Y. Kawarski
Rok vydání:	2015
Předmět:	Pharmacology Antioxidant Chemistry medicine.medical_treatment Caspase 1 Organic Chemistry Inflammation medicine.disease_cause Caspase Inhibitors Biochemistry Small molecule Antioxidants Autoimmunity Small Molecule Libraries Immune system Drug Discovery medicine Humans Molecular Medicine Reversible inhibition medicine.symptom
Zdroj:	Chemical Biology & Drug Design. 86:1049-1054
ISSN:	1747-0277
DOI:	10.1111/cbdd.12572
Popis:	Caspase-1 is involved in inflammatory processes and is overactive in autoimmunity and autoinflammation. Antioxidant small molecules also play a role in the immune response by decreasing inflammation. An 84-membered library of pro- and antioxidant small molecules was screened for potential inhibitors of caspase-1. Thirteen compounds were discovered to reduce the activity of caspase-1 below 30%. The most potent inhibitors were lazaroid antioxidant molecules, U83836E (B8) and U74389G (B9), displaying apparent Ki values of 48.0 and 50.0 nm, respectively. Both demonstrated a time-dependent and reversible inhibition.
Databáze:	OpenAIRE
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