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Can I read Acylideneoxoindoles: A new class of reversible inhibitors of human transglutaminase 2 on EtoBox?
Acylideneoxoindoles: A new class of reversible inhibitors of human transglutaminase 2 by Cornelius Klöck; Xi Jin; Kihang Choi; Chaitan Khosla; Peter B. Madrid; Andrew Spencer; Brian C. Raimundo; Paul Boardman; Guido Lanza; John H. Griffin is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Acylideneoxoindoles: A new class of reversible inhibitors of human transglutaminase 2 about?
Inhibitors of human transglutaminase 2 (TG2) are anticipated to be useful in the therapy of a variety of diseases including celiac sprue as well as certain CNS disorders and cancers. A class of 3-acylidene-2-oxoindoles was identified as potent reversible inhibitors of human TG2. Structure-activity relationship analysis of a lead compound led to the generation of several potent, competitive inhibitors. Analogs with significant non-competitive character were also identified, suggesting that the compounds bind at one or more allosteric regulatory sites on this multidomain enzyme. The most active compounds had K(i) values below 1.0 μM in two different kinetic assays for human TG2, and may therefore be suitable for investigations into the role of TG2 in physiology and disease in animals.
Who reads Acylideneoxoindoles: A new class of reversible inhibitors of human transglutaminase 2?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Cornelius Klöck; Xi Jin; Kihang Choi; Chaitan Khosla; Peter B. Madrid; Andrew Spencer; Brian C. Raimundo; Paul Boardman; Guido Lanza; John H. Griffin
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)
- Published
- 2011
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)