| Literature DB >> 22119462 |
Arthur Oubrie1, Allard Kaptein, Edwin de Zwart, Niels Hoogenboom, Rianne Goorden, Bas van de Kar, Maaike van Hoek, Vera de Kimpe, Ruud van der Heijden, Judith Borsboom, Bert Kazemier, Jeroen de Roos, Michiel Scheffers, Jos Lommerse, Carsten Schultz-Fademrecht, Tjeerd Barf.
Abstract
Optimization of our previously described pyrrolopiperidone series led to the identification of a new benzamide sub-series, which exhibits consistently high potency in biochemical and cell-based assays throughout the series. Strong inhibition of LPS-induced production of the cytokine TNFα is coupled to the regulation of HSP27 phosphorylation, indicating that the observed cellular effects result from the inhibition of MK2. X-ray crystallographic and computational analyses provide a rationale for the high potency of the series.Entities:
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Year: 2011 PMID： 22119462 DOI： 10.1016/j.bmcl.2011.10.071
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823