Low-molecular-weight MK2 inhibitors: a tough nut to crack!
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Schlapbach, Achim and Huppertz, Christine (2009) Low-molecular-weight MK2 inhibitors: a tough nut to crack! Future Medicinal Chemistry, 1 (7). pp. 1243-1257. ISSN 1756-8927
Abstract
The p38 pathway has been at the center of interest for anti-inflammatory drug discovery for many years as it is crucial for the biosynthesis of TNF-α, IL-1β and other mediators. Most of the anti-inflammatory effects of p38 inhibition are mediated through MAPK-activated protein kinase-2 (MK2), a direct downstream target of p38, which makes MK2 a very interesting drug target. Within the last 5 years, several classes of low-molecular-weight MK2 inhibitors were disclosed in the patent and primary literature. Advanced compounds could be optimized to nanomolar potencies and inhibit TNF-α release, as well as the phosphorylation of the MK2 substrate heat-shock protein 27 in cellular assays. This article will review the recent progress in this field and will highlight and discuss the most promising compound series disclosed so far.
| Item Type: | Article |
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| Keywords: | p38 pathway; MK2 inhibitors |
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| Date Deposited: | 13 Oct 2015 13:15 |
| Last Modified: | 13 Oct 2015 13:15 |
| URI: | https://oak.novartis.com/id/eprint/3499 |