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Literature DB >> 23602398

Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.

Dong Xiao¹, Anandan Palani, Xianhai Huang, Michael Sofolarides, Wei Zhou, Xiao Chen, Robert Aslanian, Zhuyan Guo, James Fossetta, Fang Tian, Prashant Trivedi, Peter Spacciapoli, Charles E Whitehurst, Daniel Lundell.

Abstract

Conformation restriction of linear N-alkylanilide MK2 inhibitors to their E-conformer was developed. This strategy enabled rapid advance in identifying a series of potent non-ATP competitive inhibitors that exhibited cell based activity in anti-TNFα assay.

Entities: Chemical Gene

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Year: 2013 PMID： 23602398 DOI： 10.1016/j.bmcl.2013.03.109

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

5 in total

1. A reversible gene-targeting strategy identifies synthetic lethal interactions between MK2 and p53 in the DNA damage response in vivo.

Authors: Sandra Morandell; H Christian Reinhardt; Ian G Cannell; Jacob S Kim; Daniela M Ruf; Tanya Mitra; Anthony D Couvillon; Tyler Jacks; Michael B Yaffe
Journal: Cell Rep Date: 2013-11-14 Impact factor: 9.423

Review 2. Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials.

Authors: Mario Fiore; Stefano Forli; Fabrizio Manetti
Journal: J Med Chem Date: 2015-11-09 Impact factor: 7.446

Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.

1. A reversible gene-targeting strategy identifies synthetic lethal interactions between MK2 and p53 in the DNA damage response in vivo.

Review 2. Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials.

3. Microwave-Assisted Synthesis of a MK2 Inhibitor by Suzuki-Miyaura Coupling for Study in Werner Syndrome Cells.

Review 4. MAPKAPK2: the master regulator of RNA-binding proteins modulates transcript stability and tumor progression.

5. IL-33 regulates cytokine production and neutrophil recruitment via the p38 MAPK-activated kinases MK2/3.