Literature DB >> 17576063

The discovery of carboline analogs as potent MAPKAP-K2 inhibitors.

Jiang-Ping Wu1, Ji Wang, Asitha Abeywardane, Denise Andersen, Michel Emmanuel, Elda Gautschi, Daniel R Goldberg, Mohammed A Kashem, Susan Lukas, Wang Mao, Leslie Martin, Tina Morwick, Neil Moss, Christopher Pargellis, Usha R Patel, Lori Patnaude, Gregory W Peet, Donna Skow, Roger J Snow, Yancey Ward, Brian Werneburg, Andre White.   

Abstract

The discovery of a series of potent, carboline-based MK2 inhibitors is described. These compounds inhibit MK2 with IC50s as low as 10 nM, as measured in a DELFIA assay. An X-ray crystal structure reveals that they bind in a region near the p-loop and the hinge region of MK2a.

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Year:  2007        PMID： 17576063     DOI： 10.1016/j.bmcl.2007.05.101

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


  15 in total

1.  The p38 MAP Kinase Family as Regulators of Proinflammatory Cytokine Production in Degenerative Diseases of the CNS.

Authors:  Adam D Bachstetter; Linda J Van Eldik
Journal:  Aging Dis       Date:  2010-09-24       Impact factor: 6.745

Review 2.  Targeting innate immunity protein kinase signalling in inflammation.

Authors:  Matthias Gaestel; Alexey Kotlyarov; Michael Kracht
Journal:  Nat Rev Drug Discov       Date:  2009-06       Impact factor: 84.694

3.  Discovering protein-ligand chalcogen bonding in the protein data bank using endocyclic sulfur-containing heterocycles as ligand search subsets.

Authors:  Miguel O Mitchell
Journal:  J Mol Model       Date:  2017-09-24       Impact factor: 1.810

4.  Discovery of a Potent Dihydrooxadiazole Series of Non-ATP-Competitive MK2 (MAPKAPK2) Inhibitors.

Authors:  Jun Qin; Pawan Dhondi; Xianhai Huang; Robert Aslanian; James Fossetta; Fang Tian; Daniel Lundell; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2011-12-23       Impact factor: 4.345

5.  Structure of the β-form of human MK2 in complex with the non-selective kinase inhibitor TEI-L03090.

Authors:  Aiko Fujino; Kei Fukushima; Takaharu Kubota; Yoshiyuki Matsumoto; Midori Takimoto-Kamimura
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2013-11-28

6.  Novel and Potential Small Molecule Scaffolds as DYRK1A Inhibitors by Integrated Molecular Docking-Based Virtual Screening and Dynamics Simulation Study.

Authors:  Mir Mohammad Shahroz; Hemant Kumar Sharma; Abdulmalik S A Altamimi; Mubarak A Alamri; Abuzer Ali; Amena Ali; Safar Alqahtani; Ali Altharawi; Alhumaidi B Alabbas; Manal A Alossaimi; Yassine Riadi; Ahmad Firoz; Obaid Afzal
Journal:  Molecules       Date:  2022-02-09       Impact factor: 4.411

Review 7.  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

8.  The gramine route to pyrido[4,3-b]indol-3-ones - identification of a new cytotoxic lead.

Authors:  Uwe Wollein; Franz Bracher
Journal:  Sci Pharm       Date:  2010-12-18

9.  A physicochemical descriptor-based scoring scheme for effective and rapid filtering of kinase-like chemical space.

Authors:  Narender Singh; Hongmao Sun; Sidhartha Chaudhury; Mohamed Diwan M Abdulhameed; Anders Wallqvist; Gregory Tawa
Journal:  J Cheminform       Date:  2012-02-08       Impact factor: 5.514

10.  A computational study on thiourea analogs as potent MK-2 inhibitors.

Authors:  Ming Hao; Hong Ren; Fang Luo; Shuwei Zhang; Jieshan Qiu; Mingjuan Ji; Hongzong Si; Guohui Li
Journal:  Int J Mol Sci       Date:  2012-06-08       Impact factor: 6.208
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