Literature DB >> 19616945

Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency.

David R Anderson1, Marvin J Meyers, Ravi G Kurumbail, Nicole Caspers, Gennadiy I Poda, Scott A Long, Betsy S Pierce, Matthew W Mahoney, Robert J Mourey.   

Abstract

Identification of potent benzothiophene inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2), structure-activity relationship (SAR) studies, selectivity assessments against CDK2, cellular potency and mechanism of action are presented. Crystallographic data provide a rationale for the observed MK2 potency as well as selectivity over CDK2 for this class of inhibitors.

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Year:  2009        PMID： 19616945     DOI： 10.1016/j.bmcl.2009.02.015

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


  14 in total

1.  Dynamic undocking and the quasi-bound state as tools for drug discovery.

Authors:  Sergio Ruiz-Carmona; Peter Schmidtke; F Javier Luque; Lisa Baker; Natalia Matassova; Ben Davis; Stephen Roughley; James Murray; Rod Hubbard; Xavier Barril
Journal:  Nat Chem       Date:  2016-11-14       Impact factor: 24.427

2.  Inhibition of the protein kinase MK-2 protects podocytes from nephrotic syndrome-related injury.

Authors:  Ruma Pengal; Adam J Guess; Shipra Agrawal; Joshua Manley; Richard F Ransom; Robert J Mourey; Rainer Benndorf; William E Smoyer
Journal:  Am J Physiol Renal Physiol       Date:  2011-05-25

3.  1,4-Thienodiazepine-2,5-diones via MCR (II): scaffold hopping by Gewald and Ugi-deprotection-cyclization strategy.

Authors:  Yijun Huang; Alexander Dömling
Journal:  Chem Biol Drug Des       Date:  2010-06-09       Impact factor: 2.817

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

Review 6.  Privileged diazepine compounds and their emergence as bromodomain inhibitors.

Authors:  Steven G Smith; Roberto Sanchez; Ming-Ming Zhou
Journal:  Chem Biol       Date:  2014-04-17

7.  Benzofuran-, benzothiophene-, indazole- and benzisoxazole-quinones: excellent substrates for NAD(P)H:quinone oxidoreductase 1.

Authors:  Jeffery J Newsome; Mary Hassani; Elizabeth Swann; Jane M Bibby; Howard D Beall; Christopher J Moody
Journal:  Bioorg Med Chem       Date:  2013-04-06       Impact factor: 3.641

Review 8.  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

9.  Pharmacological and genetic inhibition of downstream targets of p38 MAPK in experimental nephrotic syndrome.

Authors:  Xiaojing Nie; Melinda A Chanley; Ruma Pengal; David B Thomas; Shipra Agrawal; William E Smoyer
Journal:  Am J Physiol Renal Physiol       Date:  2017-11-29

10.  Binding affinity prediction for ligands and receptors forming tautomers and ionization species: inhibition of mitogen-activated protein kinase-activated protein kinase 2 (MK2).

Authors:  Senthil Natesan; Rajesh Subramaniam; Charles Bergeron; Stefan Balaz
Journal:  J Med Chem       Date:  2012-02-17       Impact factor: 7.446
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