Literature DB >> 19364658

Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).

Frank Lovering1, Steve Kirincich, Weiheng Wang, Kerry Combs, Lynn Resnick, Joan E Sabalski, John Butera, Julie Liu, Kevin Parris, J B Telliez.   

Abstract

A novel series of inhibitors for mitogen activated protein kinase-activated protein kinase 2 (MK-2) are reported. These squarate based inhibitors were identified via a high-throughput screen. An MK2 co-structure with the starting ligand was obtained and a structure based approach was followed to optimize potency and selectivity.

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Year:  2009        PMID: 19364658     DOI: 10.1016/j.bmc.2009.03.041

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  4 in total

1.  Diamine Ligands in Copper-Catalyzed Reactions.

Authors:  David S Surry; Stephen L Buchwald
Journal:  Chem Sci       Date:  2010       Impact factor: 9.825

2.  Molecular Properties of Drugs Interacting with SLC22 Transporters OAT1, OAT3, OCT1, and OCT2: A Machine-Learning Approach.

Authors:  Henry C Liu; Anne Goldenberg; Yuchen Chen; Christina Lun; Wei Wu; Kevin T Bush; Natasha Balac; Paul Rodriguez; Ruben Abagyan; Sanjay K Nigam
Journal:  J Pharmacol Exp Ther       Date:  2016-08-03       Impact factor: 4.030

Review 3.  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

4.  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

  4 in total

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