Literature DB >> 16242327

Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative.

Takayoshi Kinoshita1, Masaichi Warizaya, Makoto Ohori, Kentaro Sato, Masahiro Neya, Takashi Fujii.   

Abstract

A series of pyrazolopyridazine compounds were briefly investigated as ERK2 inhibitors. The crystal structure of ERK2 complexed with an allyl derivative was determined. The compound induces structural change including movement of the glycine-rich loop and peptide flip between Met108-Glu109. As a result, the newly formed subsite can recognize small hydrophobic substituents but not hydrophilic ones.

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Year:  2005        PMID: 16242327     DOI: 10.1016/j.bmcl.2005.09.055

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


  7 in total

1.  A computational workflow for the design of irreversible inhibitors of protein kinases.

Authors:  Alberto Del Rio; Miriam Sgobba; Marco Daniele Parenti; Gianluca Degliesposti; Rosetta Forestiero; Claudia Percivalle; Pier Franco Conte; Mauro Freccero; Giulio Rastelli
Journal:  J Comput Aided Mol Des       Date:  2010-03-21       Impact factor: 3.686

2.  Norathyriol suppresses skin cancers induced by solar ultraviolet radiation by targeting ERK kinases.

Authors:  Jixia Li; Margarita Malakhova; Madhusoodanan Mottamal; Kanamata Reddy; Igor Kurinov; Andria Carper; Alyssa Langfald; Naomi Oi; Myoung Ok Kim; Feng Zhu; Carlos P Sosa; Keyuan Zhou; Ann M Bode; Zigang Dong
Journal:  Cancer Res       Date:  2011-11-14       Impact factor: 12.701

3.  Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors.

Authors:  Bernhard C Lechtenberg; Peter D Mace; E Hampton Sessions; Robert Williamson; Romain Stalder; Yann Wallez; Gregory P Roth; Stefan J Riedl; Elena B Pasquale
Journal:  ACS Med Chem Lett       Date:  2017-06-12       Impact factor: 4.345

4.  A high throughput assay to identify substrate-selective inhibitors of the ERK protein kinases.

Authors:  Chad J Miller; Yagmur Muftuoglu; Benjamin E Turk
Journal:  Biochem Pharmacol       Date:  2017-06-21       Impact factor: 5.858

5.  Multi-gram scale synthesis of FR180204.

Authors:  Samarjit Patnaik; Harry C Dietz; Wei Zheng; Christopher Austin; Juan J Marugan
Journal:  J Org Chem       Date:  2009-11-20       Impact factor: 4.354

6.  A chemical genetic approach demonstrates that MPK3/MPK6 activation and NADPH oxidase-mediated oxidative burst are two independent signaling events in plant immunity.

Authors:  Juan Xu; Jie Xie; Chengfei Yan; Xiaoqin Zou; Dongtao Ren; Shuqun Zhang
Journal:  Plant J       Date:  2013-12-17       Impact factor: 6.417

7.  Using a Genetically Encoded Sensor to Identify Inhibitors of Toxoplasma gondii Ca2+ Signaling.

Authors:  Saima M Sidik; Miryam A Hortua Triana; Aditya S Paul; Majida El Bakkouri; Caroline G Hackett; Fanny Tran; Nicholas J Westwood; Raymond Hui; William J Zuercher; Manoj T Duraisingh; Silvia N J Moreno; Sebastian Lourido
Journal:  J Biol Chem       Date:  2016-03-01       Impact factor: 5.157

  7 in total

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