Literature DB >> 25529738

5Z-7-Oxozeaenol covalently binds to MAP2K7 at Cys218 in an unprecedented manner.

Yuri Sogabe1, Takashi Matsumoto2, Takuma Hashimoto1, Yasuyuki Kirii3, Masaaki Sawa3, Takayoshi Kinoshita4.   

Abstract

5Z-7-Oxozeaenol (5Z7O) is a covalent bonding inhibitor against the several protein kinases (e.g., ERK2 and TAK1) that possess a free cysteine at the gatekeeper-2 position. In addition to this cysteine, MAP2K7 has three other cysteine residues that are candidate for covalent bonding by the inhibitor 5Z7O. The crystal structure of the MAP2K7/5Z7O complex revealed that the inhibitor binds to MAP2K7 at a cysteine residue located at the end of the hinge region and not at the gatekeeper-2 residue. The structural insights into the interaction of 5Z7O with MAP2K7 should aid the development of 5Z7O derivatives with improved potency and selectivity.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Covalent bonding inhibitor; Crystal structure; Cysteine; MAP kinase kinase 7

Mesh：

Substances：

Year:  2014        PMID： 25529738     DOI： 10.1016/j.bmcl.2014.12.011

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.940


  8 in total

1.  Structure-guided development of covalent TAK1 inhibitors.

Authors:  Li Tan; Deepak Gurbani; Ellen L Weisberg; John C Hunter; Lianbo Li; Douglas S Jones; Scott B Ficarro; Samar Mowafy; Chun-Pong Tam; Suman Rao; Guangyan Du; James D Griffin; Peter K Sorger; Jarrod A Marto; Kenneth D Westover; Nathanael S Gray
Journal:  Bioorg Med Chem       Date:  2016-12-09       Impact factor: 3.641

Review 2.  JNK Signaling: Regulation and Functions Based on Complex Protein-Protein Partnerships.

Authors:  András Zeke; Mariya Misheva; Attila Reményi; Marie A Bogoyevitch
Journal:  Microbiol Mol Biol Rev       Date:  2016-07-27       Impact factor: 11.056

Review 3.  Non-'classical' MEKs: A review of MEK3-7 inhibitors.

Authors:  Ada J Kwong; Karl A Scheidt
Journal:  Bioorg Med Chem Lett       Date:  2020-04-23       Impact factor: 2.823

4.  Inhibition of the MAP2K7-JNK pathway with 5Z-7-oxozeaenol induces apoptosis in T-cell acute lymphoblastic leukemia.

Authors:  Taylor J Chen; Wa Du; Jacob J Junco; Cory Seth Bridges; Ye Shen; Monica Puppi; Karen R Rabin; H Daniel Lacorazza
Journal:  Oncotarget       Date:  2021-08-31

5.  Co-Inflammatory Roles of TGFβ1 in the Presence of TNFα Drive a Pro-inflammatory Fate in Mesenchymal Stem Cells.

Authors:  Shalom Lerrer; Yulia Liubomirski; Alexander Bott; Khalid Abnaof; Nino Oren; Afsheen Yousaf; Cindy Körner; Tsipi Meshel; Stefan Wiemann; Adit Ben-Baruch
Journal:  Front Immunol       Date:  2017-05-11       Impact factor: 7.561

6.  Probing the interaction interface of the GADD45β/MKK7 and MKK7/DTP3 complexes by chemical cross-linking mass spectrometry.

Authors:  Camilla Rega; Rosita Russo; Annalia Focà; Annamaria Sandomenico; Emanuela Iaccarino; Domenico Raimondo; Edoardo Milanetti; Laura Tornatore; Guido Franzoso; Paolo Vincenzo Pedone; Menotti Ruvo; Angela Chambery
Journal:  Int J Biol Macromol       Date:  2018-03-20       Impact factor: 6.953

Review 7.  MKK7, the essential regulator of JNK signaling involved in cancer cell survival: a newly emerging anticancer therapeutic target.

Authors:  Jae Gwang Park; Nur Aziz; Jae Youl Cho
Journal:  Ther Adv Med Oncol       Date:  2019-09-24       Impact factor: 8.168

Review 8.  Ca(2+) signaling in the myocardium by (redox) regulation of PKA/CaMKII.

Authors:  Alex S Johnston; Stephan E Lehnart; Joseph R Burgoyne
Journal:  Front Pharmacol       Date:  2015-08-10       Impact factor: 5.810
  8 in total

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