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Song T, Wang Z, Ji F, et al. Deactivation of Mcl-1 by Dual-Function Small-Molecule Inhibitors Targeting the Bcl-2 Homology 3 Domain and Facilitating Mcl-1 Ubiquitination. Angew Chem Int Ed Engl. 2016;55(46):14250-14256doi: 10.1002/anie.201606543.
Song, T., Wang, Z., Ji, F., Feng, Y., Fan, Y., Chai, G., Li, X., Li, Z., & Zhang, Z. (2016). Deactivation of Mcl-1 by Dual-Function Small-Molecule Inhibitors Targeting the Bcl-2 Homology 3 Domain and Facilitating Mcl-1 Ubiquitination. Angewandte Chemie (International ed. in English), 55(46), 14250-14256. https://doi.org/10.1002/anie.201606543
Song, Ting, et al. "Deactivation of Mcl-1 by Dual-Function Small-Molecule Inhibitors Targeting the Bcl-2 Homology 3 Domain and Facilitating Mcl-1 Ubiquitination." Angewandte Chemie (International ed. in English) vol. 55,46 (2016): 14250-14256. doi: https://doi.org/10.1002/anie.201606543
Song T, Wang Z, Ji F, Feng Y, Fan Y, Chai G, Li X, Li Z, Zhang Z. Deactivation of Mcl-1 by Dual-Function Small-Molecule Inhibitors Targeting the Bcl-2 Homology 3 Domain and Facilitating Mcl-1 Ubiquitination. Angew Chem Int Ed Engl. 2016 Nov 07;55(46):14250-14256. doi: 10.1002/anie.201606543. Epub 2016 Oct 04. PMID: 27701804.
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Angew Chem Int Ed Engl. 2016 Nov 07;55(46):14250-14256. doi: 10.1002/anie.201606543. Epub 2016 Oct 04.

Deactivation of Mcl-1 by Dual-Function Small-Molecule Inhibitors Targeting the Bcl-2 Homology 3 Domain and Facilitating Mcl-1 Ubiquitination.

Angewandte Chemie (International ed. in English)

Ting Song, Ziqian Wang, Fangling Ji, Yingang Feng, Yudan Fan, Gaobo Chai, Xiangqian Li, Zhiqiang Li, Zhichao Zhang

Affiliations

  1. State Key Laboratory of Fine Chemicals, Zhang Dayu School of Chemistry, Dalian University of Technology, Dalian, Liaoning, China.
  2. School of Chemistry, Dalian University of Technology, Dalian, Liaoning, China.
  3. School of Life Science and Technology, Dalian University of Technology, China.
  4. Shandong Key Laboratory of Synthetic Biology, CAS Key Laboratory of Biofuels, Qingdao Institute of Bioenergy and Bioprocess Technology, Chinese Academy of Sciences, Qingdao, Shandong, China.
  5. Institute of Oceanology, Chinese Academy of Sciences, Qingdao, Shandong, China.
  6. School of Chemistry, Dalian University of Technology, Dalian, Liaoning, China. [email protected].

PMID: 27701804 DOI: 10.1002/anie.201606543

Abstract

By means of limited proteolysis assay, three-dimensional NMR, X-ray crystallography and alanine mutations, a dynamic region at the Q221R222N223 motif in the Bcl-2 homology 3 (BH3) domain of Mcl-1 has been identified as a conformational switch which controls Mcl-1 ubiquitination. Noxa

© 2016 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Keywords: apoptosis; conformation analysis; drug design; inhibitors; structure elucidation

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