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Title: Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction

Authors:
 [1];  [1];  [1];  [1];  [1];  [2];  [2];  [1];  [3];  [1];  [1];  [1];  [1];  [1]; ORCiD logo [1]
  1. Comprehensive Cancer and Departments of Internal Medicine, Pharmacology and Medicinal Chemistry, University of Michigan, 1600 Huron Parkway Ann Arbor MI 48109 USA
  2. Life Sciences Institute, University of Michigan, 210 Washtenaw Ann Arbor MI 48109 USA
  3. Department of Pathology, University of Michigan, 1600 Huron Parkway Ann Arbor MI 48109 USA
Publication Date:
Sponsoring Org.:
USDOE
OSTI Identifier:
1416992
Grant/Contract Number:  
AC02-06CH11357
Resource Type:
Publisher's Accepted Manuscript
Journal Name:
Angewandte Chemie (International Edition)
Additional Journal Information:
Journal Name: Angewandte Chemie (International Edition) Journal Volume: 57 Journal Issue: 6; Journal ID: ISSN 1433-7851
Publisher:
Wiley Blackwell (John Wiley & Sons)
Country of Publication:
Germany
Language:
English

Citation Formats

Xu, Shilin, Aguilar, Angelo, Xu, Tianfeng, Zheng, Ke, Huang, Liyue, Stuckey, Jeanne, Chinnaswamy, Krishnapriya, Bernard, Denzil, Fernández-Salas, Ester, Liu, Liu, Wang, Mi, McEachern, Donna, Przybranowski, Sally, Foster, Caroline, and Wang, Shaomeng. Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction. Germany: N. p., 2018. Web. doi:10.1002/anie.201711828.
Xu, Shilin, Aguilar, Angelo, Xu, Tianfeng, Zheng, Ke, Huang, Liyue, Stuckey, Jeanne, Chinnaswamy, Krishnapriya, Bernard, Denzil, Fernández-Salas, Ester, Liu, Liu, Wang, Mi, McEachern, Donna, Przybranowski, Sally, Foster, Caroline, & Wang, Shaomeng. Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction. Germany. doi:10.1002/anie.201711828.
Xu, Shilin, Aguilar, Angelo, Xu, Tianfeng, Zheng, Ke, Huang, Liyue, Stuckey, Jeanne, Chinnaswamy, Krishnapriya, Bernard, Denzil, Fernández-Salas, Ester, Liu, Liu, Wang, Mi, McEachern, Donna, Przybranowski, Sally, Foster, Caroline, and Wang, Shaomeng. Mon . "Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction". Germany. doi:10.1002/anie.201711828.
@article{osti_1416992,
title = {Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction},
author = {Xu, Shilin and Aguilar, Angelo and Xu, Tianfeng and Zheng, Ke and Huang, Liyue and Stuckey, Jeanne and Chinnaswamy, Krishnapriya and Bernard, Denzil and Fernández-Salas, Ester and Liu, Liu and Wang, Mi and McEachern, Donna and Przybranowski, Sally and Foster, Caroline and Wang, Shaomeng},
abstractNote = {},
doi = {10.1002/anie.201711828},
journal = {Angewandte Chemie (International Edition)},
number = 6,
volume = 57,
place = {Germany},
year = {2018},
month = {1}
}

Journal Article:
Free Publicly Available Full Text
Publisher's Version of Record
DOI: 10.1002/anie.201711828

Citation Metrics:
Cited by: 8 works
Citation information provided by
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Works referenced in this record:

Menin Critically Links MLL Proteins with LEDGF on Cancer-Associated Target Genes
journal, July 2008


Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia
journal, January 2012

  • Grembecka, Jolanta; He, Shihan; Shi, Aibin
  • Nature Chemical Biology, Vol. 8, Issue 3
  • DOI: 10.1038/nchembio.773

The role of MLL in hematopoiesis and leukemia
journal, January 2002


The molecular biology of mixed lineage leukemia
journal, June 2009


Mechanisms of leukemogenesis by MLL fusion proteins: Review
journal, December 2010


Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia
journal, November 2012


MLL: How complex does it get?
journal, January 2005

  • Popovic, Relja; Zeleznik-Le, Nancy J.
  • Journal of Cellular Biochemistry, Vol. 95, Issue 2
  • DOI: 10.1002/jcb.20430

Interaction of MLL Amino Terminal Sequences with Menin Is Required for Transformation
journal, August 2007


Potent inhibition of DOT1L as treatment of MLL-fusion leukemia
journal, August 2013


Pharmacologic Inhibition of the Menin-MLL Interaction Blocks Progression of MLL Leukemia In Vivo
journal, April 2015


The cellular thermal shift assay for evaluating drug target interactions in cells
journal, August 2014

  • Jafari, Rozbeh; Almqvist, Helena; Axelsson, Hanna
  • Nature Protocols, Vol. 9, Issue 9
  • DOI: 10.1038/nprot.2014.138

Structure-Based Design of High-Affinity Macrocyclic Peptidomimetics to Block the Menin-Mixed Lineage Leukemia 1 (MLL1) Protein–Protein Interaction
journal, January 2013

  • Zhou, Haibin; Liu, Liu; Huang, Jing
  • Journal of Medicinal Chemistry, Vol. 56, Issue 3
  • DOI: 10.1021/jm3015298

The resurgence of covalent drugs
journal, April 2011

  • Singh, Juswinder; Petter, Russell C.; Baillie, Thomas A.
  • Nature Reviews Drug Discovery, Vol. 10, Issue 4
  • DOI: 10.1038/nrd3410

The tumor suppressor menin regulates hematopoiesis and myeloid transformation by influencing Hox gene expression
journal, January 2006

  • Chen, Y. -X.; Yan, J.; Keeshan, K.
  • Proceedings of the National Academy of Sciences, Vol. 103, Issue 4
  • DOI: 10.1073/pnas.0510347103

Disordered epigenetic regulation in MLL-related leukemia
journal, September 2012


Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay
journal, July 2013

  • Molina, Daniel Martinez; Jafari, Rozbeh; Ignatushchenko, Marina
  • Science, Vol. 341, Issue 6141
  • DOI: 10.1126/science.1233606

When epigenetics kills: MLL fusion proteins in leukemia
journal, March 2005

  • Slany, Robert K.
  • Hematological Oncology, Vol. 23, Issue 1
  • DOI: 10.1002/hon.739

WDR5 Interacts with Mixed Lineage Leukemia (MLL) Protein via the Histone H3-binding Pocket
journal, October 2008

  • Song, Ji-Joon; Kingston, Robert E.
  • Journal of Biological Chemistry, Vol. 283, Issue 50
  • DOI: 10.1074/jbc.M806900200

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2
journal, April 2013

  • Knutson, S. K.; Warholic, N. M.; Wigle, T. J.
  • Proceedings of the National Academy of Sciences, Vol. 110, Issue 19
  • DOI: 10.1073/pnas.1303800110

High-Affinity Small-Molecule Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction Closely Mimic a Natural Protein–Protein Interaction
journal, February 2014

  • He, Shihan; Senter, Timothy J.; Pollock, Jonathan
  • Journal of Medicinal Chemistry, Vol. 57, Issue 4
  • DOI: 10.1021/jm401868d

The Menin Tumor Suppressor Protein Is an Essential Oncogenic Cofactor for MLL-Associated Leukemogenesis
journal, October 2005