Identification of an allosteric benzothiazolopyrimidone inhibitor of the oncogenic protein tyrosine phosphatase SHP2
- Authors:
- Publication Date:
- Sponsoring Org.:
- USDOE
- OSTI Identifier:
- 1496372
- Grant/Contract Number:
- DEAC02-06CH11357
- Resource Type:
- Publisher's Accepted Manuscript
- Journal Name:
- Bioorganic and Medicinal Chemistry
- Additional Journal Information:
- Journal Name: Bioorganic and Medicinal Chemistry Journal Volume: 25 Journal Issue: 24; Journal ID: ISSN 0968-0896
- Publisher:
- Elsevier
- Country of Publication:
- United Kingdom
- Language:
- English
Citation Formats
LaRochelle, Jonathan R., Fodor, Michelle, Ellegast, Jana M., Liu, Xiaoxi, Vemulapalli, Vidyasiri, Mohseni, Morvarid, Stams, Travis, Buhrlage, Sara J., Stegmaier, Kimberly, LaMarche, Matthew J., Acker, Michael G., and Blacklow, Stephen C. Identification of an allosteric benzothiazolopyrimidone inhibitor of the oncogenic protein tyrosine phosphatase SHP2. United Kingdom: N. p., 2017.
Web. doi:10.1016/j.bmc.2017.10.025.
LaRochelle, Jonathan R., Fodor, Michelle, Ellegast, Jana M., Liu, Xiaoxi, Vemulapalli, Vidyasiri, Mohseni, Morvarid, Stams, Travis, Buhrlage, Sara J., Stegmaier, Kimberly, LaMarche, Matthew J., Acker, Michael G., & Blacklow, Stephen C. Identification of an allosteric benzothiazolopyrimidone inhibitor of the oncogenic protein tyrosine phosphatase SHP2. United Kingdom. https://doi.org/10.1016/j.bmc.2017.10.025
LaRochelle, Jonathan R., Fodor, Michelle, Ellegast, Jana M., Liu, Xiaoxi, Vemulapalli, Vidyasiri, Mohseni, Morvarid, Stams, Travis, Buhrlage, Sara J., Stegmaier, Kimberly, LaMarche, Matthew J., Acker, Michael G., and Blacklow, Stephen C. Fri .
"Identification of an allosteric benzothiazolopyrimidone inhibitor of the oncogenic protein tyrosine phosphatase SHP2". United Kingdom. https://doi.org/10.1016/j.bmc.2017.10.025.
@article{osti_1496372,
title = {Identification of an allosteric benzothiazolopyrimidone inhibitor of the oncogenic protein tyrosine phosphatase SHP2},
author = {LaRochelle, Jonathan R. and Fodor, Michelle and Ellegast, Jana M. and Liu, Xiaoxi and Vemulapalli, Vidyasiri and Mohseni, Morvarid and Stams, Travis and Buhrlage, Sara J. and Stegmaier, Kimberly and LaMarche, Matthew J. and Acker, Michael G. and Blacklow, Stephen C.},
abstractNote = {},
doi = {10.1016/j.bmc.2017.10.025},
journal = {Bioorganic and Medicinal Chemistry},
number = 24,
volume = 25,
place = {United Kingdom},
year = {Fri Dec 01 00:00:00 EST 2017},
month = {Fri Dec 01 00:00:00 EST 2017}
}
Free Publicly Available Full Text
Publisher's Version of Record
https://doi.org/10.1016/j.bmc.2017.10.025
https://doi.org/10.1016/j.bmc.2017.10.025
Other availability
Cited by: 36 works
Citation information provided by
Web of Science
Web of Science
Save to My Library
You must Sign In or Create an Account in order to save documents to your library.
Works referenced in this record:
Potent Stimulation of SH-PTP2 Phosphatase Activity by Simultaneous Occupancy of Both SH2 Domains
journal, February 1995
- Pluskey, Scott; Wandless, Thomas J.; Walsh, Christopher T.
- Journal of Biological Chemistry, Vol. 270, Issue 7
Synthesis and properties of new benzo[4,5]thiazolo[3,2-a]pyrimidine derivatives
journal, May 2015
- Harutyunyan, A. A.; Panosyan, G. A.; Chishmarityan, S. G.
- Russian Journal of Organic Chemistry, Vol. 51, Issue 5
Structural and Functional Consequences of Three Cancer-Associated Mutations of the Oncogenic Phosphatase SHP2
journal, April 2016
- LaRochelle, Jonathan R.; Fodor, Michelle; Xu, Xiang
- Biochemistry, Vol. 55, Issue 15
PTPN11 Is a Central Node in Intrinsic and Acquired Resistance to Targeted Cancer Drugs
journal, September 2015
- Prahallad, Anirudh; Heynen, Guus J. J. E.; Germano, Giovanni
- Cell Reports, Vol. 12, Issue 12
PD-1/SHP-2 Inhibits Tc1/Th1 Phenotypic Responses and the Activation of T Cells in the Tumor Microenvironment
journal, December 2014
- Li, J.; Jie, H. -B.; Lei, Y.
- Cancer Research, Vol. 75, Issue 3
Druggability analysis and classification of protein tyrosine phosphatase active sites
journal, January 2016
- Ghattas, Mohammad; Raslan, Noor; Sadeq, Asil
- Drug Design, Development and Therapy, Vol. Volume 10
Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases
journal, June 2016
- Chen, Ying-Nan P.; LaMarche, Matthew J.; Chan, Ho Man
- Nature, Vol. 535, Issue 7610
Protein-tyrosine phosphatases and cancer
journal, April 2006
- Östman, Arne; Hellberg, Carina; Böhmer, Frank D.
- Nature Reviews Cancer, Vol. 6, Issue 4
The Chemistry and Bio-Medicinal Significance of Pyrimidines & Condensed Pyrimidines
journal, September 2016
- S. Jain, K.; Arya, N.; N. Inamdar, N.
- Current Topics in Medicinal Chemistry, Vol. 16, Issue 28
Somatic mutations in PTPN11 in juvenile myelomonocytic leukemia, myelodysplastic syndromes and acute myeloid leukemia
journal, April 2003
- Tartaglia, Marco; Niemeyer, Charlotte M.; Fragale, Alessandra
- Nature Genetics, Vol. 34, Issue 2
Structural and Evolutionary Relationships among Protein Tyrosine Phosphatase Domains
journal, November 2001
- Andersen, J. N.; Mortensen, O. H.; Peters, G. H.
- Molecular and Cellular Biology, Vol. 21, Issue 21
XDS
journal, January 2010
- Kabsch, Wolfgang
- Acta Crystallographica Section D Biological Crystallography, Vol. 66, Issue 2
Features and development of Coot
journal, March 2010
- Emsley, P.; Lohkamp, B.; Scott, W. G.
- Acta Crystallographica Section D Biological Crystallography, Vol. 66, Issue 4
Mutations in PTPN11, encoding the protein tyrosine phosphatase SHP-2, cause Noonan syndrome
journal, November 2001
- Tartaglia, Marco; Mehler, Ernest L.; Goldberg, Rosalie
- Nature Genetics, Vol. 29, Issue 4
Mutations of the BRAF gene in human cancer
journal, June 2002
- Davies, Helen; Bignell, Graham R.; Cox, Charles
- Nature, Vol. 417, Issue 6892
PTPN11 is the first identified proto-oncogene that encodes a tyrosine phosphatase
journal, October 2006
- Chan, Rebecca J.; Feng, Gen-Sheng
- Blood, Vol. 109, Issue 3
The tyrosine phosphatase Shp2 (PTPN11) in cancer
journal, February 2008
- Chan, Gordon; Kalaitzidis, Demetrios; Neel, Benjamin G.
- Cancer and Metastasis Reviews, Vol. 27, Issue 2
Structural, Functional, and Clinical Characterization of a Novel PTPN11 Mutation Cluster Underlying Noonan Syndrome: HUMAN MUTATION
journal, February 2017
- Pannone, Luca; Bocchinfuso, Gianfranco; Flex, Elisabetta
- Human Mutation, Vol. 38, Issue 4
Screensaver: an open source lab information management system (LIMS) for high throughput screening facilities
journal, May 2010
- Tolopko, Andrew N.; Sullivan, John P.; Erickson, Sean D.
- BMC Bioinformatics, Vol. 11, Issue 1
Exploiting structure similarity in refinement: automated NCS and target-structure restraints in BUSTER
journal, March 2012
- Smart, Oliver S.; Womack, Thomas O.; Flensburg, Claus
- Acta Crystallographica Section D Biological Crystallography, Vol. 68, Issue 4
Fiji: an open-source platform for biological-image analysis
journal, June 2012
- Schindelin, Johannes; Arganda-Carreras, Ignacio; Frise, Erwin
- Nature Methods, Vol. 9, Issue 7
Crystal Structure of the Tyrosine Phosphatase SHP-2
journal, February 1998
- Hof, Peter; Pluskey, Scott; Dhe-Paganon, Sirano
- Cell, Vol. 92, Issue 4