Publications by authors named "Tinghu Zhang"

63Publications

Discovery of Covalent MKK4/7 Dual Inhibitor.

Cell Chem Biol 2020 Sep 7. Epub 2020 Sep 7.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02215, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2020.08.014DOI Listing
September 2020

Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library.

ACS Chem Biol 2020 10 28;15(10):2722-2730. Epub 2020 Sep 28.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States.

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http://dx.doi.org/10.1021/acschembio.0c00520DOI Listing
October 2020

Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface.

ACS Med Chem Lett 2020 Jun 3;11(6):1269-1273. Epub 2020 Apr 3.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02115, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.0c00111DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7294706PMC
June 2020

Structure and Characterization of a Covalent Inhibitor of Src Kinase.

Front Mol Biosci 2020 19;7:81. Epub 2020 May 19.

Departments of Biochemistry and Radiation Oncology, The University of Texas Southwestern Medical Center at Dallas, Dallas, TX, United States.

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http://dx.doi.org/10.3389/fmolb.2020.00081DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7248381PMC
May 2020

Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.

J Med Chem 2020 07 25;63(13):6708-6726. Epub 2020 Jun 25.

Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.9b01929DOI Listing
July 2020

Development of CDK2 and CDK5 Dual Degrader TMX-2172.

Angew Chem Int Ed Engl 2020 08 3;59(33):13865-13870. Epub 2020 Jun 3.

Department of Cancer Biology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.

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http://dx.doi.org/10.1002/anie.202004087DOI Listing
August 2020

Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors.

Cell Chem Biol 2020 05 3;27(5):525-537.e6. Epub 2020 Mar 3.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2020.02.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7286548PMC
May 2020

Light-induced control of protein destruction by opto-PROTAC.

Sci Adv 2020 02 21;6(8):eaay5154. Epub 2020 Feb 21.

Department of Pathology, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02215, USA.

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http://dx.doi.org/10.1126/sciadv.aay5154DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7034987PMC
February 2020

A Quantitative Tissue-Specific Landscape of Protein Redox Regulation during Aging.

Cell 2020 03 27;180(5):968-983.e24. Epub 2020 Feb 27.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA; Department of Cell Biology, Harvard Medical School, Boston, MA, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2020.02.012DOI Listing
March 2020

Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.

J Med Chem 2020 02 30;63(4):1624-1641. Epub 2020 Jan 30.

Department of Biological Chemistry and Molecular Pharmacology , Harvard Medical School , Boston , Massachusetts 02115 , United States.

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http://dx.doi.org/10.1021/acs.jmedchem.9b01502DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7493195PMC
February 2020

Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation.

Cell Chem Biol 2019 11 17;26(11):1486-1500. Epub 2019 Oct 17.

Department of Cancer Biology, Dana-Farber Cancer Institute, 450 Brookline Avenue, Boston, MA 02215, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2019.09.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6886688PMC
November 2019

Tumors with TSC mutations are sensitive to CDK7 inhibition through NRF2 and glutathione depletion.

J Exp Med 2019 11 10;216(11):2635-2652. Epub 2019 Sep 10.

Cancer Genetics Laboratory, Pulmonary and Critical Care Medicine, Department of Medicine, Brigham and Women's Hospital and Harvard Medical School, Boston, MA

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http://dx.doi.org/10.1084/jem.20190251DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6829598PMC
November 2019

JNK2 Is Required for the Tumorigenic Properties of Melanoma Cells.

ACS Chem Biol 2019 07 17;14(7):1426-1435. Epub 2019 May 17.

Department of Translational Molecular Pathology , The University of Texas M. D. Anderson Cancer Center , Houston , Texas 77030 , United States.

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http://dx.doi.org/10.1021/acschembio.9b00083DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7181303PMC
July 2019

Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype.

Cell Chem Biol 2019 06 21;26(6):792-803.e10. Epub 2019 Mar 21.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biology Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02215, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2019.02.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6588464PMC
June 2019

Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6.

Angew Chem Int Ed Engl 2019 05 29;58(19):6321-6326. Epub 2019 Mar 29.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.

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http://dx.doi.org/10.1002/anie.201901336DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7678623PMC
May 2019

Broad-spectrum antiviral JL122 blocks infection and inhibits transmission of aquatic rhabdoviruses.

Virology 2018 12 1;525:143-149. Epub 2018 Oct 1.

Department of Microbiology and Immunology, College of Veterinary Medicine, Cornell University, Ithaca, NY 14853, USA. Electronic address:

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http://dx.doi.org/10.1016/j.virol.2018.09.009DOI Listing
December 2018

Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors.

J Med Chem 2018 09 23;61(17):7560-7572. Epub 2018 Aug 23.

The Norwegian Structural Biology Centre, Department of Chemistry , UiT The Arctic University of Norway , N-9037 Tromsø , Norway.

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http://dx.doi.org/10.1021/acs.jmedchem.7b01847DOI Listing
September 2018

SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform.

Cell Chem Biol 2018 04 22;25(4):460-470.e6. Epub 2018 Feb 22.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S24519456183003
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http://dx.doi.org/10.1016/j.chembiol.2018.01.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5973797PMC
April 2018

Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR1 Activating Mutations.

Cancer Cell 2018 02;33(2):173-186.e5

Center for Functional Cancer Epigenetics, Dana Farber Cancer Institute, Boston, MA 02210, USA; Department of Medical Oncology, Dana Farber Cancer Institute, Boston, MA 02210, USA; Department of Medicine, Brigham and Women's Hospital and Harvard Medical School, Boston, MA 02210, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2018.01.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5813700PMC
February 2018

High MITF Expression Is Associated with Super-Enhancers and Suppressed by CDK7 Inhibition in Melanoma.

J Invest Dermatol 2018 07 8;138(7):1582-1590. Epub 2018 Feb 8.

Wellman Center for Photomedicine and Department of Dermatology, Massachusetts General Hospital, Harvard Medical School, Boston, Massachusetts, USA. Electronic address:

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http://dx.doi.org/10.1016/j.jid.2017.09.056DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6019629PMC
July 2018

EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma.

Cancer Cell 2018 02 18;33(2):202-216.e6. Epub 2018 Jan 18.

Department of Pediatric Oncology, Dana-Farber Cancer Institute and Boston Children's Hospital, Harvard Medical School, 450 Brookline Avenue, Boston, MA 02215, USA; The Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S15356108173056
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http://dx.doi.org/10.1016/j.ccell.2017.12.009DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5846483PMC
February 2018

Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors.

Cell Chem Biol 2018 02 21;25(2):135-142.e5. Epub 2017 Dec 21.

Department of Pediatric Oncology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Pediatrics, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2017.11.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6389506PMC
February 2018

The mechanism of activation of IRAK1 and IRAK4 by interleukin-1 and Toll-like receptor agonists.

Biochem J 2017 06 6;474(12):2027-2038. Epub 2017 Jun 6.

MRC Protein Phosphorylation and Ubiquitylation Unit, Sir James Black Centre, University of Dundee, Dundee DD1 5EH, U.K.

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http://dx.doi.org/10.1042/BCJ20170097DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5460469PMC
June 2017

Discovery of a Series of 5,11-Dihydro-6-benzo[]pyrimido[5,4-][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors.

ACS Med Chem Lett 2016 Oct 2;7(10):908-912. Epub 2016 Aug 2.

Department of Cancer Biology, Dana-Farber Cancer Institute , Boston, Massachusetts 02215, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.6b00209DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5066161PMC
October 2016

Inhibition of IKKα by BAY61-3606 Reveals IKKα-Dependent Histone H3 Phosphorylation in Human Cytomegalovirus Infected Cells.

PLoS One 2016 1;11(3):e0150339. Epub 2016 Mar 1.

Institute of Infection & Immunity, St George's, University of London, Cranmer Terrace, London, SW17 0RE, United Kingdom.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0150339PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4773098PMC
July 2016

YAP Drives Growth by Controlling Transcriptional Pause Release from Dynamic Enhancers.

Mol Cell 2015 Oct 1;60(2):328-37. Epub 2015 Oct 1.

Stem Cell Program, Boston Children's Hospital, Boston, MA 02115, USA; Department of Stem Cell and Regenerative Biology, Harvard University, Cambridge, MA 02138, USA; Harvard Stem Cell Institute, Boston, MA 02115, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S10972765150069
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http://dx.doi.org/10.1016/j.molcel.2015.09.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4624327PMC
October 2015

CDK7-dependent transcriptional addiction in triple-negative breast cancer.

Cell 2015 Sep;163(1):174-86

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2015.08.063DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4583659PMC
September 2015

CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer.

Cell 2014 Nov 6;159(5):1126-1139. Epub 2014 Nov 6.

Department of Pediatric Hematology/Oncology, Dana-Farber Cancer Institute and Boston Children's Hospital, Boston, MA 02215, USA; Department of Pediatrics, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2014.10.024DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4243043PMC
November 2014

Targeting transcription regulation in cancer with a covalent CDK7 inhibitor.

Nature 2014 Jul 22;511(7511):616-20. Epub 2014 Jun 22.

1] Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02115, USA [2] Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115, USA.

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http://dx.doi.org/10.1038/nature13393DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4244910PMC
July 2014

Developing irreversible inhibitors of the protein kinase cysteinome.

Chem Biol 2013 Feb;20(2):146-59

Department of Cancer Biology, Dana-Farber Cancer Institute, 450 Brookline Avenue, Boston, MA 02115, USA.

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http://linkinghub.elsevier.com/retrieve/pii/S107455211200487
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http://dx.doi.org/10.1016/j.chembiol.2012.12.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3583020PMC
February 2013

BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner.

PLoS One 2012 18;7(7):e41343. Epub 2012 Jul 18.

Molecular Pathology Unit, Center for Cancer Research, Massachusetts General Hospital, Charlestown, Massachusetts, United States of America.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0041343PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3399817PMC
January 2013

Deficiency and inhibition of cathepsin K reduce body weight gain and increase glucose metabolism in mice.

Arterioscler Thromb Vasc Biol 2008 Dec 25;28(12):2202-8. Epub 2008 Sep 25.

Department of Medicine, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA.

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http://dx.doi.org/10.1161/ATVBAHA.108.172320DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2736686PMC
December 2008