Publications by authors named "Nicholas Kwiatkowski"

48Publications

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

J Med Chem 2020 Jul 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 Aug 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

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

Identification of small molecule inhibitors targeting the Zika virus envelope protein.

Antiviral Res 2019 04 13;164:147-153. Epub 2019 Feb 13.

Department of Microbiology and Blavatnik Institute, Harvard Medical School, 77 Avenue Louis Pasteur, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.antiviral.2019.02.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6675404PMC
April 2019

Small Molecules Targeting the Flavivirus E Protein with Broad-Spectrum Activity and Antiviral Efficacy in Vivo.

ACS Infect Dis 2019 03 14;5(3):460-472. Epub 2019 Jan 14.

Department of Microbiology, Blavatnik Institute , Harvard Medical School , 77 Avenue Louis Pasteur , Boston , Massachusetts 02115 , United States.

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http://dx.doi.org/10.1021/acsinfecdis.8b00322DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6548335PMC
March 2019

Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein.

ACS Infect Dis 2018 09 29;4(9):1395-1406. Epub 2018 Aug 29.

Department of Microbiology and Immunobiology , Harvard Medical School , 77 Avenue Louis Pasteur , Boston , Massachusetts 02115 , United States.

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http://pubs.acs.org/doi/10.1021/acsinfecdis.8b00127
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http://dx.doi.org/10.1021/acsinfecdis.8b00127DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6392429PMC
September 2018

Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8.

ACS Med Chem Lett 2018 Jun 18;9(6):540-545. Epub 2018 Mar 18.

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

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https://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00011
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http://dx.doi.org/10.1021/acsmedchemlett.8b00011DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6004574PMC
June 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

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

Tivantinib (ARQ 197) efficacy is independent of MET inhibition in non-small-cell lung cancer cell lines.

Mol Oncol 2015 Jan 29;9(1):260-9. Epub 2014 Aug 29.

Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Medicine, Brigham and Women's Hospital and Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.molonc.2014.08.011DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5528687PMC
January 2015

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

Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.

ACS Chem Biol 2012 Jan 21;7(1):185-96. Epub 2011 Oct 21.

Department of Cancer Biology, Dana Farber Cancer Institute, Harvard Medical School, Boston, Massachusetts 02115, United States.

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http://pubs.acs.org/doi/10.1021/cb200305u
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http://dx.doi.org/10.1021/cb200305uDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3262907PMC
January 2012

Cut homeobox 1 causes chromosomal instability by promoting bipolar division after cytokinesis failure.

Proc Natl Acad Sci U S A 2011 Feb 18;108(5):1949-54. Epub 2011 Jan 18.

Department of Biochemistry Oncology, and Medicine, McGill University, Rosalind and Morris Goodman Cancer Research Centre, Montreal, QC, Canada.

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http://www.pnas.org/lookup/doi/10.1073/pnas.1008403108
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http://dx.doi.org/10.1073/pnas.1008403108DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3033318PMC
February 2011

Release of Mps1 from kinetochores is crucial for timely anaphase onset.

J Cell Biol 2010 Oct 11;191(2):281-90. Epub 2010 Oct 11.

Department of Physiological Chemistry and Cancer Genomics Centre, UMC Utrecht, 3584 CG, Utrecht, Netherlands.

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http://dx.doi.org/10.1083/jcb.201003038DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2958484PMC
October 2010

Structural origin of selectivity in class II-selective histone deacetylase inhibitors.

J Med Chem 2008 May 16;51(10):2898-906. Epub 2008 Apr 16.

Walther Cancer Research Center, Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556-5670, USA.

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http://dx.doi.org/10.1021/jm7015254DOI Listing
May 2008

Discovery of selective aminothiazole aurora kinase inhibitors.

ACS Chem Biol 2008 Mar 29;3(3):180-92. Epub 2008 Feb 29.

Department of Biological Chemistry, Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, California 92121, USA.

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http://graylab.dfci.harvard.edu/assets/files/publication%20p
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http://pubs.acs.org/doi/abs/10.1021/cb700200w
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http://dx.doi.org/10.1021/cb700200wDOI Listing
March 2008

MT FdR: a ferredoxin reductase from M. tuberculosis that couples to MT CYP51.

Biochim Biophys Acta 2005 Apr-May;1707(2-3):157-69. Epub 2004 Dec 15.

Department of Biology, Trinity College, 300 Summit Street Hartford, CT 06106, United States.

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http://dx.doi.org/10.1016/j.bbabio.2004.11.010DOI Listing
July 2005