Hwan Geun Choi

Hwan Geun Choi

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Hwan Geun Choi

Hwan Geun Choi

Publications by authors named "Hwan Geun Choi"

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47Publications

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Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.

J Med Chem 2019 Oct 7. Epub 2019 Oct 7.

KU-KIST Graduate School of Converging Science and Technology , Korea University , 145 Anam-ro, Seongbuk-gu , Seoul 02841 , Republic of Korea.

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http://dx.doi.org/10.1021/acs.jmedchem.9b01025DOI Listing
October 2019

Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4).

J Biol Chem 2019 03 24;294(12):4511-4519. Epub 2019 Jan 24.

From the Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115,

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http://www.jbc.org/lookup/doi/10.1074/jbc.RA118.005428
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http://dx.doi.org/10.1074/jbc.RA118.005428DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6433055PMC
March 2019

Small-Molecule Inhibitors of LRRK2.

Adv Neurobiol 2017 ;14:241-264

Department of Cancer Biology, Dana Farber Cancer Institute, 450 Brookline Ave, Boston, MA, 02215, USA.

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http://dx.doi.org/10.1007/978-3-319-49969-7_13DOI Listing
September 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

First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.

J Med Chem 2018 09 11;61(18):8353-8373. Epub 2018 Sep 11.

KU-KIST Graduate School of Converging Science and Technology , Korea University , 145 Anam-ro, Seongbuk-gu , Seoul 02841 , Republic of Korea.

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http://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00882
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http://dx.doi.org/10.1021/acs.jmedchem.8b00882DOI Listing
September 2018

A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader.

Cell Chem Biol 2018 01 9;25(1):88-99.e6. Epub 2017 Nov 9.

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/S24519456173038
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http://dx.doi.org/10.1016/j.chembiol.2017.10.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6427047PMC
January 2018

Discovery of a potent dual ALK and EGFR T790M inhibitor.

Eur J Med Chem 2017 Aug 3;136:497-510. Epub 2017 May 3.

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

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http://dx.doi.org/10.1016/j.ejmech.2017.04.079DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5800871PMC
August 2017

Structural basis of mutant-selectivity and drug-resistance related to CO-1686.

Oncotarget 2017 Aug 21;8(32):53508-53517. Epub 2017 Jun 21.

Institute of Systems Biomedicine, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, China.

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http://dx.doi.org/10.18632/oncotarget.18588DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5581126PMC
August 2017

A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin.

Cell Rep 2017 06;19(11):2177-2184

Cutaneous Biology Research Center, Department of Dermatology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2017.05.042DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5549921PMC
June 2017

Identification of the First Selective Activin Receptor-Like Kinase 1 Inhibitor, a Reversible Version of L-783277.

J Med Chem 2017 02 6;60(4):1495-1508. Epub 2017 Feb 6.

KU-KIST Graduate School of Converging Science and Technology, Korea University , 145 Anam-ro, Seongbuk-gu, Seoul 02841, Republic of Korea.

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http://pubs.acs.org/doi/10.1021/acs.jmedchem.6b01679
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http://dx.doi.org/10.1021/acs.jmedchem.6b01679DOI Listing
February 2017

Covalent Guanosine Mimetic Inhibitors of G12C KRAS.

ACS Med Chem Lett 2017 Jan 30;8(1):61-66. Epub 2016 Nov 30.

Department of Cancer Biology, Dana Farber Cancer Institute, 450 Brookline Avenue, Boston, Massachusetts 02115, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02215, United States.

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http://pubs.acs.org/doi/10.1021/acsmedchemlett.6b00373
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http://dx.doi.org/10.1021/acsmedchemlett.6b00373DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5238463PMC
January 2017

Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase.

PLoS One 2015 5;10(6):e0128364. Epub 2015 Jun 5.

Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università di Napoli "Federico II", Naples, Italy; Istituto di Endocrinologia ed Oncologia Sperimentale del CNR, Naples, Italy.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0128364PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4457528PMC
March 2016

Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.

J Med Chem 2015 Dec 25;58(23):9296-9308. Epub 2015 Nov 25.

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

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http://dx.doi.org/10.1021/acs.jmedchem.5b01136DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4907642PMC
December 2015

EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors.

Clin Cancer Res 2015 Sep 6;21(17):3913-23. Epub 2015 May 6.

Lowe Center for Thoracic Oncology, Dana Farber Cancer Institute, Boston, Massachusetts. Department of Medical Oncology, Dana Farber Cancer Institute, Boston, Massachusetts. Belfer Institute for Applied Cancer Science, Dana Farber Cancer Institute, Boston, Massachusetts.

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http://dx.doi.org/10.1158/1078-0432.CCR-14-2789DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4791951PMC
September 2015

A Discovery Strategy for Selective Inhibitors of c-Src in Complex with the Focal Adhesion Kinase SH3/SH2-binding Region.

Chem Biol Drug Des 2015 Aug 28;86(2):144-55. Epub 2014 Nov 28.

Department of Microbiology and Molecular Genetics, University of Pittsburgh School of Medicine, 450 Technology Drive, Pittsburgh, PA, 15219, USA.

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http://dx.doi.org/10.1111/cbdd.12473DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4444405PMC
August 2015

Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor.

ACS Med Chem Lett 2015 May 7;6(5):584-9. Epub 2015 Apr 7.

Department of Cancer Biology, Dana-Farber Cancer Institute , Boston, Massachusetts 02115, United States ; Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School , 360 Longwood Avenue, Longwood Center LC-2209, Boston, Massachusetts 02115, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.5b00064DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4434483PMC
May 2015

EPHA2 is a mediator of vemurafenib resistance and a novel therapeutic target in melanoma.

Cancer Discov 2015 Mar 26;5(3):274-87. Epub 2014 Dec 26.

Wellman Center for Photomedicine, Massachusetts General Hospital, Boston, Massachusetts. Department of Dermatology, Harvard Medical School, Boston, Massachusetts. MGH Cancer Center, Massachusetts General Hospital, Boston, Massachusetts.

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http://dx.doi.org/10.1158/2159-8290.CD-14-0295DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4355085PMC
March 2015

Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.

Eur J Med Chem 2013 29;70:758-67. Epub 2013 Oct 29.

Department of Cancer Biology, Dana-Farber Cancer Institute, Harvard Medical School, 250 Longwood Ave, SGM 628, Boston, MA 02115, USA; Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 250 Longwood Ave, SGM 628, Boston, MA 02115, USA.

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http://dx.doi.org/10.1016/j.ejmech.2013.10.052DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3914206PMC
September 2014

Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor.

Angew Chem Int Ed Engl 2014 Jan 20;53(1):199-204. Epub 2013 Nov 20.

Department of Cancer Biology, Dana-Farber Cancer Institute, 450 Brookline Avenue, Boston, MA 02215 (USA); Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 250 Longwood Avenue, Boston, MA 02115 (USA); Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, MA 02138 (USA).

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http://ccc.chem.pitt.edu/wipf/Current%20Literature/Evan_3.pd
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http://doi.wiley.com/10.1002/anie.201307387
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http://dx.doi.org/10.1002/anie.201307387DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3914205PMC
January 2014

Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.

ACS Chem Biol 2013 Oct 13;8(10):2145-50. Epub 2013 Aug 13.

Cutaneous Biology Research Center, Massachusetts General Hospital and Harvard Medical School , Charlestown, Massachusetts 02129, United States.

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http://dx.doi.org/10.1021/cb400430tDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3800496PMC
October 2013

Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 - 2011).

Expert Opin Ther Pat 2012 Dec 6;22(12):1415-26. Epub 2012 Nov 6.

Xiamen University, School of Life Sciences, State Key Laboratory of Cellular Stress Biology, Fujian 361005, China.

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http://dx.doi.org/10.1517/13543776.2012.729041DOI Listing
December 2012

Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages.

Proc Natl Acad Sci U S A 2012 Oct 2;109(42):16986-91. Epub 2012 Oct 2.

Medical Research Council Protein Phosphorylation Unit, College of Life Sciences, Sir James Black Centre, University of Dundee, Dundee, DD1 5EH, United Kingdom.

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http://dx.doi.org/10.1073/pnas.1215450109DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3479463PMC
October 2012

Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.

Bioorg Med Chem Lett 2012 Aug 23;22(16):5297-302. Epub 2012 Jun 23.

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

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http://dx.doi.org/10.1016/j.bmcl.2012.06.036DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3415686PMC
August 2012

Brain Penetrant LRRK2 Inhibitor.

ACS Med Chem Lett 2012 Aug 18;3(8):658-662. Epub 2012 Jun 18.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA ; Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 250 Longwood Ave, SGM 628, Boston, MA 02115, USA.

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http://dx.doi.org/10.1021/ml300123aDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3467149PMC
August 2012

Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cells.

J Biol Chem 2012 Jun 16;287(23):19216-28. Epub 2012 Apr 16.

MRC Protein Phosphorylation Unit, The Sir James Black Centre, College of Life Sciences, University of Dundee, Scotland DD1 5EH, United Kingdom.

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http://dx.doi.org/10.1074/jbc.M112.345405DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3365954PMC
June 2012

Characterization of TAE684 as a potent LRRK2 kinase inhibitor.

Bioorg Med Chem Lett 2012 Mar 28;22(5):1864-9. Epub 2012 Jan 28.

MRC Protein Phosphorylation Unit, College of Life Sciences, University of Dundee, Dow Street, Dundee DD1 5EH, Scotland, United Kingdom.

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http://dx.doi.org/10.1016/j.bmcl.2012.01.084DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3433743PMC
March 2012

Discovery and characterization of novel mutant FLT3 kinase inhibitors.

Mol Cancer Ther 2010 Sep 31;9(9):2468-77. Epub 2010 Aug 31.

Department of Medical Oncology/Hematologic Neoplasia, Dana-Farber Cancer Institute, Boston, Massachusetts 02115, USA.

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http://dx.doi.org/10.1158/1535-7163.MCT-10-0232DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3967795PMC
September 2010

A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.

J Med Chem 2010 Aug;53(15):5439-48

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

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http://dx.doi.org/10.1021/jm901808wDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4134510PMC
August 2010

Novel diarylsulfonylurea derivatives as potent antimitotic agents.

Bioorg Med Chem Lett 2004 Dec;14(24):6075-8

LG Life Sciences, Ltd/R&D Park, 104-1 Moonji-dong, Yuseong-gu, Daejon 305-380, South Korea.

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http://dx.doi.org/10.1016/j.bmcl.2004.09.069DOI Listing
December 2004