Cai-Hong Yun

Cai-Hong Yun

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Cai-Hong Yun

Publications by authors named "Cai-Hong Yun"

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Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.

J Med Chem 2020 Mar 17;63(5):2114-2130. Epub 2019 Jun 17.

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), College of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China.

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http://dx.doi.org/10.1021/acs.jmedchem.9b00664DOI Listing
March 2020

Functional Characterization and Structural Basis of an Efficient Di--glycosyltransferase from .

J Am Chem Soc 2020 Feb 11;142(7):3506-3512. Epub 2020 Feb 11.

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences , Peking University , 38 Xueyuan Road , Beijing 100191 , China.

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http://dx.doi.org/10.1021/jacs.9b12211DOI Listing
February 2020

A non-covalent inhibitor XMU-MP-3 overrides ibrutinib-resistant Btk mutation in B-cell malignancies.

Br J Pharmacol 2019 Dec 9;176(23):4491-4509. Epub 2019 Dec 9.

State Key Laboratory of Cellular Stress Biology, Innovation Center for Cell Signaling Network, State-Province Joint Engineering Laboratory of Targeted Drugs from Natural Products, School of Life Science, Xiamen University, Xiamen, China.

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http://dx.doi.org/10.1111/bph.14809DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6932946PMC
December 2019

Molecular and Structural Characterization of a Promiscuous C-Glycosyltransferase from Trollius chinensis.

Angew Chem Int Ed Engl 2019 Aug 8;58(33):11513-11520. Epub 2019 Jul 8.

State Key Laboratory of Natural and Biomimetic Drugs & Key Laboratory of Molecular Cardiovascular Sciences of Ministry of Education, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing, 100191, China.

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http://doi.wiley.com/10.1002/anie.201905505
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http://dx.doi.org/10.1002/anie.201905505DOI Listing
August 2019

Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFR).

J Med Chem 2019 Aug 23;62(15):7302-7308. Epub 2019 Jul 23.

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy , Jinan University , 601 Huangpu Avenue West , Guangzhou 510632 , China.

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http://dx.doi.org/10.1021/acs.jmedchem.9b00576DOI Listing
August 2019

Discovery of JND3229 as a New EGFR Mutant Inhibitor with In Vivo Monodrug Efficacy.

ACS Med Chem Lett 2018 Nov 8;9(11):1123-1127. Epub 2018 Oct 8.

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China.

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http://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00373
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http://dx.doi.org/10.1021/acsmedchemlett.8b00373DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6231186PMC
November 2018

A Novel Microtubule Inhibitor Overcomes Multidrug Resistance in Tumors.

Cancer Res 2018 10 22;78(20):5949-5957. Epub 2018 Aug 22.

State Key Laboratory for Medical Genomics, Shanghai Institute of Hematology, Collaborative Innovation Center of Hematology, Collaborative Innovation Center of System Biology, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.

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http://dx.doi.org/10.1158/0008-5472.CAN-18-0455DOI Listing
October 2018

Crystal structures of pan-IDH inhibitor AG-881 in complex with mutant human IDH1 and IDH2.

Authors:
Rui Ma Cai-Hong Yun

Biochem Biophys Res Commun 2018 09 18;503(4):2912-2917. Epub 2018 Aug 18.

Department of Biophysics, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, China; Institute of Systems Biomedicine, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, China; Beijing Key Laboratory of Tumor Systems Biology, Peking University Health Science Center, Beijing 100191, China. Electronic address:

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http://dx.doi.org/10.1016/j.bbrc.2018.08.068DOI Listing
September 2018

Crystal structure of EGFR T790M/C797S/V948R in complex with EAI045.

Biochem Biophys Res Commun 2018 07;502(3):332-337

Department of Biophysics, School of Basic Medical Sciences, Peking University Health Science Center, Beijing, 100191, China; Institute of Systems Biomedicine, School of Basic Medical Sciences, Peking University Health Science Center, Beijing, 100191, China; Beijing Key Laboratory of Tumor Systems Biology, Peking University Health Science Center, Beijing, 100191, China. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S0006291X183122
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http://dx.doi.org/10.1016/j.bbrc.2018.05.154DOI Listing
July 2018

Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia.

Eur J Med Chem 2018 Apr 20;150:366-384. Epub 2018 Mar 20.

High Magnetic Field Laboratory, Chinese Academy of Sciences, Mailbox 1110, 350 Shushanhu Road, Hefei, Anhui, 230031, PR China; CHMFL-HCMTC Target Therapy Joint Laboratory, 350 Shushanhu Road, Hefei, Anhui, 230031, PR China; Hefei Science Center, Chinese Academy of Sciences, 350 Shushanhu Road, Hefei, 230031, Anhui, PR China. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2018.03.003DOI Listing
April 2018

Structural insights into drug development strategy targeting EGFR T790M/C797S.

Oncotarget 2018 Mar 10;9(17):13652-13665. Epub 2018 Jan 10.

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.24113DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5862605PMC
March 2018

Acetylation of 53BP1 dictates the DNA double strand break repair pathway.

Nucleic Acids Res 2018 01;46(2):689-703

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

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http://dx.doi.org/10.1093/nar/gkx1208DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5778472PMC
January 2018

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

Structural pharmacological studies on EGFR T790M/C797S.

Biochem Biophys Res Commun 2017 06 26;488(2):266-272. Epub 2017 Apr 26.

Institute of Systems Biomedicine, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, China; Department of Biophysics, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, China; Beijing Key Laboratory of Tumor Systems Biology, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, China. Electronic address:

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http://dx.doi.org/10.1016/j.bbrc.2017.04.138DOI Listing
June 2017

Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.

Eur J Med Chem 2017 May 2;131:107-125. Epub 2017 Mar 2.

High Magnetic Field Laboratory, Chinese Academy of Sciences, Mailbox 1110, 350 Shushanhu Road, Hefei, Anhui 230031, PR China; CHMFL-HCMTC Target Therapy Joint Laboratory, 350 Shushanhu Road, Hefei, Anhui 230031, PR China. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2017.03.001DOI Listing
May 2017

Structural and biochemical studies of the PDGFRA kinase domain.

Biochem Biophys Res Commun 2016 09 24;477(4):667-672. Epub 2016 Jun 24.

Institute of Systems Biomedicine, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, PR China; Department of Biophysics, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, PR China. Electronic address:

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http://dx.doi.org/10.1016/j.bbrc.2016.06.117DOI Listing
September 2016

Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration.

Sci Transl Med 2016 08;8(352):352ra108

State Key Laboratory of Cellular Stress Biology, Innovation Center for Cell Signaling Network, School of Life Sciences, Xiamen University, Xiamen, Fujian 361102, China. State-Province Joint Engineering Laboratory of Targeted Drugs from Natural Products, Xiamen University, Xiamen, Fujian 361102, China.

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http://stm.sciencemag.org/content/scitransmed/8/352/352ra108
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http://dx.doi.org/10.1126/scitranslmed.aaf2304DOI Listing
August 2016

Structure and function of human Naa60 (NatF), a Golgi-localized bi-functional acetyltransferase.

Sci Rep 2016 08 23;6:31425. Epub 2016 Aug 23.

Department of Biophysics, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, P. R. China.

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http://dx.doi.org/10.1038/srep31425DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4993997PMC
August 2016

Lack of Evidence that CYTH2/ARNO Functions as a Direct Intracellular EGFR Activator.

Cell 2016 May;165(5):1031-1034

Department of Research, Advanced Diagnostics and Technological Innovation, Regina Elena National Cancer Institute, via Chianesi 53, 00144, Rome, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2016.05.009DOI Listing
May 2016

EGF-receptor specificity for phosphotyrosine-primed substrates provides signal integration with Src.

Nat Struct Mol Biol 2015 Dec 9;22(12):983-90. Epub 2015 Nov 9.

Division of Signal Transduction, Beth Israel Deaconess Medical Center, Boston, Massachusetts, USA.

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http://dx.doi.org/10.1038/nsmb.3117DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4824005PMC
December 2015

Active-State Structures of a Small Heat-Shock Protein Revealed a Molecular Switch for Chaperone Function.

Structure 2015 Nov 1;23(11):2066-75. Epub 2015 Oct 1.

Institute of Systems Biomedicine, Department of Biophysics, Beijing Key Laboratory of Tumor Systems Biology and Center for Molecular and Translational Medicine, School of Basic Medical Sciences, Peking University Health Science Center, Beijing 100191, P.R. China. Electronic address:

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http://dx.doi.org/10.1016/j.str.2015.08.015DOI Listing
November 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

Cartilage oligomeric matrix protein is a natural inhibitor of thrombin.

Blood 2015 Aug 4;126(7):905-14. Epub 2015 Jun 4.

Department of Physiology and Pathophysiology, School of Basic Medical Sciences, Peking University, Peking, People's Republic of China; Key Laboratory of Molecular Cardiovascular Science, Ministry of Education, Beijing, People's Republic of China;

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http://dx.doi.org/10.1182/blood-2015-01-621292DOI Listing
August 2015

Structure-guided inhibitor design expands the scope of analog-sensitive kinase technology.

ACS Chem Biol 2013 Sep 23;8(9):1931-8. Epub 2013 Jul 23.

Howard Hughes Medical Institute and Department of Cellular & Molecular Pharmacology, University of California, San Francisco , San Francisco, California 94158, United States.

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http://dx.doi.org/10.1021/cb400376pDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3938192PMC
September 2013

Mechanism for activation of mutated epidermal growth factor receptors in lung cancer.

Proc Natl Acad Sci U S A 2013 Sep 9;110(38):E3595-604. Epub 2013 Sep 9.

Division of Hematology/Oncology, Department of Medicine, Vanderbilt University, Nashville, TN 37232.

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http://dx.doi.org/10.1073/pnas.1220050110DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3780914PMC
September 2013

Structural and mechanistic underpinnings of the differential drug sensitivity of EGFR mutations in non-small cell lung cancer.

Biochim Biophys Acta 2010 Mar 22;1804(3):559-66. Epub 2009 Dec 22.

Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School and Department of Cancer Biology, Dana-Farber Cancer Institute, 44 Binney Street, Boston, MA 02115, USA.

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http://linkinghub.elsevier.com/retrieve/pii/S157096390900368
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http://dx.doi.org/10.1016/j.bbapap.2009.12.010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2859716PMC
March 2010

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.

Proc Natl Acad Sci U S A 2008 Feb 28;105(6):2070-5. Epub 2008 Jan 28.

Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, 25 Shattuck Street, Boston, MA 02115, USA.

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http://dx.doi.org/10.1073/pnas.0709662105DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2538882PMC
February 2008

Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.

Nat Chem Biol 2007 Apr 4;3(4):229-38. Epub 2007 Mar 4.

Department of Chemistry, University of California, Berkeley, Berkeley, California 94720, USA.

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http://dx.doi.org/10.1038/nchembio866DOI Listing
April 2007

1.88 A crystal structure of the C domain of hCyP33: a novel domain of peptidyl-prolyl cis-trans isomerase.

Biochem Biophys Res Commun 2005 Aug;333(3):845-9

National Key Laboratory of Biomacromolecules, Institute of Biophysics, Chinese Academy of Sciences, 15 Datun Road, Chaoyang District, Beijing 100101, PR China.

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http://dx.doi.org/10.1016/j.bbrc.2005.06.006DOI Listing
August 2005

1.42A crystal structure of mini-IGF-1(2): an analysis of the disulfide isomerization property and receptor binding property of IGF-1 based on the three-dimensional structure.

Biochem Biophys Res Commun 2005 Jan;326(1):52-9

National Key Laboratory of Biomacromolecules, Institute of Biophysics, Chinese Academy of Sciences, 15 Datun Road, Chaoyang District, Beijing 100101, PR China.

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http://dx.doi.org/10.1016/j.bbrc.2004.10.203DOI Listing
January 2005

Structure of potato calmodulin PCM6: the first report of the three-dimensional structure of a plant calmodulin.

Acta Crystallogr D Biol Crystallogr 2004 Jul 22;60(Pt 7):1214-9. Epub 2004 Jun 22.

National Laboratory of Biomacromolecules, Institute of Biophysics, Chinese Academy of Sciences, Beijing 100101, People's Republic of China.

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http://dx.doi.org/10.1107/S0907444904009771DOI Listing
July 2004