Faculty Directory
- Name
- Byung Il LEE, Ph.D.(adjunct professor)
- Faculty Appointment
(title, department)
- Professor, Department of Cancer Biomedical Science, Chief Scientist, Division of Technology Convergence
- Area of Expertise
- Structural biology, Biochemistry, AI-based de novo Protein Design, Structure Based Drug Discovery
- E-mail
- bilee@ncc.re.kr
- Work Experience
- Chief Scientist, National Cancer Center Korea (2016~ Present)
Principal Investigator, National Cancer Center Korea (2007~ Present)
Research Fellow, Dana-Farber Cancer Institute & Harvard Medical School, Boston, MA, USA (2005~2007)
- Educational Background
- 1994-1998, BS, Chemistry, Seoul National University
1998-2000, MS, Chemistry (Biochemistry), Seoul National University
2000-2004, Ph.D., Chemistry (Biochemistry), Seoul National University
- Research Interests
- My research focuses on the three-dimensional structures (X-ray crystallography and cryo-electron microscopy) and functions of cancer-related proteins, as well as structure-based drug discovery. More recently, his work has expanded to include the de novo design and development of therapeutic artificial proteins using artificial intelligence (AI).
- Achievements
- 2026 SCI-E Transglutaminase 2 exacerbates ovarian cancer survival by directly inactivating GSK3β: Cell Death Dis. 17(1):199 (9.6)
2025 SCI-E Narciclasine as a potential therapeutic agent to overcome EGFR-TKI resistance in non-small cell lung cancer: Journal of Translational Medicine. 23(1):1380 (7.5)
2025 SCI-E Crystal structure of Fis1 and Bap31 provides information on protein-protein interactions at mitochondria-associated ER membranes: Communications Biology. 8:1161. (5.1)
2025 SCI-E Structural analysis of EPOP BC-box binding to the elongin BC complex: Biochemical and Biophysical Research Communications. 759:151691 (2.2)
2025 SCI-E ER-mitochondria contacts mediate lipid radical transfer via RMDN3/PTPIP51 phosphorylation to reduce mitochondrial oxidative stress: Nature Communications. 16:1508 (15.7)
2025 SCI-E Identification of novel 7-hydroxycoumarin derivatives as ELOC binders with potential to modulate CRL2 complex formation: Scientific Reports. 15(1):3622 (3.9)
2025 SCI-E Two Cysteines in Raf Kinase Inhibitor Protein Make Differential Contributions to Structural Dynamics In Vitro: Molecules. 30(2):384 (4.6)
2024 SCI-E Comparative crystal structure analysis of the human EP300 and CBP KIX domains: Biochemical and Biophysical Research Communications. 741:151064 (2.5)
2024 SCI-E Activatable near-infrared fluorescence probe for real-time imaging of PD-L1 expression in tumors: Journal of Materials Chemistry B. 12(42):10877~10885 (6.1)
2023 SCI-E Crystal structure of [1,2,4]triazolo[4,3-b]pyridazine derivatives as BRD4 bromodomain inhibitors and structure-activity relationship study: Scientific Reports. 13(1):10805 (4.6)
2022 SCI-E BMS794833 inhibits macrophage efferocytosis by directly binding to MERTK and inhibiting its activity: Experimental and Molecular Medicine. 54(9):1450~1460 (12.172)
2022 SCI-E Discovery of BET specific bromodomain inhibitors with a novel scaffold: Bioorganic & Medicinal Chemistry. 72:116967 (3.461)
2022 SCI-E The structure of Deinococcus radiodurans transcriptional regulator HucR retold with the urate bound: Biochemical and Biophysical Research Communications. 615:63~69 (3.322)
2021 SCI-E Phosphorylation of OGFOD1 by Cell Cycle-Dependent Kinase 7/9 Enhances the Transcriptional Activity of RNA Polymerase II in Breast Cancer Cells: Cancers. 13(14):3418 (6.639)
2021 SCI-E Phospholipid transfer function of PTPIP51 at mitochondria-associated ER membranes: EMBO Reports. :e51323 (8.807)
2021 SCI-E Synthesis and Structure-Activity Relationships of Aristoyagonine Derivatives as Brd4 Bromodomain Inhibitors with X-ray Co-Crystal Research: Molecules. 26(6):1686 (4.412)
2020 SCI-E Crystal Structure of the Kinase Domain of MerTK in Complex with AZD7762 Provides Clues for Structure-Based Drug Development: International Journal of Molecular Sciences. 21(21):7878 (4.556)
2020 SCI-E Phosphorylation of OCT4 Serine 236 Inhibits Germ Cell Tumor Growth by Inducing Differentiation: Cancers. 12(9):E2601 (6.126)
2020 SCI Regulation of mRNA export through API5 and nuclear FGF2 interaction. Nucleic Acids Res. Online published (11.147)
2019 SCI-E Gossypol Suppresses Growth of Temozolomide-Resistant Glioblastoma Tumor Spheres. Biomolecules. 10;9(10). (4.694)
2019 SCI-E Zwitterionic near-infrared fluorophore-conjugated epidermal growth factor for fast, real-time, and target-cell-specific cancer imaging. Theranostics. 9(4):1085-1095. (8.063)
2019 SCI A NCAPG2-Derived Phosphopeptide Selectively Binds to the Polo-Box Domain of PLK1 and Inhibits Cancer Cell Proliferation. Int J Pept Res Ther 25:1397-1403. (1.219)
2018 SCI Farnesyl diphosphate synthase is important for the maintenance of glioblastoma stemness. Exp Mol Med. 50(10):1-12. (5.584)
2018 Crystallization and preliminary X-ray analysis of API5-FGF2 complex: BioDesign. 6(4):92~95.
2018 SCI Crystal Structures of Spleen Tyrosine Kinase in Complex with Two Novel 4-Aminopyrido[4,3-d] Pyrimidine Derivative Inhibitors. Mol Cells.41(6):545-552. (3.533)
2017 SCI Sporadic Early-onset Diffuse Gastric Cancers Have High Frequency of Somatic CDH1 Alterations but Low Frequency of Somatic RHOA Mutations Compared with Late-onset Cancers: Gastroenterology. 153(2):536~549 (18.392)
2017 SCI-E Daurinol blocks breast and lung cancer metastasis and development by inhibition of focal adhesion kinase (FAK): Oncotarget. 8(34):57058~57071 (5.168)
2017 SCI Apoptosis inhibitor 5 is an endogenous inhibitor of caspase-2.: EMBO reports. 18(5):733~744 (8.568)
2017 SCI-E Antigen-responsive molecular sensor enables real-time tumor-specific imaging: Theranostics. 7(4):952~961 (8.712)
2017 SCI-E API5 confers cancer stem cell-like properties through the FGF2-NANOG axis: Oncogenesis. 6(1):e285~e285 (4.143)
2016 SCI-E Oncogenic function and clinical implications of SLC3A2-NRG1 fusion in invasive mucinous adenocarcinoma of the lung: Oncotarget. 7(43):69450~69465 (5.008)
2016 SCI Crystal structures of spleen tyrosine kinase in complex with novel inhibitors: structural insights for design of anticancer drugs: FEBS Journal. 283(19):3613~3625 (4.237)
2016 SCI-E Clinically Significant Unclassified Variants in BRCA1 and BRCA2 Genes Among Korean Breast Cancer Patients: Cancer Research and Treatment. Online:Published (4.245)
2016 SCI-E Crystal Structure of Human Myotubularin-Related Protein 1 Provides Insight into the Structural Basis of Substrate Specificity.: PLoS One. 11:e0152611~e0152611 (3.057)
2015 SCI Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors: Bioorganic & Medicinal Chemistry Letters. 25:4441~4446 (2.42)
2015 SCI The Cell Shape-determining Csd6 Protein from Helicobacter pylori Constitutes a New Family of l,d-Carboxypeptidase.: The Journal of biological chemistry. 290:25103~25117 (4.573)
2015 SCI Structural and biochemical insights into the role of testis-expressed gene 14 (TEX14) in forming the stable intercellular bridges of germ cells: Proceedings of the National Academy of Sciences of the USA. 112:12372~12377 (9.674)
2015 기타 Recombinant Human Laforin Expressed in Insect Cells: Expression, Purification, and Biochemical Characterizations: Journal of the Korean Chemical Society. 59:466~470 (0)
2015 SCI Structure and mechanism of activity-based inhibition of the EGF receptor by Mig6: Nature Structural & Molecular Biology. 22:703~711 (13.309)
2015 SCI-E Crystallization and preliminary X-ray crystallographic analysis of human myotubularin-related protein 1: Acta crystallographica. Section F, Structural biology communications. 71(Pt3):261~265 (0.527)
2015 기타 Crystal structure of a class 2 D-xylose isomerase from the human intestinal tract microbe Bacteroides thetaiotaomicron: BioDesign. 3:41~47 (0)
2015 SCI Structure of Csd3 from Helicobacter pylori, a cell shape-determining metallopeptidase: Acta crystallographica. Section D, Biological crystallography. 71(Pt3):675~686 (2.674)
2014 SCI Structural basis for the recognition of muramyltripeptide by Helicobacter pylori Csd4, a D,L-carboxypeptidase controlling the helical cell shape: Acta crystallographica. Section D, Biological crystallography. 70(pt11):2800~2812 (7.232)
2014 SCI-E Overproduction, crystallization and preliminary X-ray crystallographic analysis of Escherichia coli tRNA N(6)-threonylcarbamoyladenosine dehydratase: Acta crystallographica. Section F, Structural biology communications. 70(Pt11):1517~1520 (0.568)
2014 SCI The condensin component NCAPG2 regulates microtubule-kinetochore attachment through recruitment of Polo-like kinase 1 to kinetochores.: Nature Communications. 5:4588~4588 (10.742)
2014 SCI Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors: Organic and biomolecular chemistry. 12(27):4932~4940 (3.487)
2013 SCI Identification of Potent Inhibitors against Human Peptide Deformylase as Anticancer Agents: Bulletin of the Korean Chemical Society. 34:3885~3887 (0.982)
2013 SCI-E Overexpression, crystallization and preliminary X-ray crystallographic analysis of a putative xylose isomerase from Bacteroides thetaiotaomicron: Acta Crystallographica Section F: Structural Biology and Crystallization Communications. F69:1127~1130 (0.552)
2013 SCI-E Crystal Structure of Pim1 Kinase in Complex with a Pyrido[4,3-D]Pyrimidine Derivative Suggests a Unique Binding Mode: PLoS One. 8(7):e70358~e70358 (3.73)
2012 SCI Structures of Staphylococcus aureus peptide deformylase in complex with two classes of new inhibitors: Acta Crystallographica Section D: Biological Crystallography. 68(7):784~793 (12.619)
2012 SCI Crystal structure of Pyrococcus furiosus PF2050, a member of the DUF2666 protein family: FEBS Letters. 586(9):1384~1388 (3.538)
2012 SCI Helical Repeat Structure of Apoptosis Inhibitor 5 Reveals Protein-Protein Interaction Modules: JOURNAL OF BIOLOGICAL CHEMISTRY. 287(14):10727~10737 (4.773)
2012 SCI Direct characterization of protein oligomers and their quaternary structures by single-molecule FRET: Chemical Communications. 48(8):1138~1140 (6.169)
2011 SCI Quantitative measurement of anti-aquaporin-4 antibodies by enzyme-linked immunosorbent assay using purified recombinant human aquaporin-4: Multiple Sclerosis. 18(5):578~586 (4.255)
2011 SCI Cancer cells promote survival through depletion of the von Hippel Lindau tumor suppressor by protein crosslinking: Oncogene. 30(48):4780~4790 (7.414)
2011 SCI Crystal structures of Pseudomonas aeruginosa guanidinobutyrase and guanidinopropionase, members of the ureohydrolase superfamily: Journal of Structural Biology. 175:329~338 (3.5)
2011 SCI-E Overexpression, crystallization and preliminary X-ray crystallographic analysis of Pyrococcus furiosus PF2050, a member of the DUF2666 protein family: Acta Crystallographica Section F. 67(Pt8):930~932 (0.563)
2011 SCI Crystal structure of the catalytic domain of cholesterol-a-glucosyltransferase from Helicobacter pylori: PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS. 79(7):2321~2326 (2.813)
2011 SCI Pyrogallin, an ATP-Competitive Inhibitor of JAK3: Bulletin of the Korean Chemical Society. 32:1077~1079 (0.871)
2010 SCI Helicobacter pylori proinflammatory protein upregulates NF-κB as a cell-translocating Ser/Thr kinase: Proceedings of the National Academy of Sciences USA (PNAS). 107(50):21418~21423 (9.432)
2010 SCI I-kappaBalpha depletion by transglutaminase 2 and mu-calpain occurs in parallel with the ubiquitin-proteasome pathway: Biochemical and biophysical research communications. 399(2):300~306 (2.548)
2010 SCI Crystal structure of human transglutaminase 2 in complex with adenosine triphosphate: International journal of biological macromolecules. ;47(2):190~195 (2.366)
2010 SCI Refined Structure of Human NM23-H1 from a Hexagonal Crystal: Bulletin of the Koeran Chemical Society. 31:1397~1399 (0.936)
2010 SCI Expression, purification and biochemical characterization of the N-terminal regions of human TIG3 and HRASLS3 proteins.: Protein Expression and Purification. 71(1):103~107 (1.563)
2010 SCI-E Antinociceptive effects of Alpinia katsumadai via cyclooxygenase-2 inhibition: Biomolecules & Therapeutics. 18:159~165 (0.292)
2010 SCI The mechanism of transglutaminase 2 inhibition with glucosamine: implications of a possible anti-inflammatory effect through transglutaminase inhibition: Journal of Cancer Research and Clinical Oncology. 136(1):143~150 (2.261)
2009 SCI Crystal Structure of the TNF-α-Inducing Protein (Tipα) from Helicobacter pylori: Insights into Its DNA-Binding Activity: J Mol Biol.. 392(1):191~197 (4.146)
2009 SCI Depletion of nucleophosmin via transglutaminase 2 cross-linking increases drug resistance in cancer cells: Cancer Letters. 274:201~207 (3.504)
2008 SCI Molecular modeling and biochemical studies of transglutaminase 2 mutation found in patients with early-onset type 2 diabetes: Bulletin of the Korean Chemical Society. 29:1797~1799 (1.156)
2007 SCI Crystal structure of human nucleophosmin-core reveals plasticity of the pentamer-pentamer interface: Proteins. 69:672~678 ()
2006 SCI Crystal structure of PilF: functional implication in the type 4 pilus biogenesis in Pseudomonas aeruginosa: Biochem Biophys Res Commun. 340:1028~1038 ()
2005 SCI Crystallization and preliminary X-ray crystallographic analysis of UDP-N-acetylglucosamine enolpyruvyl transferase from Haemophilus influenzae in complex with UDP-N-acetylglucosamine and fosfomycin: Mol Cells. 19:398~401 ()
2004 SCI Crystal Structure of the Schiff Base Intermediate Prior to Decarboxylation in the Catalytic Cycle of Aspartate α-Decarboxylase: J. Mol. Biol.. 340:1~7 (5.229)
2004 SCI Ring-shaped architecture of RecR: Implications for its role in homologous recombinational DNA repair: EMBO J.. 23:2029~2038 (10.053)
2004 SCI Crystallization and preliminary X-ray crystallographic analysis of nicotinic acid mononucleotide adenylyltransferase from Pseudomonas aeruginosa.: Acta Crystallogr. D. 60:948~949 (1.401)
2004 SCI Crystal structure of chorismate synthase complex with FMN: A novel fold and functional insights: J. Mol. Biol.. 336:904~915 (5.229)
2004 SCI Crystallization and preliminary X-ray crystallographic analysis of recombinational DNA repair protein RecR from Deinoccus radiodurans: Acta Crystallogr. D. 60:379~381 (1.401)
2004 SCI Crystal structure of ß-D-xylosidase from Thermoanaerobacterium saccharolyticum, a family 39 glycoside hydrolase: J. Mol. Biol.. 335:155~165 (5.229)
2003 SCI Crystal structure of the UDP-N-acetylglucosamine acyltransferase from Helicobacter pylori: Proteins. 53:772~774 (4.684)
2003 SCI Crystal structure of tRNA(m(1)G37)methyltransferase: insights into tRNA recognition: EMBO J.. 22:2593~2603 (10.053)
2003 SCI Crystal structure of the type II 3-dehydroquinase from Helicobacter pylori: Proteins. 51:616~617 (4.684)
2003 SCI Crystal structure of class I acetohydroxy Acid isomeroreductase from Pseudomonas aeruginosa: J. Mol. Biol.. 328:505~515 (5.229)
2003 SCI Crystallization and preliminary X-ray crystallographic studies of chorismate synthase from Helicobacter pylori: Acta Crystallogr. D. 328:505~515 (1.401)
2003 SCI The TB structural genomics consortium: a resource for Mycobacterium tuberculosis biology: Tuberculosis. 83:223~249 (3.899)
2002 SCI Crystallization and preliminary X-ray crystallographic analysis of acetohydroxy acid isomeroreductase from Pseudomonas aeruginosa: Acta Crystallogr. D. 58:2145~2146 (1.401)
2002 SCI Crystallization and preliminary X-ray crystallographic analysis of peptide deformylase from Pseudomonas aeruginosa: Acta Crystallogr. D. 58:1874~1875 (1.401)
2002 SCI Crystallization and preliminary X-ray crystallographic analysis of enoyl-acyl carrier protein reductase from from Helicobacter pylori: Acta Crystallgr. D. 58:1071~1073 (1.401)
2002 SCI Crystallization and preliminary X-ray crystallographic analysis of UDP-N-acetyl glucosamine acyltransferase from Helicobacter pylori: Acta Crystallgr. D. 58:864~866 (1.401)
2002 SCI Crystallization and preliminary X-ray crystallographic analysis of Aspartate 1-decarboxylase from from Helicobacter pylori: Acta Crystallgr. D. 58:861~863 (1.401)
2002 SCI Crystallization and preliminary X-ray crystallographic analysis of ß-xylosidase from Thermoanaerobacterium saccharolyticum, a?thermophilic anaerobe: Acta Crystallgr. D. 58:531~532 (1.401)
2002 SCI Crystallization and preliminary X-ray crystallographic analysis of the Rv2002 gene product from Mycobacterium tuberculosis, a ß-ketoacyl?carrier protein reductase homologue: Acta Crystallgr. D. 58:303~305 (1.401)
2001 SCI Crystallization and preliminary X-ray crystallographic analysis of deoxyuridine triphosphate nucleotidohydrolase from Saccharomyces cerevisiae: Acta Crystallogr. D. 57:1147~1149 (1.401)
2001 SCI Crystal structure of the MJ0490 gene product of the hyperthermophilic archaebacterium Methanococcus jannaschii,a novel member of lactate/malate family of dehydrogenases: J. Mol. Biol.. 307:1351~1362 (5.229)
2001 SCI Crystallization and preliminary X-ray crystallographic analysis of the TM1442 gene product from Thermotoga maritima, a homolog of Bacillus subtilis anti-anti-sigma factor: Acta Crystallogr. D. 57:276~278 (1.401)
2000 SCI Lactate dehydorgenase from the hyperthermophilic archaeon Methanococcus jannaschii: Overexpression,Crystallization,and Preliminary X-ray analysis: Acta Crystallogr. D. 56:81~83 (1.401)
