Taebo Sim

发表

Enantiospecific synthesis of carbapentostatins.

T. Sim, R. Mohareb, H. Rapoport, 2003, The Journal of organic chemistry.

Two-photon probes for the endoplasmic reticulum: its detection in a live tissue by two-photon microscopy.

B. Cho, T. Sim, Seunghye Choi, 2020, Chemical communications.

Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors.

W. Hur, T. Sim, E. Roh, 2018, Bioorganic & medicinal chemistry letters.

Identification of Existing Drugs That Effectively Target NTRK1 and ROS1 Rearrangements in Lung Cancer

Taebo Sim, Takayuki Kosaka, Nathanael S. Gray, 2016, Clinical Cancer Research.

Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor.

N. Gray, J. Griffin, R. Stone, 2016, ACS medicinal chemistry letters.

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

P. Jänne, N. Gray, H. Choi, 2015, Journal of medicinal chemistry.

Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors

P. Jänne, N. Gray, Xianming Deng, 2011, ACS medicinal chemistry letters.

Discovery of inhibitors that overcome the G1202R ALK Resistance Mutation

P. Jänne, N. Gray, H. Choi, 2016 .

The first small molecules capable of strongly suppressing proliferation of cancer cells harboring BRAF class I/II/III mutations.

I. Shin, T. Sim, Namdoo Kim, 2020, Biochemical and biophysical research communications.

Discovery of potent and selective covalent inhibitors of JNK.

Taebo Sim, Mario Niepel, Scott B Ficarro, 2012, Chemistry & biology.

Covalent Guanosine Mimetic Inhibitors of G12C KRAS.

Taebo Sim, Sang Min Lim, John Hunter, 2017, ACS medicinal chemistry letters.

Small Molecule Kinase Inhibitors Provide Insight into Mps1 Cell Cycle Function

Taebo Sim, Stefan Knapp, Panagis Filippakopoulos, 2010, Nature chemical biology.

Chemical kinomics: a powerful strategy for target deconvolution.

Taebo Sim, Do-Hee Kim, T. Sim, 2010, BMB reports.

Development of ATP-competitive mTOR inhibitors.

D. Sabatini, N. Gray, Qingsong Liu, 2012, Methods in molecular biology.

An ATP-competitive Mammalian Target of Rapamycin Inhibitor Reveals Rapamycin-resistant Functions of mTORC1*

D. Sabatini, N. Gray, Qingsong Liu, 2009, Journal of Biological Chemistry.

Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development

N. Gray, Yanke Liang, Jinhua Wang, 2020, Cell.

Targeting transcription regulation in cancer with a covalent CDK7 inhibitor

Sridhar Ramaswamy, Taebo Sim, Richard A Young, 2014, Nature.

Natural and Synthetic Lactones Possessing Antitumor Activities

T. Sim, Younghoon Kim, Sandip Sengupta, 2021, International journal of molecular sciences.

Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.

D. Sabatini, N. Gray, Qingsong Liu, 2010, Journal of medicinal chemistry.

Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.

N. Gray, Jianwei Che, P. Ren, 2009, Bioorganic & medicinal chemistry letters.

Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.

N. Gray, Jianwei Che, P. Ren, 2008, Bioorganic & medicinal chemistry letters.

The efficient one-step chlorination of methylsulfanyl group on pyrimidine ring system with sulfuryl chloride

H. Choi, J. Hah, T. Sim, 2010 .

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

Taebo Sim, Yongping Xie, Nathanael S Gray, 2010, Journal of medicinal chemistry.

Structural Revision of Baulamycin A and Structure-Activity Relationships of Baulamycin A Derivatives.

D. Oh, I. Shin, M. Bae, 2017, The Journal of organic chemistry.

Anti-leukemia activity of a Hsp70 inhibitor and its hybrid molecules

E. Zuiderweg, I. Shin, Nak-Kyoon Kim, 2017, Scientific Reports.

Anti-glioma effects of 2-aminothiophene-3-carboxamide derivatives, ANO1 channel blockers.

I. Shin, Seongshick Ryu, T. Sim, 2020, European journal of medicinal chemistry.

Pharmacological Targeting of the Pseudokinase Her3

P. Jänne, N. Gray, K. Westover, 2014, Nature chemical biology.

A Bcr-Abl Inhibitor GNF-2 Attenuates Inflammatory Activation of Glia and Chronic Pain

Y. Bae, K. Suk, In-kyu Lee, 2019, Front. Pharmacol..

Pharmacophore based 3D-QSAR study of VEGFR-2 inhibitors

Taebo Sim, Seung Joo Cho, F. A. Pasha, 2009, Medicinal Chemistry Research.

Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach.

N. Gray, Qingsong Liu, J. Griffin, 2015, Blood.

A general strategy for creating

M. Warmuth, N. Gray, G. Spraggon, 2006 .

A general strategy for creating "inactive-conformation" abl inhibitors.

Taebo Sim, Yi Liu, Yongping Xie, 2006, Chemistry & biology.

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

Charles Y. Lin, P. Sorger, N. Gray, 2019, Cell chemical biology.

Development of a Selective CDK 7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype Graphical

Charles Y. Lin, P. Sorger, N. Gray, 2019 .

Discovery of a selective inhibitor of Doublecortin Like Kinase 1

Charles Y. Lin, W. Hahn, A. Look, 2020, Nature Chemical Biology.

Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains.

M. McKeown, Xiang Xu, Dennis L. Buckley, 2018, ACS chemical biology.

Characterization of a highly selective inhibitor of the Aurora kinases.

S. Knapp, N. Gray, A. Chaikuad, 2017, Bioorganic & medicinal chemistry letters.

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

N. Gray, Tinghu Zhang, Xianming Deng, 2016, ACS medicinal chemistry letters.

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

S. Knapp, N. Gray, Xianming Deng, 2013, European journal of medicinal chemistry.

Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1

U. McDermott, N. Gray, Xianming Deng, 2011, ACS medicinal chemistry letters.

Synthesis and structure-activity relationships of targeted protein degraders for the understudied kinase NEK9

N. Gray, I. Shin, Seongshick Ryu, 2021 .

Identification of methyl violet 2B as a novel blocker of focal adhesion kinase signaling pathway in cancer cells.

Jiyeon Lee, G. Han, T. Sim, 2013, Biochemical and biophysical research communications.

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors

Rachel G Liao, S. Gaudet, P. Jänne, 2014, Proceedings of the National Academy of Sciences.

Identification of Pyridinyltriazine Derivatives as Potent panFGFR Inhibitors against Gatekeeper Mutants for Overcoming Drug Resistance.

Seongshick Ryu, T. Sim, Younghoon Kim, 2022, Journal of medicinal chemistry.

Novel Small Molecules Capable of Blocking mtRAS-Signaling Pathway

Seongshick Ryu, T. Sim, Chaeyoung Lee, 2021, Frontiers in Oncology.

Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as potent ALK-L1196M inhibitors

H. Seo, T. Sim, K. Selim, 2019, Journal of enzyme inhibition and medicinal chemistry.

Anti-Tumor Activity of AZD4547 Against NTRK1 Fusion Positive Cancer Cells Through Inhibition of NTRKs

T. Sim, Hanna Cho, T. Murakami, 2021, Frontiers in Oncology.

Novel and Potent Small Molecules against Melanoma Harboring BRAF Class I/II/III Mutants for Overcoming Drug Resistance

I. Shin, Seongshick Ryu, T. Sim, 2021, International journal of molecular sciences.

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

N. Gray, W. Hur, H. Choi, 2018, Journal of medicinal chemistry.

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

Taebo Sim, Sang Min Lim, John Hunter, 2014, Angewandte Chemie.

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

W. Hur, H. Choi, N. Jeon, 2017, Journal of medicinal chemistry.

Identification of a novel 5-amino-3-(5-cyclopropylisoxazol-3-yl)-1-isopropyl-1H-pyrazole-4-carboxamide as a specific RET kinase inhibitor.

I. Shin, T. Sim, N. Kim, 2017, European journal of medicinal chemistry.

Targeted kinase degradation via the KLHDC2 ubiquitin E3 ligase.

Younghoon Kim, Ha-soon Choi, S. Hinshaw, 2023, Cell chemical biology.

Targeted Kinase Degradation via the KLHDC2 Ubiquitin E3 Ligase

N. Gray, Younghoon Kim, Ha-soon Choi, 2022, bioRxiv.

AK2 is an AMP-sensing negative regulator of BRAF in tumorigenesis

H. Yu, Dae-Yeul Yu, Yong-Keun Jung, 2022, Cell Death & Disease.

Optimization of Bipyridinyl Pyrazole Scaffolds via Design, Synthesis and Screening of a New Series of ROS1 Kinase‐modulating Compounds

M. M. Al-Sanea, K. Yoo, So Ha Lee, 2015 .

Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.

Mi-hyun Kim, J. Hah, T. Sim, 2011, Bioorganic & medicinal chemistry.

Synthesis of 1H‐Pyrazole‐1‐carboxamide Derivatives and Their Antiproliferative Activity against Melanoma Cell Line

T. Sim, M. El-Gamal, C. Oh, 2011, Archiv der Pharmazie.

One step synthesis of quantum dot-magnetic nanoparticle heterodimers for dual modal imaging applications.

T. Sim, Jiyeon Lee, Gyoyeon Hwang, 2015, The Analyst.

A new quantum dot-platinum conjugate for self-assembled nanoconjugates by coordination bonding mediated recognition.

Rita Song, T. Sim, Jiyeon Lee, 2013, Chemical communications.

A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.

T. Sim, Hanna Cho, N. Kim, 2016, Journal of medicinal chemistry.

Synthesis of novel arylaminoquinazolinylurea derivatives and their antiproliferative activities against bladder cancer cell line.

T. Sim, E. Roh, J. Choi, 2016, Bioorganic & medicinal chemistry letters.

Expanding the Diversity of Allosteric Bcr-Abl Inhibitors†

G. Rummel, N. Gray, Xianming Deng, 2010, Journal of medicinal chemistry.

Discovery of Type II Inhibitors of TGFβ-Activated Kinase 1 (TAK1) and Mitogen-Activated Protein Kinase Kinase Kinase Kinase 2 (MAP4K2)

P. Cohen, N. Gray, K. Westover, 2014, Journal of medicinal chemistry.

Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer.

C. Paweletz, P. Jänne, L. Sholl, 2016, Cancer discovery.

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.

J. Caldwell, N. Gray, O. Ohmori, 2006, Bioorganic & medicinal chemistry letters.

Novel small molecule Raf kinase inhibitors for targeted cancer therapeutics

T. Sim, Do-Hee Kim, Taebo Sim, 2012, Archives of pharmacal research.

Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors

John T. Powers, G. Daley, W. Jahnke, 2010, Nature.

Allosteric inhibitors of Bcr-abl–dependent cell proliferation

J. Mestan, D. Fabbro, N. Gray, 2006, Nature chemical biology.

Development of small molecules targeting the pseudokinase Her3.

P. Jänne, N. Gray, K. Westover, 2015, Bioorganic & medicinal chemistry letters.

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

N. Gray, Nicholas Kwiatkowski, T. Sim, 2018, ACS medicinal chemistry letters.

Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome.

P. Sorger, R. Everley, S. Knapp, 2019, Cell chemical biology.

Novel small molecule Raf kinase inhibitors for targeted cancer therapeutics

T. Sim, Do-Hee Kim, Taebo Sim, 2012, Archives of Pharmacal Research.

N-Myristoylated c-Abl Tyrosine Kinase Localizes to the Endoplasmic Reticulum upon Binding to an Allosteric Inhibitor*

N. Gray, Xianming Deng, M. Seeliger, 2009, The Journal of Biological Chemistry.

Discovery of Covalent CDK14 Inhibitors with Pan-TAIRE Family Specificity.

Jared L. Johnson, P. Sorger, N. Gray, 2019, Cell chemical biology.

Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.

N. Gray, S. Ficarro, J. Marto, 2019, Bioorganic & medicinal chemistry letters.

Design and Synthesis of New [1,2,3]Triazolo[4,5-d]pyrimidine Derivatives as Potential Antiproliferative Agents

M. M. Al-Sanea, T. Sim, E. Roh, 2015 .

Inverse Agonist of Nuclear Receptor ERRγ Mediates Antidiabetic Effect Through Inhibition of Hepatic Gluconeogenesis

S. Koo, In-kyu Lee, D. Ryu, 2013, Diabetes.

Suppression of TRPM7 enhances TRAIL‐induced apoptosis in triple‐negative breast cancer cells

T. Sim, Chiman Song, Ki-Bong Oh, 2020, Journal of cellular physiology.

Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors.

Bongjin Moon, Jung-Eun Park, T. Sim, 2013, Bioorganic & medicinal chemistry letters.

Identification of highly selective type II kinase inhibitors with chiral peptidomimetic tails

Kyung-Sook Chung, K. Lee, Jeon-Soo Shin, 2022, Journal of enzyme inhibition and medicinal chemistry.

1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives: a novel type II Raf kinase inhibitors.

J. Hah, T. Sim, Junghun Lee, 2010, Bioorganic & medicinal chemistry letters.

Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines.

J. Hah, T. Sim, C. Oh, 2010, Bioorganic & medicinal chemistry letters.

An ATP-competitive Mammalian Target of Rapamycin Inhibitor Reveals Rapamycin-resistant Functions of mTORC1*

D. Sabatini, N. Gray, Qingsong Liu, 2009, Journal of Biological Chemistry.

In situ imaging of quantum dot-AZD4547 conjugates for tracking the dynamic behavior of fibroblast growth factor receptor 3

T. Sim, Dong-Kwon Lim, Jiyeon Lee, 2017, International journal of nanomedicine.

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants.

James D. Griffin, Andrew L. Kung, Taebo Sim, 2010, Blood.

Raman-Based in Situ Monitoring of Changes in Molecular Signatures during Mitochondrially Mediated Apoptosis

Ji Hye Lee, I. Shin, T. Sim, 2019, ACS omega.

Structure-based optimization and biological evaluation of trisubstituted pyrazole as a core structure of potent ROS1 kinase inhibitors.

Byung Sun Park, M. M. Al-Sanea, T. Sim, 2014, Bioorganic & medicinal chemistry.

Rhodium-catalyzed reductive cyclization of 1,6-enynes and stereoselective synthesis of the putative structure of lucentamycin A and its stereoisomers

H. Choi, J. Hah, T. Sim, 2012 .

Synthesis and antihyperglycemic activity of erythrose, ribose and substituted pyrrolidine containing thiazolidinedione derivatives.

S. Ahn, J. Shin, T. Sim, 2003, Chemical & pharmaceutical bulletin.

Procaspase activating compound 1 controls tetracycline repressor-regulated gene expression system

Jiyeon Lee, T. Sim, Chiman Song, 2018, Bioscience reports.

Anti-cancer effects of 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one derivatives on hepatocellular carcinoma harboring FGFR4 activation

I. Shin, Seongshick Ryu, T. Sim, 2021, Neoplasia.

Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo.

R. Xavier, S. Schreiber, A. Shamji, 2016, ACS chemical biology.

Structure-based optimization and biological evaluation of trisubstituted pyrazole as a core structure of potent ROS1 kinase inhibitors.

Byung Sun Park, M. M. Al-Sanea, E. Roh, 2014, Bioorganic & medicinal chemistry.

Efficient synthesis of enantiomerically pure 2-acylaziridines: Facile syntheses of N-Boc-safingol, N-Boc-D-erythro-sphinganine, and N-Boc-spisulosine from a common intermediate.

T. Sim, H. S. Hahm, H. Ha, 2003, The Journal of organic chemistry.

A novel synthesis of 5-functionalized oxazolidin-2-ones from enantiomerically pure 2-substituted N-[(R)-(+)-alpha-methylbenzyl]aziridines.

H. Yun, T. Sim, H. Ha, 2003, The Journal of organic chemistry.

An efficient synthesis of 1,4-dideoxy-1,4-imino-d- and l-arabinitol and 1,4-dideoxy-1,4-imino-d- and l-xylitol from chiral aziridines

H. Choi, T. Sim, W. Lee, 2013 .

An efficient and enantioselective total synthesis of naturally occurring L-783277

H. Choi, J. Hah, T. Sim, 2010 .

Amphiphilic small peptides for delivery of plasmid DNAs and siRNAs

W. Hur, T. Sim, Eun‐Kyoung Bang, 2018, Chemical biology & drug design.

Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors.

Byung Sun Park, Hye-Mi Park, M. M. Al-Sanea, 2015, European journal of medicinal chemistry.