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Publications

Home Publications

Publications

Ubiquitin-conjugating enzyme UbcH10 promotes gastric cancer growth and is a potential biomarker for gastric cancer
Oncology Reports.,2016, 36(2): 779-86
Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window
J. Med. Chem., 2016, 59 (11), 5520–5541.
Identification of GNE-131: A potent and selective hNaV1.7 inhibitor for the treatment of pain
National Medicinal Chemistry Symposium, 2016, Jun. 26-29, Chicago
Optimization of isoxazoline amide benzoxaboroles for identification of a development candidate as an oral long acting animal ectoparasiticide
Bioorganic & Medicinal Chemistry Letters 26 (2016) 3182–3186
Identification of Novel EZH2 Inhibitors through Pharmacophore-based Virtual Screening and Biological Assays
Bioorganic & Medicinal Chemistry Letters. 2016, 26, 3813–3817
Identification of Novel Disruptor of Telomeric Silencing 1-Like (DOT1L) Inhibitors through Structure-Based Virtual Screening and Biological Assays
J. Chem. Inf. Model. 2016, 56 (3), 527–534
Design and Discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 Inhibitor
Bioorg Med Chem Lett. 2016, 26(3), 721-725
Discovery of novel inhibitors targeting menin-mixed lineage leukemia (MLL) interface using pharmacophore- and docking-based virtual screening
Journal of Chemical Information and Modeling. ahead of print
Fragment-Based Drug Discovery of 2‑Thiazolidinones as BRD4 Inhibitors: 2. Structure-Based Optimization
J. Med. Chem. 2015, 58, 1281−1297
Mutant IDH is sufficient to initiate enchondromatosis in mice
PNAS. ( in process)
From Ergolines to Indoles: Improved Inhibitors of the Human H3 Receptor for the Treatment of Narcolepsy
ChemMedChem. 2015 Feb;10(2):266-75.
Neuroactive Steroids.1.Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21
J. Med. Chem. 2015, 58, 3500-3511.
人源性胃癌移植瘤模型的建立及其评价
实验动物与比较医学. 34:259-65
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders
J. Med. Chem., 2015, 58 (23), 9154–9170
Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series
ACS Med. Chem. Lett., 2015, 6 (6), 711–715
Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety
ACS Med. Chem. Lett., 2015, 6 (12), 1241–1246.
SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF
WO/2015/078374
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists
Bioorganic & Medicinal Chemistry Letters 2015 (25), 2907–2912
Neuroactive Steroids.1.Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21
J. Med. Chem. 2015, 58, 3500-3511.
Discovery of an orally bioavailable isoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide
Bioorganic & Medicinal Chemistry Letters 25 (2015) 5589–5593
Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening
J. Med. Chem. 2015, 58, 8166−8181
Identifying Novel Selective Non-Nucleoside DNA Methyltransferase 1 Inhibitors through Docking-Based Virtual Screening
J. Med. Chem. 2014, 57, 9028−9041
Virtual screening and biological evaluation of novel small molecular inhibitors against protein arginine methyltransferase 1 (PRMT1)
Org. Biomol. Chem., 2014, 12, 9665–9673
Ergoline-derived inverse agonists of the human h3 receptor for the treatment of narcolepsy
ChemMedChem. 2014 Aug;9(8):1683-96
Establishment and Characterization of 7 Novel Hepatocellular Carcinoma Cell Lines from Patient-Derived Tumor Xenografts
Plos One. 9(1): e85308
Steric and Electronic Factors Influence Regio-isomeric Thiazole Formations Between Substituted Benzothioamides and Ethyl Bromopyruvate
J. Heterocyclic. Chem. 2014, 51, 1137−1146
Novel synthesis of isoxazoline indolizine amides for potential application to tropical diseases
Tetrahedron Letters, Volume 55, 2014, Pages 1936–1938
Vortioxetine disinhibits pyramidal cell function and enhances synaptic plasticity in the rat hippocampus.
J Psychopharmacol. 2014 Oct;28(10):891-902.
Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation
Science,2013, 340(6132),622-6
人源性食管癌移植瘤模型的建立、评价及其应用的初步研究
实验动物与比较医学: 33(1)
HZ08 reverse the aneuploidy-induced cisplatin-resistance in Gastric cancer by modulating the p53 pathway.
European Journal of Pharmacology. 720(1-3): 84-97
食管癌动物模型的建立
上海师范大学学报(自然科学版). 42(4): 398-404
Small Molecule Activation of PKM2 in Cancer Cells Induces Serine Auxotrophy
Chem. Biol. 2012, 19(9), 1187-98
Intrinsic gemcitabine resistance in a novel pancreatic cancer cell line is associated with cancer stem cell-like phenotype.
Int J Oncol. 40 (3): 798-806
Identification of NME5 as a contributor to innate resistance to gemcitabine in pancreatic cancer cells.
FEBS J. 279(7): 1261-73
Transactivation of the human NME5 gene by Sp1 in pancreatic cancer cells.
Gene. 503(2): 200-7
Full-length human glutaminase in complex with an allosteric inhibitor
Biochem. 2011, 50(50), 10764 -70
INHIBITORS OF AKT ACTIVITY
WO/2011/130921
Differential Aspartate Usage Identifies a Subset of Cancer Cells Particularly
Cell Reports 17, 876–890, October 11, 2016
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers
ACS Med Chem Lett. 2018 Jan 19;9(4):300-305.
AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency
Blood. 2017 Sep 14;130(11):1347-1356.
AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations
Cancer Discov. 2017 May;7(5):478-493.
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions
ACS Med Chem Lett. 2017 Nov 28;8(12):1224-1229.
A small molecule activator of Nav1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo
European Journal of Neuroscience, Vol. 46, pp. 1887–1896, 2017
First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway
Cancer Discov. 2015 Apr;5(4):424-37.
H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma
Cancer Res. 2017 Dec 15;77(24):6999-7013.
Precision Targeted Therapy with BLU-667 for RET -Driven Cancers
“Cancer Discovery (July 1 2018 8 (7) 836-849; DOI:10.1158/2159-8290.CD-18-0338)”
“Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2”
PNAS | May 7, 2013 | vol. 110 | no. 19 | 7923
EZH2 inhibition by tazemetostat results in altered dependency on B-cell activation signaling in DLBCL
AACR August 23, 2017; DOI: 10.1158/1535-7163.MCT-16-0840
Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma
SCIEntIfIC Reports | (2017) 7:17993 | DOI:10.1038/s41598-017-18446-z
Selective Killing of SMARCA2- and SMARCA4- deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models
AACR Mol Cancer Ther; 16(5) May 2017
“Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas”
PLOS ONE| DOI:10.1371/journal.pone.0111840 December 10, 2014
Patent Application Publication
US 2016/0303135 A1
Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in VivoACS Med. Chem. Lett. 3, 10, 850-855
Pyrimidine hydroxyl amide compounds as protein deacetylase inhibitors and methods of use thereof.
WO2011307115
ANALOGS OF CELASTROL
WO2017070615A1
“Discovery of A‑971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders”
J. Med. Chem. 2015, 58, 9154-9170
一类黄酮衍生物及其制备方法和用途
CN1172946
一种6-甲氧基水杨醛的制备方法
CN101768065A
一类磺内酰胺类化合物及其制备方法和中间体
CN102115466B
一种螺环丙基甲酰衍生物的中间体化合物的制备方法
CN102557941B
一种米诺环素的制备方法及其中间体
CN103387512B
一种山环素的制备方法
CN103387511B
一种3-氯-5,6,7,8-四氢异喹啉的制备方法
201810781489.9
一种4-溴甲基-2-三甲基硅乙炔苯基-1-磺酰氟的制备方法
201810781490.1
一种5-氨甲基-哌啶-2-酮的制备方法
201810785216.1
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions
ACS Med. Chem. Lett. 2017, 8, 1224-1229
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