基本信息
孔祥谦  男  博导  中国科学院广州生物医药与健康研究院
电子邮件: kong_xiangqian@gibh.ac.cn
通信地址: 广州市黄埔区开源大道190号E105房间
邮政编码:

招生信息

   
招生专业
071009-细胞生物学
071010-生物化学与分子生物学
100104-病理学与病理生理学
招生方向
肿瘤表观遗传学和药物精准应用
肿瘤转录异常的分子机制和创新药物发现
基于表观遗传调控新机制的靶标确证和创新药物发现

教育背景

2009-09--2014-07   中国科学院上海药物研究所   博士学位
2005-09--2009-07   山东大学药学院   学士学位

工作经历

   
工作简历
2020-08~现在, 中国科学院广州生物医药与健康研究院, 研究员
2015-02~2020-07,Johns Hopkins University, 博士后
2009-09~2014-07,中国科学院上海药物研究所, 博士学位
2005-09~2009-07,山东大学药学院, 学士学位
社会兼职
2021-01-09-今,广东省药理学会药物筛选与评价专业委员会, 常务委员

教授课程

生物技术制药
现代医药生物技术概论
生物技术前沿

专利与奖励

   
奖励信息
(1) AACR-Get Your Rear in Gear Philadelphia Scholar in Training Award, 一等奖, 其他, 2019
专利成果
( 1 ) 芬戈莫德或其盐在治疗囊肿性疾病中的用途, 2020, 第 9 作者, 专利号: CN105560219B

( 2 ) 阿司咪唑、其盐或溶剂合物在制备预防和/或治疗恶性淋巴瘤的药物中的用途, 2019, 第 2 作者, 专利号: CN105078983B

( 3 ) 2-取代-5-苯基呋喃类化合物、其制备方法、药物组合物及其用途, 2014, 第 4 作者, 专利号: CN103509009A

出版信息

   
发表论文
(1) Epigenetic Therapy Inhibits Metastases by Disrupting Premetastatic Niches, Nature, 2021, 
(2) A Cost-Effective and Non-Invasive pfeRNA-Based Test Differentiates Benign and Suspicious Pulmonary Nodules from Malignant Ones, Non-Coding RNA, 2021, 
(3) Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction, JOURNAL OF MEDICINAL CHEMISTRY, 2021, 第 16 作者
(4) High-resolution Epigenome Mapping Reveals Distinct and Divergent Roles for UHRF1 in the Maintenance of DNA Methylation, FASEB JOURNAL, 2020, 第 4 作者
(5) Defining UHRF1 Domains that Support Maintenance of Human Colon Cancer DNA Methylation and Oncogenic Properties, CANCER CELL, 2019, 第 1 作者
(6) Aging-like Spontaneous Epigenetic Silencing Facilitates WntActivation, Stemness, and Braf V600E -InducedTumorigenesis, CANCER CELL, 2019, 第 7 作者
(7) Biochemical Studies and Molecular Dynamic Simulations Reveal the Molecular Basis of Conformational Changes in DNA Methyltransferase-1, ACS CHEMICAL BIOLOGY, 2018, 第 2 作者
(8) DNA Methylation Patterns Separate Senescence from Transformation Potential and Indicate Cancer Risk, CANCER CELL, 2018, 第 7 作者
(9) Development of a high-throughput fluorescence polarization assay for the discovery of EZH2-EED interaction inhibitors, ACTA PHARMACOLOGICA SINICA, 2018, 第 7 作者
(10) Critical threshold levels of DNA methyltransferase 1 are required to maintain DNA methylation across the genome in human cancer cells, GENOME RESEARCH, 2017, 第 5 作者
(11) Functional interplay between the RK motif and linker segment dictates Oct4–DNA recognition, NUCLEIC ACIDS RESEARCH, 2015, 第 1 作者
(12) An Arginine-rich Motif of Ring Finger Protein 4 (RNF4) Oversees the Recruitment and Degradation of the Phosphorylated and SUMOylated Kruppel-associated Box Domain-associated Protein 1 (KAP1)/TRIM28 Protein during Genotoxic Stress, JOURNAL OF BIOLOGICAL CHEMISTRY, 2014, 第 3 作者
(13) An Arginine-rich Motif of Ring Finger Protein 4 (RNF4) Oversees the Recruitment and Degradation of the Phosphorylated and SUMOylated Krüppel-associated Box Domain-associated Protein 1 (KAP1)/TRIM28 Protein during Genotoxic Stress, Journal of Biological Chemistry, 2014, 第 3 作者
(14) Catalytic Mechanism of Histone Acetyltransferase p300: From the Proton Transfer to Acetylation Reaction, JOURNAL OF PHYSICAL CHEMISTRY B, 2014, 第 3 作者
(15) Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants, CANCER SCIENCE, 2014, 第 4 作者
(16) K63-linked polyubiquitination of transcription factor IRF1 is essential for IL-1-induced production of chemokines CXCL10 and CCL5, NATURE IMMUNOLOGY, 2014, 第 10 作者
(17) Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2., JOURNAL OF MEDICINAL CHEMISTRY, 2014, 第 1 作者
(18) Discovery of two aminoglycoside antibiotics as inhibitors targeting the menin–mixed lineage leukaemia interface, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2014, 第 8 作者
(19) c-MET kinase inhibitors: a patent review (2011-2013), EXPERT OPINION ON THERAPEUTIC PATENTS, 2014, 第 2 作者
(20) DNA和组蛋白表观遗传修饰与糖尿病和肥胖的关系以及小分子抑制剂的研究进展, DNA or histone epigenetics modification and obesity or diabetes:mechanism and inhibitors, 中国药物化学杂志, 2013, 第 4 作者
(21) Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAFV600E inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 第 4 作者
(22) Targeting Epigenetics in Nervous System Disease, CNS & NEUROLOGICAL DISORDERS-DRUG TARGETS, 2013, 第 3 作者
(23) Salvianolic Acid A, a Novel Matrix Metalloproteinase-9 Inhibitor, Prevents Cardiac Remodeling in Spontaneously Hypertensive Rats, PLOS ONE, 2013, 第 7 作者
(24) Application of epigenome-modifying small molecules in induced pluripotent stem cells., MEDICINAL RESEARCH REVIEWS, 2013, 第 2 作者
(25) Structure-based computational study of the hydrolysis of New Delhi metallo-beta-lactmase-1, BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2013, 第 5 作者
(26) Theoretical Insights into Catalytic Mechanism of Protein Arginine Methyltransferase 1, PLOS ONE, 2013, 第 6 作者
(27) A quantum mechanics/molecular mechanics study on the hydrolysis mechanism of New Delhi metallo-beta-lactamase-1, JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN, 2013, 第 4 作者
(28) Helix Unfolding/Refolding Characterizes the Functional Dynamics of Staphylococcus aureus Clp Protease, JOURNAL OF BIOLOGICAL CHEMISTRY, 2013, 第 6 作者
(29) 组蛋白乙酰转移酶hMOF小分子抑制剂的发现及应用研究, 2013, 第 1 作者
(30) Computational drug discovery, ACTA PHARMACOLOGICA SINICA, 2012, 第 3 作者
(31) Quorum-sensing agr mediates bacterial oxidation response via an intramolecular disulfide redox switch in the response regulator AgrA, PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2012, 第 3 作者
(32) Development of a novel class of B-Raf V600E -selective inhibitors through virtual screening and hierarchical hit optimization, ORGANIC & BIOMOLECULAR CHEMISTRY, 2012, 第 1 作者
(33) Discovering potent inhibitors against c-Met kinase: molecular design, organic synthesis and bioassay, ORGANIC & BIOMOLECULAR CHEMISTRY, 2012, 第 4 作者
(34) Theoretical Study of the Mechanism of Proton Transfer in the Esterase Estb from Burkholderia Gladioli, JOURNAL OF PHYSICAL CHEMISTRY B, 2011, 第 2 作者
(35) Catalytic Mechanism Investigation of Lysine-Specific Demethylase 1 (LSD1): A Computational Study, PLOS ONE, 2011, 通讯作者
(36) Molecular Basis of NDM-1, a New Antibiotic Resistance Determinant, PLOS ONE, 2011, 第 5 作者
(37) Identification and synthesis of N′-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 第 6 作者
(38) 鞘氨醇磷酸酯调控机制的研究进展, ADVANCE IN THE STUDY OF THE MECHANISMS REGULATED BY SPHINGOSINE-1-PHOSPHATE, 中国科学基金, 2010, 第 2 作者

科研活动

   
科研项目
( 1 ) 中科院广州生物医药与健康研究院启动费, 负责人, 研究所自选, 2020-07--2025-07
( 2 ) 粤桂特色药用植物中靶向UHRF1的活性天然产物发现、优化和抗肿瘤活性研究, 负责人, 地方任务, 2020-12--2024-11
( 3 ) DNA甲基化维持蛋白UHRF1特异性抑制剂的发现和抗肿瘤活性研究, 负责人, 国家任务, 2022-01--2024-12
( 4 ) 基于全新作用机制的DNA甲基化抑制剂发现和抗实体瘤研究, 负责人, 其他任务, 2022-01--2024-12
参与会议
(1)基于新靶标、新机制的DNA甲基化抑制剂发现和抗肿瘤活性研究   第六届表观遗传与生物医药研发国际学术会议   2021-11-25
(2)Defining UHRF1 domains that support maintenance of human colon cancer DNA methylation and tumorigenicity   2019-03-29