基本信息
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职业迁徙
个人简介
Specialization: Cancer Biology & Therapeutics, Chemical Biology, Drug Discovery, Medicinal Chemistry, Cellular Signaling, Protein Tyrosine Phosphatases
Research
Chemical Biology and Therapeutic Targeting of Protein Tyrosine Phosphatases: From Target Identification/Validation to Hit/Lead Generation and Preclinical Evaluation
Our research spans the disciplines of chemistry and biology with an emphasis on protein tyrosine phosphatases (PTPs), enzymes that remove phosphoryl groups from tyrosine phosphorylated proteins and regulate a plethora of cellular processes, including growth, differentiation, metabolism, and the immune response. Abnormal PTP activity leads to aberrant cellular signaling, which is linked to the development of cancer, diabetes/obesity, neurodegenerative and autoimmune disorders, and infectious diseases. Consequently, there is heightened interest to control disease progression at the level of PTPs.
Using state-of-the-art molecular, cellular and mouse genetic techniques (e.g. CRISPR gene editing, siRNA silencing, and gene knockout), we seek to fully characterize the >100 members of the PTP family and understand how PTP activity is regulated to modulate cellular signaling and how PTP malfunction causes diseases. To promote therapeutic application of drugging the PTPs as a target class, we employ fragment-based, and structure-guided medicinal chemistry to develop potent and selective chemical probes (orthosteric and allosteric inhibitors, covalent modifiers, and PROTAC-based small molecule degraders) for PTP functional interrogation, target validation, and therapeutic development. Current efforts aim to advance our target validation and lead generation paradigm and to create a ‘PTP-based drug discovery platform’ that will ultimately impact the therapeutic portfolio of tomorrow.
Our research program is multifaceted and incorporates both established and emerging technologies, across disciplines. Students have ample opportunity to interact with a highly interactive, collaborative and multi-disciplinary group of individuals with expertise ranging from biochemistry, cell biology, mouse genetics, structural biology, mass spectrometry, organic synthesis, medicinal chemistry, chemical biology and in vivo pharmacology.
Research
Chemical Biology and Therapeutic Targeting of Protein Tyrosine Phosphatases: From Target Identification/Validation to Hit/Lead Generation and Preclinical Evaluation
Our research spans the disciplines of chemistry and biology with an emphasis on protein tyrosine phosphatases (PTPs), enzymes that remove phosphoryl groups from tyrosine phosphorylated proteins and regulate a plethora of cellular processes, including growth, differentiation, metabolism, and the immune response. Abnormal PTP activity leads to aberrant cellular signaling, which is linked to the development of cancer, diabetes/obesity, neurodegenerative and autoimmune disorders, and infectious diseases. Consequently, there is heightened interest to control disease progression at the level of PTPs.
Using state-of-the-art molecular, cellular and mouse genetic techniques (e.g. CRISPR gene editing, siRNA silencing, and gene knockout), we seek to fully characterize the >100 members of the PTP family and understand how PTP activity is regulated to modulate cellular signaling and how PTP malfunction causes diseases. To promote therapeutic application of drugging the PTPs as a target class, we employ fragment-based, and structure-guided medicinal chemistry to develop potent and selective chemical probes (orthosteric and allosteric inhibitors, covalent modifiers, and PROTAC-based small molecule degraders) for PTP functional interrogation, target validation, and therapeutic development. Current efforts aim to advance our target validation and lead generation paradigm and to create a ‘PTP-based drug discovery platform’ that will ultimately impact the therapeutic portfolio of tomorrow.
Our research program is multifaceted and incorporates both established and emerging technologies, across disciplines. Students have ample opportunity to interact with a highly interactive, collaborative and multi-disciplinary group of individuals with expertise ranging from biochemistry, cell biology, mouse genetics, structural biology, mass spectrometry, organic synthesis, medicinal chemistry, chemical biology and in vivo pharmacology.
研究兴趣
论文共 410 篇作者统计合作学者相似作者
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Methods in molecular biology (Clifton, N.J.) (2024): 301-316
Zihan Qu,Frederick Nguele Meke, Zheng Zhang,Yunpeng Bai,Aaron D. Krabill, Christine S. Muli, Brenson A. Jassim,Jiajun Dong, Jinyue Li, Nguyen Yuyen, Andy W. Tao,Darci T. Trader,
Cancer Researchno. 6_Supplement (2024): 1973-1973
Yiming Miao,Yunpeng Bai, Jinmin Miao, Allison A. Murray,Jianping Lin,Jiajun Dong,Zihan Qu,Ruo-Yu Zhang,Quyen Nguyen,Shaomeng Wang,Zhong-Yin Zhang
Cancer Researchno. 6_Supplement (2024): 1969-1969
Soren Charmsaz,Nicole E. Gross,Jae W. Lee,Jianping Lin,Alexei G. Hernandez, Erin M. Coyne,Sarah M. Shin, Courtney Cannon,Xuan Yuan,Zhong-Yin Zhang,Elizabeth M. Jaffee,Won Jin Ho
Cancer Researchno. 6_Supplement (2024): 5306-5306
Frederick Nguele Meke,Yunpeng Bai, Diego Ruiz-Avila,Colin Carlock, Jinan Ayub,Jinmin Miao,Yanyang Hu,Qinglin Li,Zhong-Yin Zhang
CANCER RESEARCH COMMUNICATIONSno. 1 (2024): 5-17
Expert opinion on therapeutic targets (2024)
CHEMMEDCHEMpp.e202300669-e202300669, (2024)
Hongxia Chen,Yunpeng Bai,Michihiro Kobayashi,Shiyu Xiao,Sergio Barajas,Wenjie Cai,Sisi Chen,Jinmin Miao,Frederick Nguele Meke,Chonghua Yao, Yuxia Yang, Katherine Strube,
MOLECULAR CANCER RESEARCHno. 1 (2024): 94-103
BRITISH JOURNAL OF PHARMACOLOGY (2024)
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