周璐｜复旦大学｜学者主页

2026

Discovery of a Covalent Inhibitor Targeting the PHGDH Dimer Interface with Antitumor Efficacy

Lei Feng, Liu Y, Yiwei Zhang, Zhongjiao Fan, Xinyuan Wu, Xiancheng Yang, Leyi Liu, Zhibei Qu, Ye Shen, Xiaojie Lu, Lu Zhou

Journal of Medicinal Chemistry

DOI

2026

Design, Synthesis, and Evaluation of Phenylpyrrole Derivatives as Small-Molecule Activators of BAX

Wei Cai, Zuo Li, Meiling Zhao, Yiwen Gu, Chenyang Qiu, Mi Zhou, Wei Deng, Lu Zhou, Yan Li, Renxiao Wang

Journal of Medicinal Chemistry

DOI

2026

Discovery of 1-(Azetidin-3-ylmethyl)-1 H -benzo[ d ]imidazole Derivatives as Efficient GSTP1 Inhibitors for Gastric Cancer Treatment via Warhead Removal Strategy

Wenhao Xie, Yuehong Chen, Lulu Jiang, Xinyuan Wu, Zhiyuan Qi, Tianbai Shuai, Mingzhong Yang, Zhiyang Wang, Jinghan Gao, Yingjie Zhu, Xiaojie Lu, Meng-Lin Huang, Zhibei Qu, Wenfu Tan, Jian Ding, Lu Zhou

Journal of Medicinal Chemistry

DOI

2025

靶向蛋白翻译后修饰的药物化学生物学研究

陶泓儒，张元元，陈文韬，陈子墨，徐颖，李昊，周璐，韩记昌，邓贤明，李林，陈国强，罗成

《中国科学:化学》

2025

Biocatalytic- and Chemoproteomic-Guided Discovery of a PHGDH Inhibitor from Chemoenzymatic-Promoted DNA-Encoded Libraries Selection Platform

Yiwei Zhang, Yuqiu Lan, Rufeng Fan, Lei Feng, Guoliang Wang, Xinyuan Wu, Lulu Wen, Zhiqiang Duan, Yueyue Xia, Xudong Wang, Lingrui Zhang, Lu Zhou, Minjia Tan, Cangsong Liao, Xiaojie Lu

Journal of the American Chemical Society

DOI

2025

Expanding the Chemistry of Acyl Diazo Electrophile as a Tunable Warhead for Covalent Targeting of KRAS (G12D) Mutant

Tianbai Shuai, Rong Zhang, Zi-Hang Yuan, Mingya Zhang, Zhongjiao Fan, Xiaoxue Ruan, Zhiyuan Qi, Wenhao Xie, Ping Liu, Motonari Uesugi, Qing Li, Zhibei Qu, Minjia Tan, Hua Su, Lu Zhou

Journal of Medicinal Chemistry

DOI

2025

Discovery of N -(1,3,4-Thiadiazol-2-yl)amide Derivatives as Uncompetitive Inhibitors of 6-Phosphogluconate Dehydrogenase

Rong Zhang, Mingming Sun, Xin Xiao, Huiti Li, Lulu Jiang, Jing Chen, Mingzhong Yang, Xueying Yao, Changliang Shan, Lu Zhou

Journal of Medicinal Chemistry

DOI

2025

Residue-Selective Inhibitors Discovery via Covalent DNA-Encoded Chemical Libraries with Diverse Warheads

Xinyuan Wu, Jian Pan, Rufeng Fan, Yiwei Zhang, Chao Wang, Guoliang Wang, Jiaxiang Liu, Mengqing Cui, Jinfeng Yue, Rui Jin, Zhiqiang Duan, Mingyue Zheng, Lianghe Mei, Lu Zhou, Minjia Tan, Jing Ai, Xiaojie Lu

Journal of the American Chemical Society

DOI

2025

Proteome‐Wide Data Guides the Discovery of Lysine‐Targeting Covalent Inhibitors Using DNA‐Encoded Chemical Libraries

Xinyuan Wu, Shunyao Li, Ting Bo Liang, Qing Yu, Yiwei Zhang, Jiaxiang Liu, Kaige Li, Zijian Liu, Mengqing Cui, Yongchao Zhao, Xin Han, Rui Jin, Minjia Tan, Xiao‐Hua Chen, Yujun Zhao, Mingyue Zheng, Yi Eve Sun, Lu Zhou, Xiaojie Lu

Angewandte Chemie

DOI

2024

靶向肿瘤代谢酶小分子药物研究进展

李顺尧，冯磊，张昕晨，黄逸洋，姚雪莹，周璐

《药学进展》

2024

Discovery of a novel thiophene carboxamide analogue as a highly potent and selective sphingomyelin synthase 2 inhibitor for dry eye disease therapy

Jintong Yang, Yiteng Lu, Kexin Hu, Xinchen Zhang, Wei Wang, Deyong Ye, Mingguang Mo, Xin Xiao, Xichen Wan, Yuqing Wu, Shuxian Zhang, He Huang, Zhibei Qu, Yimin Hu, Yu Cao, Jiaxu Hong, Lu Zhou

Acta Pharmaceutica Sinica B

DOI

2024

A phosphoglycerate mutase 1 allosteric inhibitor restrains TAM-mediated colon cancer progression

Cheng Wang, Minghao Zhang, Shunyao Li, Miaomiao Gong, Mingyu Luo, Mo-cong Zhang, Jing-Hua Zou, Ningxiang Shen, Lu Xu, Hui-min Lei, Ling Bi, Liang Zhu, Zhengting Wang, Hongzhuan Chen, Lu Zhou, Ying H. Shen

Acta Pharmaceutica Sinica B

DOI

2024

Cryo-EM structure of human sphingomyelin synthase and its mechanistic implications for sphingomyelin synthesis

Kexin Hu, Qing Zhang, Yang Chen, Jintong Yang, Ying Xia, Bing Rao, Shaobai Li, Yafeng Shen, Cao Mi, Hongliang Lu, An Qin, Xian‐Cheng Jiang, Deqiang Yao, Jie Zhao, Lu Zhou, Yu Cao

Nature Structural & Molecular Biology

DOI

2023

ABPP-CoDEL: Activity-Based Proteome Profiling-Guided Discovery of Tyrosine-Targeting Covalent Inhibitors from DNA-Encoded Libraries

Lulu Jiang, Sixiu Liu, Xinglong Jia, Qinting Gong, Xin Wen, Weiwei Lu, Jintong Yang, Xinyuan Wu, Xuan Wang, Yanrui Suo, Yilin Li, Motonari Uesugi, Zhibei Qu, Minjia Tan, Xiaojie Lu, Lu Zhou

Journal of the American Chemical Society

DOI

2023

PGAM1 Inhibition Promotes HCC Ferroptosis and Synergizes with Anti‐PD‐1 Immunotherapy

Yi-Min Zheng, Yining Wang, Lu Zhou, Jinkai Wan, Lulu Jiang, Danjun Song, Chuanyuan Wei, Chao Gao, Guo‐Ming Shi, Jian Zhou, Jia Fan, Ai‐Wu Ke, Lu Zhou, Jiabin Cai

Advanced Science

DOI

2023

Drug discovery by targeting the protein–protein interactions involved in autophagy

Honggang Xiang, Mi Zhou, Yan Li, Lu Zhou, Renxiao Wang

Acta Pharmaceutica Sinica B

DOI

2023

Adamantaniline Derivatives Target ATP5B to Inhibit Translation of Hypoxia Inducible Factor‐1α

Huiti Li, Yali Liu, Zian Xue, Li Zhang, Xiaoxue Ruan, Jintong Yang, Zhongjiao Fan, Hongfang Zhao, Yu Cao, Guoqiang Chen, Ying Xu, Lu Zhou

Advanced Science

DOI

2023

Discovery of Small-Molecule Autophagy Inhibitors by Disrupting the Protein–Protein Interactions Involving Autophagy-Related 5

Honggang Xiang, Ruiqi Liu, Xiangying Zhang, Ran An, Mi Zhou, Chang‐Heng Tan, Qing Li, Minyi Su, Chun Guo, Lu Zhou, Yingxia Li, Renxiao Wang

Journal of Medicinal Chemistry

DOI

2022

Benzo[d]isoxazole Derivatives as Hypoxia-Inducible Factor (HIF)-1α Inhibitors

Zian Xue, Huiti Li, Wenhao Xie, Ying Xu, Lu Zhou, Zhibei Qu

ACS Medicinal Chemistry Letters

DOI

2022

Discovery of Non-Cysteine-Targeting Covalent Inhibitors by Activity-Based Proteomic Screening with a Cysteine-Reactive Probe

Ye‐Jin Jung, Naotaka Noda, Junichiro Takaya, Masahiro Abo, Kohei Toh, Ken Tajiri, Changyi Cui, Lu Zhou, Shin‐ichi Sato, Motonari Uesugi

ACS Chemical Biology

DOI

2021

Design, synthesis, and biological evaluation of 1,3,6,7-tetrahydroxyxanthone derivatives as phosphoglycerate mutase 1 inhibitors

Kaixuan Jiang, Biao Gao, Jing Yuan Yu, Lulu Jiang, Ao Niu, Yihe Jia, Tao Meng, Lu Zhou, Jinxin Wang

Bioorganic & Medicinal Chemistry Letters

DOI

2020

Novel octapeptide-DTX prodrugs targeting MMP-7 as effective agents for the treatment of colorectal cancer with lower systemic toxicity

Zhengyu Liu, Mei‐Lin Tang, Jin-Feng Ning, Yunpeng Hao, Lu Zhou, Xun Sun

European Journal of Medicinal Chemistry

DOI

2020

Sphingomyelin synthase 2 facilitates M2-like macrophage polarization and tumor progression in a mouse model of triple-negative breast cancer

Yan Deng, Jia-chun Hu, Shuhua He, Bin Lou, Tingbo Ding, Jintong Yang, Mingguang Mo, De-yong Ye, Lu Zhou, Xian‐Cheng Jiang, Ker Yu, Jibin Dong

Acta Pharmacologica Sinica

DOI

2020

HKB99, an allosteric inhibitor of phosphoglycerate mutase 1, suppresses invasive pseudopodia formation and upregulates plasminogen activator inhibitor-2 in erlotinib-resistant non-small cell lung cancer cells

Qian Liang, Wei-ming Gu, Ke Huang, Mingyu Luo, Jing-Hua Zou, Guanglei Zhuang, Hui-min Lei, Hongzhuan Chen, Liang Zhu, Lu Zhou, Ying H. Shen

Acta Pharmacologica Sinica

DOI

2020

Chemoproteomic Profiling of a Pharmacophore-Focused Chemical Library

Louvy Lynn Punzalan, Lulu Jiang, Di Mao, Amarjyoti Das Mahapatra, Shin‐ichi Sato, Yasushi Takemoto, Mari Tsujimura, Kosuke Kusamori, Makiya Nishikawa, Lu Zhou, Motonari Uesugi

Cell chemical biology

DOI

2020

Site-Selective Phosphoglycerate Mutase 1 Acetylation by a Small Molecule

Xiaodan Zhang, Lulu Jiang, Ke Huang, Chuantao Fang, Jian Li, Jintong Yang, Huiti Li, Xiaoxue Ruan, Penghui Wang, Mingguang Mo, Ping Wu, Yanhui Xu, Chao Peng, Motonari Uesugi, Deyong Ye, Fa‐Xing Yu, Lu Zhou

ACS Chemical Biology

DOI

2019

An allosteric PGAM1 inhibitor effectively suppresses pancreatic ductal adenocarcinoma

Chenlei Wen, Ke Huang, Lu-Lu Jiang, Xiongxiong Lu, Yuting Dai, Min-Min Shi, Xiao-Mei Tang, Qingbing Wang, Xiaodan Zhang, Peng‐Hui Wang, Huiti Li, Xiaoxue Ruan, Liwen Wang, Xinjing Wang, Qian Wang, Wei Lü, Xiaoqiang Xiang, Xun Sun, Yanhui Xu, Luhua Lai, Qian Zhan, Hongwei Li, Chenghong Peng, Jing Chen, Jin-Yan Huang, Deyong Ye, Sai‐Juan Chen, Chen Ying Zhu, Min Li, Yuan Fang, Baiyong Shen, Lu Zhou

Proceedings of the National Academy of Sciences

DOI

2019

A Novel Allosteric Inhibitor of Phosphoglycerate Mutase 1 Suppresses Growth and Metastasis of Non-Small-Cell Lung Cancer

Ke Huang, Qian Liang, Ye Zhou, Lu-lu Jiang, Wei-ming Gu, Mingyu Luo, Ya‐Bin Tang, Yang Wang, Wei Lü, Min Huang, Shengzhe Zhang, Guanglei Zhuang, Qing Dai, Qiancheng Shen, Jian Zhang, Hui-min Lei, Liang Zhu, De-yong Ye, Hongzhuan Chen, Lu Zhou, Ying H. Shen

Cell Metabolism

DOI

2019

Synthesis and biological evaluation of anthraquinone derivatives as allosteric phosphoglycerate mutase 1 inhibitors for cancer treatment

Ke Huang, Lulu Jiang, Ronghui Liang, Huiti Li, Xiaoxue Ruan, Changliang Shan, Deyong Ye, Lu Zhou

European Journal of Medicinal Chemistry

DOI

2019

Development of Anthraquinone Analogues as Phosphoglycerate Mutase 1 Inhibitors

Ke Huang, Lulu Jiang, Huiti Li, Deyong Ye, Lu Zhou

Molecules

DOI

2018

Discovery, synthesis and anti-atherosclerotic activities of a novel selective sphingomyelin synthase 2 inhibitor

Yali Li, Taomin Huang, Bin Lou, Deyong Ye, Xiangyu Qi, Xiaoxia Li, Shuang Hu, Tingbo Ding, Yan Chen, Yang Cao, Mingguang Mo, Jibin Dong, Min Wei, Yong Chu, Huiti Li, Xian‐Cheng Jiang, Nengneng Cheng, Lu Zhou

European Journal of Medicinal Chemistry

DOI

2018

Discovery of 4-Benzyloxybenzo[d]isoxazole-3-amine Derivatives as Highly Selective and Orally Efficacious Human Sphingomyelin Synthase 2 Inhibitors that Reduce Chronic Inflammation in db/db Mice

Mingguang Mo, Jintong Yang, Xian‐Cheng Jiang, Yu Cao, Jinyu Fei, Yang Chen, Xiangyu Qi, Yong Chu, Lu Zhou, Deyong Ye

Journal of Medicinal Chemistry

DOI

2018

The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors

Penghui Wang, Lulu Jiang, Yang Cao, Deyong Ye, Lu Zhou

Molecules

DOI

2018

Design and Synthesis of the Diazirine-based Clickable Photo-affinity Probe Targeting Sphingomyelin Synthase 2

Penghui Wang, Zhining Li, Lulu Jiang, Lu Zhou, Deyong Ye

Letters in Drug Design & Discovery

DOI

2018

Xanthone derivatives as phosphoglycerate mutase 1 inhibitors: Design, synthesis, and biological evaluation

Penghui Wang, Lulu Jiang, Yang Cao, Xiaodan Zhang, Bangjing Chen, Shiyu Zhang, Ke Huang, Deyong Ye, Lu Zhou

Bioorganic & Medicinal Chemistry

DOI

2017

Conformation and dynamics of the C-terminal region in human phosphoglycerate mutase 1

Shien Liu, Junchi Hu, Hao Zhang, Pan Xu, Wei Wan, Ming-yue Zheng, Kunqian Yu, Hong Ding, Hualiang Jiang, Lu Zhou, Cheng Luo

Acta Pharmacologica Sinica

DOI

2017

Discovery of the selective sphingomyelin synthase 2 inhibitors with the novel structure of oxazolopyridine

Xiangyu Qi, Yang Cao, Yali Li, Mingguang Mo, Lu Zhou, Deyong Ye

Bioorganic & Medicinal Chemistry Letters

DOI

2016

抗肿瘤代谢靶标磷酸甘油酸变位酶1及其抑制剂的研究进展

江露露，周璐，叶德泳

《药学进展》

2015

Discovery, synthesis and biological evaluation of 2-(4-(N-phenethylsulfamoyl)phenoxy)acetamides (SAPAs) as novel sphingomyelin synthase 1 inhibitors

Yali Li, Xiangyu Qi, Hui Jiang, Xiaodong Deng, Yanping Dong, Tingbo Ding, Lu Zhou, Peng Men, Yong Chu, Renxiao Wang, Xian‐Cheng Jiang, De-yong Ye

Bioorganic & Medicinal Chemistry

DOI

2013

Identification of small molecule sphingomyelin synthase inhibitors

Xiaodong Deng, Lin Fu, Ya Ping Zhang, Yan Li, Lu Zhou, Bin Lou, Yue Li, Jibin Dong, Tingbo Ding, Xian‐Cheng Jiang, Renxiao Wang, Deyong Ye

European Journal of Medicinal Chemistry

DOI

2013

Design, Synthesis, and Biological Evaluation of Novel Dual Inhibitors of Secretory Phospholipase A2 and Sphingomyelin Synthase

Xing Gao, Haojun Gong, Peng Men, Lu Zhou, Deyong Ye

Chinese Journal of Chemistry

DOI

2012

Development, Validation, and Application of a Novel Method for Mammalian Sphingomyelin Synthase Activity Measurement

Xiaodong Deng, Hong Yuan Sun, Xing Gao, Haojun Gong, Wenbo Lu, Yong Chu, Lu Zhou, Deyong Ye

Analytical Letters

DOI

精选作品

期刊论文

Discovery of a Covalent Inhibitor Targeting the PHGDH Dimer Interface with Antitumor Efficacy

Design, Synthesis, and Evaluation of Phenylpyrrole Derivatives as Small-Molecule Activators of BAX

Discovery of 1-(Azetidin-3-ylmethyl)-1 H -benzo[ d ]imidazole Derivatives as Efficient GSTP1 Inhibitors for Gastric Cancer Treatment via Warhead Removal Strategy

靶向蛋白翻译后修饰的药物化学生物学研究

Biocatalytic- and Chemoproteomic-Guided Discovery of a PHGDH Inhibitor from Chemoenzymatic-Promoted DNA-Encoded Libraries Selection Platform

Expanding the Chemistry of Acyl Diazo Electrophile as a Tunable Warhead for Covalent Targeting of KRAS (G12D) Mutant

Discovery of N -(1,3,4-Thiadiazol-2-yl)amide Derivatives as Uncompetitive Inhibitors of 6-Phosphogluconate Dehydrogenase

Residue-Selective Inhibitors Discovery via Covalent DNA-Encoded Chemical Libraries with Diverse Warheads

Proteome‐Wide Data Guides the Discovery of Lysine‐Targeting Covalent Inhibitors Using DNA‐Encoded Chemical Libraries

靶向肿瘤代谢酶小分子药物研究进展

Discovery of a novel thiophene carboxamide analogue as a highly potent and selective sphingomyelin synthase 2 inhibitor for dry eye disease therapy

A phosphoglycerate mutase 1 allosteric inhibitor restrains TAM-mediated colon cancer progression

Cryo-EM structure of human sphingomyelin synthase and its mechanistic implications for sphingomyelin synthesis

ABPP-CoDEL: Activity-Based Proteome Profiling-Guided Discovery of Tyrosine-Targeting Covalent Inhibitors from DNA-Encoded Libraries

PGAM1 Inhibition Promotes HCC Ferroptosis and Synergizes with Anti‐PD‐1 Immunotherapy

Drug discovery by targeting the protein–protein interactions involved in autophagy

Adamantaniline Derivatives Target ATP5B to Inhibit Translation of Hypoxia Inducible Factor‐1α

Discovery of Small-Molecule Autophagy Inhibitors by Disrupting the Protein–Protein Interactions Involving Autophagy-Related 5

Benzo[d]isoxazole Derivatives as Hypoxia-Inducible Factor (HIF)-1α Inhibitors

Discovery of Non-Cysteine-Targeting Covalent Inhibitors by Activity-Based Proteomic Screening with a Cysteine-Reactive Probe

Design, synthesis, and biological evaluation of 1,3,6,7-tetrahydroxyxanthone derivatives as phosphoglycerate mutase 1 inhibitors

Novel octapeptide-DTX prodrugs targeting MMP-7 as effective agents for the treatment of colorectal cancer with lower systemic toxicity

Sphingomyelin synthase 2 facilitates M2-like macrophage polarization and tumor progression in a mouse model of triple-negative breast cancer

HKB99, an allosteric inhibitor of phosphoglycerate mutase 1, suppresses invasive pseudopodia formation and upregulates plasminogen activator inhibitor-2 in erlotinib-resistant non-small cell lung cancer cells

Chemoproteomic Profiling of a Pharmacophore-Focused Chemical Library

Site-Selective Phosphoglycerate Mutase 1 Acetylation by a Small Molecule

An allosteric PGAM1 inhibitor effectively suppresses pancreatic ductal adenocarcinoma

A Novel Allosteric Inhibitor of Phosphoglycerate Mutase 1 Suppresses Growth and Metastasis of Non-Small-Cell Lung Cancer

Synthesis and biological evaluation of anthraquinone derivatives as allosteric phosphoglycerate mutase 1 inhibitors for cancer treatment

Development of Anthraquinone Analogues as Phosphoglycerate Mutase 1 Inhibitors

Discovery, synthesis and anti-atherosclerotic activities of a novel selective sphingomyelin synthase 2 inhibitor

Discovery of 4-Benzyloxybenzo[d]isoxazole-3-amine Derivatives as Highly Selective and Orally Efficacious Human Sphingomyelin Synthase 2 Inhibitors that Reduce Chronic Inflammation in db/db Mice

The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors

Design and Synthesis of the Diazirine-based Clickable Photo-affinity Probe Targeting Sphingomyelin Synthase 2

Xanthone derivatives as phosphoglycerate mutase 1 inhibitors: Design, synthesis, and biological evaluation

Conformation and dynamics of the C-terminal region in human phosphoglycerate mutase 1

Discovery of the selective sphingomyelin synthase 2 inhibitors with the novel structure of oxazolopyridine

抗肿瘤代谢靶标磷酸甘油酸变位酶1及其抑制剂的研究进展

Discovery, synthesis and biological evaluation of 2-(4-(N-phenethylsulfamoyl)phenoxy)acetamides (SAPAs) as novel sphingomyelin synthase 1 inhibitors

Identification of small molecule sphingomyelin synthase inhibitors

Design, Synthesis, and Biological Evaluation of Novel Dual Inhibitors of Secretory Phospholipase A2 and Sphingomyelin Synthase

Development, Validation, and Application of a Novel Method for Mammalian Sphingomyelin Synthase Activity Measurement

会议论文

抗肿瘤代谢新靶点磷酸甘油酸变位酶1的发现及化学生物学研究

PGAM1的C端构象变化及功能的计算研究

书籍章节

Drug Development in the Field of Sphinogolipid Metabolism

研究方向