Yu RAO's Lab

Research

This page showcases research articles published by Yu RAO’s lab in recent years.

Highlighted

A Dual-Target and Dual-Mechanism Design Strategy by Combining Inhibition and Degradation Together
A Dual-Target and Dual-Mechanism Design Strategy by Combining Inhibition and Degradation Together
Yongbo Liu, Xiuyun Sun, Qianlong Liu, Chi Han, Yu Rao
Journal of the American Chemical Society  ·  02 Dec 2024  ·  doi:10.1021/jacs.4c11930
BRD4-targeting PROTAC as a unique tool to study biomolecular condensates
BRD4-targeting PROTAC as a unique tool to study biomolecular condensates
Yi Shi, Yuan Liao, Qianlong Liu, Zhihao Ni, Zhenzhen Zhang, Minglei Shi, Pilong Li, Haitao Li, Yu Rao
Cell Discovery  ·  09 May 2023  ·  doi:10.1038/s41421-023-00544-0
Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently
Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently
Zimo Yang, Yonghui Sun, Zhihao Ni, Celi Yang, Yan Tong, Yujie Liu, Haitao Li, Yu Rao
Cell Research  ·  20 Aug 2021  ·  doi:10.1038/s41422-021-00533-6
A chemical approach for global protein knockdown from mice to non-human primates
A chemical approach for global protein knockdown from mice to non-human primates
Xiuyun Sun, Jun Wang, Xia Yao, Wen Zheng, Yang Mao, …, Jianguo Zhao, Rui-Ping Xiao, Xiuqin Zhang, Guangju Ji, Yu Rao
Cell Discovery  ·  05 Feb 2019  ·  doi:10.1038/s41421-018-0079-1
PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies
PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies
Yonghui Sun, Xingwang Zhao, Ning Ding, Hongying Gao, Yue Wu, …, Meng Zhao, Jinseok Hwang, Yuqin Song, Wanli Liu, Yu Rao
Cell Research  ·  06 Jun 2018  ·  doi:10.1038/s41422-018-0055-1
Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy
Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy
Liguo Wang, Xuejing Shao, Tianbai Zhong, Yue Wu, Aixiao Xu, …, Haiteng Deng, Bo Yang, Qiaojun He, Meidan Ying, Yu Rao
Nature Chemical Biology  ·  04 Mar 2021  ·  doi:10.1038/s41589-021-00742-5

All

2024

A Dual-Target and Dual-Mechanism Design Strategy by Combining Inhibition and Degradation Together
A Dual-Target and Dual-Mechanism Design Strategy by Combining Inhibition and Degradation Together
Yongbo Liu, Xiuyun Sun, Qianlong Liu, Chi Han, Yu Rao
Journal of the American Chemical Society  ·  02 Dec 2024  ·  doi:10.1021/jacs.4c11930
The application of PROTACs in immune-inflammation diseases
The application of PROTACs in immune-inflammation diseases
Chao Zhang, Xiuyun Sun, Peilu Song, Yu Rao
Bioorganic & Medicinal Chemistry  ·  01 Dec 2024  ·  doi:10.1016/j.bmc.2024.117967
Developing selective PI3K degraders to modulate both kinase and non-kinase functions
Developing selective PI3K degraders to modulate both kinase and non-kinase functions
Zimo Yang, Yan Tong, Yongbo Liu, Qianlong Liu, Zhihao Ni, Yuna He, Yu Rao
Chinese Chemical Letters  ·  01 Nov 2024  ·  doi:10.1016/j.cclet.2024.109577
PROTAC for Bruton s tyrosine kinase degradation alleviates inflammation in autoimmune diseases
PROTAC for Bruton’s tyrosine kinase degradation alleviates inflammation in autoimmune diseases
Can Zhu, Zimo Yang, Yuxiao Zhang, Zhenjun Li, Guangchen Li, …, Jingwen Wang, Yonghui Sun, Ning Ding, Yu Rao, Wanli Liu
Cell Discovery  ·  06 Aug 2024  ·  doi:10.1038/s41421-024-00711-x
CDK9 targeting PROTAC L055 inhibits ERα-positive breast cancer
CDK9 targeting PROTAC L055 inhibits ERα-positive breast cancer
Wenmin Chen, Yue Wu, Chuanyu Yang, Wenlong Ren, Lei Hou, …, Tingyue Wu, Yanjie Kong, Jiao Wu, Yu Rao, Ceshi Chen
Biomedicine & Pharmacotherapy  ·  01 Aug 2024  ·  doi:10.1016/j.biopha.2024.116972
PI3K PROTAC overcomes the lapatinib resistance in PIK3CA-mutant HER2 positive breast cancer
PI3K PROTAC overcomes the lapatinib resistance in PIK3CA-mutant HER2 positive breast cancer
Hongyan Zhang, Longlong Zhang, Yuna He, Dewei Jiang, Jian Sun, …, Yu Tang, Zimo Yang, Wenjing Liu, Yu Rao, Ceshi Chen
Cancer Letters  ·  01 Aug 2024  ·  doi:10.1016/j.canlet.2024.217112
Targeting Smurf1 to block PDK1 Akt signaling in KRAS-mutated colorectal cancer
Targeting Smurf1 to block PDK1–Akt signaling in KRAS-mutated colorectal cancer
Zhiqiang Peng, Wei Fang, Bo Wu, Ming He, Shaohua Li, …, Zhijie Chang, Yu Rao, Xueli Zhang, Chun-Ping Cui, Lingqiang Zhang
Nature Chemical Biology  ·  22 Jul 2024  ·  doi:10.1038/s41589-024-01683-5
Targeting the undruggables the power of protein degraders
Targeting the undruggables—the power of protein degraders
Chao Zhang, Yongbo Liu, Guangchen Li, Zhouli Yang, Chi Han, Xiuyun Sun, Chunquan Sheng, Ke Ding, Yu Rao
Science Bulletin  ·  01 Jun 2024  ·  doi:10.1016/j.scib.2024.03.056
Degradation Based Protein Profiling: A Case Study of Celastrol
Degradation‐Based Protein Profiling: A Case Study of Celastrol
Zhihao Ni, Yi Shi, Qianlong Liu, Liguo Wang, Xiuyun Sun, Yu Rao
Advanced Science  ·  25 Apr 2024  ·  doi:10.1002/advs.202308186

2023

Discovery of small molecule degraders for modulating cell cycle
Discovery of small molecule degraders for modulating cell cycle
Liguo Wang, Zhouli Yang, Guangchen Li, Yongbo Liu, Chao Ai, Yu Rao
Frontiers of Medicine  ·  01 Oct 2023  ·  doi:10.1007/s11684-023-1027-5
Developing potent BTKC481S PROTACs for ibrutinib-resistant malignant lymphoma
Developing potent BTKC481S PROTACs for ibrutinib-resistant malignant lymphoma
Yonghui Sun, Xin Luo, Zimo Yang, Wenxing Lv, Lixia Chen, Hua Li, Yu Rao
Chinese Chemical Letters  ·  01 Jun 2023  ·  doi:10.1016/j.cclet.2022.107924
BRD4-targeting PROTAC as a unique tool to study biomolecular condensates
BRD4-targeting PROTAC as a unique tool to study biomolecular condensates
Yi Shi, Yuan Liao, Qianlong Liu, Zhihao Ni, Zhenzhen Zhang, Minglei Shi, Pilong Li, Haitao Li, Yu Rao
Cell Discovery  ·  09 May 2023  ·  doi:10.1038/s41421-023-00544-0
Design, synthesis, and evaluation of BTK-targeting PROTACs with optimized bioavailability i in vitro i and i in vivo i
Design, synthesis, and evaluation of BTK-targeting PROTACs with optimized bioavailability in vitro and in vivo
Yonghui Sun, Zimo Yang, Zhimin Zhang, Zhen Li, Liubin Guo, Hao Pan, Xin Luo, Dongzhou Liu, Yu Rao
RSC Medicinal Chemistry  ·  01 Jan 2023  ·  doi:10.1039/d3md00216k
PROTACs targeting epigenetic proteins
PROTACs targeting epigenetic proteins
Chao Zhang, Yuna He, Xiuyun Sun, Wenyi Wei, Yanlong Liu, Yu Rao
Acta Materia Medica  ·  01 Jan 2023  ·  doi:10.15212/AMM-2023-0039

2022

PROTACs: great opportunities for academia and industry an update from 2020 to 2021
PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
Ming He, Chaoguo Cao, Zhihao Ni, Yongbo Liu, Peilu Song, Shuang Hao, Yuna He, Xiuyun Sun, Yu Rao
Signal Transduction and Targeted Therapy  ·  09 Jun 2022  ·  doi:10.1038/s41392-022-00999-9
PROTAC mediated FKBP12 degradation enhances Hepcidin expression via BMP signaling without immunosuppression activity
PROTAC mediated FKBP12 degradation enhances Hepcidin expression via BMP signaling without immunosuppression activity
Tianbai Zhong, Xiuyun Sun, Li Yu, Yongbo Liu, Xin Lin, Yu Rao, Wei Wu
Signal Transduction and Targeted Therapy  ·  27 May 2022  ·  doi:10.1038/s41392-022-00970-8
CDK2 Inhibition Enhances Antitumor Immunity by Increasing IFN Response to Endogenous Retroviruses
CDK2 Inhibition Enhances Antitumor Immunity by Increasing IFN Response to Endogenous Retroviruses
Yu Chen, Qiaomei Cai, Chaohu Pan, Wancheng Liu, Lili Li, …, Xiaorong Li, Liguo Wang, Yu Rao, Heng Yang, Genhong Cheng
Cancer Immunology Research  ·  18 Feb 2022  ·  doi:10.1158/2326-6066.CIR-21-0806
Chemistries of bifunctional PROTAC degraders
Chemistries of bifunctional PROTAC degraders
Chaoguo Cao, Ming He, Liguo Wang, Yuna He, Yu Rao
Chemical Society Reviews  ·  01 Jan 2022  ·  doi:10.1039/d2cs00220e

2021

Rapamycin recruits SIRT2 for FKBP12 deacetylation during mTOR activity modulation in innate immunity
Rapamycin recruits SIRT2 for FKBP12 deacetylation during mTOR activity modulation in innate immunity
Lin Hu, Fuxian Chen, Chao Wu, Jun Wang, Si-si Chen, …, Yu Sun, Zhijie Chang, Wei Deng, Cheng Luo, Y. Eugene Chin
iScience  ·  01 Nov 2021  ·  10.1016/j.isci.2021.103177
Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently
Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently
Zimo Yang, Yonghui Sun, Zhihao Ni, Celi Yang, Yan Tong, Yujie Liu, Haitao Li, Yu Rao
Cell Research  ·  20 Aug 2021  ·  doi:10.1038/s41422-021-00533-6
Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation
Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation
Ming He, Wenxing Lv, Yu Rao
Frontiers in Cell and Developmental Biology  ·  22 Jun 2021  ·  doi:10.3389/fcell.2021.685106
Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy
Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy
Liguo Wang, Xuejing Shao, Tianbai Zhong, Yue Wu, Aixiao Xu, …, Haiteng Deng, Bo Yang, Qiaojun He, Meidan Ying, Yu Rao
Nature Chemical Biology  ·  04 Mar 2021  ·  doi:10.1038/s41589-021-00742-5

2020

Global PROTAC Toolbox for Degrading BCR ABL Overcomes Drug-Resistant Mutants and Adverse Effects
Global PROTAC Toolbox for Degrading BCR–ABL Overcomes Drug-Resistant Mutants and Adverse Effects
Yiqing Yang, Hongying Gao, Xiuyun Sun, Yonghui Sun, Yueping Qiu, Qinjie Weng, Yu Rao
Journal of Medicinal Chemistry  ·  13 Jul 2020  ·  10.1021/acs.jmedchem.0c00967
FAK-targeting PROTAC as a chemical tool for the investigation of non-enzymatic FAK function in mice
FAK-targeting PROTAC as a chemical tool for the investigation of non-enzymatic FAK function in mice
Hongying Gao, Chunwei Zheng, Jian Du, Yue Wu, Yonghui Sun, Chunsheng Han, Kehkooi Kee, Yu Rao
Protein & Cell  ·  25 May 2020  ·  10.1007/s13238-020-00732-8
Degradation versus Inhibition: Development of Proteolysis-Targeting Chimeras for Overcoming Statin-Induced Compensatory Upregulation of 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase
Degradation versus Inhibition: Development of Proteolysis-Targeting Chimeras for Overcoming Statin-Induced Compensatory Upregulation of 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase
Mei-Xin Li, Yiqing Yang, Qiuye Zhao, Yue Wu, Lei Song, …, Ming He, Hongying Gao, Bao-Liang Song, Jie Luo, Yu Rao
Journal of Medicinal Chemistry  ·  22 Apr 2020  ·  10.1021/acs.jmedchem.0c00339
PROTAC Technology: Opportunities and Challenges
PROTAC Technology: Opportunities and Challenges
Hongying Gao, Xiuyun Sun, Yu Rao
ACS Medicinal Chemistry Letters  ·  12 Mar 2020  ·  doi:10.1021/acsmedchemlett.9b00597

2019

PROTACs as Potential Therapeutic Agents for Cancer Drug Resistance
PROTACs as Potential Therapeutic Agents for Cancer Drug Resistance
Xiuyun Sun, Yu Rao
Biochemistry  ·  29 Oct 2019  ·  doi:10.1021/acs.biochem.9b00848
Design, Synthesis, and Evaluation of Highly Potent FAK-Targeting PROTACs
Design, Synthesis, and Evaluation of Highly Potent FAK-Targeting PROTACs
Hongying Gao, Yue Wu, Yonghui Sun, Yiqing Yang, Guangbiao Zhou, Yu Rao
ACS Medicinal Chemistry Letters  ·  22 Oct 2019  ·  doi:10.1021/acsmedchemlett.9b00372
Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders
Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders
Shang Su, Zimo Yang, Hongying Gao, Haiyan Yang, Songbiao Zhu, …, Qing Li, Sarat Chandarlapaty, Haiteng Deng, Wei Wu, Yu Rao
Journal of Medicinal Chemistry  ·  22 Jul 2019  ·  doi:10.1021/acs.jmedchem.9b00871
Degradation of Bruton s tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas
Degradation of Bruton’s tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas
Yonghui Sun, Ning Ding, Yuqin Song, Zimo Yang, Wanli Liu, Jun Zhu, Yu Rao
Leukemia  ·  11 Mar 2019  ·  doi:10.1038/s41375-019-0440-x
A chemical approach for global protein knockdown from mice to non-human primates
A chemical approach for global protein knockdown from mice to non-human primates
Xiuyun Sun, Jun Wang, Xia Yao, Wen Zheng, Yang Mao, …, Jianguo Zhao, Rui-Ping Xiao, Xiuqin Zhang, Guangju Ji, Yu Rao
Cell Discovery  ·  05 Feb 2019  ·  doi:10.1038/s41421-018-0079-1
Developing potent PROTACs tools for selective degradation of HDAC6 protein
Developing potent PROTACs tools for selective degradation of HDAC6 protein
Zixuan An, Wenxing Lv, Shang Su, Wei Wu, Yu Rao
Protein & Cell  ·  02 Jan 2019  ·  doi:10.1007/s13238-018-0602-z
Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule
Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule
Qiuye Zhao, Tianlong Lan, Shang Su, Yu Rao
Chemical Communications  ·  01 Jan 2019  ·  doi:10.1039/c8cc07813k
Plasticity in designing PROTACs for selective and potent degradation of HDAC6
Plasticity in designing PROTACs for selective and potent degradation of HDAC6
Haiyan Yang, Wenxing Lv, Ming He, Haiteng Deng, Haitao Li, Wei Wu, Yu Rao
Chemical Communications  ·  01 Jan 2019  ·  doi:10.1039/C9CC08509B

2018

PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies
PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies
Yonghui Sun, Xingwang Zhao, Ning Ding, Hongying Gao, Yue Wu, …, Meng Zhao, Jinseok Hwang, Yuqin Song, Wanli Liu, Yu Rao
Cell Research  ·  06 Jun 2018  ·  doi:10.1038/s41422-018-0055-1