骆国顺｜中国药科大学｜学者主页

2026

Lysine-targeted covalent inhibitors: mechanistic advances, pharmacological perspectives and translational challenges

Mingjin Luo, Luyu Ma, Guoshun Luo, Hua Xiang

Biochemical Pharmacology

DOI

2026

The PROTAC milestone: FDA approval of vepdegestrant (ARV-471) for ESR1-mutated breast cancer

Xin Lin, Hua Xiang, Guoshun Luo

Drug Discovery Today

DOI

2026

Optimization of a Second-Generation, Highly Selective Polθ/PARP1 Dual Inhibitor with Improved Pharmacokinetics and Potent Activity against HR-Deficient Tumors

Luyu Ma, Mingzhe Zhong, Yingxuan Chang, Mingjin Luo, Xinyan Liu, Xiaofan Ge, Sitian Xu, Yun Zhang, Ziye Liu, Hua Xiang, Guoshun Luo

Journal of Medicinal Chemistry

DOI

2026

Discovery of an orally bioavailable selenium-containing Polθ inhibitor with a dual mechanism of DNA damage and immune activation for HR-deficient cancers

Luyu Ma, Mingjin Luo, Mingjin Luo, Xiangchi Liu, Jinyue Yang, Jianyu Li, Mingzhe Zhong, Xinyan Liu, Maoxu Xiao, Hua Xiang, Guoshun Luo

European Journal of Medicinal Chemistry

DOI

2026

A patent review of DNA polymerase theta (Polθ) targeted therapies (2019–2025)

Luyu Ma, Mingjin Luo, Hua Xiang, Guoshun Luo

Expert Opinion on Therapeutic Patents

DOI

2026

Approved Steroidal Drugs (2000–2025): A Medicinal Chemistry Perspective

Jiacheng Zhu, Guoshun Luo, Hua Xiang

Journal of Medicinal Chemistry

DOI

2025

Targeted degradation of Werner syndrome helicase (WRN) via ligand-directed covalent hydrophobic tagging

Wenxiang Tao, Jiacheng Zhu, Zixuan Fu, Xiangchi Liu, Shunlin Tang, Hua Xiang, Guoshun Luo

European Journal of Medicinal Chemistry

DOI

2025

Discovery of a Highly Potent and Selective Tyrosine Kinase 2 (TYK2) Degrader with In Vivo Therapeutic Efficacy in a Murine Psoriasis Model

Shuangshuang Xiong, Jiaqi Yang, Ming Yang, Maoxu Xiao, Si Ha, Wenxiang Tao, Luyu Ma, Chenxuan Ji, Hua Xiang, Guoshun Luo

Journal of Medicinal Chemistry

DOI

2024

Discovery of a highly potent, N-terminal domain-targeting degrader of AR-FL/AR-V7 for the treatment of prostate cancer

Si Ha, Chenxuan Ji, Jiaqi Yang, Maoxu Xiao, Ziyi Xu, Wei-Wei Pan, Hua Xiang, Guoshun Luo

European Journal of Medicinal Chemistry

DOI

2024

Targeting Protein Kinase, Membrane-Associated Tyrosine/Threonine 1 (PKMYT1) for Precision Cancer Therapy: From Discovery to Clinical Trial

Ming Yang, Hua Xiang, Guoshun Luo

Journal of Medicinal Chemistry

DOI

2024

Targeting focal adhesion kinase (FAK) for cancer therapy: FAK inhibitors, FAK-based dual-target inhibitors and PROTAC degraders

Ming Jen Yang, Hua Xiang, Guoshun Luo

Biochemical Pharmacology

DOI

2024

Dual-target inhibitors based on ERα: Novel therapeutic approaches for endocrine resistant breast cancer

Shuangshuang Xiong, Ke Song, Hua Xiang, Guoshun Luo

European Journal of Medicinal Chemistry

DOI

2024

Structure–Activity Relationship (SAR) Studies of Novel Monovalent AR/AR-V7 Dual Degraders with Potent Efficacy against Advanced Prostate Cancer

Maoxu Xiao, Si Ha, Jiacheng Zhu, Wenxiang Tao, Zixuan Fu, Hanlin Wei, Qiangqiang Hou, Guoshun Luo, Hua Xiang

Journal of Medicinal Chemistry

DOI

2024

Discovery and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors

Luyu Ma, Wei Chen, Ming Yang, Si Ha, Shuangshuang Xiong, Jiacheng Zhu, Hua Xiang, Guoshun Luo

Journal of Medicinal Chemistry

DOI

2023

X-ray crystallography study and optimization of novel benzothiophene analogs as potent selective estrogen receptor covalent antagonists (SERCAs) with improved potency and safety profiles

Chengfeng Bai, Yang Lv, Shuangshuang Xiong, Shuangjie Wu, Lin Qi, Shengnan Ren, Meiqi Zhu, Haijuan Dong, Hongtao Shen, Zhaoxing Li, Yinxue Zhu, Hui Ye, Haiping Hao, Yibei Xiao, Hua Xiang, Guoshun Luo

Bioorganic Chemistry

DOI

2023

Structural optimization of tetrahydroisoquinoline-hydroxamate hybrids as potent dual ERα degraders and HDAC inhibitors

Shuangshuang Xiong, Xin Wang, Meiqi Zhu, Ke Song, Yefan Li, Jiaqi Yang, Xinyan Liu, Mofei Liu, Haijuan Dong, Mingqi Chen, Deying Chen, Hua Xiang, Guoshun Luo

Bioorganic Chemistry

DOI

2022

Novel 6-amino-1,3,5-triazine derivatives as potent BTK inhibitors: structure-activity relationship (SAR) analysis and preliminary mechanism investigation

Maoxu Xiao, Meiqi Zhu, Shuangjie Wu, Luyu Ma, Lin Qi, Si Ha, Shuangshuang Xiong, Mingqi Chen, Deying Chen, Guoshun Luo, Hua Xiang

Bioorganic Chemistry

DOI

2022

Novel 11β-substituted estradiol conjugates: Transition from ERα agonizts to effective PROTAC degraders

Guoshun Luo, Xinyu Li, Xin Lin, Xiang Lu, Zhenbang Li, Hua Xiang

The Journal of Steroid Biochemistry and Molecular Biology

DOI

2021

Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer

Guoshun Luo, Xin Lin, Shengnan Ren, Shuangjie Wu, Xin Wang, Luyu Ma, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2021

Benzothiophene derivatives as selective estrogen receptor covalent antagonists: Design, synthesis and anti-ERα activities

Chengfeng Bai, Shuangjie Wu, Shengnan Ren, Meiqi Zhu, Guoshun Luo, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2021

Synthesis and evaluation of novel thiosemicarbazone and semicarbazone analogs with both anti-proliferative and anti-metastatic activities against triple negative breast cancer

Chengfeng Bai, Shuangjie Wu, Shengnan Ren, Meiqi Zhu, Guoshun Luo, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2021

Discovery of novel 2H-chromene-3-carbonyl derivatives as selective estrogen receptor degraders (SERDs): Design, synthesis and biological evaluation

Xiang Lu, Yu Teng, Xin Lin, Maoxu Xiao, Chenna Liu, Xinglong Chi, Yulan Zhang, Guoshun Luo, Hua Xiang

Bioorganic Chemistry

DOI

2020

Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator

Guoshun Luo, Xin Lin, Zhenbang Li, Maoxu Xiao, Xinyu Li, Dayong Zhang, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2020

Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity

Yu Teng, Xinyu Li, Shengnan Ren, Yu Cheng, Kun Xi, Hongtao Shen, Wenzhuo Ma, Guoshun Luo, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2020

Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance

Xin Lin, Hua Xiang, Guoshun Luo

European Journal of Medicinal Chemistry

DOI

2020

Discovery of potent and highly selective covalent inhibitors of Bruton’s tyrosine kinase bearing triazine scaffold

Yu Teng, Xiang Lü, Maoxu Xiao, Zhenbang Li, Yumei Zou, Shengnan Ren, Yu Cheng, Guoshun Luo, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2020

A new class of 1,3,5-triazine-based selective estrogen receptor degraders (SERDs): Lead optimization, molecular docking and dynamic simulation

Xiang Lu, Ali Huang, Maoxu Xiao, Liang Sun, Jiashun Mao, Guoshun Luo, Hua Xiang

Bioorganic Chemistry

DOI

2019

Progress in PD-1/PD-L1 pathway inhibitors: From biomacromolecules to small molecules

Xin Lin, Xiang Lu, Guoshun Luo, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2018

3, 9-di-O-substituted coumestrols incorporating basic amine side chains act as novel apoptosis inducers with improved pharmacological selectivity

Guoshun Luo, Zhengpu Tang, Xinyu Li, Qiangqiang Hou, Yu Chen, Kejing Lao, Hua Xiang

Bioorganic Chemistry

DOI

2018

Structure-guided design and synthesis of isoflavone analogs of GW4064 with potent lipid accumulation inhibitory activities

Rongmao Qiu, Guoshun Luo, Xuerong Cai, Linyi Liu, Mingqi Chen, Deying Chen, Qidong You, Hua Xiang

Bioorganic & Medicinal Chemistry Letters

DOI

2018

Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ

Linyi Liu, Bingyu Shi, Xinyu Li, Xiangqian Wang, Xiang Lu, Xuerong Cai, Ali Huang, Guoshun Luo, Qidong You, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2018

Lipid accumulation inhibitory activities of novel isoxazole-based chenodeoxycholic acids: Design, synthesis and preliminary mechanism study

Rongmao Qiu, Guoshun Luo, Xinyu Li, Fan Zheng, Haolin Li, Jin Zhang, Qidong You, Hua Xiang

Bioorganic & Medicinal Chemistry Letters

DOI

2018

Lipid reducing activity of novel cholic acid (CA) analogs: Design, synthesis and preliminary mechanism study

Guoshun Luo, Zhouyang Qian, Rongmao Qiu, Qidong You, Hua Xiang

Bioorganic Chemistry

DOI

2017

Design, synthesis and biological evaluation of novel 3-substituted 4-anilino-coumarin derivatives as antitumor agents

Guoshun Luo, Moses Muyaba, Weiting Lyu, Zhichao Tang, Ruheng Zhao, Qian Xu, Qidong You, Hua Xiang

Bioorganic & Medicinal Chemistry Letters

DOI

2016

Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents

Zhichao Tang, Cheng-Zhe Wu, Tianlin Wang, Kejing Lao, Yejun Wang, Linyi Liu, Moses Muyaba, Pei Xu, Conghui He, Guoshun Luo, Zhouyang Qian, Shaoxiong Niu, Lijun Wang, Ying Wang, Hong Xiao, Qidong You, Hua Xiang

European Journal of Medicinal Chemistry

DOI

骆国顺

精选作品

期刊论文

Lysine-targeted covalent inhibitors: mechanistic advances, pharmacological perspectives and translational challenges

The PROTAC milestone: FDA approval of vepdegestrant (ARV-471) for ESR1-mutated breast cancer

Optimization of a Second-Generation, Highly Selective Polθ/PARP1 Dual Inhibitor with Improved Pharmacokinetics and Potent Activity against HR-Deficient Tumors

Discovery of an orally bioavailable selenium-containing Polθ inhibitor with a dual mechanism of DNA damage and immune activation for HR-deficient cancers

A patent review of DNA polymerase theta (Polθ) targeted therapies (2019–2025)

Approved Steroidal Drugs (2000–2025): A Medicinal Chemistry Perspective

Targeted degradation of Werner syndrome helicase (WRN) via ligand-directed covalent hydrophobic tagging

Discovery of a Highly Potent and Selective Tyrosine Kinase 2 (TYK2) Degrader with In Vivo Therapeutic Efficacy in a Murine Psoriasis Model

Discovery of a highly potent, N-terminal domain-targeting degrader of AR-FL/AR-V7 for the treatment of prostate cancer

Targeting Protein Kinase, Membrane-Associated Tyrosine/Threonine 1 (PKMYT1) for Precision Cancer Therapy: From Discovery to Clinical Trial

Targeting focal adhesion kinase (FAK) for cancer therapy: FAK inhibitors, FAK-based dual-target inhibitors and PROTAC degraders

Dual-target inhibitors based on ERα: Novel therapeutic approaches for endocrine resistant breast cancer

Structure–Activity Relationship (SAR) Studies of Novel Monovalent AR/AR-V7 Dual Degraders with Potent Efficacy against Advanced Prostate Cancer

Discovery and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors

X-ray crystallography study and optimization of novel benzothiophene analogs as potent selective estrogen receptor covalent antagonists (SERCAs) with improved potency and safety profiles

Structural optimization of tetrahydroisoquinoline-hydroxamate hybrids as potent dual ERα degraders and HDAC inhibitors

Novel 6-amino-1,3,5-triazine derivatives as potent BTK inhibitors: structure-activity relationship (SAR) analysis and preliminary mechanism investigation

Novel 11β-substituted estradiol conjugates: Transition from ERα agonizts to effective PROTAC degraders

Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer

Benzothiophene derivatives as selective estrogen receptor covalent antagonists: Design, synthesis and anti-ERα activities

Synthesis and evaluation of novel thiosemicarbazone and semicarbazone analogs with both anti-proliferative and anti-metastatic activities against triple negative breast cancer

Discovery of novel 2H-chromene-3-carbonyl derivatives as selective estrogen receptor degraders (SERDs): Design, synthesis and biological evaluation

Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator

Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity

Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance

Discovery of potent and highly selective covalent inhibitors of Bruton’s tyrosine kinase bearing triazine scaffold

A new class of 1,3,5-triazine-based selective estrogen receptor degraders (SERDs): Lead optimization, molecular docking and dynamic simulation

Progress in PD-1/PD-L1 pathway inhibitors: From biomacromolecules to small molecules

3, 9-di-O-substituted coumestrols incorporating basic amine side chains act as novel apoptosis inducers with improved pharmacological selectivity

Structure-guided design and synthesis of isoflavone analogs of GW4064 with potent lipid accumulation inhibitory activities

Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ

Lipid accumulation inhibitory activities of novel isoxazole-based chenodeoxycholic acids: Design, synthesis and preliminary mechanism study

Lipid reducing activity of novel cholic acid (CA) analogs: Design, synthesis and preliminary mechanism study

Design, synthesis and biological evaluation of novel 3-substituted 4-anilino-coumarin derivatives as antitumor agents

Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents