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作品数：67被引量：128H指数：5
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相关机构：北京大学北京师范大学复旦大学燕山大学更多>>
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Design, synthesis and pharmacological evaluation of 1,2,3,4-tetrahydrobenzofuro[2,3-c] pyridine derivatives as p21-activated kinase 4 inhibitors for treatment of pancreatic cancer
《Acta Pharmaceutica Sinica B》2025年第1期438-466,共29页Yang Li Yan Fang Xiaoyu Chen Linjiang Tong Fang Feng Qianqian Zhou Shulun Chen Jian Ding Hua Xie Ao Zhang 
support from the China National Innovation of Science and Technology-2030(Program of Brain Science and Brain-Inspired Intelligence Technology,2021ZD0204004);the National Natural Science Foundation of China(Grants Nos.82273767,82073073,82122045,and 82273948);the Major Projects for Shanghai Zhang jiang National Independent Innovation of China(ZJ2021-ZD-007);Innovative research team of high-level local universities in Shanghai(SHSMU-ZDCX20210802,China);the Project of Shanghai Institute of Materia Medica,CAS(SIMM0120231001,China);the High-level Innovative Research Institute,Department of Science and Technology of Guangdong Province(2021B0909050003,China).
The p21-activated kinase 4(PAK4),a key regulator of malignancy,is negatively correlated with immune infiltration and has become an emergent drug target of cancer therapy.Given the lack of high efficacy PAK4 inhibitors...
关键词：P21-activated kinase 4 Tetrahydrobenzofuro[2 3-clpyridine Structure-activity relationship Allosteric inhibitor Pharmacokinetics properties 
Identification of USP2 as a novel target to induce degradation of KRAS in myeloma cells
《Acta Pharmaceutica Sinica B》2024年第12期5235-5248,共14页Yingying Wang Youping Zhang Hao Luo Wei Wei Wanting Liu Weiwei Wang Yunzhao Wu Cheng Peng Yanjie Ji Jianfang Zhang Chujiao Zhu Wenhui Bai Li Xia Hu Lei Hanzhang Xu Leimiao Yin Wei Weng Li Yang Ligen Liu Aiwu Zhou Yueyue Wei Qi Zhu Weiliang Zhu Yongqing Yang Zhijian Xu Yingli Wu 
supported in part by grants from the National Natural Science Foundation of China(82170145,82322067,82100156,and 82374583);CAMS Innovation Fund for Medical Sciences(CIFMS):2019-I2M-5-051;Shanghai Science and Technology Commission(20ZR1430600,20JC1410100);Shanghai Municipal Commission of Health and Family Planning,NO.ZY(2021-2023)-0208;Shandong Provincial Natural Science Foundation(ZR2020QH095);China Postdoctoral Science Foundation funded project(2023M742311).
Inducing the degradation of KRAS represents a novel strategy to combat cancers with KRAS mutation.In this study,we identify ubiquitin-specific protease 2(USP2)as a novel deubiquitinating enzyme of KRAS in multiple mye...
关键词：Ubiquitin-specific protease 2 KRAS Gambogic acid Multiple myeloma DEGRADATION UBIQUITINATION Allosteric pocket DEUBIQUITINATION 
A phosphoglycerate mutase 1 allosteric inhibitor restrains TAM-mediated colon cancer progression
《Acta Pharmaceutica Sinica B》2024年第11期4819-4831,共13页Cheng Wang Minghao Zhang Shunyao Li Miaomiao Gong Ming-yu Luo Mo-cong Zhang Jing-Hua Zou Ningxiang Shen Lu Xu Hui-min Lei Ling Bi Liang Zhu Zhengting Wang Hong-zhuan Chen Lu Zhou Ying Shen 
National Natural Science Foundation of China(82073868);Science and Technology Commission of Shanghai Municipality(20S11900100 and 21TQ016,China);China Postdoctoral Science Foundation(2022M722138).
Colorectal cancer (CRC) is a prevalent malignant tumor often leading to liver metastasis and mortality. Despite some success with PD-1/PD-L1 immunotherapy, the response rate for colon cancer patients remains relativel...
关键词：Phosphoglyceratemutase 1 Allostericinhibitor Tumor-associated macrophages 
Identification of novel small-molecule inhibitors of SARS-CoV-2 by chemical genetics
《Acta Pharmaceutica Sinica B》2024年第9期4028-4044,共17页Chris Chun-Yiu Chan Qian Guo Jasper Fuk-Woo Chan Kaiming Tang Jian-Piao Cai Kenn Ka-Heng Chik Yixin Huang Mei Dai Bo Qin Chon Phin Ong Allen Wing-Ho Chu Wan-Mui Chan Jonathan Daniel Ip Lei Wen Jessica Oi-Ling Tsang Tong-Yun Wang Yubin Xie Zhenzhi Qin Jianli Cao Zi-Wei Ye Hin Chu Kelvin Kai-Wang To Xing-Yi Ge Tao Ni Dong-Yan Jin Sheng Cui Kwok-Yung Yuen Shuofeng Yuan 
National Natural Science Foundation of China(NSFC)/Research Grants Council(RGC)Joint Research Scheme(N_HKU767/22 and 82261160398);Health and Medical Research Fund(COVID190121);the Food and Health Bureau,The Government of the Hong Kong Special Administrative Region;the National Natural Science Foundation of China(32322087,32300134,and 82272337);Guangdong Natural Science Foundation(2023A1515012907);Health@-InnoHK,Innovation and Technology Commission,the Government of the Hong Kong Special Administrative Region;the Collaborative Research Fund(C7060-21G and C7002-23Y)and Theme-Based Research Scheme(T11-709/21-N)of the Research Grants Council,The Government of the Hong Kong Special Administrative Region;Partnership Programme of Enhancing Laboratory Surveillance and Investigation of Emerging Infectious Diseases and Antimicrobial Resistance for the Department of Health of the Hong Kong Special Administrative Region Government;Sanming Project of Medicine in Shenzhen,China(SZSM201911014);the High Level-Hospital Program,Health Commission of Guangdong Province,China;the research project of Hainan Academician Innovation Platform(YSPTZX202004);Emergency Collaborative Project of Guangzhou Laboratory(EKPG22-01);and the National Key R&D Program of China(projects 2021YFC0866100 and 2023YFC3041600);The University of Hong Kong Seed Fund for Collaborative Research(2207101537);and Hunan University(521119400156);donations of Providence Foundation Limited(in memory of the late Lui Hac Minh).
There are only eight approved small molecule antiviral drugs for treating COVID-19.Among them,four are nucleotide analogues(remdesivir,JT001,molnupiravir,and azvudine),while the other four are protease inhibitors(nirm...
关键词：SARS-CoV-2 High throughput screening Broad-spectrum antiviral treatment 3CLpro inhibitor Allosteric-site inhibitor Animal models Chemical genetics Reverse genetics 
Discovery of TK-642 as a highly potent,selective,orally bioavailable pyrazolopyrazine-based allosteric SHP2 inhibitor
《Acta Pharmaceutica Sinica B》2024年第8期3624-3642,共19页Kai Tang Shu Wang Siqi Feng Xinyu Yang Yueyang Guo Xiangli Ren Linyue Bai Bin Yu Hong-Min Liu Yihui Song 
the financial support from the Natural Science Foundation of China(Nos.U21A20416,32371317,22277110,and 82104279);Natural Science Foundation of Henan Province(No.222300420069,China);“Chunhui Plan”Cooperative Scientific Research Project of the Ministry of Education(No.HZKY20220280,China);State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University(KF-202303,China)。
Src homology-2-containing protein tyrosine phosphatase 2(SHP2)is a promising therapeutic target for cancer therapy.In this work,we presented the structure-guided design of 5,6-fused bicyclic allosteric SHP2 inhibitors...
关键词：Protein tyrosine phosphatase Pyrazolopyrazine SHP2 inhibitor Esophageal cancer 
Therapeutic potential of targeting protein tyrosine phosphatases in liver diseases
《Acta Pharmaceutica Sinica B》2024年第8期3295-3311,共17页Ao Wang Yi Zhang Xinting Lv Guang Liang 
supported by National Natural Science Foundation of China(81930108 to Guang Liang);Zhejiang Provincial Key Scientific Project(2021C03041 to Guang Liang,China).
Protein tyrosine phosphorylation is a post-translational modification that regulates protein structure to modulate demic organisms’homeostasis and function.This physiological process is regulated by two enzyme famili...
关键词：Tyrosine phosphorylation PTPs Signal transduction CLDs HCC Allosteric inhibitor PROTACs Drug development 
Allosteric DNAzyme-based encoder for molecular information transfer
《Chinese Chemical Letters》2024年第7期235-241,共7页Minghao Hu Tianci Xie Yuqiang Hu Longjie Li Ting Wang Tongbo Wu 
financially supported by the National Natural Science Foundation of China(No.82172372);the Opening Research Fund of State Key Laboratory of Digital Medical Engineering(No.2023-M04)。
Dynamic DNA nanotechnology plays a significant role in nanomedicine and information science due to its high programmability based on Watson-Crick base pairing and nanoscale dimensions.Intelligent DNA machines and netw...
关键词：DNAZYME ENCODER Nucleic acids DNA circuit DNA strand displacement Dynamic DNA nanotechnology 
Allosterically activating SHP2 by oleanolic acid inhibits STAT3-Th17 axis for ameliorating colitis
《Acta Pharmaceutica Sinica B》2024年第6期2598-2612,共15页Jinbo Hu Wen Liu Yi Zou Chenyang Jiao Jiazhen Zhu Qiang Xu Jianjun Zou Yang Sun Wenjie Guo 
supported by the National Natural Science Foundation of China(82173820,82073856,82273933);Fundamental Research Funds for the Central Universities(020814380160,China);Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine(ZYYCXTD-C-202208,China);the Young Scholar Foundation from Cyrus Tang Foundation(China).
Src homology 2 domain-containing tyrosine phosphatase 2(SHP2)is an essential tyrosine phosphatase that is pivotal in regulating various cellular signaling pathways such as cell growth,differentiation,and survival.The ...
关键词：Oleanolic acid SHP2 STAT3 TH17 COLITIS Allosteric activator 
Exploring structure-based drug discovery of GPCRs beyond the orthosteric binding site
《hLife》2024年第5期211-226,共16页Zhao Chen Xintong Ren Yu Zhou Niu Huang 
This work is supported by Beijing Municipal Science&Technology Commission(Z201100005320012 to N.H.)and Tsinghua University.
G-protein coupled receptors(GPCRs)are the largest family of druggable targets.In recent years,GPCR structural biology has made great advances,revealing the three-dimensional structures of many GPCRs and their interact...
关键词：G-protein coupled receptor(GPCR) allosteric pocket structure-based virtual screening(SBVS) negative allosteric modulator(NAM) positive allosteric modulator(PAM) artificial intelligence(AI) 
From bench to bedside: current development and emerging trend of KRAS-targeted therapy
《Acta Pharmacologica Sinica》2024年第4期686-703,共18页Yi Chen Qiu-pei Liu Hua Xie Jian Ding 
supported by grants from the National Natural Science Foundation of China(82273948);High-level Innovative Research Institute(2021B0909050003);State Key Laboratory of Drug Research(SKLDR-2023-TT-01 and SIMM2205KF-09).
Kirsten rat sarcoma 2 viral oncogene homolog (KRAS) is the most frequently mutated oncogene in human cancers with mutations predominantly occurring in codon 12. These mutations disrupt the normal function of KRAS by i...
关键词：KRAS mutation KRAS^(G12C)inhibitor Pan-KRAS inhibitor SHP2 allosteric inhibitor SOS1 inhibitor combination therapy 
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