作者： Huang, Yunyuan;Wang, Jiqun;Liu, Jiaqi;Shi, Donglei;Li, Xiaokang;...

期刊： Journal of Chemical Information and Modeling,2022年62(21):5223-5232 ISSN：1549-9596

通讯作者： Yixiang Xu<&wdkj&>Jian Li

作者机构： [Xu, Yixiang; Wang, Manjiong; Wang, Jiqun; Lu, Taotao; Shi, Donglei; Huang, Yunyuan; Li, Xiaokang; Li, Jian] East China Univ Sci, Sch Pharm, State Key Lab Bioreactor Engn, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China.;[Liu, Jiaqi] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol CCNU, Minist Educ, Wuhan 430079, Peoples R China.;[Xia, Conglong; Jiang, Bei; Li, Jian] Dali Univ, Coll Pharm & Chem, Dali 671000, Peoples R China.;[Lin, Houwen] Shanghai Jiao Tong Univ, Renji Hosp, Res Ctr Marine Drugs, Sch Med,State Key Lab Oncogenes & Related Genes, Shanghai 200127, Peoples R China.;[Li, Jian] Tongji Univ, Shanghai Peoples Hosp 10, Clin Med Sci & Tech Innovat Ctr, Sch Med, Shanghai 200092, Peoples R China.

通讯机构： [Yixiang Xu; Jian Li] S;State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Mei Long Road, Shanghai 200237, China<&wdkj&>College of Pharmacy and Chemistry, Dali University, 5 Xue Ren Road, Dali 671000, China<&wdkj&>Clinical Medicine Scientific and Technical Innovation Center, Shanghai Tenth People’s Hospital, Tongji University School of Medicine, Shanghai 200092, China<&wdkj&>State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Mei Long Road, Shanghai 200237, China

摘要： Combination drugs, characterized by high efficacy and few side effects, have received extensive attention from pharmaceutical companies and researchers for the treatment of complex diseases such as heart failure (HF). Traditional combination drug discovery depends on large-scale high-throughput experimental approaches that are time-consuming and costly. Herein we developed a novel, rapid, and potentially universal computer-guided combination drug-network-screening approach based on a set of databases and web services that are easy for individuals to obtain and operate, and we discovered for the first time that the menthol-allethrin combination screened by this approach exhibited a significant synergistic cardioprotective effect <i>in vitro</i>. Further mechanistic studies indicated that allethrin and menthol could synergistically block calcium channels. Allethrin bound to the central cavity of the voltage-dependent L-type calcium channel subunit alpha-1S (CACNA1S) lead to a conformational change in an allosteric site of CACNA1S, thereby enhancing the binding of menthol to this allosteric site. In summary, we reported a potentially universal computational approach to combination drug screening that has been used to discover a new combination of menthol-allethrin against HF <i>in vitro</i>, providing a new synergistic mechanism and prospective agent for HF treatment.

语种： 英文

作者： Fang, Qie;Qin, Ying;Wang, Hengjia;Xu, Weiqing;Yan, Hongye;...

期刊： Analytical Chemistry,2022年94(31):11030-11037 ISSN：0003-2700

通讯作者： Zhu, Chengzhou(czzhu@ccnu.edu.cn)

作者机构： [Qin, Ying; Zhu, Chengzhou; Yan, Hongye; Li, Jinli; Jiao, Lei; Gu, Wenling; Xu, Weiqing; Fang, Qie; Liu, Mingwang; Wei, Xiaoqian; Luo, Xin; Wang, Hengjia; Hu, Liuyong] Cent China Normal Univ, Coll Chem, Int Joint Res Ctr Intelligent Biosensing Technol &, Key Lab Pesticides, Wuhan 430079, Peoples R China.

通讯机构： [Chengzhou Zhu] K;Key Laboratory of Pesticides and Chemical Biology of Ministry of Education, International Joint Research Center for Intelligent Biosensing Technology and Health, College of Chemistry, Central China Normal University, Wuhan 430079, P.R. China

摘要： Effective glucose surveillance provides a strong guarantee for the high-quality development of human health. Au nanomaterials possess compelling applications in nonenzymatic electrochemical glucose biosensors owing to superior catalytic performances and intriguing biocompatibility properties. However, it has been a grand challenge to accurately control the architecture and composition of Au nanomaterials to optimize their optical, electronic, and magnetic properties for further improving the performance of electrocatalytic sensing. Herein, ultra-low content Bi-anchored Au aerogels are synthesized via a one-step reduction strategy. Benefiting from the unique structure of aerogels as well as the synergistic effect between Au and Bi, the optimized Au200Bi aerogels greatly boost the activity of glucose oxidation compared with Au aerogels. Under plasmon resonance excitation, bimetallic Au200Bi aerogels with wider photics-dependent properties further show plasmon-promoted glucose electro-oxidation activity, which is derived from the photothermal and photoelectric effects caused by the local surface plasmon resonance. Thanks to the enhanced performance, a nonenzymatic electrochemical glucose biosensor is constructed to detect glucose with high sensitivity. This plasmon-promoted electrocatalytic activity through the synergetic strategy of bimetallic aerogels has potential applications in various research fields. © 2022 American Chemical Society. All rights reserved.

语种： 英文

作者： Fu, Yi-Xuan;Guo, Wu-Yingzheng;Wang, Nan;Dai, Yi-Jie;Zhang, Zi-Ye;...

期刊： Analytical Chemistry,2022年94(50):17692-17699 ISSN：0003-2700

通讯作者： Yang, Wen-Chao(tomyang@mail.ccnu.edu.cn)

作者机构： [Yang, Guang-Fu; Wang, Nan; Yang, Wen-Chao; Dai, Yi-Jie; Guo, Wu-Yingzheng; Fu, Yi-Xuan; Zhang, Zi-Ye; Sun, Xin-Lin] Cent China Normal Univ, Coll Chem, Int Joint Res Ctr Intelligent Biosensor Technol &, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.

通讯机构： [Wen-Chao Yang] K;Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, International Joint Research Center for Intelligent Biosensor Technology and Health, College of Chemistry, Central China Normal University, Wuhan430079, P.R. China

摘要： Plant diseases caused by bacteria have become one of the serious problems that threaten human food security, which led to the remarkable reduction of agricultural yields and economic loss. Nitroreductase (NTR), as an important biomarker, is highly expressed in bacteria, and the level of NTR is closely related to the progression of pathogen infection. Therefore, the design of small-molecule fluorescent sensors targeting NTR is of great significance for the detection and diagnosis of plant pathogenic bacteria. In this study, a new fluorescent sensor targeting NTR was discovered and then successfully applied to the imaging of zebrafish and pathogenic bacteria. Most importantly, the developed sensor achieved the real-time diagnosis of Brassica napus L. infected with bacteria, which provides a promising tool for examining the temporal and spatial infection of plant pathogens in precision agriculture. © 2022 American Chemical Society. All rights reserved.

语种： 英文

作者： Fu, Yi-Xuan;Zhang, Zi-Ye;Guo, Wu-Yingzheng;Dai, Yi-Jie;Wang, Zheng-Yu;...

期刊： Pest Management Science,2022年78(11):4947-4955 ISSN：1526-498X

通讯作者： Wen-Chao Yang<&wdkj&>Guang-Fu Yang

作者机构： [Yang, Guang-Fu; Wang, Zheng-Yu; Yang, Wen-Chao; Dai, Yi-Jie; Guo, Wu-Yingzheng; Fu, Yi-Xuan; Zhang, Zi-Ye] Cent China Normal Univ, Coll Chem, Int Joint Res Ctr Intelligent Biosensor Technol &, Key Lab Pesticide & Chem Biol,Minist Educ, 152 Luoyu Rd, Wuhan 430079, Hubei, Peoples R China.

通讯机构： [Wen-Chao Yang; Guang-Fu Yang] K;Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, International Joint Research Center for Intelligent Biosensor Technology and Health, College of Chemistry, Central China Normal University, Wuhan, P. R. China

关键词： herbicide;4-hydroxyphenylpyruvate dioxygenase;fluorescent sensors;imaging

摘要： BACKGROUND: 4-Hydroxyphenylpyruvate dioxygenase (HPPD), playing a critical role in vitamin E and plastoquinone biosynthesis in plants, has been recognized as one of the most important targets for herbicide discovery for over 30 years. Structure-based rational design of HPPD inhibitors has received more and more research interest. However, a critical challenge in the discovery of new HPPD inhibitors is the common inconsistency between molecular-level HPPD-based bioevaluation and the weed control efficiency in fields, due to the unpredictable biological processes of absorption, distribution, metabolism, and excretion. RESULTS: In this study, we developed a fluorescent-sensing platform of efficient in vivo screening for HPPD-targeted herbicide discovery. The refined sensor has good capability of in situ real-time fluorescence imaging of HPPD in living cells and zebrafish. More importantly, it enabled the direct visible monitoring of HPPD inhibition in plants in a real-time manner. CONCLUSION: We developed a highly efficient in vivo fluorescent screening method for HPPD-targeted herbicide discovery. This discovery not only offers a promising tool to advance HPPD-targeted herbicide discovery, but it also demonstrates a general path to develop the highly efficient, target-based, in vivo screening for pesticide discovery. © 2022 Society of Chemical Industry.

语种： 英文

作者： Liu, Yijia;Feng, Shumin;Gong, Shengyi;Feng, Guoqiang

期刊： Analytical Chemistry,2022年94(50):17439-17447 ISSN：0003-2700

通讯作者： Feng, Guoqiang(gf256@mail.ccnu.edu.cn)

作者机构： [Feng, Guoqiang; Gong, Shengyi; Liu, Yijia; Feng, Shumin] Cent China Normal Univ, Coll Chem, Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.

通讯机构： [Guoqiang Feng] K;Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, 152 Luoyu Road, Wuhan 430079, China

摘要： Nonalcoholic fatty liver disease (NAFLD) is a global health issue. Peroxynitrite and liver viscosity have recently been found to be potential biomarkers of NAFLD. Therefore, it is of great significance to develop dual-response fluorescent probes for simultaneous detecting peroxynitrite and viscosity. We report herein a new probe (CQ) that can simultaneously detect peroxynitrite and viscosity at two independent fluorescent channels without signal crosstalk. CQ shows high selectivity, rapid response, good water solubility, low cytotoxicity, and mitochondrial localization properties. In particular, CQ responds sensitively to viscosity and peroxynitrite with off-on fluorescence changes at 710 and 505 nm, respectively. The wavelength gap between these two channels is more than 200 nm, ensuring that there is no signal crosstalk during detection. With this property, the probe was applied to simultaneously detect mitochondrial viscosity and peroxynitrite and image the changes of liver viscosity and peroxynitrite concentration during the pathogenesis of NAFLD. All results show that the CQ probe is a powerful tool for simultaneous detection of viscosity and peroxynitrite and provides a potential new diagnostic method for NAFLD. © 2022 American Chemical Society. All rights reserved.

语种： 英文

作者： Li, Ya-Qian;Yan, Cheng;Wang, Xi-Feng;Xian, Mao-Ying;Zou, Guo-Qing;...

期刊： ACS INFECTIOUS DISEASES,2022年8(10):2161-2170 ISSN：2373-8227

通讯作者： Luo, R.;Liu, Z.

作者机构： [Luo, Rui; Li, Ya-Qian] Huazhong Agr Univ, Coll Vet Med, State Key Lab Agr Microbiol, Wuhan 430070, Hubei, Peoples R China.;[Wang, Xi-Feng; Zou, Guo-Qing; Yan, Cheng; Xian, Mao-Ying; Liu, Zheng] Cent China Normal Univ, Coll Chem, Int Joint Res Ctr Intelligent Biosensing Technol &, Key Lab Pesticide & Chem Biol,Minist Educ,Hubei In, Wuhan 430079, Hubei, Peoples R China.;[Gao, Xiao-Fei] East China Univ Technol, Jiangxi Key Lab Mass Spectrometry & Instrumentat, Nanchang 330013, Jiangxi, Peoples R China.

通讯机构： [Rui Luo] S;[Zheng Liu] K;Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, Hubei International Scientific and Technological Cooperation Base of Pesticide and Green Synthesis, International Joint Research Center for Intelligent Biosensing Technology and Health, College of Chemistry, Central China Normal University, Wuhan, Hubei 430079, PR China<&wdkj&>State Key Laboratory of Agricultural Microbiology, College of Veterinary Medicine, Huazhong Agricultural University, Wuhan, Hubei 430070, PR China

关键词： RBD-Fc;SARS-CoV-2;adjuvant;iNKT cell;subunit vaccine;α-galactosylceramide

摘要： Adjuvants are essential components of vaccines. Invariant natural killer T (iNKT) cells are a distinct subset of T cells that function to bridge the innate and adaptive immunities and are capable of mediating strong and rapid responses to a range of diseases, including cancer and infectious disease. An increasing amount of evidence suggests that iNKT cells can help fight viral infection. In particular, iNKT-secreting IL-4 is a key mediator of humoral immunity and has a positive correlation with the levels of neutralizing antibodies. As iNKT cell agonists, αGC glycolipid (α-galactosylceramide, or KRN7000) and its analogues as vaccine adjuvants have begun to provide vaccinologists with a new toolset. Herein we found that a new iNKT-cell agonist αGC-CPOEt elicited a strong cytokine response with increased IL-4 production. Remarkably, after three immunizations, SARS-CoV-2 RBD-Fc adjuvanted by αGC-CPOEt evoked robust neutralizing antibody responses that were about 5.5-fold more than those induced by αGC/RBD-Fc and 25-fold greater than those induced by unadjuvanted RBD-Fc. These findings imply that αGC-CPOEt could be investigated further as a new COVID-19 vaccine adjuvant to prevent current and future infectious disease outbreaks. © 2022 American Chemical Society.

语种： 英文

作者： Li, Qian;Zhao, Jingjing;Shang, Huan;Ma, Zhong;Cao, Haiyan;...

期刊： Environmental Science & Technology,2022年56(9):5830-5839 ISSN：0013-936X

通讯作者： Zhang, Dieqing(dqzhang@shnu.edu.cn)

作者机构： [Li, Qian; Cao, Haiyan; Zhao, Jingjing; Li, Hexing; Zhang, Dieqing; Li, Guisheng; Zhou, Yue] Shanghai Normal Univ, Shanghai Frontiers Sci Ctr Biomimet Catalysis, Key Lab Resource Chem, Joint Int Res Lab Resource Chem,Minist Educ, Shanghai 200234, Peoples R China.;[Li, Qian; Cao, Haiyan; Zhao, Jingjing; Li, Hexing; Zhang, Dieqing; Li, Guisheng; Zhou, Yue] Shanghai Normal Univ, Shanghai Frontiers Sci Ctr Biomimet Catalysis, Shanghai Key Lab Rare Earth Funct Mat, Shanghai 200234, Peoples R China.;[Shang, Huan] Cent China Normal Univ, Coll Chem, Inst Environm & Appl Chem, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.;[Ma, Zhong] Univ Waterloo, Dept Chem Engn, Waterloo, ON N2L 3G1, Canada.;[Ma, Zhong] Univ Waterloo, Waterloo Inst Nanotechnol WIN, Waterloo, ON N2L 3G1, Canada.

通讯机构： [Dieqing Zhang] T;The Education Ministry Key Lab of Resource Chemistry, Joint International Research Laboratory of Resource Chemistry, Ministry of Education, and Shanghai Key Laboratory of Rare Earth Functional Materials, Shanghai Frontiers Science Center of Biomimetic Catalysis, Shanghai Normal University, Shanghai 200234, P. R. China

关键词： NOx oxidation;hydroxyl radicals;photocatalysis;singlet oxygen;synergistic effect

摘要： Learning from the important role of porphyrin-based chromophores in natural photosynthesis, a bionic photocatalytic system based on tetrakis (4-carboxyphenyl) porphyrin-coupled TiO2was designed for photo-induced treating low-concentration NOxindoor gas (550 parts per billion), achieving a high NO removal rate of 91% and a long stability under visible-light (λ ≥ 420 nm) irradiation. Besides the great contribution of the conventional •O2-reactive species, a synergic effect between a singlet oxygen (1O2) and mobile hydroxyl radicals (•OHf) was first illustrated for removing NOxindoor gas (1O2+ 2NO → 2NO2, NO2+ •OHf→ HNO3), inhibiting the production of the byproducts of NO2. This work is helpful for understanding the surface mechanism of photocatalytic NOxoxidation and provides a new perspective for the development of highly efficient air purification systems. © 2022 American Chemical Society. All rights reserved.

语种： 英文

作者： Tu, Le;Li, Chonglu;Liu, Chang;Bai, Suya;Yang, Jingfang;...

期刊： Chemical Communications,2022年58(65):9068-9071 ISSN：1359-7345

通讯作者： Xu, Liying(aying0923@foxmail.com);Xiong, Xiaoxing(xiaoxingxiong@whu.edu.cn);Sun, Yao(sunyaogbasp@ccnu.edu.cn)

作者机构： [Tu, Le; Xiong, Xiaoxing] Wuhan Univ, Remin Hosp, Dept Neurosurg, Wuhan 430079, Peoples R China.;[Zhang, Xian; Tu, Le; Bai, Suya; Sun, Yao; Li, Chonglu; Yang, Jingfang; Liu, Chang] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[Xu, Liying] Wuhan Univ, Zhongnan Hosp, Wuhan 430062, Peoples R China.

通讯机构： [Liying Xu] Z;[Xiaoxing Xiong] D;[Yao Sun] K;Key Laboratory of Pesticide and Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, P. R. China<&wdkj&>Zhongnan Hospital of Wuhan University, Wuhan 430062, P. R. China<&wdkj&>Department of Neurosurgery, Remin Hospital of Wuhan University, Wuhan 430079, P. R. China

摘要： Herein, we construct a series of Ru(ii) metallacycles with multimodal chemo-phototherapeutic properties, which exhibited much higher anticancer activity and better cancer-cell selectivity than cisplatin. The antitumor mechanism could be ascribed to the activation of caspase 3/7 and the resulting apoptosis. These results open new possibilities for Ru(ii) metallacycles in biomedicine. © 2022 The Royal Society of Chemistry.

语种： 英文

作者： Li, Chonglu;Guan, Xiaofang;Zhang, Xian;Zhou, Di;Son, Subin;...

期刊： Biosensors and Bioelectronics,2022年216:114620 ISSN：0956-5663

通讯作者： Kim, J.S.;Sun, Y.;Guo, Z.

作者机构： [Deng, Mengtian; Guo, Zhenzhong; Li, Chonglu] Wuhan Univ Sci & Technol, Hubei Prov Key Lab Occupat Hazard Identificat & Co, Wuhan 430065, Peoples R China.;[Zhang, Xian; Guan, Xiaofang; Sun, Yao; Li, Chonglu] Cent China Normal Univ, Coll Chem, Key Lab Pesticides & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.;[Zhou, Di] Huazhong Univ Sci & Technol, Tongji Hosp, Tongji Med Coll, Expt Med Ctr, Wuhan 430074, Peoples R China.;[Xu, Yunjie; Kim, Jong Seung; Son, Subin] Korea Univ, Dept Chem, Seoul 02841, South Korea.

通讯机构： [Kim, J.S.] D;[Sun, Y.] K;[Guo, Z.] H;Department of Chemistry, Korea University, Seoul, 02841, South Korea<&wdkj&>Key Laboratory of Pesticides and Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan, 430079, China

关键词： Disease diagnosis;NIR-II bioimaging Small-molecule fluorophores;Preclinical practice

摘要： Due to the low autofluorescence and deep-photo penetration, the second near-infrared region fluorescence imaging technology (NIR-II, 1000–2000 nm) has been widely utilized in basic scientific research and preclinical practice throughout the past decade. The most attractive candidates for clinical translation are organic NIR-II fluorophores with a small-molecule framework, owing to their low toxicity, high synthetic repeatability, and simplicity of chemical modification. In order to enhance the translation of small molecule applications in NIR-II bioimaging, NIR-II fluorescence imaging technology has evolved from its usage in cells to the diagnosis of diseases in large animals and even humans. Although several examples of NIR-II fluorescence imaging have been used in preclinical studies, there are still many challenges that need to be addressed before they can finally be used in clinical settings. In this paper, we reviewed the evolution of the chemical structures and photophysical properties of small-molecule fluorophores, with an emphasis on their biomedical applications ranging from small animals to humans. We also explored the potential of small-molecule fluorophores. © 2022 Elsevier B.V.

语种： 英文

作者： Cheng, Jing*;Huang, Xiaolan;Chen, Linfeng;Yan, Ling;Zhu, Fei;...

期刊： Analytica Chimica Acta,2022年1192:339374 ISSN：0003-2670

通讯作者： Cheng, Jing;Li, Haibing

作者机构： [Huang, Xiaolan; Yan, Ling; Li, Haibing; Cheng, Jing; Li, HB; Chen, Linfeng; Zhu, Fei] Cent China Normal Univ, Coll Chem, Inst Environm Chem, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.

通讯机构： [Cheng, J; Li, HB] C;Cent China Normal Univ, Coll Chem, Inst Environm Chem, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.

关键词： Artificial nanochannel membrane;Molecularly imprinted polymer;Surface grafting technique;Triphenyl phosphate;Ultra-sensitive electrochemical sensor

摘要： Driven by the urgent need for the determination of trace level triphenyl phosphate (TPhP) present in environment, a simple, rapid and ultrasensitive sensor has been fabricated for detection of TPhP by directly measuring transmembrane current. The transmembrane containing artificial nanochannel named polyethylene terephthalate (PET) nanochannel membrane is designed to be grafted by TPhP molecularly imprinted polymers (TPhP-MIPs) on its outer surface and inner surface of nanochannel. After the fabricated membrane banded TPhP, the transmembrane current decreased. The rate of current change is linearly proportional to the logarithm value of TPhP concentrations in the range of 0.001 ng mL−1 -800 ng mL−1. Meanwhile, the limit of detection (LOD) was 0.0003 ng mL−1. This LOD value is much lower than most results acquired by using chromatography-mass spectrometry and electrochemistry (EC) sensor based on the functionalization of electrode, whereas the cost of our fabricated EC sensor is much lower. The newly developed sensor is suitable for real-time or field detection of TPhP. The interference of analogs and non-analogs with similar structure of TPhP can be effectively avoided. The sensor not only exhibits high selectivity for TPhP, but also shows ultrasensitive assay for measuring TPhP in real environmental water. © 2021 Elsevier B.V.

语种： 英文

作者： Wen, Wuqiang;Cao, Hongxuan;Xu, Yixiang;Ren, Yanliang;Rao, Li;...

期刊： JOURNAL OF MEDICINAL CHEMISTRY,2022年65(13):9126-9143 ISSN：0022-2623

通讯作者： Yanliang Ren<&wdkj&>Yunyuan Huang<&wdkj&>Jian Wan

作者机构： [Rao, Li; Shao, Xubo; Wen, Wuqiang; Liu, Jiaqi; Wu, Lixia; Wan, Jian; Chen, Han; Ren, Yanliang; Cao, Hongxuan; Huang, Yunyuan] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol CCNU, Minist Educ, Wuhan 430079, Peoples R China.;[Xu, Yixiang; Ren, Yanliang; Huang, Yunyuan] East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China.;[Su, Chen; Peng, Chao] Zhangjiang Lab, Natl Facil Prot Sci Shanghai, Shanghai 201210, Peoples R China.

通讯机构： [Yanliang Ren; Yunyuan Huang; Jian Wan] K;Key Laboratory of Pesticide & Chemical Biology (CCNU), Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, China<&wdkj&>Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China<&wdkj&>Key Laboratory of Pesticide & Chemical Biology (CCNU), Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, China

摘要： With a resurgence of covalent drugs, there is an urgent need for the identification of new moieties capable of cysteine bond formation. Herein, we report on the N-acylamino saccharin moieties capable of novel covalent reactions with cysteine. Their utility as alternative electrophilic warheads was demonstrated through the covalent modification of fructose-1,6-bisphosphatase (FBPase), a promising target associated with cancer and type 2 diabetes. The cocrystal structure of title compound W8 bound with FBPase unexpectedly revealed that the N-acylamino saccharin moiety worked as an electrophile warhead that covalently modified the noncatalytic C128 site in FBPase while releasing saccharin, suggesting a previously undiscovered covalent reaction mechanism of saccharin derivatives with cysteine. Treatment of title compound W8 displayed potent inhibition of glucose production in vitro and in vivo. This newly discovered reactive warhead supplements the current repertoire of cysteine covalent modifiers while avoiding some of the limitations generally associated with established moieties. © 2022 American Chemical Society. All rights reserved.

语种： 英文

作者： Nie, Gang;Zhou, Yinxing;Song, Mengzi;Xu, Jingya;Cui, Zheng;...

期刊： ANALYTICAL METHODS,2022年14(19):1847-1855 ISSN：1759-9660

通讯作者： Wang, KP;Zhang, Y;Chen, DG

作者机构： [Wang, KP; Wang, Kaiping; Xu, Jingya; Nie, Gang; Song, Mengzi; Zhou, Yinxing] Huazhong Univ Sci & Technol, Tongji Med Coll Pharm, Hubei Key Lab Nat Med Chem & Resource Evaluat, Wuhan, Peoples R China.;[Zhang, Yu; Cui, Zheng; Zhang, Y] Huazhong Univ Sci & Technol, Union Hosp Tongji Med Coll, Wuhan, Peoples R China.;[Chen, Dugang; Chen, DG; Feng, Yangzhen] Wuhan Inst Technol, Sch Chem Engn & Pharm, Key Lab Green Chem Proc, Minist Educ, Wuhan, Peoples R China.;[Wang, Huiling] Cent China Normal Univ, Int Joint Res Ctr Intelligent Biosensing Technol, Chem Biol Ctr, Coll Chem,Key Lab Pesticide & Chem Biol,Minist Ed, Wuhan, Peoples R China.

通讯机构： [Chen, DG ] W;[Wang, KP ; Zhang, Y ] H;Huazhong Univ Sci & Technol, Tongji Med Coll Pharm, Hubei Key Lab Nat Med Chem & Resource Evaluat, Wuhan, Peoples R China.;Huazhong Univ Sci & Technol, Union Hosp Tongji Med Coll, Wuhan, Peoples R China.;Wuhan Inst Technol, Sch Chem Engn & Pharm, Key Lab Green Chem Proc, Minist Educ, Wuhan, Peoples R China.

摘要： Acute alcoholic liver injury (AALI) is hard to diagnose on account of no obvious clinical symptoms, and thereby it easily develops into serious liver diseases and threatens people's health. However, traditional methods for detecting AALI are far from satisfactory due to the low sensitivity, invasiveness and non-visualization, and the development of new techniques is in urgent demand. Near-infrared (NIR)-II fluorescence imaging has been widely studied in biochemistry and biomedicine. As the blood flow velocity of the liver is closely related to the progression of AALI, herein, a NIR-II fluorescent nanoprobe, NTPB-NPs, was applied to diagnose AALI by monitoring the fluorescence intensity changes in the liver caused by the variations of the blood flow velocity. More importantly, when medication was applied to alleviate the liver injury of AALI mice, NTPB-NPs could also track the therapeutic effect in situ. In this study, the relationship between hepatic vascular velocity and the progression of AALI was confirmed with NTPB-NPs via NIR-II imaging. To the best of our knowledge, this is the first time that a NIR-II fluorescence imaging technique has been used to diagnose AALI mice and evaluate the therapeutic effect on AALI mice. This study may also provide a potential NIR-II imaging agent for clinical research to improve the management of liver injury related diseases. © 2022 The Royal Society of Chemistry

语种： 英文

作者： Peng, Xing;Chen, Na;Wei, Kai;Li, Shengbiao;Shang, Huan;...

期刊： Science of The Total Environment,2022年838(Pt 3):156336 ISSN：0048-9697

通讯作者： Chen, N.

作者机构： [Wei, Kai; Li, Shengbiao; Zhang, Lizhi; Peng, Xing; Shang, Huan; Sun, Hongwei; Chen, Na] Cent China Normal Univ, Inst Environm & Appl Chem, Coll Chem, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.

通讯机构： Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, Institute of Environmental & Applied Chemistry, College of Chemistry, Central China Normal University, Wuhan, China

关键词： Calcium hydroxide;Fluoride removal;Magnetic separation;Zero-valent iron

摘要： The removal of concentrated fluoride in acidic wastewater by the conventional Ca(OH)(2) method is challenged by the insufficient efficiency and difficult separation of fine CaF(2) precipitate. Herein, we construct a strategy to tackle these challenges by coupling zero-valent iron (ZVI) with Ca(OH)(2). ZVI reduces fluoride concentration from 12,000 to 3980 mg L(-1) under optimal conditions primarily through the in-situ growth of porous FeF(2)·4H(2)O shell on its surface, which simultaneously assists fluoride removal via adsorption. The residual fluoride after ZVI treatment then decreases to 6.74 mg L(-1) via precipitation with Ca(OH)(2). Interestingly, the iron ions dissolved from ZVI also participate in the precipitation to form magnetite. This co-precipitation reinforces the fluoride removal and meanwhile endows the resulted precipitates with magnetism, thus enabling the perfect solid-liquid separation by the magnetic field before discharge. The application prospect of this coupling strategy is further verified by its ability in decreasing the concentrations of fluoride and other coexisting heavy metals (Zn(2+), Cd(2+) and Pb(2+)) in real smeltery wastewater below their discharge limitations. This study provides a promising strategy for the treatment of concentrated fluoride in acidic wastewater and also highlights ZVI as a good candidate to couple with conventional methods for enhanced pollution control.

语种： 英文

作者： Li, Mengna;Tang, Yuchen;Zhao, Rumeng;Gao, Tingjuan;Zhang, Lizhi

期刊： Journal of Hazardous Materials,2022年433:128809 ISSN：0304-3894

通讯作者： Tingjuan Gao

作者机构： [Zhang, Lizhi; Li, Mengna; Tang, Yuchen; Zhao, Rumeng; Gao, Tingjuan] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.

通讯机构： [Tingjuan Gao] K;Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, China

关键词： *Contaminated lands;*Hexavalent chromium;*MicroProbing imaging platform;*Rapid ultrasensitive detection;*Soil and groundwater

摘要： Rapid detection methods are needed to investigate the environmental quality risk of soil and groundwater in contaminated lands. Currently there is lack of rapid detection methods to sensitively and accurately analyze contaminations of hexavalent chromium in soil due to the challenge of complex sample pretreatment or expensive instrumentation. Here we report a rapid accurate detection platform for quantifying hexavalent chromium in soil and groundwater with ultrasensitivity. The platform consists of a novel sensor of microProbing beads and a portable microscope. Each microProbing bead was a nanoliter reactor to selectively sequestrate Cr (VI) with the enrichment factor up to 150 ×. The microProbing beads presented the signal uniformity of ~97% for the statistical colorimetric imaging analysis. Combined with a miniaturized microscope, the microProbing beads allowed for detecting aqueous Cr (VI) and soluble Cr (VI) in soil within 45 min. The platform achieved high sensitivity with the detection limits of 0.003 ppb for aqueous Cr (VI) and 0.07 ppm for soil Cr (VI). It accurately detected soil and groundwater samples from a chromium contaminated land in Yangtze River Basin of China. The consistency to the laboratory standard methods was achieved with the low cost of ~0.20 US dollar per test. The microProbing imaging platform with the operational simplicity and device portability is highly promising for the field analysis of Cr (VI) in contaminated lands. © 2022 Elsevier B.V.

语种： 英文

作者： Li, Junrong;Wuethrich, Alain;Zhang, Zhen;Wang, Jing;Lin, Lynlee L.;...

期刊： Analytical Chemistry,2022年94(42):14573-14582 ISSN：0003-2700

通讯作者： Wang, Jing(jing.wang@fjnu.edu.cn);Behren, Andreas(Andreas.Behren@onjcri.org.au);Wang, Yuling(yuling.wang@mq.edu.au);Trau, Matt(m.trau@uq.edu.au)

作者机构： [Li, Junrong] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, R China, Wuhan 430079, Peoples R China.;[Wuethrich, Alain; Trau, Matt; Zhang, Zhen; Li, Junrong] Univ Queensland, Australian Inst Bioengn & Nanotechnol, Ctr Personalized Nanomed, Brisbane, Qld 4072, Australia.;[Lin, Lynlee L.] Univ Queensland, Diamantina Inst, Dermatol Res Ctr, Brisbane, Qld 4102, Australia.;[Wang, Jing] Fujian Normal Univ, Key Lab OptoElect Sci & Technol Med, Fujian Prov Key Lab Photon Technol, Minist Educ, R China, Fuzhou 350007, Peoples R China.;[Behren, Andreas] La Trobe Univ, Oliva Newton John Canc Res Inst, Sch Canc Med, Heidelberg, Vic 3086, Australia.

通讯机构： [Jing Wang] K;[Andreas Behren] O;[Yuling Wang] S;[Matt Trau] C;School of Natural Sciences, Faculty of Science and Engineering, Macquarie University, Sydney, NSW2109, Australia<&wdkj&>Centre for Personalized Nanomedicine, Australian Institute for Bioengineering and Nanotechnology, The University of Queensland, Brisbane, QLD4072, Australia<&wdkj&>School of Chemistry and Molecular Biosciences, The University of Queensland, Brisbane, QLD4072, Australia<&wdkj&>Key Laboratory of OptoElectronic Science and Technology for Medicine of Ministry of Education, Fujian Provincial Key Laboratory of Photonics Technology, Fujian Normal University, Fuzhou350007, P. R. China<&wdkj&>Oliva Newton-John Cancer Research Institute, School of Cancer Medicine, La Trobe University, Heidelberg, VIC3086, Australia<&wdkj&>Department of Medicine, University of Melbourne, Heidelberg, VIC3010, Australia

摘要： Immune checkpoint blockade (ICB) therapy has achieved remarkable success in many cancers including melanoma. However, ICB therapy benefits only a small proportion of patients and produces severe side effects for some patients. Thus, there is an urgent need to identify patients who are more likely to respond to ICB therapy to improve outcomes and minimize side effects. To predict ICB therapy responses, we design a surface-enhanced Raman scattering (SERS) assay for multiplex profiling of circulating tumor cells (CTCs) under basal and interferon-γ(IFN-γ) stimulation. Through simultaneous ensemble and single-cell measurements of CTCs, the SERS assay can reveal tumor heterogeneity and offer a comprehensive CTC phenotype for decision-making. Anisotropic gold-silver alloy nanoboxes are utilized as SERS plasmonic substrates for improved signal readouts of CTC surface biomarkers. By generating a unique CTC signature with four surface biomarkers, the developed assay enables the differentiation of CTCs from three different patient-derived melanoma cell lines. Significantly, in a cohort of 14 melanoma patients who received programmed cell death-1 blockade therapy, the changes of CTC signature induced by IFN-γstimulation to CTCs show the potential to predict responders. We expect that the SERS assay can help select patients for receiving ICB therapy in other cancers. © 2022 American Chemical Society. All rights reserved.

语种： 英文

作者： Wang, Jian;Wen, Yu;Zhou, Shi-Hao;Zhang, Hai-Wei;Peng, Xiao-Qian;...

期刊： JOURNAL OF MEDICINAL CHEMISTRY,2022年65(3):2558-2570 ISSN：0022-2623

通讯作者： Rui Gong<&wdkj&>Guang-Fu Yang<&wdkj&>Jun Guo

作者机构： [Wang, Jian; Yang, Guang-Fu; Zhang, Ru-Yan; Wen, Yu; Yin, Xu-Guang; Peng, Xiao-Qian; Guo, Jun; Zhou, Shi-Hao] Cent China Normal Univ, Coll Chem,Hubei Int Sci & Technol Cooperat Base P, Int Joint Res Ctr Intelligent Biosensing Technol, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.;[Gong, Rui; Zhang, Hai-Wei] Chinese Acad Sci, Ctr Biosafety Megasci, Wuhan Inst Virol, CAS Key Lab Special Pathogens & Biosafety, Wuhan 430071, Peoples R China.;[Qiu, Hong] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China.

通讯机构： Key Laboratory of Pesticide and Chemical Biology, Ministry of Education, International Joint Research Center for Intelligent Biosensing Technology and Health, Hubei International Scientific and Technological Cooperation Base of Pesticide and Green Synthesis, College of Chemistry, Central China Normal University, Wuhan, China

摘要： Safe and effective vaccines against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and its variants are the best approach to successfully combat the COVID-19 pandemic. The receptor-binding domain (RBD) of the viral spike protein is a major target to develop candidate vaccines. α-Galactosylceramide (αGalCer), a potent invariant natural killer T cell (iNKT) agonist, was site-specifically conjugated to the N-terminus of the RBD to form an adjuvant-protein conjugate, which was anchored on the liposome surface. This is the first time that an iNKT cell agonist was conjugated to the protein antigen. Compared to the unconjugated RBD/αGalCer mixture, the αGalCer-RBD conjugate induced significantly stronger humoral and cellular responses. The conjugate vaccine also showed effective cross-neutralization to all variants of concern (B.1.1.7/alpha, B.1.351/beta, P.1/gamma, B.1.617.2/delta, and B.1.1.529/omicron). These results suggest that the self-adjuvanting αGalCer-RBD has great potential to be an effective COVID-19 vaccine candidate, and this strategy might be useful for designing various subunit vaccines. © 2022 American Chemical Society. All rights reserved.

语种： 英文

作者： Wu, Nannan;Zhong, Hong;Zhang, Yu;Wei, Xiaoqian;Jiao, Lei;...

期刊： Biosensors and Bioelectronics,2022年216:114609 ISSN：0956-5663

通讯作者： Chengzhou Zhu

作者机构： [Huang, Jiajia; Zhu, Chengzhou; Zhang, Yu; Wei, Xiaoqian; Wu, Nannan; Jiao, Lei; Gu, Wenling; Wang, Hengjia; Wu, Zhichao] Cent China Normal Univ, Coll Chem, Int Joint Res Ctr Intelligent Biosensing Technol &, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.;[Zhong, Hong; Beckman, Scott P.] Washington State Univ, Sch Mech & Mat Engn, Pullman, WA 99164 USA.

通讯机构： [Chengzhou Zhu] K;Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, International Joint Research Center for Intelligent Biosensing Technology and Health, College of Chemistry, Central China Normal University, Wuhan, 430079, PR China

关键词： Atomically dispersed metal catalysts;Electrocatalysis;Electrochemical sensors;Ru(3) site catalysts;Uric acid

摘要： Rational design and construction of electrochemical sensing platforms with high sensitivity and selectivity is one of the challenges in practical application. Although single-atom catalysts (SACs) have attracted extensive attention, atomically dispersed metal catalysts (ADCs) with multi-atom sites can further compensate for the deficiencies of SACs, which have gradually been a research hotspot in recent years. Herein, atomically dispersed Ru(3) site catalyst (Ru(3)/NC) is employed to catalyze small biomolecule oxidation, which exhibits much superior electrocatalytic ability of uric acid (UA) to Ru single-atom catalyst (Ru(1)/NC). What's more, theoretical calculations reveal that the enhanced performance is mainly derived from the dominant electronic structure of ADCs with multi-atom sites compared to SACs, leading to the more favorable adsorption of hydroxy anion groups, which can serve as one part of the active moiety and "promoter" to achieve the fast oxidation of small biomolecules. Our findings provide a new paradigm for designing promising catalysts to realize highly sensitive and selective small biomolecule detection and explore the catalytic mechanisms of small biomolecules at the atomic scale.

语种： 英文

作者： Shi, Yanbiao;Yang, Zhiping;Shi, Lujia;Li, Hao;Liu, Xupeng;...

期刊： Environmental Science & Technology,2022年56(20):14478-14486 ISSN：0013-936X

通讯作者： Li, Hao(hao_li@sjtu.edu.cn);Zhang, Lizhi(zhanglizhi@sjtu.edu.cn)

作者机构： [Zhang, Lizhi; Shi, Yanbiao; Li, Hao] Shanghai Jiao Tong Univ, Sch Environm Sci & Engn, Shanghai 200240, Peoples R China.;[Zhang, Lizhi; Liang, Chuan; Liu, Xupeng; Yang, Zhiping; Cheng, Jundi; Shi, Yanbiao; Guo, Furong; Zhang, Xu; Liu, Xiao; Ai, Zhihui; Cao, Shiyu; Shi, Lujia] Cent China Normal Univ, Coll Chem, Inst Environm & Appl Chem, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.

通讯机构： [Hao Li; Lizhi Zhang] S;School of Environmental Science and Engineering, Shanghai Jiao Tong University, Shanghai 200240, P. R. China<&wdkj&>Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, Institute of Environmental & Applied Chemistry, College of Chemistry, Central China Normal University, Wuhan 430079, P. R. China<&wdkj&>School of Environmental Science and Engineering, Shanghai Jiao Tong University, Shanghai 200240, P. R. China

关键词： O2 activation;photocatalysis;excitonic effects;NO oxidation;surface boronizing

摘要： The photocatalytic O2activation for pollutant removal highly depends on the controlled generation of desired reactive oxygen species (ROS). Herein, we demonstrate that the robust excitonic effect of BiOBr nanosheets, which is prototypical for singlet oxygen (1O2) production to partially oxidize NO into a more toxic intermediate NO2, can be weakened by surface boronizing via inducing a staggered band alignment from the surface to the bulk and simultaneously generating more surface oxygen vacancy (VO). The staggered band alignment destabilizes excitons and facilitates their dissociation into charge carriers, while surface VOtraps electrons and efficiently activates O2into a superoxide radical (•O2-) via a one-electron-transfer pathway. Different from 1O2 •O2-enables the complete oxidation of NO into nitrate with high selectivity that is more desirable for safe indoor NO remediation under visible light irradiation. This study provides a facile excitonic effect manipulating method for layered two-dimensional photocatalysts and sheds light on the importance of managing ROS production for efficient pollutant removal. © 2022 American Chemical Society. All rights reserved.

语种： 英文

作者： Li, Yu;Li, Wenjie;Xu, Weiwei;Huang, Jinmei;Sun, Zhongyue*;...

期刊： Chemical Communications,2022年58(66):9278-9281 ISSN：1359-7345

通讯作者： Sun, Zhongyue;Liao, Tangbin;Xu, Chuanlai;Cheng, Jing;Li, Haibing

作者机构： [Li, Yu; Xu, Chuanlai; Li, Haibing; Cheng, Jing] Jiangnan Univ, State Key Lab Food Sci & Technol, Wuxi, Jiangsu, Peoples R China.;[Li, Yu; Li, Wenjie; Huang, Jinmei; Li, Haibing; Xu, Weiwei; Cheng, Jing] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol CCNU, Minist Educ, Wuhan 430079, Peoples R China.;[Sun, Zhongyue] Hubei Univ Chinese Med, Sch Lab Med, Wuhan 430065, Peoples R China.;[Liao, Tangbin] Hubei Univ Chinese Med, Sch Pharm, Wuhan 430065, Peoples R China.;[Kovaleva, Elena G.] Ural Fed Univ, Dept Technol Organ Synth, Mira St 28, Ekaterinburg 620002, Russia.

通讯机构： [Zhongyue Sun; Tangbin Liao; Chuanlai Xu; Jing Cheng; Haibing Li] S;School of Laboratory Medicine, Hubei University of Chinese Medicine, Wuhan 430065, P. R. China<&wdkj&>State Key Laboratory of Food Science and Technology, Jiangnan University, China<&wdkj&>School of Pharmacy, Hubei University of Chinese Medicine, Wuhan 430065, P. R. China<&wdkj&>State Key Laboratory of Food Science and Technology, Jiangnan University, China<&wdkj&>Key Laboratory of Pesticide and Chemical Biology (CCNU), Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, P. R. China

摘要： The rapid extraction of high-purity nucleic acids from complex biological samples using conventional methods is complicated. Therefore, in this study, glycine-pillar[6]arene (Gly-P6)-functionalized tapered nanochannels were constructed using 32-mer single-stranded E. coli DNA (ssDNA) as a model sequence, which can selectively transport ssDNA by multiple noncovalent forces (transport flux of 2.65 nM cm−2 h−1) under the interference of amino acids and other substances. In view of these prospective results, the selective transport of nucleic acids with nanochannels could be applied in the design of nucleic acid enrichment and separation systems in the future. © 2022 The Royal Society of Chemistry.

语种： 英文

作者： Liu, Shi-Yu;Wang, Huiling;Nie, Gang

期刊： ACS SENSORS,2022年7(7):1837-1846 ISSN：2379-3694

通讯作者： Shi-Yu Liu

作者机构： [Liu, Shi-Yu] Department of Laboratory Medicine, School of Medicine, Yangtze University, Jingzhou 434023, P. R. China;[Nie, Gang] Hubei Key Laboratory of Nature Medicinal Chemistry and Resource Evaluation, Tongji Medical College of Pharmacy, Huazhong University of Science and Technology, Wuhan 430030, P. R. China;[Wang, Huiling] College of Chemistry, Central China Normal University, 152 Luoyu Road, Wuhan 430079, P. R. China

通讯机构： [Shi-Yu Liu] D;Department of Laboratory Medicine, School of Medicine, Yangtze University, Jingzhou 434023, P. R. China

关键词： fibroblast activation protein-α;fluorescent probe;live imaging;melanoma;theranostic

摘要： Melanoma is a malignant cancer with a high risk of metastasis and continued increase in death rates over the past decades, and its prognosis is highly related to the disease's stage, while early detection and treatment of melanoma are significant to the improvement of its therapy outcome. Different from the traditional methods for disease diagnosis, enzyme-activated fluorescent probes were developed rapidly due to their high sensitivity and temporal-spatial ratio and have been widely applied in tumor detection, surgical navigation, and cancer-related research. Fibroblast activation protein-α (FAPα), a serine-type cell surface protease that plays important roles in cell invasion and extracellular matrix degradation, is widely involved in tumor progression such as malignant melanoma, so developing a FAPα activity-based molecular tool would be of great potential for the early diagnosis and therapy of melanoma. However, few fluorescent probes targeting FAPα have been applied in melanoma-related studies, and thus, the construction of FAPα activity-based fluorescent probes for melanoma detection is in urgent need. By incorporating the selective recognition unit with a red-emission fluorophore, cresyl violet, we herein report an ultrasensitive (limit of detection = 5.3 ng/mL) fluorogenic probe for FAPα activity sensing, named CV-FAP; the acquired probe showed a significantly higher binding affinity (15.7-fold) and overall catalytic efficiency (2.6-fold) when compared with those of the best reported FAPα probes. The good performance of CV-FAP made it possible to discriminate malignant melanoma cells and tumor-bearing mice from normal cells and mice with high contrast. More importantly, CV-FAP showed significant antitumor activity toward melanoma in cultured cells and tumor-bearing nude mice (over 95% inhibited tumor growth) with good safety, which made it an ideal theranostic agent for melanoma. © 2022 American Chemical Society. All rights reserved.

语种： 英文