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Trinuclear gold-catalyzed site-selective alkylation of peptides

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science china Chemistry 2024年

作者： Qingyun Fang chengyihan Gu Yinghan chen Wencheng Yan Yong Liang Weipeng Li chengjian Zhu jie Han Jin Xie state key laboratory of Coordination Chemistry Jiangsu Key Laboratory of Advanced Organic MaterialsChemistry and Biomedicine Innovation Center (ChemBIC)School of Chemistry and Chemical EngineeringNanjing University Green Catalysis Center College of ChemistryZhengzhou University state key laboratory of Natural Medicines China Pharmaceutical University

Selective modification of peptides has always been a challenging *** selective alkylation of peptides can alter the biological activity and physical properties of molecules,and it has gained significant research *** herein disclose an intriguing gold-catalyzed alkylation of peptides using bench-stable unactivated alkyl bromides under photoredox catalysis.A wide range of structurally diverse primary,secondary and tertiary alkyl bromides serve as effective coupling partners to precisely connect with the α-C(sp3)–H in glycine residue of *** protocol demonstrates an exceptionally broad scope for alkyl halides and excellent tolerance for a wide range of useful functional groups.A series of relay transformations to construct cyclic peptides,to proceed click reaction and to realize peptide fluorescence labeling further enhance its synthetic *** addition,mechanistic studies and density functional theory (DFT) calculations reveal an inner-sphere and subsequent outersphere single electron transfer (SET) mechanism.

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Endoplasmic reticulum-targeted delivery of celastrol and PD-L1 siRNA for reinforcing immunogenic cell death and potentiating cancer immunotherapy

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Acta Pharmaceutica Sinica B 2024年第8期14卷 3643-3660页

作者： jie Wang Zilong Zhang Yan Zhuo Zhuan Zhang Rongrong chen Li Liang Xiaohe Jiang Di Nie Chang Liu Zhiwen Zou Xiang Li Jiaxin Li Bingqi Wang Rui Wang Yong Gan Miaorong Yu School of Pharmacy Shanghai University of Traditional Chinese MedicineShanghai 201203China state key laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China Jiangxi Medical college Nanchang UniversityNanchang 330006China School of Pharmacy Nanjing University of Chinese MedicineNanjing 210023China university of Chinese Academy of sciences Beijing 100049China NMPA key laboratory for Quality Research and Evaluation of pharmaceutical Excipients National Institutes for Food and Drug ControlBeijing 100050China

The prospect of employing chemoimmunotherapy targeted towards the endoplasmic reticulum(ER)presents an opportunity to amplify the synergistic effects of chemotherapy and *** this study,we initially validated celastrol(CEL)as an inducer of immunogenic cell death(ICD)by promoting ER stress and autophagy in colorectal cancer(CRC)***,an ER-targeted strategy was posited,involving the codelivery of CEL with PD-L1 small interfering RNAs(siRNA)using KDEL peptide-modified exosomes derived from milk(KME),to enhance chemoimmunotherapy *** findings demonstrate the efficient transportation of KME to the ER via the Golgi-to-ER *** to their non-targeting counterparts,KME exhibited a significant augmentation of the CEL-induced ICD ***,it facilitated the release of danger signaling molecules(DAMPs),thereby stimulating the antigen-presenting function of dendritic cells and promoting the infiltration of T cells into the ***,the ER-targeted delivery of PD-L1 siRNA resulted in the downregulation of both intracellular and membrane PD-L1 protein expression,consequently fostering the proliferation and activity of CD8^(+)T ***,the ER-targeted formulation exhibited enhanced anti-tumor efficacy and provoked anti-tumor immune responses against orthotopic colorectal tumors in ***,a robust ER-targeted delivery strategy provides an encouraging approach for achieving potent cancer chemoimmunotherapy.

关键词： Chemoimmunotherapy Targeted drug delivery Endoplasmic reticulum Endoplasmic reticulum stress Immunogenic cell death siRNA Chemoimmunotherapy Targeted drug delivery Endoplasmic reticulum Endoplasmic reticulum stress Immunogenic cell death siRNA

Notopterygium Incisum Extract Promotes Apoptosis by Preventing the Degradation of BIM in Colorectal Cancer

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Current Medical science 2024年第4期44卷 833-840页

作者： Jun-he chen cheng-ming WEI Qian-yu LIN Zi WANG Fu-ming ZHANG Mei-na SHI Wen-jian LAN Chang-gang SUN Wan-jun LIN Wen-zhe MA state key laboratory of Quality Research in Chinese Medicine Macao University of Science and TechnologyMacao999078China School of pharmaceutical sciences Sun Yat-sen UniversityGuangzhou510006China college of Traditional Chinese Medicine Weifang Medical UniversityWeifang261053China

Objective Colorectal cancer(CRC),a prevalent malignancy worldwide,has prompted extensive research into anticancer *** Chinese medicinal materials offer promising avenues for cancer management due to their diverse pharmacological *** study investigated the effects of Notopterygium incisum,a traditional Chinese medicine named Qianghuo(QH),on CRC cells and the underlying *** The sulforhodamine B assay and colony formation assay were employed to assess the effect of QH extract on the proliferation of CRC cell lines HCT116 and *** iodide(PI)staining was utilized to detect cell cycle progression,and PE Annexin V staining to detect *** blotting was conducted to examine the levels of apoptotic proteins,including B-cell lymphoma 2-interacting mediator of cell death(BIM),B-cell lymphoma 2(Bcl-2),Bcl-2-associated X protein(BAX)and cleaved caspase-3,as well as BIM stability after treatment with the protein synthesis inhibitor *** expression of BAX was suppressed using lentivirus-mediated shRNA to validate the involvement of the BIM/BAX axis in QH-induced *** in vivo effects of QH extract on tumor growth were observed using a xenograft ***,APC^(Min+)mice were used to study the effects of QH extract on primary intestinal *** QH extract exhibited significant in vitro anti-CRC activities evidenced by the inhibition of cell proliferation,perturbation of cell cycle progression,and induction of ***,QH extract significantly increased the stability of BIM proteins,which undergo rapid degradation under unstressed *** of BAX,the downstream effector of BIM,significantly rescued QH-induced ***,the in vitro effect of QH extract was recapitulated in *** extract significantly inhibited the tumor growth of HCT116 xenografts in nude mice and decreased the number of intestinal polyps in the APC^(Min+)*** QH extract

关键词： Notopterygium incisum colorectal cancer apoptosis B-cell lymphoma 2-interacting mediator of cell death

2-APQC,a small-molecule activator of Sirtuin-3(SIRT3),alleviates myocardial hypertrophy and fibrosis by regulating mitochondrial homeostasis

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Signal Transduction and Targeted Therapy 2024年第6期9卷 2748-2764页

作者： Fu Peng Minru Liao Wenke Jin Wei Liu Zixiang Li Zhichao Fan Ling Zou Siwei chen Lingjuan Zhu Qian Zhao Gu Zhan Liang Ouyang cheng Peng Bo Han Jin Zhang Leilei Fu West china School of Pharmacy and Department of Biotherapy Cancer Center and State Key Laboratory of BiotherapyWest China HospitalSichuan UniversityChengdu 610041China Sichuan Engineering Research Center for Biomimetic Synthesis of Natural Drugs School of Life Science and EngineeringSouthwest Jiaotong UniversityChengdu 610031China state key laboratory of Southwestern Chinese Medicine Resources Hospital of Chengdu University of Traditional Chinese MedicineSchool of PharmacyChengdu University of Traditional Chinese MedicineChengdu 611137China School of pharmaceutical sciences Health Science CenterShenzhen UniversityShenzhen 518060China School of Traditional Chinese Materia Medica Key Laboratory of Structure-Based Drug Design&Discovery of Ministry of EducationShenyang Pharmaceutical UniversityShenyang 110016China

Sirtuin 3(SIRT3)is well known as a conserved nicotinamide adenine dinucleotide^(+)(NAD^(+))-dependent deacetylase located in the mitochondria that may regulate oxidative stress,catabolism and ATP *** evidence has recently revealed that SIRT3 plays its critical roles in cardiac fibrosis,myocardial fibrosis and even heart failure(HF),through its deacetylation ***,discovery of SIRT3 activators and elucidating their underlying mechanisms of HF should be urgently ***,we identified a new small-molecule activator of SIRT3(named 2-APQC)by the structure-based drug designing strategy.2-APQC was shown to alleviate isoproterenol(ISO)-induced cardiac hypertrophy and myocardial fibrosis in vitro and in vivo rat ***,in SIRT3 knockout mice,2-APQC could not relieve HF,suggesting that 2-APQC is dependent on SIRT3 for its protective ***,2-APQC was found to inhibit the mammalian target of rapamycin(mTOR)-p70 ribosomal protein S6 kinase(p70S6K),c-jun N-terminal kinase(JNK)and transforming growth factor-β(TGF-β)/small mother against decapentaplegic 3(Smad3)pathways to improve ISO-induced cardiac hypertrophy and myocardial *** upon RNA-seq analyses,we demonstrated that SIRT3-pyrroline-5-carboxylate reductase 1(PYCR1)axis was closely assoiated with *** activating PYCR1,2-APQC was shown to enhance mitochondrial proline metabolism,inhibited reactive oxygen species(ROS)-p38 mitogen activated protein kinase(p38MAPK)pathway and thereby protecting against ISO-induced mitochondrialoxidative ***,activation of SIRT3 by 2-APQC could facilitate AMP-activated protein kinase(AMPK)-Parkin axis to inhibit ISO-induced ***,our results demonstrate that 2-APQC is a targeted SIRT3 activator that alleviates myocardial hypertrophy and fibrosis by regulating mitochondrial homeostasis,which may provide a new clue on exploiting a promising drug candidate for the future HF therapeutics.

关键词： SIRT3 homeostasis metabolism

Visible-light-induced selective alkylsulfonylation of unactivated alkenes via remote heteroaryl migrations

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Green Synthesis and Catalysis

Green Synthesis and Catalysis 2024年第2期5卷 126-130页

作者： Xin Yuan jie Liu Hao Lv Long-Zhou Qin Xiu Duan Jian Wang Meng-Yu Wu Beining chen Jiang-Kai Qiu Kai Guo college of biotechnology and pharmaceutical Engineering Nanjing Tech UniversityNanjing 211816China state key laboratory of Materials-Oriented Chemical Engineering Nanjing Tech UniversityNanjing 211816China university of Sheffield BrookhillSheffield S37HFUK

Photocatalyzed alkylsulfonylation of unactivated alkenes using DABCO.(SO_(2))_(2) and thianthrenium salts via a distal heteroaryl migration process has been developed,which provides a new means of synthesizing a variety of valuable alkylsulfonyl-substituted *** alkylsulfonyl radicals couple with unactivated alkenes to undergo efficient intermolecular reactions,followed by distal heteroaryl *** mild catalytic method is tolerant of functional groups and affords medicinally relevant alkylsulfonylated heterocycles.

关键词： Visible-light-induced Remote heteroaryl migrations Alkylsulfonylation Radical reaction Unactivated alkenes

整合素α6靶向自组装促凋亡纳米多肽对中枢神经系统急性淋巴细胞白血病的靶向治疗

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Engineering 2024年第4期35卷 226-240页

作者： Jia-Cong Ye Wan-Qiong Li Mei-Ling chen Qian-Kun Shi Hua Wang Xin-Ling Li Ying-He Li jie yang Qiao-Li Wang Fang Hu Yan-Feng Gao Shu-Wen Liu Mu-Sheng Zeng Guo-Kai Feng Guangdong Provincial key laboratory of New Drug Screening&NMPA key laboratory of Drug Metabolism Research and Evaluation School of Pharmaceutical SciencesSouthern Medical UniversityGuangzhou 510515China state key laboratory of Oncology in South china&Guangdong key laboratory of Nasopharyngeal Carcinoma Diagnosis and Therapy Guangdong Provincial Clinical Research Center for CancerSun Yat-sen University Cancer CenterGuangzhou 510060China School of pharmaceutical sciences(Shenzhen) Shenzhen Campus of Sun Yat-sen UniversityShenzhen 518107China Guangdong Provincial key laboratory of Construction and Detection in Tissue Engineering Biomaterials Research CenterSchool of Biomedical EngineeringSouthern Medical UniversityGuangzhou 510515China state key laboratory of Organ Failure Research Guangdong Provincial Institute of NephrologySouthern Medical UniversityGuangzhou 510515China

There is currently no effective targeted therapeutic strategy for the treatment of central nervous system acute lymphoblastic leukemia(CNS-ALL).Integrinα6 is considered a potential target for CNS-ALL diagnosis and therapy because of its role in promoting CNS-ALL disease *** targeted peptide D(RWYD)(abbreviated RD),with nanomolar affinity to integrinα6 was identified by peptide scanning techniques such as alanine scanning,truncation,and ***,we developed a therapeutic nanoparticle based on the integrinα6-targeted peptide for treating *** self-assembled proapoptotic nanopeptide_(D)(RWYD)-_(D)(KLAKLAK)_(2)-G_(D)(FFY)(abbreviated RD-KLA-Gffy)contains the integrinα6-targeted peptide RD,the well-known proapoptotic peptide_(D)(KLAKLAK)_(2)(abbreviated KLA),and the self-assembling tetrapeptide GD(FFY)(abbreviated Gffy).The functional mechanism of RD-KLA-Gffy is clarified using different *** results demonstrate that RD-KLA-Gffy is highly enriched in CNS-ALL lesions and induces tumor cell apoptosis,thus reducing CNS-ALL disease burden and prolonging the survival of CNS-ALL mice without obvious ***,the combined use of RD-KLA-Gffy and methotrexate(MTX)shows a potent antitumor effect in treating CNS-ALL,indicating that RD-KLA-Gffy plays an important role in suppressing CNS-ALL progression either as a single agent or in combination with MTX,which shows promise for application in CNS-ALL therapy.

关键词： Central nervous system acute lymphoblastic leukemia Integrinα6 Targeted peptide Proapoptotic Nanopeptide

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基于水传热和红外热成像的煤矸识别方法

工矿自动化 2024年第1期50卷 66-71,137页

作者：程刚陈杰潘泽烨魏溢凡陈森森安徽理工大学深部煤矿采动响应与灾害防控国家重点实验室安徽淮南232001 安徽理工大学机械工程学院安徽淮南232001

基于可见光图像的煤矸识别方法准确率不高、识别速度慢;基于高能射线透射的煤矸识别方法具有很大辐射导致较少应用。红外热成像具有穿透性强、不受光线影响等优点,但煤和矸石的表面温度在室温下相对接近,导致煤和矸石在红外热图像中没... 详细信息

基于可见光图像的煤矸识别方法准确率不高、识别速度慢;基于高能射线透射的煤矸识别方法具有很大辐射导致较少应用。红外热成像具有穿透性强、不受光线影响等优点,但煤和矸石的表面温度在室温下相对接近,导致煤和矸石在红外热图像中没有明显差异,难以获得较好的识别效果。针对上述问题,提出了一种基于水传热和红外热成像的煤矸识别方法。在不同水温(18,21,24,27,30℃)条件下进行煤和矸石红外热成像实验,通过煤和矸石红外热图像和温度变化之间的差异来区分煤和矸石。实验结果表明:不同水温下煤和矸石红外热图像不同,当水温低于环境温度时,煤和矸石红外热图像之间的差异较大;在相同水温条件下,煤和矸石红外热图像之间的差异随着时间增加逐渐增大;煤和矸石表面温度变化均随水温升高和时间增加呈增大趋势,但矸石表面温度变化大于煤表面温度变化;当水温为18℃、时间为180 s时,煤和矸石红外热图像之间差异和温差均达到最大。这说明低温的水可作为一种传热介质,更有利于使煤和矸石之间产生较大的温差,从而实现煤和矸石红外热图像准确、快速识别。

关键词：煤矸识别水传热红外热成像红外热图像温差

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A Cullin 5-based complex serves as an essential modulator of ORF9b stability in SARS-CoV-2 replication

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Signal Transduction and Targeted Therapy 2024年第7期9卷 3112-3129页

作者： Yuzheng Zhou Zongpeng chen Sijie Liu Sixu Liu Yujie Liao Ashuai Du Zijun Dong Yongxing Zhang Xuan chen Siyi Tao Xin Wu Aroona Razzaq Gang Xu De-an Tan Shanni Li Youwen Deng Jian Peng Shuyan Dai Xu Deng Xianwen Zhang Taijiao Jiang Zheng Zhang Gong cheng Jincun Zhao Zanxian Xia Department of Cell Biology School of Life SciencesCentral South University410013 ChangshaChina Institute for Hepatology National Clinical Research Center for Infectious DiseaseShenzhen Third People’s HospitalThe Second Affiliated HospitalSchool of MedicineSouthern University of Science and Technology518112 ShenzhenChina Department of Basic Medicine School of MedicineHunan Normal University410081 ChangshaChina Department of spine surgery The Third Xiangya HospitalCentral South University410013 ChangshaChina School of Basic Medical sciences Anhui Medical University230032 HefeiChina Hunan key laboratory of Neurorestoratology 921 Hospital of Joint Logistics Support Force People’s Liberation Army of China(The Second Affiliated Hospital of Hunan Normal University)410003 ChangshaHunanChina Department of Geriatric Surgery Xiangya HospitalCentral South University410008 ChangshaChina Xiangya School of pharmaceutical sciences Central South University410013 ChangshaChina Institute of Infectious Diseases Shenzhen Bay Laboratory518132 ShenzhenChina Guangzhou laboratory 510005 GuangzhouChina Tsinghua university-Peking university Joint Center for life sciences School of MedicineTsinghua University100084 BeijingChina state key laboratory of Respiratory Disease National Clinical Research Center for Respiratory DiseaseGuangzhou Institute of Respiratory HealthThe First Affiliated Hospital of Guangzhou Medical University510120 GuangzhouChina Hunan key laboratory of Animal Models for Human Diseases Hunan Key Laboratory of Medical Genetics&Center for Medical GeneticsSchool of Life SciencesCentral South University410008 ChangshaChina

The ORF9b protein,derived from the nucleocapsid’s open-reading frame in both SARS-CoV and SARS-CoV-2,serves as an accessory protein crucial for viral immune evasion by inhibiting the innate immune *** its significance,the precise regulatory mechanisms underlying its function remain *** the present study,we unveil that the ORF9b protein of SARS-CoV-2,including emerging mutant strains like Delta and Omicron,can undergo ubiquitination at the K67 site and subsequent degradation via the proteasome pathway,despite certain mutations present among these ***,our investigation further uncovers the pivotal role of the translocase of the outer mitochondrial membrane 70(TOM70)as a substrate receptor,bridging ORF9b with heat shock protein 90 alpha(HSP90α)and Cullin 5(CUL5)to form a *** this complex,CUL5 triggers the ubiquitination and degradation of ORF9b,acting as a host antiviral factor,while HSP90αfunctions to stabilize ***,treatment with HSP90 inhibitors such as GA or 17-AAG accelerates the degradation of ORF9b,leading to a pronounced inhibition of SARS-CoV-2 ***-cell sequencing data revealed an up-regulation of HSP90αin lung epithelial cells from COVID-19 patients,suggesting a potential mechanism by which SARS-CoV-2 may exploit HSP90αto evade the host *** study identifies the CUL5-TOM70-HSP90αcomplex as a critical regulator of ORF9b protein stability,shedding light on the intricate host–virus immune response dynamics and offering promising avenues for drug development against SARS-CoV-2 in clinical settings.

关键词： stability modulator offering

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基于红外热成像的煤矸识别方法研究

工矿自动化 2024年第4期50卷 69-77页

作者：程刚潘择烨魏溢凡陈杰安徽理工大学深部煤矿采动响应与灾害防控国家重点实验室安徽淮南232001 安徽理工大学机电工程学院安徽淮南232001

基于重介选煤、跳汰选煤、浮选、干法选煤、γ射线检测法的煤矸分选方法投资成本高、分选效率低、环境污染严重,基于CCD相机的煤矸分选方法准确率不高,基于X射线的煤矸分选技术会危害工作人员的健康。红外热成像技术不受光照、粉尘影响... 详细信息

基于重介选煤、跳汰选煤、浮选、干法选煤、γ射线检测法的煤矸分选方法投资成本高、分选效率低、环境污染严重,基于CCD相机的煤矸分选方法准确率不高,基于X射线的煤矸分选技术会危害工作人员的健康。红外热成像技术不受光照、粉尘影响,且不会对人体造成伤害。提出了一种基于红外热成像的煤矸识别方法。首先,煤和矸石在传送带的输送下经过加热区域,红外热成像仪监测经均匀加热后的煤和矸石中心点的温度,得到煤和矸石加热后的温度并对经加热区域均匀加热后的煤和矸石进行拍摄,得到煤和矸石的红外灰度图像和红外彩色图像。然后,选用高斯滤波对煤和矸石的红外灰度图像、红外彩色图像进行预处理并提取特征,将红外灰度图像的灰度均值、最大频数对应的灰度值特征和红外彩色图像的G通道一阶矩、G通道二阶矩特征作为分选特征,将上述4个特征作为分类模型的输入。最后,采用支持向量机(SVM)进行分类识别,从而达到识别煤和矸石的目的。实验结果表明:基于红外热成像的煤矸识别方法对烟煤、无烟煤、褐煤的分选准确率均达到了98%以上,有良好的分类效果。

关键词：煤矸识别红外热成像红外灰度图像红外彩色图像灰度均值 SVM 图像预处理

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