Discovery of highly potent HDAC8 PROTACs with anti-tumor activity (English)
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In:
Bioorganic Chemistry
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136
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2023
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ISSN:
- Article (Journal) / Electronic Resource
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Title:Discovery of highly potent HDAC8 PROTACs with anti-tumor activity
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Contributors:Zhao, Chunlong ( author ) / Chen, Deng ( author ) / Suo, Fengzhi ( author ) / Setroikromo, Rita ( author ) / Quax, Wim J. ( author ) / Dekker, Frank J. ( author )
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Published in:Bioorganic Chemistry ; 136
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Publisher:
- New search for: The Author(s)
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Publication date:2023-04-12
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ISSN:
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DOI:
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Type of media:Article (Journal)
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Type of material:Electronic Resource
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Language:English
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Keywords:Histone deacetylase 8 (HDAC8) , Proteolysis Targeting Chimeras (PROTACs) , Triple-Negative Breast Cancer (TNBC) , Migration , T-cell leukemia , Apoptosis , CRBN , cereblon , CREB , cAMP response element-binding protein , DCM , dichlorometane , DEC1 , deleted in esophageal cancer 1 , DIPEA , N,N-diisopropylethylamine , DMF , N,N-dimethylformamide , EDCI , 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide , ERRα , estrogen-related receptor alpha , HDAC , histone deacetylase , HATU , 1-[Bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxide hexafluorophosphate , HOBT , hydroxybenzotriazole , MTS , 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)–2H-tetrazolium , MeOH , methanol , NAD+ , nicotinamide adenine dinucleotide , POI , protein of interest , PROTAC , proteolysis targeting chimera , SMC3 , structural maintenance of chromosomes protein 3 , STAT3 , signal transducer and activator of transcription 3 , TFA , trifluoroacetic acid , THF , tetrahydrofuran , TNBC , triple-negative breast cancer
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Source:
Table of contents – Volume 136
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
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Enlarging the substrate binding pocket of penicillin G acylase from Achromobacter sp. for highly efficient biosynthesis of β-lactam antibioticsYan, Zhen / Huang, Bin / Yang, Kai / Anaman, Richmond / Amanze, Charles / Jin, Jing / Zhou, Hongbo / Qiu, Guanzhou / Zeng, Weimin et al. | 2023
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Identification of three key enzymes involved in the biosynthesis of tetracyclic oxindole alkaloids in Uncaria rhynchophyllaGuo, Eryan / Yuan, Mengting / Xu, Lijun / Ren, Qinjia / Wang, Zihan / Li, Zixin / Wu, Zongyao / Liu, Wenyuan / Zhao, Yucheng / Feng, Feng et al. | 2023
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Discovery of highly potent HDAC8 PROTACs with anti-tumor activityZhao, Chunlong / Chen, Deng / Suo, Fengzhi / Setroikromo, Rita / Quax, Wim J. / Dekker, Frank J. et al. | 2023
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Topoisomerase II inhibitors design: Early studies and new perspectivesSwedan, Hadeer K. / Kassab, Asmaa E. / Gedawy, Ehab M. / Elmeligie, Salwa E. et al. | 2023
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Quorum sensing inhibitors as Therapeutics: Bacterial biofilm inhibitionVashistha, Aditi / Sharma, Nikhil / Nanaji, Yerramsetti / Kumar, Deepak / Singh, Gurpal / Barnwal, Ravi P. / Yadav, Ashok Kumar et al. | 2023
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Design, synthesis and evaluation of monoketene compounds as novel potential Parkinson's disease agents by suppressing ER stress via AKTChen, Jun / Zheng, Zhiwei / Li, Mingqi / Cao, Chengkun / Zhou, Xuli / Wang, Bozhen / Gan, Xin / Huang, Zhicheng / Liu, Yugang / Huang, Wenting et al. | 2023
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A novel benzothiophene incorporated Schiff base acting as a “turn-on” sensor for the selective detection of Serine in organic mediumDhanya, T.M. / Krishnan, Aravind / Anjali Krishna, G. / Francis, Shijo / Aswathy, P.V. / Augustine, Maria / Shanty, A.A. / Divya, K.M. / Savitha, D.P. / Mohanan, P.V. et al. | 2023
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Design, synthesis, and biological evaluation of pyrido[3,2-d]pyrimidine derivatives as novel ATR inhibitorsDuan, Yunxin / Zhuang, Lili / Xu, Yerong / Cheng, Haodong / Xia, Jiawei / Lu, Tao / Chen, Yadong et al. | 2023
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Design, synthesis, and biological evaluation of novel napabucasin-melatonin hybrids as potent STAT3 inhibitorsZhang, Chong / Yang, Limin / Yang, Xiaojuan / Gao, Qinghe / Qu, Yan / Wu, Liqiang et al. | 2023
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Identification of a novel extracellular inhibitor of FGF2/FGFR signaling axis by combined virtual screening and NMR spectroscopy approachPagano, Katiuscia / Listro, Roberta / Linciano, Pasquale / Rossi, Daniela / Longhi, Elisa / Taraboletti, Giulia / Molinari, Henriette / Collina, Simona / Ragona, Laura et al. | 2023
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Synthesis, biological evaluation and mechanistic studies of 4-(1,3-thiazol-2-yl)morpholine-benzimidazole hybrids as a new structural class of antimicrobialsAaghaz, Shams / Digwal, Chander S. / Neshat, Naziya / Maurya, Indresh K. / Kumar, Vinod / Tikoo, Kulbhushan / Jain, Rahul / Kamal, Ahmed et al. | 2023
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LY103, a pomalidomide derivative, alleviates taxol resistance in NSCLC via energy metabolism crosstalk and tumor microenvironment interventionWang, Xing / Wang, Xiaohan / Zhao, Yongfei / Qi, Zhengjian et al. | 2023
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Issue TOC| 2023
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Abietane diterpenoids from Orthosiphon wulfenioides with NLRP3 inflammasome inhibitory activityTu, Wen-Chao / Zhao, Ying-Xin / Yang, Chang-Lin / Zhang, Xing-Jie / Li, Xiao-Li / Sakah, Kaunda-Joseph / Zhang, Rui-Han / Xiao, Wei-Lie / Liu, Mei-Feng et al. | 2023
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Intelligent delivery system targeting PD-1/PD-L1 pathway for cancer immunotherapyLiu, Ning / Zhang, Renshuai / Shi, Qiang / Jiang, Hongfei / Zhou, Qihui et al. | 2023
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Corrigendum to “Lithocholic acid-based design of noncalcemic vitamin D receptor agonists” [Bioorg. Chem. 111 (2021) 104878]Gaikwad, Sunil / González, Carmen M. / Vilariño, Daniel / Lasanta, Gonzalo / Villaverde, Carmen / Mouriño, Antonio / Verlinden, Lieve / Verstuyf, Annemieke / Peluso-Iltis, Carole / Rochel, Natacha et al. | 2023
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Click synthesis of pyrrolidine-based 1,2,3-triazole derivatives as antifungal agents causing cell cycle arrest and apoptosis in Candida aurisYounus Wani, Mohmmad / Saeed Saleh Alghamidi, Majed / Srivastava, Vartika / Ahmad, Aijaz / Aqlan, Faisal M. / Saad Al-Bogami, Abdullah et al. | 2023
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An expeditious on-water regioselective synthesis of novel arylidene-hydrazinyl-thiazoles as DNA targeting agentsAggarwal, Ranjana / Hooda, Mona / Kumar, Prince / Kumar, Suresh / Singh, Snigdha / Chandra, Ramesh et al. | 2023
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Design of Orally-bioavailable Tetra-cyclic phthalazine SOS1 inhibitors with high selectivity against EGFRHe, Huan / Chen, Ruiqi / Wang, Ziwei / Qing, Luolong / Zhang, Yu / Liu, Yi / Pan, Weidong / Fang, Huaxiang / Zhang, Silong et al. | 2023
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Design, synthesis and biological evaluation of oxadiazole clubbed piperazine derivatives as potential antidepressant agentsSahu, Bhaskar / Bhatia, Rohit / Kaur, Dilpreet / Choudhary, Diksha / Rawat, Ravi / Sharma, Shilpa / Kumar, Bhupinder et al. | 2023
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Quinolines and isoquinolines as HIV-1 inhibitors: Chemical structures, action targets, and biological activitiesHu, Sha / Chen, Jiong / Cao, Jin-Xu / Zhang, Shuang-Shuang / Gu, Shuang-Xi / Chen, Fen-Er et al. | 2023
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Exploring new cyclohexane carboxamides based GABA agonist: Design, synthesis, biological evaluation, in silico ADME and docking studiesHamada Abd-Allah, Walaa / Abd El-Mohsen Anwar, Mostafa / Mohammed, Eman R. / Elbaset, Marawan A. / El Moghazy, Samir M. et al. | 2023
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Discovery of novel phenyl triazole analogs as TRK/ALK dual inhibitors with prospective antitumor effectsCao, Zhi / Zhang, Jiahao / Guo, Mengrao / Shao, Bin / Wei, Xiujian / Li, Sen / Wang, Peng / Zhai, Xin et al. | 2023
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Absolute configuration of cyclopropanes and the structural revision of pyrones from Marine-derived fungus Stagonospora sp. SYSU-MS7888Wu, Zhenger / Guo, Heng / Wu, Qilin / Jiang, Minghua / Chen, Junjie / Chen, Bin / Li, Hanxiang / Liu, Lan / Chen, Senhua et al. | 2023
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Discovery of urea-based pleuromutilin derivatives as potent gram-positive antibacterial agentsWu, Zhenhua / Zhu, Xiaoli / Hong, Anjin / He, Guanghui / Wang, Zheng / Xu, Qingyan / Hu, Zhiyu / Wu, Xiaobing / Wang, Yuezhou / Chen, Qiufang et al. | 2023
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Photosensitizer-based small molecule theranostic agents for tumor-targeted monitoring and phototherapyGao, Jiake / Jiang, Hongfei / Chen, Pengwei / Zhang, Renshuai / Liu, Ning et al. | 2023
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Discovery of a miniaturized PROTAC with potent activity and high selectivityGong, Lidong / Li, Ridong / Gong, Jingjing / Ning, Xianling / Sun, Jiawei / Ma, Qiang / Zhu, Chuanda / Yang, Yuanyuan / Lin, Kerui / Li, Yanglonghao et al. | 2023
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Syntheses and evaluation of acridone derivatives as anticancer agents targeting Kras promoter i-motif structureWei, Zuzhuang / Lin, Xiaomin / Wang, Siyi / Zhang, Jiahui / Ji, Dongsheng / Gong, Xue / Huang, Zhi-Shu / Shu, Bing / Li, Ding et al. | 2023
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Nano zinc Oxide-Ruthenium (III) complex of novel coumarin derivative: Synthesis, Characterization, DNA Cleavage, anticancer and bioimaging activitiesSumi, M. / Nevaditha, N.T. / Sindhu Kumari, B. et al. | 2023
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Design and synthesis optimization of novel diimide indoles derivatives for ameliorating acute lung injury through modulation of NF-κB signaling pathwayZheng, Zhiwei / Li, Xiaobo / Chen, Pan / Zou, Yu / Shi, Xiaojian / Li, Xiang / Young Kim, Eun / Liao, Jing / Yang, Jun / Chattipakorn, Nipon et al. | 2023
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Editorial Board| 2023
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Structural analysis and biological activities of C25-amino and C25-nitro vitamin D analogsGómez-Bouzó, Uxía / Belorusova, Anna Y. / Rivadulla, Marcos L. / Santalla, Hugo / Verlinden, Lieve / Verstuyf, Annemieke / Ferronato, Maria J / Curino, Alejandro C. / Facchinetti, Maria M. / Fall, Yagamare et al. | 2023
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Pegriseofamines A−E: Five cyclopiazonic acid related indole alkaloids from the fungus Penicillium griseofulvumLiang, Yu / Liao, Hong / Chen, Xuanni / Wang, Qiwei / Li, Qin / Shen, Yong / Zheng, Yuyi / Li, Xiao-Nian / Zhu, Hucheng / Li, Dongyan et al. | 2023
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Design and synthesis of uracil/thiouracil based quinoline scaffolds as topoisomerases I/II inhibitors for chemotherapy: A new hybrid navigator with DFT calculationEl-Kalyoubi, Samar / Elbaramawi, Samar S. / Zordok, Wael A. / Malebari, Azizah M. / Safo, Martin K. / Ibrahim, Tarek S. / Taher, Ehab S. et al. | 2023
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Pyrimido[1,2-a]benzimidazoles as inhibitors of oncoproteins ubiquitin specific protease 5 and MYCN in the childhood cancer neuroblastomaGadde, Satyanarayana / Kleynhans, Ane / Holien, Jessica K. / Bhadbhade, Mohan / Nguyen, Phuoc Linh Dan / Mittra, Ritu / Yu, Tsz Tin / Carter, Daniel R. / Parker, Michael W. / Marshall, Glenn M. et al. | 2023
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GFP-based red-emissive fluorescent probes for dual imaging of β-amyloid plaques and mitochondrial viscosityLeng, Huaxiang / Yang, Jinrong / Long, Liansheng / Yan, Yiyong / Shi, Wen-Jing / Zhang, Lei / Yan, Jin-wu et al. | 2023