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| 1 | Developing potent PROTACs tools for selective degradation of HDAC6 protein显示文摘Dear Editor, Histone deacetylases (HDACs) are a family of enzymes that remove acetyl groups on histone and non-histone proteins, thereby playing a vital role in the modulation of gene expression and protein activity. Eighteen HDACs have been identified in human and subdivided into four classes including I, II (Ila, lib), III and IV (Seto et al., 2014). Among them, HDAC6 is a unique lib HD AC with dominant cytoplasmic localization and two functional catalytic domains. Besides the functions for deacetylation of histone, and modulation of a-tubulin, HSP90 and cortactin, HDAC6 also participates in protein trafficking and degradation, cell shape and migration (Valenzuela-Fernandez et al., 2008). The deregulation of HDAC6 is related to various diseases, such as neurodegenerative diseases, cancer and pathological autoimmune response (Batchu et al., 2016). Hence, it is especially important for directly controlling cellular HDAC6 protein levels to achieve therapeutic purposes. The traditional approaches of red u ci ng cellular protein levels mainly rely on genetic modifications, such as RNA interference, transcription activator-like effector nucleases, recombination-based gene knockout and clustered regularly interspaced short palindromic repeats (CRISPR-Cas9)(Boettcher et al., 2015). However, these approaches have failed to a certain degree to achieve acute and reversible changes of gene function. Furthermore, the complications of potential genetic compensation and/or spontaneous mutations arising in geneknockout models may lead to misinterpretations (Davisson etal., 2012;El-Brolosy etal., 2017). Therefore, it is urgent for developing a rapid, robust, and reversible approach to directly modulate HDAC6 protein levels. | Zixuan An Wenxing Lv Shang Su Wei Wu Yu Rao | 2019 | Protein & Cell2019，10，8： | 7 |
| 2 | Enhanced electrocatalytic oxidation of dyes in aqueous solution using cobalt phthalocyanine modified activated carbon fiber anode显示文摘Cobalt tetra(2,4-dichloro-1,3,5-triazine)aminophthalocyanine(CoPc)was immobilized covalently on activated carbon fiber(ACF)felt to obtain CoPc-modified ACF(CoPc-ACF)catalyst,and an electrocatalytic oxidation system using CoPc-ACF as the anode was constructed.The electrocatalytic oxidation of Acid Red 1(AR1)was investigated in aqueous solution by an UV-vis spectrophotometer and UPLC.The results indicated that AR1 could be eliminated efficiently in this electrocatalytic oxidation system.In addition,the results of FTIR,TOC and GC-MS suggested that the electrocatalytic oxidation experienced the decoloration achieved by destroying the azo linkage and the further mineralization due to the cleavages of benzene ring and naphthalene ring.The intermediates were mainly small molecular compounds such as maleic acid and succinic acid,etc.Repetitive tests showed that CoPc-ACF can maintain high electrocatalytic activity over several cycles.The further EPR spin-trap experiments indicated that the hydroxyl radicals did not dominate the reaction in this electrocatalytic system,which was completely different from the traditional electro-Fenton system.Based on the non-radical reaction mechanism,the CoPc-modified ACF electrocatalyst has potential application in treating actual dyestuffs wastewaters,which are accompanied with high concentration of hydroxyl radical scavengers such as chlorine ions and additives in the textile printing and dyeing industry. | LI Nan DONG SuSu LV WangYang HUANG SanQing CHEN HaiXiang YAO YuYuan CHEN WenXing | 2013 | Science China Chemistry2013，56，12： | 2 |
| 3 | Correction to: Developing potent PROTACs tools for selective degradation of HDAC6 protein显示文摘In the original publication the title of X axis in Fig.1G is in correctly published as'Compound(pmol/L)'.The correct title of X axis in Fig.1G should be read as'Compound(nmol/L)M.Figure 1.Development of selective HDAC6-degrading PROTACs.(A)The principle of PROTAC.(B)The structure of PROTAC,as shown in the upper portion.A binding mode of PROTAC(ball stick),HDAC6(PDB 5G0J,purple)and CRL4-CRBN(PDB 2HYE and 4CI3,colored cyan and gray)was simulated by Pymol. | Zixuan An Wenxing Lv Shang Su Wei Wu Yu Rao | 2019 | Protein & Cell2019，10，11： | 1 |
| 4 | Exosome-Coated Zeolitic Imidazolate Framework Nanoparticles for Intracellular Detection of ATP显示文摘The intracellular delivery of metal-organic frameworks(MOFs)encapsulated with functional biomolecules represents a promising av-enue in the field of biomedicine and biosensing.To improve the cellular uptake efficiency of MOFs,here we report the fabrication of cancer cell-derived exosome membra ne(EM)-coated zeolitic imidazolate framework-8(EM-ZIF-8)nan oparticles by using a microfluidic son ication device. | Wenxing Lv Ziwei Han Yike Li Yanjuan Huang Jiashu Sun Xiaoquan Lu Chao Liu | 2021 | Chinese Journal of Chemistry2021，39，8： | 0 |
| 5 | Developing potent BTK^(C481S)PROTACs for ibrutinib-resistant malignant lymphoma显示文摘Ibrutinib is a first-line treatment drug for B-cell malignancies.However,resistance to ibrutinib has been reported due to BTKC481Smutation.Although PROTAC strategy is expected to overcome this clinical resistance,it has limitations such as large molecular weight and moderate bioactivity,which restrict its potential clinical application.Herein,we report a new type of potent BTKC481S-targeting PROTAC degrader.Through design,computer-assisted optimization and SAR studies,we have developed a representative BTKC481Sdegrader L6 with a much smaller molecular weight and improved solubility.Notably,L6 demonstrates better BTK degrading activity and lower IC50value in ibrutinib-resistant cell line than the first-generation BTK degrader P13I.Optimization strategy of L6 provides a general approach in the development of PROTACs targeting BTK and other proteins for future study. | Yonghui Sun Xin Luo Zimo Yang Wenxing Lv Lixia Chen Hua Li Yu Rao | 2023 | Chinese Chemical Letters2023，34，6： | 0 |
| 6 | Microfluidic one-step, aqueous synthesis of size-tunable zeolitic imidazolate framework-8 for protein delivery显示文摘Zeolitic imidazolate framework-8(ZIF-8)with porous structure,biocompatibility,and pH-sensitive release behavior is a promising nanoplatform for protein delivery.However,it is still a challenging task for a practical synthesis of protein-loaded ZIF-8 nanoparticles.Here we report an all-aqueous microfluidic reactor for one-step,rapid,and highly controlled synthesis of ZIF-8 nanoparticles with high protein loading at room temperature.Microfluidic reactor allows for an ultrafast(<35 ms),complete mixing of Zn2+ions and 2-methylimidazole(2-MIM)at different molecular ratios,leading to the formation of stable ZIF-8 nanoparticles with tunable sizes(13.2–191.4 nm)in less than 30 s.By pre-mixing various proteins such as bovine serum albumin(BSA)(isoelectric point(pI)=5.82),ovalbumin(OVA)(pI=4.82),or RNase A(pI=8.93)with 2-MIM,ZIF-8 nanoparticles can be synthesized with protein encapsulation efficiency over 97%.Among the nanoparticles with different sizes,25 nm ZIF-8 nanoparticles show the best performance in promoting the cellular uptake of protein payload.Using OVA as a model protein,we demonstrate that 25 nm ZIF-8 nanoparticles significantly enhance the cytosolic delivery of antigen,as indicated by the effective activation of dendritic cells.We anticipate that this microfluidic synthesis of nanomaterials may advance the emerging field of cytosolic protein delivery. | Wenxing Lv Ziwei Han Shaokun Dong Yanjuan Huang Jinqi Deng Chao Liu Qiang Feng Jiashu Sun | 2023 | Nano Research2023，16，12： | 0 |
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