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Jun12682, a potent SARS-CoV-2 papain-like protease inhibitor with exceptional antiviral efficacy in mice

ACTA PHARMACEUTICA SINICA B 2024年第9期14卷 4189-4192页

作者： Yang, Mianling Kim, Meehyein Zhan, Peng Shandong Univ Sch Pharmaceut Sci Dept Med Chem Key Lab Chem BiolMinist Educ Jinan 250012 Peoples R China korea res inst chem technol krict Infect Dis Therapeut Res Ctr Daejeon 34114 South Korea

Recently,a collaborative research study published in Science,led by Jun Wang,Xufang Deng,Eddy Arnold,and Francesc Xavier Ruiz1,identified a series of potent small molecule inhibitors that specifically target SARS-CoV-2 papain-like protease(PLpro).The study demonstrated nanomolar PLpro inhibitory potency with Ki values ranging from 13.2 to 88.2 nmol/*** employing a structure-based drug design strategy,the researchers discovered an exceptionally promising compound,named Jun12682,that effectively targets both the newly discovered ubiquitin Val70(Val70Ub)-binding site and the known blocking loop(BL2)groove near the S4 subsite of ***,studies on the mechanism of action revealed that Jun12682 inhibits the deubiquitinating and deISGylating activities of PLpro,which are crucial for antagonizing the host’s innate immune response upon viral *** biology studies confirmed the“two-pronged”binding mode of Jun12682,aligning perfectly with their drug design ***,Jun12682 exhibited potent antiviral activity against SARS-CoV-2 and its variants,including nirmatrelvir-resistant mutants,in Caco-2 cells(EC50:0.44e2.02 mmol/L).It is noteworthy that its oral administration significantly improved survival rates and alleviated both lung virus loads and histopathological lesions in a lethal SARS-CoV-2 mouse *** conclusion。

关键词： SARS-CoV-2 Papain-like protease Broad-spectrum Anti-drug resistance Drug candidate

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Nanocrystalline low-silica X zeolite as an efficient ion-exchanger enabling fast radioactive strontium capture

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FRONTIERS OF chemICAL SCIENCE AND ENGINEERING 2024年第9期18卷 98-0页

作者： Jeon, Hyungmin Lee, Susung Kim, Jeong-Chul Choi, Minkee korea Adv inst Sci & technol KAIST Dept Chem & Biomol Engn BK21 Four Daejeon 34141 South Korea inst Basic Sci IBS Ctr Nanomat & Chem React Daejeon 34141 South Korea

NaA zeolite (Si/Al = 1.00) has been commercially applied for capturing radioactive Sr-90(2+) because of its high surface charge density, effectively stabilizing the multivalent cation. However, owing to its narrow micropore opening (4.0 & Aring;), large micron-sized crystallites, and bulkiness of hydrated Sr2+, the Sr2+ exchange over NaA has been limited by very slow kinetics. In this study, we synthesized nanocrystalline low-silica X by minimizing a water content in a synthesis gel and utilizing a methyl cellulose hydrogel as a crystal growth inhibitor. The resulting zeolite exhibited high crystallinity and Al-rich framework (Si/Al of approximately 1.00) with the sole presence of tetrahedral Al sites, which are capable of high Sr2+ uptake and ion selectivity. Meanwhile, the zeolite with a FAU topology has a much larger micropore opening size (7.4 & Aring;) and a much smaller crystallite size (similar to 340 nm) than NaA, which enable significantly enhanced ionexchange kinetics. Compared to conventional NaA, the nanocrystalline low-silica X exhibited remarkably increased Sr2+-exchange kinetics (> 18-fold larger rate constant) in batch experiments. Although both the nanocrystalline low-silica X and NaA exhibited comparable Sr2+ capacities under equilibrated conditions, the former demonstrated a 5.5-fold larger breakthrough volume than NaA under dynamic conditions, attributed to its significantly faster Sr2+-exchange kinetics.

关键词： Sr2+ removal low-silica X zeolite nanocrystal hydrogel methyl cellulose CESIUM RADIONUCLIDE SELECTIVITY REMOVAL AGENTS LTA

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Over 18.2% efficiency of layer-by-layer all-polymer solar cells enabled by homoleptic iridium(III) carbene complex as solid additive

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SCIENCE BULLETIN 2024年第18期69卷 2862-2869页

作者： Zhou, Hang Sun, Yingjie Zhang, Miao Ni, Yuheng Zhang, Fenghua Jeong, Sang Young Huang, Tianhuan Li, Xiong Woo, Han Young Zhang, Jian Wong, Wai-Yeung Ma, Xiaoling Zhang, Fujun Beijing Jiaotong Univ Key Lab Luminescence & Opt Informat Minist Educ Beijing 100044 Peoples R China Beijing Jiaotong Univ Tangshan Res Inst Tangshan 063000 Peoples R China Hong Kong Polytech Univ Res Inst Smart Energy Dept Appl Biol & Chem Technol Hong Kong 999077 Peoples R China Beijing technol & Business Univ Dept Phys Beijing 100048 Peoples R China korea Univ Coll Sci Dept Chem Organ Optoelect Mat Lab Seoul 02841 South Korea Guilin Univ Elect technol Engn Res Ctr Elect Informat Mat & Devices Sch Mat Sci & Engn Minist EducGuangxi Key Lab Informat Mat Guilin 541004 Peoples R China

The vertical phase distribution of active layers plays a vital role in balancing exciton dissociation and charge transport for achieving efficient polymer solar cells (PSCs). The layer-by-layer (LbL) PSCs are commonly prepared by using sequential spin-coating method from donor and acceptor solutions with distinct solvents and solvent additives. The enhanced exciton dissociation is expected in the LbL PSCs with efficient charge transport in the relatively neat donor or acceptor layers. In this work, a series of LbL all-polymer solar cells (APSCs) were fabricated with PM6 as donor and PY-DT as acceptor, and triplet material m-Ir(CPmPB)3 is deliberately incorporated into PY-DT layer to prolong exciton lifetimes of active layers. The power conversion efficiency (PCE) of LbL APSCs is improved to 18.24% from 17.32% by incorporating 0.3 wt% m-Ir(CPmPB)3 in PY-DT layer, benefiting from the simultaneously enhanced short-circuit current density (JSC) of 25.17 mA cm-2 and fill factor (FF) of 74.70%. The enhancement of PCE is attributed to the efficient energy transfer of m-Ir(CPmPB)3 to PM6 and PY-DT, resulting in the prolonged exciton lifetime in the active layer and the increased exciton diffusion distance. The efficient energy transfer from m-Ir(CPmPB)3 to PM6 and PY-DT layer can be confirmed by the increased photoluminescence (PL) intensity and the prolonged PL lifetime of PM6 and PY-DT in PM6 + m-Ir(CPmPB)3 and PY-DT + m-Ir(CPmPB)3 films. This study indicates that the triplet material as solid additive has great potential in fabricating efficient LbL APSCs by prolonging exciton lifetimes in active layers. (c) 2024 Science China Press. Published by Elsevier B.V. and Science China Press. All rights are reserved, including those for text and data mining, AI training, and similar technologies.

关键词： Layer-by-layer All-polymer solar cells Additive strategy Triplet material Energy transfer

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