Results 51 to 60 of about 3,370 (187)

Molecular Editing Reveals a Bilobalide Chemotype that Attenuates Prolyl Endopeptidase (PREP)‐Linked Neuroinflammation

Advanced Science, EarlyView.
Molecular editing of bilobalide uncovers BB56, a PREP‐engaging chemotype with enhanced anti‐inflammatory activity in microglia. Integrated CETSA‐MS, SAR, and pathway analyses link BB56 to attenuation of p38 MAPK/NF‐κB and NLRP3‐associated inflammatory signaling, highlighting bilobalide editing as a strategy for developing neuroinflammation‐modulating ...
Chanin Sillapachaiyaporn, Wenjing Wang, Yao Qin, Lili Yan, Stephan Scheeff, Xu He, Qiong Wu, Yue Lin, Jinsai Shang, Xin Ye, Jing Liu, Kailei Sun, Chun Wai Yeung, Junzhe Huang, Zhenghui Chen, Xiaodong Liu, Yiqun Geng, Shannon Wing Ngor Au, Bonaventure Y. Ip, Ho Ko, Billy Wai‐Lung Ng   +20 more
wiley   +1 more source

Leonurine Ameliorates Doxorubicin‐Induced Cardiotoxicity via STING/NF‐κB/NLRP3 Inflammasome Signaling Pathway

Advanced Science, EarlyView.
ABSTRACT Doxorubicin‐induced cardiomyopathy (DIC) remains a dose‐limiting clinical challenge. This study reveals that cardiac vascular endothelial cells (CVECs) act as initial sensors of doxorubicin cardiotoxicity: circulating doxorubicin activates the cGAS‑STING pathway in CVECs, triggering NLRP3 inflammasome‑mediated pyroptosis and release of ...
Wang Jun, Chen Xiaoyang, Xu Jianglin, Yang Zhi, Tao Meijiao, He Jiale, Zhao Jiangfeng, Hei Xuanding, Xu Xuegong, Wang Wei, Li Chun   +10 more
wiley   +1 more source

A superior loading control for the cellular thermal shift assay

Scientific Reports, 2022
The cellular thermal shift assay (CETSA), as a method to determine protein–ligand interaction and cellular protein modification, has rapidly become routine laboratory practice. However, current options to determine that (1) sample was loaded in each lane
Alexandré Delport, Raymond Hewer
doaj   +1 more source

Targeting DNGR‐1 with Fangchinoline Elevates Dendritic Cell Antigen Cross‐Presentation‐Mediated Antitumor Immunity in Melanoma

Advanced Science, EarlyView.
Fangchinoline is identified as a small‐molecule DNGR‐1 modulator that enhances dendritic‐cell cross‐presentation of tumor antigens. By engaging DNGR‐1 and activating Syk–Nox2 signaling, it promotes phagosomal ROS, antigen escape, MHC‐I presentation, and CD8+ T‐cell priming, thereby strengthening antitumor immunity and sensitizing tumors to PD‐1 ...
Yuan Liao, Zhenyang Ren, Jing Zhou, He Luo, Yuling Li, Dan Chen, Yuxiao Jiang, Canzhe Li, Mengyi Zheng, Anqi Li, Yao Wang, Yang Zhang, Dingye Wang, Yanjun Jiang, Jiangyong Gu, Biaoyan Du, Yafei Shi, Fang Liu, Jianyong Xiao, Kun Wang   +19 more
wiley   +1 more source

Versatile Detection of Cellular Protein via Fluorescence Anisotropy

Advanced Science, EarlyView.
Cell Lysate Fluorescence Anisotropy (CFAST) utilizes long lifetime dye‐labeled nanobodies for rapid protein quantification in minimally purified, complex cell lysate. When coupled with cellular thermal shift, CFAST allows high‐throughput detection of endogenous protein‐small molecule engagement, facilitating the discovery of novel binders for ...
Qing Tang, Yuan‐Ping Wei, Ricky Ruiqi Ma, Na Wei, Tammy Zihan Zhou, Hilary Kung‐Yu Ho, Zafar Iqbal Bhat, Iqra Ishrat, Xiaoyu Li, Judy Wai Ping Yam, Yung Hou Wong, Qiankun Wang, Justin L. Tan   +12 more
wiley   +1 more source

绿色缓蚀阻垢剂S-羧乙基硫代琥珀酸的合成及应用研究

Gongye shui chuli, 2010
在实验室中合成了S-羧乙基硫代琥珀酸(CETSA),并对其合成条件进行了优化研究,确定出最佳的合成工艺。首先以NaHS和丙烯腈合成β-巯基丙酸,再用它与无水马来酸酐聚合生成CETSA。对产品的阻垢及缓蚀性能分别进行了测试,结果表明它对冷却水水质有很强的适应性,能够与多种金属离子发生螯合作用,从而有效抑制结垢。与此同时,CETSA还能在金属表面生成致密的保护膜,有效抑制金属腐蚀。将其与几种其他药剂复配后缓蚀效果大幅度提高,用量减少,使成本大大降低。复配后的缓蚀阻垢剂效果明显优于传统磷系缓蚀阻垢剂 ...
曾德芳, 肖建国
doaj   +2 more sources

Cellular thermal shift analysis for interrogation of CRISPR-assisted proteomic changes

BioTechniques, 2020
CRISPR–Cas9 has proven to be a versatile tool for the discovery of essential genetic elements involved in various disease states. CRISPR-assisted dense mutagenesis focused on therapeutically challenging protein complexes allows us to systematically ...
Nam-Gu Her, Ivan Babic, Venkata M Yenugonda, Santosh Kesari, Elmar Nurmemmedov   +4 more
doaj   +1 more source

Radiation‐Induced Tumor‐Intrinsic LTβR N‐Glycosylation Suppresses Pyroptosis Through TRIM28‐Mediated PCBP2 SUMOylation to Promote Gastric Cancer Radioresistance

Advanced Science, EarlyView.
Radiotherapy triggers LTβR N‐glycosylation, enhancing its overall protein stability and nuclear retention. This accumulation drives TRIM28‐mediated PCBP2 SUMOylation, suppressing pyroptosis and conferring gastric cancer radioresistance. Therapeutically, a targeted nanoplatform (cRGD‐Lipo@EMD) effectively disrupts this regulatory axis, offering a highly
Weijie Zang, Yunlong Ji, Chunwang Zhou, Xiwen Li, Zhuang Lu, Guangze Zhang, Yu Chen, Wanjiang Xue, Yilin Hu   +8 more
wiley   +1 more source

The use of cellular thermal shift assay (CETSA) to study Crizotinib resistance in ALK-expressing human cancers [PDF]

Scientific Reports, 2016
AbstractVarious forms of oncogenic ALK proteins have been identified in various types of human cancers. While Crizotinib, an ALK inhibitor, has been found to be therapeutically useful against a subset of ALK+ tumours, clinical resistance to this drug has been well recognized and the mechanism of this phenomenon is incompletely understood.
Abdulraheem Alshareef, Haifeng Zhang, Yung-Hsing Huang, Chenming Wu, Jing Dong Zhang, Peng Wang, Ahmed El‐Sehemy, Mohamed Fares, Raymond Lai   +8 more
openaire   +2 more sources

Targeting the HSPA8‐CMA‐ATP6V1A Axis Triggers Lysosomal Hyperacidification and Catastrophic Vacuolation in Prostate Cancer

Advanced Science, EarlyView.
Our experimental evidence supports a model in which ALO targets the HSPA8‐CMA‐ATP6V1A axis to induce lysosomal hyperacidification and initiate osmotic and lipidomic stress. These changes are associated with LMP and loss of lysosomal integrity in prostate cancer cells.
Bingzheng An, Ze Gao, Shuo Chen, Liwei Meng, Chen Zhang, Kefan Song, Haochen Cui, Lei Yan, Zhiqing Fang   +8 more
wiley   +1 more source