Dual-pharmacophore artezomibs hijack the Plasmodium ubiquitin-proteasome system to kill malaria parasites while overcoming drug resistance [0.03%]
双药效团的artezomibs劫持了疟原虫的泛素-蛋白酶体系统以杀死疟疾寄生虫并克服药物耐受性
Wenhu Zhan,Daqiang Li,Shubha Bevkal Subramanyaswamy et al.
Wenhu Zhan et al.
Artemisinins (ART) are critical anti-malarials and despite their use in combination therapy, ART-resistant Plasmodium falciparum is spreading globally. To counter ART resistance, we designed artezomibs (ATZs), molecules that link an ART wit...
Overcoming biological barriers to improve treatment of a Staphylococcus aureus wound infection [0.03%]
克服生物学障碍以改善金黄色葡萄球菌伤口感染的治疗
Virginie Papadopoulou,Ashelyn E Sidders,Kuan-Yi Lu et al.
Virginie Papadopoulou et al.
Chronic wounds frequently become infected with bacterial biofilms which respond poorly to antibiotic therapy. Aminoglycoside antibiotics are ineffective at treating deep-seated wound infections due to poor drug penetration, poor drug uptake...
IFNα primes cancer cells for Fusicoccin-induced cell death via 14-3-3 PPI stabilization [0.03%]
I型干扰素预处理的癌细胞通过稳定14-3-3蛋白互作而增强Fusicoccin诱导的细胞凋亡
Blaž Andlovic,Geronimo Heilmann,Sabrina Ninck et al.
Blaž Andlovic et al.
The natural product family of the fusicoccanes (FCs) has been shown to display anti-cancer activity, especially when combined with established therapeutic agents. FCs stabilize 14-3-3 protein-protein interactions (PPIs). Here, we tested com...
CysDB: a human cysteine database based on experimental quantitative chemoproteomics [0.03%]
CysDB：基于定量化学蛋白质组学实验的半胱氨酸数据库
Lisa M Boatner,Maria F Palafox,Devin K Schweppe et al.
Lisa M Boatner et al.
Cysteine chemoproteomics provides proteome-wide portraits of the ligandability or potential "druggability" for thousands of cysteine residues. Consequently, these studies are facilitating resources for closing the druggability gap, namely, ...
Selective killing of the human gastric pathogen Helicobacter pylori by mitochondrial respiratory complex I inhibitors [0.03%]
线粒体呼吸链复合物I抑制剂选择性杀死人类胃部病原体幽门螺旋杆菌
Clara Lettl,Franziska Schindele,Ahmad Reza Mehdipour et al.
Clara Lettl et al.
Respiratory complex I is a multicomponent enzyme conserved between eukaryotic cells and many bacteria, which couples oxidation of electron donors and quinone reduction with proton pumping. Here, we report that protein transport via the Cag ...
Angela T Fan,Bridget T Boyle,Fleur M Ferguson
Angela T Fan
Targeted protein degradation using molecular glues is a powerful method for targeting traditionally undruggable proteins. One challenge in molecular glue discovery is the absence of rational discovery methods. Here, King et al. leverage cov...
Degrading the signal amplifier: ITK as a target for targeted protein degradation [0.03%]
降解信号放大器：ITK成为靶向蛋白降解的目标
Avery August
Avery August
In this issue of Cell Chemical Biology, Jiang and colleagues show for the first time that the Tec kinase ITK can be targeted using PROTAC approaches. This new modality has implications for the treatment of T cell lymphomas, but also potenti...
Phosphorylation barcodes direct biased chemokine signaling at CXCR3 [0.03%]
磷酸化条形码可指导CXCR3偏置趋化因子信号转导
Dylan S Eiger,Jeffrey S Smith,Tujin Shi et al.
Dylan S Eiger et al.
G protein-coupled receptor (GPCR)-biased agonism, selective activation of certain signaling pathways relative to others, is thought to be directed by differential GPCR phosphorylation "barcodes." At chemokine receptors, endogenous chemokine...
ITK degradation to block T cell receptor signaling and overcome therapeutic resistance in T cell lymphomas [0.03%]
ITK信号转导通路抑制剂诱导T细胞受体信号阻滞及克服治疗抵抗性在T淋巴细胞瘤中的作用研究
Baishan Jiang,David M Weinstock,Katherine A Donovan et al.
Baishan Jiang et al.
Interleukin (IL)-2-inducible T cell kinase (ITK) is essential for T cell receptor (TCR) signaling and plays an integral role in T cell proliferation and differentiation. Unlike the ITK homolog BTK, no inhibitors of ITK are currently US Food...
Structural basis for antibody-mediated neutralization of lymphocytic choriomeningitis virus [0.03%]
针对淋巴细胞脉络丛脑膜炎病毒的抗体介导的中和机制及其结构基础
Alex Moon-Walker,Zeli Zhang,Dawid S Zyla et al.
Alex Moon-Walker et al.
The mammarenavirus lymphocytic choriomeningitis virus (LCMV) is a globally distributed zoonotic pathogen that can be lethal in immunocompromised patients and can cause severe birth defects if acquired during pregnancy. The structure of the ...