Target deconvolution with matrix-augmented pooling strategy reveals cell-specific drug-protein interactions [0.03%]
基于矩阵增强的池化策略的目标去卷积揭示了细胞特异性药物-蛋白质相互作用
Hongchao Ji,Xue Lu,Shiji Zhao et al.
Hongchao Ji et al.
Target deconvolution is a crucial but costly and time-consuming task that hinders large-scale profiling for drug discovery. We present a matrix-augmented pooling strategy (MAPS) which mixes multiple drugs into samples with optimized permuta...
Cannabidiol acts as molecular switch in innate immune cells to promote the biosynthesis of inflammation-resolving lipid mediators [0.03%]
大麻二酚可作为天然免疫细胞中的分子开关以促进抗炎脂质介质的生物合成
Lukas K Peltner,Lars Gluthmann,Friedemann Börner et al.
Lukas K Peltner et al.
Cannabinoids are phytochemicals from cannabis with anti-inflammatory actions in immune cells. Lipid mediators (LM), produced from polyunsaturated fatty acids (PUFA), are potent regulators of the immune response and impact all stages of infl...
Protomer selectivity of type II RAF inhibitors within the RAS/RAF complex [0.03%]
Ⅱ型Raf抑制剂在RAS/Raf复合物中的亚基选择性
James D Vasta,Ani Michaud,Chad A Zimprich et al.
James D Vasta et al.
RAF dimer inhibitors offer therapeutic potential in RAF- and RAS-driven cancers. The utility of such drugs is predicated on their capacity to occupy both RAF protomers in the RAS-RAF signaling complex. Here we describe a method to condition...
Mechanism-based inhibition of gut microbial tryptophanases reduces serum indoxyl sulfate [0.03%]
基于机制的肠道微生物色氨酸酶抑制可减少血清吲哚硫酸酯水平
Amanda L Graboski,Mark E Kowalewski,Joshua B Simpson et al.
Amanda L Graboski et al.
Indoxyl sulfate is a microbially derived uremic toxin that accumulates in late-stage chronic kidney disease and contributes to both renal and cardiovascular toxicity. Indoxyl sulfate is generated by the metabolism of indole, a compound crea...
A split-luciferase lysate-based approach to identify small-molecule modulators of phosphatase subunit interactions [0.03%]
基于分裂型萤火素酶粗酶制剂的小分子调节物的识别：磷酸酶亚基相互作用模型研究
Zander Claes,Mathieu Bollen
Zander Claes
An emerging strategy for the therapeutic targeting of protein phosphatases involves the use of compounds that interfere with the binding of regulatory subunits or substrates. However, high-throughput screening strategies for such interferin...
Lara Ibrahim,Caroline Stanton,Kayla Nutsch et al.
Lara Ibrahim et al.
Cross talk between metabolism and stress-responsive signaling is essential for maintaining cellular homeostasis. This cross talk is often achieved through covalent modification of proteins by endogenous, reactive metabolites that regulate k...
USP10 strikes down β-catenin by dual-wielding deubiquitinase activity and phase separation potential [0.03%]
USP10通过双重去泛素酶活性和相分离潜能降解β-catenin
Yinuo Wang,Aihua Mao,Jingwei Liu et al.
Yinuo Wang et al.
Wnt/β-catenin signaling is a conserved pathway crucially governing development, homeostasis, and oncogenesis. Discoveries of its regulators hold great values in both basic and translational research. Through screening, we identified a deub...
Inducible mismatch repair streamlines forward genetic approaches to target identification of cytotoxic small molecules [0.03%]
毒性小分子靶标鉴定的正向遗传学方法得到简化
Thu P Nguyen,Min Fang,Jiwoong Kim et al.
Thu P Nguyen et al.
Orphan cytotoxins are small molecules for which the mechanism of action (MoA) is either unknown or ambiguous. Unveiling the mechanism of these compounds may lead to useful tools for biological investigation and new therapeutic leads. In sel...
Ajit Kumar Sharma,Anish Thomas
Ajit Kumar Sharma
Circular RNAs (circRNAs) are covalently closed RNA molecules whose functions are still largely uncharacterized. In the July issue of Cancer Cell, Conn et al.1 demonstrate that circRNA can bind cognate DNA loci, forming circRNA-DNA hybrids (...
Martti Maimets
Martti Maimets
The emergence of antibody based surrogate WNT molecules has revolutionized research exploiting organoid cultures. In this issue of Cell Chemical Biology, Post et al.1 present a refined collection of WNT mimetics with unprecedented WNT/β-ca...