Daniel Lucy,Leran Zhang,Edward W Tate
Daniel Lucy
In this issue of Cell Chemical Biology, Yoo et al. (2020) use chemical proteomics to identify target proteins for the potent antimalarial natural product Salinipostin A. Polypharmacology from targeting multiple parasite serine hydrolases an...
Science that Inspires [0.03%]
激发灵感的科学
Cell Press Team
Cell Press Team
Polynuclear Ruthenium Amines Inhibit K2P Channels via a "Finger in the Dam" Mechanism [0.03%]
多核钌胺类化合物通过“指坝泄流”机制抑制钾两孔道通道
Lianne Pope,Marco Lolicato,Daniel L Minor Jr
Lianne Pope
The trinuclear ruthenium amine ruthenium red (RuR) inhibits diverse ion channels, including K2P potassium channels, TRPs, the calcium uniporter, CALHMs, ryanodine receptors, and Piezos. Despite this extraordinary array, there is limited inf...
CRISPR-Mediated Protein Tagging with Nanoluciferase to Investigate Native Chemokine Receptor Function and Conformational Changes [0.03%]
利用NanoLuciferase标记原生趋化因子受体研究其功能和构象变化的CRISPR技术
Carl W White,Birgit Caspar,Hannah K Vanyai et al.
Carl W White et al.
G protein-coupled receptors are a major class of membrane receptors that mediate physiological and pathophysiological cellular signaling. Many aspects of receptor activation and signaling can be investigated using genetically encoded lumine...
James M Johnson,Alexander S Hebert,Quentin H Drane et al.
James M Johnson et al.
Polo-like kinase 1 has hundreds of substrates and multiple functions that operate within the ∼60 min of mitosis. Herein, we describe a chemical-genetic system that allows particular substrates to be "toggled" into or out of chemical contro...
Shihua Yao,Tuong-Vi Nguyen,Alan Rolfe et al.
Shihua Yao et al.
Carbamoyl phosphate synthetase 1 (CPS1) catalyzes the first step in the ammonia-detoxifying urea cycle, converting ammonia to carbamoyl phosphate under physiologic conditions. In cancer, CPS1 overexpression supports pyrimidine synthesis to ...
Management of Hsp90-Dependent Protein Folding by Small Molecules Targeting the Aha1 Co-Chaperone [0.03%]
靶向Aha1辅助分子的的小分子对Hsp90依赖性蛋白质折叠的调控
Jay K Singh,Darren M Hutt,Bradley Tait et al.
Jay K Singh et al.
Hsp90 plays an important role in health and is a therapeutic target for managing misfolding disease. Compounds that disrupt co-chaperone delivery of clients to Hsp90 target a subset of Hsp90 activities, thereby minimizing the toxicity of pa...
Simon A Hawley,Fiona A Ross,Fiona M Russell et al.
Simon A Hawley et al.
Cordycepin (3'-deoxyadenosine) is a major bioactive agent in Cordyceps militaris, a fungus used in traditional Chinese medicine. It has been proposed to have many beneficial metabolic effects by activating AMP-activated protein kinase (AMPK...
DAGL-Beta Functions as a PUFA-Specific Triacylglycerol Lipase in Macrophages [0.03%]
DAGL-β作为巨噬细胞中的PUFA特异性三酰基甘油脂肪酶的功能研究
Myungsun Shin,Timothy B Ware,Ku-Lung Hsu
Myungsun Shin
Here, we apply quantitative chemical proteomics and untargeted lipidomics to assign a polyunsaturated fatty acid (PUFA)-specific triacylglycerol (TAG) lipase activity for diacylglycerol lipase-beta (DAGLβ) in macrophages. We demonstrate th...
Cyclization Reaction-Based Turn-on Probe for Covalent Labeling of Target Proteins [0.03%]
基于环化反应的靶蛋白共价标记“开亮”探针
Hiroyuki Kojima,Yuki Fujita,Ryosuke Takeuchi et al.
Hiroyuki Kojima et al.
Fluorescent molecules have contributed to basic biological research but there are currently only a limited number of probes available for the detection of non-enzymatic proteins. Here, we report turn-on fluorescent probes mediated by conjug...