Single-Domain Antibodies as Crystallization Chaperones to Enable Structure-Based Inhibitor Development for RBR E3 Ubiquitin Ligases [0.03%]
用于RBR泛素连接酶结构基础抑制剂研发的单域抗体作为结晶护簇蛋白
Yi-Chun Isabella Tsai,Henrik Johansson,David Dixon et al.
Yi-Chun Isabella Tsai et al.
Protein ubiquitination plays a key role in the regulation of cellular processes, and misregulation of the ubiquitin system is linked to many diseases. So far, development of tool compounds that target enzymes of the ubiquitin system has bee...
Identification of a Small Compound Targeting PKM2-Regulated Signaling Using 2D Gel Electrophoresis-Based Proteome-wide CETSA [0.03%]
基于二维凝胶电泳的蛋白质组学CETSA技术筛选PKM2调控信号通路的小分子化合物
Ikuko Nagasawa,Makoto Muroi,Makoto Kawatani et al.
Ikuko Nagasawa et al.
The cellular thermal shift assay (CETSA) has recently been devised as a label-free method for target validation of small compounds and monitoring the thermal stabilization or destabilization of proteins due to binding with the compound. Her...
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex [0.03%]
靶向EED的PROTAC降解PRC2复合体中的EED、EZH2和SUZ12蛋白质
Jessie Hao-Ru Hsu,Timothy Rasmusson,James Robinson et al.
Jessie Hao-Ru Hsu et al.
Deregulation of the PRC2 complex, comprised of the core subunits EZH2, SUZ12, and EED, drives aberrant hypermethylation of H3K27 and tumorigenicity of many cancers. Although inhibitors of EZH2 have shown promising clinical activity, preclin...
Dominique O Gaffney,Erin Q Jennings,Colin C Anderson et al.
Dominique O Gaffney et al.
Post-translational modifications (PTMs) regulate enzyme structure and function to expand the functional proteome. Many of these PTMs are derived from cellular metabolites and serve as feedback and feedforward mechanisms of regulation. We ha...
Emergence of SARM1 as a Potential Therapeutic Target for Wallerian-type Diseases [0.03%]
SARM1成为沃勒型退行性疾病的潜在治疗靶点
Heather S Loring,Paul R Thompson
Heather S Loring
Wallerian degeneration is a neuronal death pathway that is triggered in response to injury or disease. Death was thought to occur passively until the discovery of a mouse strain, i.e., Wallerian degeneration slow (WLDS), which was resistant...
Brent R Stockwell
Brent R Stockwell
In this issue of Cell Chemical Biology, Shah et al. (2019) report an in vitro, high-throughput assay that predicts the ability of compounds to suppress peroxidation of phospholipids. This approach provides a way to design and optimize targe...
Taylor M Courtney,Alexander Deiters
Taylor M Courtney
In this issue of Cell Chemical Biology, the Sterner lab reports the application of photoswitchable unnatural amino acids in controlling protein allostery in the enzyme complex imidazole glycerol phosphate synthase (Kneuttinger et al., 2019)...
Zhengnian Li,Benika J Pinch,Calla M Olson et al.
Zhengnian Li et al.
The G1/S cell cycle checkpoint is frequently dysregulated in cancer, leaving cancer cells reliant on a functional G2/M checkpoint to prevent excessive DNA damage. Wee1 regulates the G2/M checkpoint by phosphorylating CDK1 at Tyr15 to preven...
Metabolic Modifier Screen Reveals Secondary Targets of Protein Kinase Inhibitors within Nucleotide Metabolism [0.03%]
代谢调节筛选发现蛋白激酶抑制剂作用的核苷酸代谢中的二级靶点
Evan R Abt,Ethan W Rosser,Matthew A Durst et al.
Evan R Abt et al.
Biosynthesis of the pyrimidine nucleotide uridine monophosphate (UMP) is essential for cell proliferation and is achieved by the activity of convergent de novo and salvage metabolic pathways. Here we report the development and application o...
Development of Photocrosslinking Probes Based on Huwentoxin-IV to Map the Site of Interaction on Nav1.7 [0.03%]
基于胡蚊毒素-IV的光交联探针的发展以图示Nav1.7上的作用位点
Foteini Tzakoniati,Hui Xu,Tianbo Li et al.
Foteini Tzakoniati et al.
Voltage-gated sodium (Nav) channels respond to changes in the membrane potential of excitable cells through the concerted action of four voltage-sensor domains (VSDs). Subtype Nav1.7 plays an important role in the propagation of signals in ...