From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9 [0.03%]
从筛选到靶向降解：PCSK9小分子配体发现与优化策略
Whitney L Petrilli,Gregory C Adam,Roman S Erdmann et al.
Whitney L Petrilli et al.
Published Erratum
Cell chemical biology. 2021 Feb 18;28(2):243. DOI:10.1016/j.chembiol.2021.01.019 2021
Arabidopsis P-Glycoprotein19 Participates in the Inhibition of Gravitropism by Gravacin [0.03%]
拟南芥P-糖蛋白19参与gravacin抑制重力感置的研究
Marcela Rojas-Pierce,Boosaree Titapiwatanakun,Eun Ju Sohn et al.
Marcela Rojas-Pierce et al.
Published Erratum
Cell chemical biology. 2021 Feb 18;28(2):242. DOI:10.1016/j.chembiol.2021.01.014 2021
Making HSP90 Inhibitors Great Again? Unite for Better Cancer Immunotherapy [0.03%]
让HSP90抑制剂再次伟大吗？携手推动更好的癌症免疫治疗
Michael W Graner
Michael W Graner
HSP90 inhibitors are in numerous cancer clinical trials, but treatments often induce toxicity at effective dosages. In this issue of Cell Chemical Biology, Zavareh et al. (2020) serendipitously found that HSP90 inhibitors, at manageable dos...
Ku-Lung Hsu
Ku-Lung Hsu
In this issue of Cell Chemical Biology, Seneviratne et al. (2020) combine photoaffinity labeling and quantitative chemical proteomics to identify the molecular target of a lead compound discovered from a phenotypic drug screen. Their work s...
Blocking the Enablers: Selective Inhibition of CDK9 Reins in an Unchecked Master Regulator [0.03%]
阻断帮凶：选择性抑制CDK9使失控的主调控因子归于休眠状态
Aseem Z Ansari
Aseem Z Ansari
In their quest to disable androgen receptor variants that drive castration-resistant prostate cancer, Richters et al. (2020) have hit upon a selective inhibitor of a transcriptional kinase that enables full-length mRNA synthesis. Drugging t...
Reimagining dots and dashes: Visualizing structure and function of organelles for high-content imaging analysis [0.03%]
点与线的重构——利用高内涵成像分析细胞器结构和功能
Marcus Y Chin,Jether Amos Espinosa,Grace Pohan et al.
Marcus Y Chin et al.
Organelles are responsible for biochemical and cellular processes that sustain life and their dysfunction causes diseases from cancer to neurodegeneration. While researchers are continuing to appreciate new roles of organelles in disease, t...
Pauline Lejault,Jérémie Mitteaux,Francesco Rota Sperti et al.
Pauline Lejault et al.
For over two decades, the prime objective of the chemical biology community studying G-quadruplexes (G4s) has been to use chemicals to interact with and stabilize G4s in cells to obtain mechanistic interpretations. This strategy has been un...
Jayme L Dahlin,Douglas S Auld,Ina Rothenaigner et al.
Jayme L Dahlin et al.
Compounds that exhibit assay interference or undesirable mechanisms of bioactivity ("nuisance compounds") are routinely encountered in cellular assays, including phenotypic and high-content screening assays. Much is known regarding compound...
A high-performance genetically encoded fluorescent biosensor for imaging physiological peroxynitrite [0.03%]
一种高性能的遗传编码荧光生物传感器 用于生理型过氧亚硝酸盐成像
Zhijie Chen,Shen Zhang,Xinyu Li et al.
Zhijie Chen et al.
Peroxynitrite is a reactive nitrogen species (RNS) that plays critical roles in signal transduction, stress response, and numerous human diseases. Advanced molecular tools that permit the selective, sensitive, and noninvasive detection of p...
Louis P Conway,Weichao Li,Christopher G Parker
Louis P Conway
The ID of disease-modifying, chemically accessible targets remains a central priority of modern therapeutic discovery. The phenotypic screening of small-molecule libraries not only represents an attractive approach to identify compounds tha...