Discovery of a Functional Covalent Ligand Targeting an Intrinsically Disordered Cysteine within MYC [0.03%]
靶向MYC内在无序半胱氨酸的功能性共价配体的发现
Lydia Boike,Alexander G Cioffi,Felix C Majewski et al.
Lydia Boike et al.
MYC is a major oncogenic transcriptional driver of most human cancers that has remained intractable to direct targeting because much of MYC is intrinsically disordered. Here, we have performed a cysteine-reactive covalent ligand screen to i...
A Rapid and Precise Mutation-Activated Fluorescence Reporter for Analyzing Acute Mutagenesis Frequency [0.03%]
用于分析急性诱变频率的快速精确突变激活荧光报告基因
Michael D Birnbaum,Leah Nemzow,Akhilesh Kumar et al.
Michael D Birnbaum et al.
Published Erratum
Cell chemical biology. 2020 Sep 17;27(9):1220. DOI:10.1016/j.chembiol.2020.08.016 2020
Adnan Shami Shah,Hongyan Sun,Jeremy M Baskin
Adnan Shami Shah
In this issue of Cell Chemical Biology, Hong et al. (2020) use in situ chemoenzymatic labeling to discover that fucosylation of the Wnt co-receptor LRP6 induces its endocytosis and downregulates Wnt/β-catenin signaling. Their findings reve...
Networking in Circulation: Lipoproteins, PM20D1, and N-acyl Amino Acid Bioactivity [0.03%]
流通中的网络：脂蛋白，PM20D1和N-酰基氨基酸生物活性
Alan Saghatelian
Alan Saghatelian
N-acyl amino acids are a class of biologically active lipids that control thermogenesis, and their biosynthesis is facilitated by PM20D1. In this issue of Cell Chemical Biology, Kim et al. (2020) identify a lipoprotein-albumin network in th...
Winding Down: Selectively Drugging a Promiscuous Pocket in Cryptochrome Slows Circadian Rhythms [0.03%]
放缓步伐：在隐花色素中选择性地使一个多才多艺的结合口袋药物化来减缓生物钟节奏
Brian R Crane
Brian R Crane
Mammalian cryptochromes regulate sleep and metabolism as components of the circadian clock. In this issue of Cell Chemical Biology, Miller et al. (2020a) use phenotypic chemical screens to identify selective modulators of two cryptochrome i...
Jie Jiang,Baishan Jiang,Zhixiang He et al.
Jie Jiang et al.
MKK4/7 are kinases that phosphorylate JNKs and regulate the MAPK signaling pathway. Their overexpression has been associated with tumorigenesis and aggressiveness in cancers such as breast, prostate, non-small cell lung, and pediatric leuke...
Eradicating Bacterial Persisters with Combinations of Strongly and Weakly Metabolism-Dependent Antibiotics [0.03%]
用强代谢依赖性抗生素和弱代谢依赖性抗生素结合消除细菌持续感染细胞
Erica J Zheng,Jonathan M Stokes,James J Collins
Erica J Zheng
The vast majority of bactericidal antibiotics display poor efficacy against bacterial persisters, cells that are in a metabolically repressed state. Molecules that retain their bactericidal functions against such bacteria often display toxi...
Mechanism-Based Personalized Medicine for Cystic Fibrosis by Suppressing Pseudo Exon Inclusion [0.03%]
通过抑制假外显子的包含来治疗囊性纤维化的基于机制的个性化医疗
Saiko Shibata,Masahiko Ajiro,Masatoshi Hagiwara
Saiko Shibata
Cystic fibrosis (CF) is caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene that compromise its chloride channel activity. Here, we present a therapeutic strategy to ameliorate RNA splicing deficiency ...
Designed Parasite-Selective Rhomboid Inhibitors Block Invasion and Clear Blood-Stage Malaria [0.03%]
设计的寄生虫选择性菱形抑制剂可阻止疟原虫侵入并清除血液阶段疟疾
Shiv Gandhi,Rosanna P Baker,Sangwoo Cho et al.
Shiv Gandhi et al.
Rhomboid intramembrane proteases regulate pathophysiological processes, but their targeting in a disease context has never been achieved. We decoded the atypical substrate specificity of malaria rhomboid PfROM4, but found, unexpectedly, tha...
Proteostasis Regulators Restore Function of Epilepsy-Associated GABAA Receptors [0.03%]
蛋白质稳态调节因子恢复与癫痫相关的GABAa受体的功能
Xiao-Jing Di,Ya-Juan Wang,Edmund Cotter et al.
Xiao-Jing Di et al.
Proteostasis deficiency in mutated ion channels leads to a variety of ion channel diseases that are caused by excessive endoplasmic reticulum-associated degradation (ERAD) and inefficient membrane trafficking. We investigated proteostasis m...