Xin Wang,Daigo Inoyama,Riccardo Russo et al.
Xin Wang et al.
The triazine antitubercular JSF-2019 was of interest due to its in vitro efficacy and the nitro group shared with the clinically relevant delamanid and pretomanid. JSF-2019 undergoes activation requiring F420H2 and one or more nitroreductas...
A Highly Productive, One-Pot Cell-Free Protein Synthesis Platform Based on Genomically Recoded Escherichia coli [0.03%]
基于基因组重构的大肠杆菌的高效单管无细胞蛋白质合成平台
Benjamin J Des Soye,Vincent R Gerbasi,Paul M Thomas et al.
Benjamin J Des Soye et al.
The site-specific incorporation of non-canonical amino acids (ncAAs) into proteins via amber suppression provides access to novel protein properties, structures, and functions. Historically, poor protein expression yields resulting from rel...
A Selective Ligand for Estrogen Receptor Proteins Discriminates Rapid and Genomic Signaling [0.03%]
雌激素受体蛋白的配体选择性区分快速信号和基因组信号
Chetana M Revankar,Cristian G Bologa,Richard A Pepermans et al.
Chetana M Revankar et al.
Estrogen exerts extensive and diverse effects throughout the body of women. In addition to the classical nuclear estrogen receptors (ERα and ERβ), the G protein-coupled estrogen receptor GPER is an important mediator of estrogen action. E...
Jean Lehmann,Shixin Ye
Jean Lehmann
The possible mechanism(s) by which ribosomes make peptide bonds during protein synthesis have been explored for decades. Yet, there is no agreement on how the catalytic site, the peptidyl transferase center (PTC), promotes this reaction. He...
Locally Activating TrkB Receptor Generates Actin Waves and Specifies Axonal Fate [0.03%]
轴突命运的决定需要TrkB受体局部激活生成的 actin 波
Doyeon Woo,Yeji Seo,Hyunjin Jung et al.
Doyeon Woo et al.
Actin waves are filamentous actin (F-actin)-rich structures that initiate in the somato-neuritic area and move toward neurite ends. The upstream cues that initiate actin waves are poorly understood. Here, using an optogenetic approach (Opto...
Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents [0.03%]
MAP4K抑制剂的开发作为 motor neuron保护剂
Pieter H Bos,Emily R Lowry,Jonathon Costa et al.
Pieter H Bos et al.
Disease-causing mutations in many neurodegenerative disorders lead to proteinopathies that trigger endoplasmic reticulum (ER) stress. However, few therapeutic options exist for patients with these diseases. Using an in vitro screening platf...
Lucas T Gray,Emilia Puig Lombardi,Daniela Verga et al.
Lucas T Gray et al.
Heme is an essential cofactor for many enzymes, but free heme is toxic and its levels are tightly regulated. G-quadruplexes bind heme avidly in vitro, raising the possibility that they may sequester heme in vivo. If so, then treatment that ...
Identifying Anti-prion Chemical Compounds Using a Newly Established Yeast High-Throughput Screening System [0.03%]
利用新型酵母高通量筛选系统鉴定抗蛋白酶体化合物
Zhiqiang Du,Stephanie Valtierra,Luzivette Robles Cardona et al.
Zhiqiang Du et al.
Prion-like protein aggregation underlies the pathology of a group of fatal neurodegenerative diseases in humans, including Alzheimer's disease (AD), Parkinson's disease, amyotrophic lateral sclerosis, and transmissible spongiform encephalop...
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.
Proprotein convertase substilisin-like/kexin type 9 (PCSK9) is a serine protease involved in a protein-protein interaction with the low-density lipoprotein (LDL) receptor that has both human genetic and clinical validation. Blocking this pr...
Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation [0.03%]
近年共价配体的选择性和不可逆性开发及验证的进展
Tinghu Zhang,John M Hatcher,Mingxing Teng et al.
Tinghu Zhang et al.
Some of the most widely used drugs, such as aspirin and penicillin, are covalent drugs. Covalent binding can improve potency, selectivity, and duration of the effects, but the intrinsic reactivity represents a potential liability and may re...