Chemoproteomics profiling of surfactin-producing nonribosomal peptide synthetases in living bacterial cells [0.03%]
活细菌细胞中产surfactin非核糖体肽合成酶的化学蛋白质组学分析
Fumihiro Ishikawa,Sho Konno,Chiharu Uchida et al.
Fumihiro Ishikawa et al.
Much of our current knowledge on nonribosomal peptide synthetases (NRPSs) is based on studies in which the full NRPS system or each protein domain is expressed in heterologous hosts. Consequently, methods to detect the endogenous activity o...
Anthony C Varca,Dominick Casalena,Wai Cheung Chan et al.
Anthony C Varca et al.
Deubiquitinating enzymes (DUBs) are a class of isopeptidases that regulate ubiquitin dynamics through catalytic cleavage of ubiquitin from protein substrates and ubiquitin precursors. Despite growing interest in DUB biological function and ...
Peripherally active dextromethorphan derivatives lower blood glucose levels by targeting pancreatic islets [0.03%]
外周活性右美沙芬衍生物通过靶向胰岛来降低血糖水平
Okka Scholz,Silke Otter,Alena Welters et al.
Okka Scholz et al.
Dextromethorphan (DXM) acts as cough suppressant via its central action. Cell-protective effects of this drug have been reported in peripheral tissues, making DXM potentially useful for treatment of several common human diseases, such as ty...
Martin Reynders,Dirk Trauner
Martin Reynders
Molecular glues and proteolysis targeting chimeras (PROTACs) have emerged as small-molecule tools that selectively induce the degradation of a chosen protein and have shown therapeutic promise. Recently, several approaches employing light a...
Target identification for small-molecule discovery in the FOXO3a tumor-suppressor pathway using a biodiverse peptide library [0.03%]
基于生物多样性肽库的FOXO3a肿瘤抑制通路小分子靶点鉴定
Amy Emery,Bryn S Hardwick,Alex T Crooks et al.
Amy Emery et al.
Genetic screening technologies to identify and validate macromolecular interactions (MMIs) essential for complex pathways remain an important unmet need for systems biology and therapeutics development. Here, we use a library of peptides fr...
Cristina Cheng,Mi Zhou,Qiwen Su et al.
Cristina Cheng et al.
The generation of a library of variant genes is a prerequisite of directed evolution, a powerful tool for biomolecular engineering. As the number of all possible sequences often far exceeds the diversity of a practical library, methods that...
On-tissue spatially resolved glycoproteomics guided by N-glycan imaging reveal global dysregulation of canine glioma glycoproteomic landscape [0.03%]
基于N-聚糖成像的组织内空间分辨糖蛋白组学揭示了犬胶质瘤糖蛋白组景观的全局失调
Stacy Alyse Malaker,Jusal Quanico,Antonella Raffo-Romero et al.
Stacy Alyse Malaker et al.
Here, we present an approach to identify N-linked glycoproteins and deduce their spatial localization using a combination of matrix-assisted laser desorption ionization (MALDI) N-glycan mass spectrometry imaging (MSI) and spatially resolved...
Small molecules as tools for functional assessment of deubiquitinating enzyme function [0.03%]
小分子用于去泛素化酶功能表征的工具分子研究进展
Robert S Magin,Xiaoxi Liu,Alejandra Felix et al.
Robert S Magin et al.
Deubiquitinating enzymes (DUBs) are a largely understudied and untapped resource in the toolkit of protein degradation functionalities. They comprise a large repertoire of enzymes that remove ubiquitin from substrates in a variety of cellul...
Daiki Takahashi,Hirokazu Arimoto
Daiki Takahashi
Degrader technologies, which enable the chemical knockdown of disease-causing proteins, are promising for drug discovery. After two decades of research, degraders using the ubiquitin-proteasome system (UPS) are currently in clinical trials....
Native mass spectrometry and gas-phase fragmentation provide rapid and in-depth topological characterization of a PROTAC ternary complex [0.03%]
原生质谱和气相解离可快速且深入地表征PROTAC三元复合物的拓扑结构
Jong Hee Song,Nicole D Wagner,Jing Yan et al.
Jong Hee Song et al.
Proteolysis-targeting chimeras (PROTACs) represent a new direction in small-molecule therapeutics whereby a heterobifunctional linker to a protein of interest (POI) induces its ubiquitination-based proteolysis by recruiting an E3 ligase. He...