Protein acylation by saturated very long chain fatty acids and endocytosis are involved in necroptosis [0.03%]
饱和非常长链脂肪酸介导的蛋白质脂化和内吞作用参与坏死性凋亡
Apoorva J Pradhan,Daniel Lu,Laura R Parisi et al.
Apoorva J Pradhan et al.
Necroptosis is a form of cell death characterized by receptor-interacting protein kinase activity and plasma membrane permeabilization via mixed-lineage kinase-like protein (MLKL). This permeabilization is responsible for the inflammatory p...
Fragment-linking peptide design yields a high-affinity ligand for microtubule-based transport [0.03%]
片段连接肽设计获得了微管依赖型转运的高亲和力配体
Jessica A Cross,Magda S Chegkazi,Roberto A Steiner et al.
Jessica A Cross et al.
Synthetic peptides are attractive candidates to manipulate protein-protein interactions inside the cell as they mimic natural interactions to compete for binding. However, protein-peptide interactions are often dynamic and weak. A challenge...
Targeted degradation of transcription factors by TRAFTACs: TRAnscription Factor TArgeting Chimeras [0.03%]
利用TRAFTAC降解转录因子：TRAnscription Factor TArgeting Chimeras
Kusal T G Samarasinghe,Saul Jaime-Figueroa,Michael Burgess et al.
Kusal T G Samarasinghe et al.
Many diseases, including cancer, stem from aberrant activation or overexpression of oncoproteins that are associated with multiple signaling pathways. Although proteins with catalytic activity can be successfully drugged, the majority of ot...
Decoding the messaging of the ubiquitin system using chemical and protein probes [0.03%]
利用化学和蛋白质探针解码泛素系统的信号分子功能
Lukas T Henneberg,Brenda A Schulman
Lukas T Henneberg
Post-translational modification of proteins by ubiquitin is required for nearly all aspects of eukaryotic cell function. The numerous targets of ubiquitylation, and variety of ubiquitin modifications, are often likened to a code, where the ...
N-Thio-β-lactams targeting L,D-transpeptidase-2, with activity against drug-resistant strains of Mycobacterium tuberculosis [0.03%]
针对药物耐药性结核分枝杆菌且作用于L,D-转肽酶-2的N-硫代-β-内酰胺类新药
Giulia Martelli,Tomas Bohn Pessatti,Eva Maria Steiner et al.
Giulia Martelli et al.
Effective treatment of tuberculosis is frequently hindered by the emerging antimicrobial resistance of Mycobacterium tuberculosis. The present study evaluates monocyclic β-lactam compounds targeting the mycobacterial cell wall remodeling. ...
Small molecule targeting of biologically relevant RNA tertiary and quaternary structures [0.03%]
靶向生物相关RNA三级和四级结构的小分子
Martina Zafferani,Amanda E Hargrove
Martina Zafferani
Initial successes in developing small molecule ligands for non-coding RNAs have underscored their potential as therapeutic targets. More recently, these successes have been aided by advances in biophysical and structural techniques for iden...
Identification and selectivity profiling of small-molecule degraders via multi-omics approaches [0.03%]
基于多组学方法的小分子降解剂的鉴定与选择性评价
Natalie S Scholes,Cristina Mayor-Ruiz,Georg E Winter
Natalie S Scholes
The therapeutic modality of targeted protein degradation promises to overcome limitations of traditional pharmacology. Small-molecule degraders recruit disease-causing proteins to E3 ubiquitin ligases, prompting their ubiquitination and deg...
Bioorthogonal dissection of the replicase assembly of hepatitis C virus [0.03%]
用于解剖丙型肝炎病毒复制酶组装的生物正交方法
Yang Zhang,Shuiye Chen,Zhenghong Yuan et al.
Yang Zhang et al.
Positive-strand RNA viruses such as hepatitis C virus (HCV), flaviviruses, and coronaviruses are medically important. Assembly of replicase on host membranes is a conserved replication strategy and an attractive antiviral target. The mechan...
CYP27A1-dependent anti-melanoma activity of limonoid natural products targets mitochondrial metabolism [0.03%]
柠檬苦素类天然产物的抗黑色素瘤活性依赖于CYP27A1并针对线粒体代谢
Hyelim Cho,Qiong Shen,Lydia H Zhang et al.
Hyelim Cho et al.
Three limonoid natural products with selective anti-proliferative activity against BRAF(V600E) and NRAS(Q61K)-mutation-dependent melanoma cell lines were identified. Differential transcriptome analysis revealed dependency of compound activi...
The role of reversible and irreversible covalent chemistry in targeted protein degradation [0.03%]
可逆和不可逆共价化学在靶向蛋白降解中的作用
Hannah Kiely-Collins,Georg E Winter,Gonçalo J L Bernardes
Hannah Kiely-Collins
Proteolysis-targeting chimeras (PROTACs) that degrade disease-causing proteins by hijacking the endogenous ubiquitin-proteasome system have emerged as an exciting and transformative technology in both chemical biology and drug discovery. Cu...