Identification of ligands for E3 ligases with restricted expression using fragment-based methods [0.03%]
利用片段化方法鉴定特定表达E3连接酶的配体
Alex G Waterson,Brian D Lehmann,Zhenwei Lu et al.
Alex G Waterson et al.
Heterobifunctional molecules that induce targeted degradation have emerged as powerful tools in chemical biology, target validation, and drug discovery. Despite their promise, the field is constrained by the relative paucity of ligands avai...
Karen J Deane,Joel Haywood,Michael D Wallace et al.
Karen J Deane et al.
Dicamba, although a potent and useful herbicide in weed management, is notorious for its off-target movement due to volatility. Here, we describe carbohydrate esters of dicamba as an unexplored pro-herbicide approach that addresses the vola...
Profiling polyamine-protein interactions in live cells through photoaffinity labeling [0.03%]
光亲和标记活细胞中的聚胺-蛋白质相互作用
Maciej Zakrzewski,Zuzanna Sas,Benjamin Cocom-Chan et al.
Maciej Zakrzewski et al.
Polyamines are essential metabolites that play a crucial role in regulating key cellular processes. While previous studies have shown that polyamines modulate protein function through non-covalent interactions, the lack of robust analytical...
A trifunctional probe for generation of fluorogenic glycan-photocrosslinker conjugates [0.03%]
一种用于生成发光糖类光交联剂缀合物的三功能探针
Brandon Vreulz,Daphnée De Crozals,Samy Cecioni
Brandon Vreulz
Interactions between cell surface glycans and lectins mediate vital biological processes, yet their characterization is hindered by the low affinity of these binding events. While photoaffinity labeling can capture these interactions, tradi...
Convergent construction of N-terminally modified CCL5 chemokines for photoaffinity receptor pull-down using cross-aldol bioconjugations [0.03%]
使用交叉烯醇化生物连接法构建CCL5趋化因子N端修饰衍生物的光亲和力受体下拉实验
Afzaal Tufail,Matthew E Warnes,Nathalie Signoret et al.
Afzaal Tufail et al.
Chemokines such as CCL5 (RANTES) mediate immune responses via interaction with G-protein-coupled receptors like CCR5, which also serves as a co-receptor for HIV-1 entry into host cells. Modified CCL5 analogues have shown promise as CCR5 ant...
Nicole Stéphanie Galenkamp,Marco van den Noort,Giovanni Maglia
Nicole Stéphanie Galenkamp
Enzymes are powerful catalysts that perform chemical reactions with remarkable speed and specificity. Their intrinsic dynamics often play a crucial role in determining their catalytic properties. To achieve a comprehensive understanding of ...
Cell-based high-throughput screening using a target-NanoLuc fusion construct to identify molecular glue degraders of c-Myc oncoprotein [0.03%]
基于细胞的高通量筛选识别c-Myc致癌蛋白分子胶降解剂靶点-NanoLuc融合构建物
Muyu Xu,Jinying Qiu,Lin Tan et al.
Muyu Xu et al.
Oncoprotein c-Myc (Myc) plays a critical role in regulating cellular gene expression. Although Myc dysregulation is found in more than 70% of cancers and can facilitate tumor initiation and progression, it is still considered to be an "undr...
Novel terbium-sensitizing peptide substrates for cyclin-dependent kinase 5 (CDK5) and their demonstration in luminescence kinase assays [0.03%]
用于细胞周期蛋白依赖性激酶5(CDK5)的新型铽敏化肽底物及其在发光激酶测定法中的应用
Jason L Heier,Dylan J Boselli,Laurie L Parker
Jason L Heier
Novel time-resolved terbium luminescence assays were developed for CDK5 and CDK2 by designing synthetic substrates which incorporate phospho-inducible terbium sensitizing motifs with kinase substrate consensus sequences. A substrate designe...
Structural basis of SIRT2 pre-catalysis NAD+ binding dynamics and mechanism [0.03%]
SIRT2 催化前NAD+结合动力学和机制的结构基础
Nan Zhang,Kah Chee Pow,Lanfang Chen et al.
Nan Zhang et al.
Sirtuins are an evolutionarily conserved family of NAD+-dependent deacylases whose catalytic mechanism remains under active investigation. While previous studies have captured sirtuin reaction intermediates using thioacetyl-lysine analogs, ...
Biosynthesis of sydonol reveals a new bisabolene cyclase and an unusual P450 aromatase [0.03%]
_sydonol的生物合成揭示了一种新的倍半蒈烯环化酶和一种不寻常的P450芳构化酶
Peiyu Lu,Ling Liu
Peiyu Lu
In this work, the biosynthetic gene cluster and assembly line of sydonol were discovered and identified. As a result, and importantly, two unusual chemical conversions catalyzed by a new bisabolene cyclase and an unusual P450 aromatase were...