Daniel K Nomura,Mishtu Dey
Daniel K Nomura
Ashley E Modell,Sophia Lai,Tuan M Nguyen et al.
Ashley E Modell et al.
Nature takes advantage of induced proximity to perform various functions. Taking inspiration from nature, we can also trigger desired biological processes using bifunctional small molecules that artificially induce proximity. For example, b...
CETSA interaction proteomics define specific RNA-modification pathways as key components of fluorouracil-based cancer drug cytotoxicity [0.03%]
基于CETSA的蛋白质组相互作用研究定义了特定RNA修饰通路是氟尿嘧啶类抗肿瘤药物细胞毒性的关键因素
Ying Yu Liang,Smaranda Bacanu,Lekshmy Sreekumar et al.
Ying Yu Liang et al.
The optimal use of many cancer drugs is hampered by a lack of detailed understanding of their mechanism of action (MoA). Here, we apply a high-resolution implementation of the proteome-wide cellular thermal shift assay (CETSA) to follow pro...
SARS-COV-2 spike binding to ACE2 in living cells monitored by TR-FRET [0.03%]
利用TR-FRET监测SARS-CoV-2刺突蛋白与ACE2结合活细胞中的相互作用
Erika Cecon,Matilda Burridge,Longxing Cao et al.
Erika Cecon et al.
Targeting the interaction between the SARS-CoV-2 spike protein and human ACE2, its primary cell membrane receptor, is a promising therapeutic strategy to prevent viral entry. Recent in vitro studies revealed that the receptor binding domain...
The Plasmodium falciparum ABC transporter ABCI3 confers parasite strain-dependent pleiotropic antimalarial drug resistance [0.03%]
疟原虫ABC转运蛋白ABCI3产生strain依赖的多药耐药表型
James M Murithi,Ioanna Deni,Charisse Flerida A Pasaje et al.
James M Murithi et al.
Widespread Plasmodium falciparum resistance to first-line antimalarials underscores the vital need to develop compounds with novel modes of action and identify new druggable targets. Here, we profile five compounds that potently inhibit P. ...
Exploiting polypharmacology to dissect host kinases and kinase inhibitors that modulate endothelial barrier integrity [0.03%]
利用多靶标药理学解剖宿主激酶和调节内皮屏障完整性的激酶抑制剂
Selasi Dankwa,Mary-Margaret Dols,Ling Wei et al.
Selasi Dankwa et al.
Kinase inhibitors are promising drugs to stabilize the endothelial barrier following inflammatory damage. However, our limited knowledge of how kinase signaling activates barrier-restorative pathways and the complexity of multi-target drugs...
Combined morphological and proteome profiling reveals target-independent impairment of cholesterol homeostasis [0.03%]
结合形态和蛋白质谱分析揭示胆固醇稳态的靶点非依赖性受损现象
Tabea Schneidewind,Alexandra Brause,Beate Schölermann et al.
Tabea Schneidewind et al.
Unbiased profiling approaches are powerful tools for small-molecule target or mode-of-action deconvolution as they generate a holistic view of the bioactivity space. This is particularly important for non-protein targets that are difficult ...
Development of red genetically encoded biosensor for visualization of intracellular glucose dynamics [0.03%]
红光遗传编码生物传感器的开发用于可视化细胞内葡萄糖动力学
Marie Mita,Izumi Sugawara,Kazuki Harada et al.
Marie Mita et al.
Glucose is the main source of energy for organisms, and it is important to understand the spatiotemporal dynamics of intracellular glucose. Single fluorescent protein-based glucose indicators, named "Red Glifons" have been developed that ap...
NUDT15-mediated hydrolysis limits the efficacy of anti-HCMV drug ganciclovir [0.03%]
NUDT15介导的水解限制了抗HCMV药物更昔洛韦的功效
Si Min Zhang,Daniel Rehling,Ann-Sofie Jemth et al.
Si Min Zhang et al.
Ganciclovir (GCV) is the first-line therapy against human cytomegalovirus (HCMV), a widespread infection that is particularly dangerous for immunodeficient individuals. Closely resembling deoxyguanosine triphosphate, the tri-phosphorylated ...
Mapping the residue specificities of epigenome enzymes by yeast surface display [0.03%]
利用酵母表面展示技术绘制表观基因组酶的残基特异性
Alison C Waldman,Balaji M Rao,Albert J Keung
Alison C Waldman
Histone proteins are decorated with a combinatorially and numerically diverse set of biochemical modifications. Here, we describe a versatile and scalable approach which enables efficient characterization of histone modifications without th...