A synthetic RNA-based biosensor for fructose-1,6-bisphosphate that reports glycolytic flux [0.03%]
一种合成的RNA基生物传感器，用于报告果糖-1,6-二磷酸的糖酵流变速率
Alvaro Darío Ortega,Vakil Takhaveev,Silke Roelie Vedelaar et al.
Alvaro Darío Ortega et al.
RNA-based sensors for intracellular metabolites are a promising solution to the emerging issue of metabolic heterogeneity. However, their development, i.e., the conversion of an aptamer into an in vivo-functional intracellular metabolite se...
Development and pre-clinical testing of a novel hypoxia-activated KDAC inhibitor [0.03%]
一种新型低氧激活型KDAC抑制剂的开发与临床前试验
Anna Skwarska,Ewen D D Calder,Deborah Sneddon et al.
Anna Skwarska et al.
Tumor hypoxia is associated with therapy resistance and poor patient prognosis. Hypoxia-activated prodrugs, designed to selectively target hypoxic cells while sparing normal tissue, represent a promising treatment strategy. We report the pr...
Fulya Türker,Emily K Cook,Seth S Margolis
Fulya Türker
Proteasomes are multisubunit complexes that catalyze the majority of protein degradation in mammalian cells to maintain protein homeostasis and influence the regulation of most cellular processes. The proteasome, a multicatalytic protease c...
Phenotypic screen identifies calcineurin-sparing FK506 analogs as BMP potentiators for treatment of acute kidney injury [0.03%]
表型筛选发现钙调神经磷酸酶非依赖性他克莫司类似物可作为促进骨形态发生蛋白活性的治疗急性肾损伤的新药
Marie-Hélène Larraufie,Xiaolin Gao,Xiaobo Xia et al.
Marie-Hélène Larraufie et al.
Acute kidney injury (AKI) is a life-threatening disease with no known curative or preventive therapies. Data from multiple animal models and human studies have linked dysregulation of bone morphogenetic protein (BMP) signaling to AKI. Small...
Michael R Post,David Sulzer
Michael R Post
Dopamine is a modulatory neurotransmitter involved in learning, motor functions, and reward. Many neuropsychiatric disorders, including Parkinson's disease, autism, and schizophrenia, are associated with imbalances or dysfunction in the dop...
An E3 ligase guide to the galaxy of small-molecule-induced protein degradation [0.03%]
小分子诱导的蛋白质降解的E3连接酶指导手册
Predrag Jevtić,Diane L Haakonsen,Michael Rapé
Predrag Jevtić
Induced protein degradation accomplishes elimination, rather than inhibition, of pathological proteins. Key to the success of this novel therapeutic modality is the modification of proteins with ubiquitin chains, which is brought about by m...
An IMiD-inducible degron provides reversible regulation for chimeric antigen receptor expression and activity [0.03%]
一种IMiD诱导的降解域可实现嵌合抗原受体表达和活性的可逆调节
Seth Carbonneau,Sujata Sharma,Liaomin Peng et al.
Seth Carbonneau et al.
Published Erratum
Cell chemical biology. 2021 Apr 15;28(4):583. DOI:10.1016/j.chembiol.2021.02.003 2021
Whitney K Lieberman,Yihang Jing,Jordan L Meier
Whitney K Lieberman
Chromatin-modifying lysine acetyltransferases employ multiple protein domains to regulate transcription. In this issue, Vannam et al. (2021) describe dCBP-1, a small molecule degrader of the multidomain acetyltransferases EP300 and CREBBP. ...
A double on the Rocs with a twist: Rocaglamide A targets multiple DEAD-box helicases to inhibit translation initiation [0.03%]
一个新的双环木兰烷类生物碱Rocaglamide A通过靶向多个解链酶抑制蛋白质翻译起始
Daisy J DiVita,Michael G Kearse
Daisy J DiVita
In this issue of Cell Chemical Biology, Chen et al. (2020) expand the target repertoire of rocaglamide A (RocA) to now include eIF4A2 and DDX3X, converting DEAD-box helicases into dominant-negative translation repressors. These results also...
Inhibition of Staphylococcus aureus biofilm-forming functional amyloid by molecular tweezers [0.03%]
分子夹通过靶向葡萄球菌素酶抑制金黄色葡萄球菌生物被膜形成淀粉样蛋白的功能
Ravit Malishev,Nir Salinas,James Gibson et al.
Ravit Malishev et al.
Biofilms are rigid and largely impenetrable three-dimensional matrices constituting virulence determinants of various pathogenic bacteria. Here, we demonstrate that molecular tweezers, unique supramolecular artificial receptors, modulate bi...