Hit Triage and Validation in Phenotypic Screening: Considerations and Strategies [0.03%]
表型筛选中的命中分类和验证：考虑因素和策略
Fabien Vincent,Paula M Loria,Andrea D Weston et al.
Fabien Vincent et al.
The promise of phenotypic screening resides in its track record of novel biology and first-in-class therapies. However, challenges stemming from major differences between target-based and phenotypic screening do exist. These challenges prom...
Assessing IRAK4 Functions in ABC DLBCL by IRAK4 Kinase Inhibition and Protein Degradation [0.03%]
通过IRAK4激酶抑制和蛋白降解评估ABCDLBCL中的IRAK4功能
Jing Zhang,Liqiang Fu,Bin Shen et al.
Jing Zhang et al.
The interleukin-1 receptor-activated kinase 4 (IRAK4) belongs to the IRAK family of serine/threonine kinases and plays a central role in the innate immune response. However, the function of IRAK4 in tumor growth and progression remains elus...
Dioctatin Activates ClpP to Degrade Mitochondrial Components and Inhibits Aflatoxin Production [0.03%]
二倍半萜类化合物dioctatin激活ClpP降解线粒体组分并抑制黄曲霉毒素的产生
Tomohiro Furukawa,Hidekazu Katayama,Akira Oikawa et al.
Tomohiro Furukawa et al.
Aflatoxin contamination of crops is a serious problem worldwide. Utilization of aflatoxin production inhibitors is attractive, as the elucidation of their modes of action contributes to clarifying the mechanism of aflatoxin production. Here...
Mechanistic Studies of the Multiple Myeloma and Melanoma Cell-Selective Toxicity of the Rpn13-Binding Peptoid KDT-11 [0.03%]
Rpn13结合肽类KDT-11的选择性毒杀多发性骨髓瘤和黑色素瘤细胞的机制研究
Paige Dickson,Scott Simanski,John Maina Ngundu et al.
Paige Dickson et al.
We previously reported a peptoid ligand for the proteasomal ubiquitin receptor Rpn13 called KDT-11 and demonstrated that this compound is toxic to multiple myeloma cells, but not non-malignant cells. Here, we show that KDT-11 decreases the ...
Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190 [0.03%]
假定的Rpn13抑制剂RA190的物理和功能性分析
Paige Dickson,Daniel Abegg,Ekaterina Vinogradova et al.
Paige Dickson et al.
Rpn13 is one of several ubiquitin receptors in the 26S proteasome. Cys88 of Rpn13 has been proposed to be the principal target of RA190, an electrophilic small molecule with interesting anti-cancer activities. Here, we examine the claim tha...
Alexandre M J Gomila,Karin Rustler,Galyna Maleeva et al.
Alexandre M J Gomila et al.
Glycine receptors (GlyRs) are indispensable for maintaining excitatory/inhibitory balance in neuronal circuits that control reflexes and rhythmic motor behaviors. Here we have developed Glyght, a GlyR ligand controlled with light. It is sel...
Mishtu Dey,Eranthie Weerapana
Mishtu Dey
Ashley R Brown,Rebecca A Gordon,Stephen N Hyland et al.
Ashley R Brown et al.
Bacteria surround themselves with cell walls to maintain cell rigidity and protect against environmental insults. Here we review chemical and biochemical techniques employed to study bacterial cell wall biogenesis. Recent advances including...
Chemical Biology Toolbox for Studying Pancreatic Islet Function - A Perspective [0.03%]
研究胰岛功能的化学生物学工具箱 - 一种观点
Julia Huey,Kaya Keutler,Carsten Schultz
Julia Huey
The islets of Langerhans represent one of the many complex endocrine organs in mammals. Traditionally, islet function is studied by a mixture of physiological, cell biological, and molecular biological methods. Recently, novel techniques st...
Controlled Inhibition of Apoptosis by Photoactivatable Caspase Inhibitors [0.03%]
光控可激活的半胱天冬酶抑制子对细胞凋亡的调控抑制作用
Suravi Chakrabarty,Steven H L Verhelst
Suravi Chakrabarty
Caspases control regulated cell death (apoptosis), a process that is crucial in the development of multicellular organisms as well as in various diseases. In order to spatiotemporally study apoptosis, we here develop photoactivatable caspas...