The Orphan Nuclear Receptor TLX Is a Receptor for Synthetic and Natural Retinoids [0.03%]
孤儿核受体TLX是合成和天然视黄酸的受体
Kristine Griffett,Gonzalo Bedia-Diaz,Lamees Hegazy et al.
Kristine Griffett et al.
TLX is an orphan nuclear receptor that plays a critical role in both embryonic and adult neurogenesis, as well in the pathogenesis of glioblastomas. TLX functions predominately as a transcriptional repressor, but no natural ligands or high-...
Chemical Biology Toolkit for DCLK1 Reveals Connection to RNA Processing [0.03%]
DCLK1的化学生物工具包揭示其与RNA处理的关系
Yan Liu,Fleur M Ferguson,Lianbo Li et al.
Yan Liu et al.
Doublecortin-like kinase 1 (DCLK1) is critical for neurogenesis, but overexpression is also observed in multiple cancers and is associated with poor prognosis. Nevertheless, the function of DCLK1 in cancer, especially the context-dependent ...
Ukrae Cho,James K Chen
Ukrae Cho
The unique photophysical properties of lanthanides, such as europium, terbium, and ytterbium, make them versatile molecular probes of biological systems. In particular, their long-lived photoluminescence, narrow bandwidth emissions, and lar...
Site-Specific Incorporation of Genetically Encoded Photo-Crosslinkers Locates the Heteromeric Interface of a GPCR Complex in Living Cells [0.03%]
遗传编码光交联剂的特异引入定位GPCR复合物在活细胞中的异源二聚互作界面
Urjita H Shah,Rudy Toneatti,Supriya A Gaitonde et al.
Urjita H Shah et al.
G protein-coupled receptors (GPCRs) are critical mediators of cell signaling. Although capable of activating G proteins in a monomeric form, numerous studies reveal a possible association of class A GPCRs into dimers/oligomers. The relative...
Discovery of Protein-Protein Interaction Inhibitors by Integrating Protein Engineering and Chemical Screening Platforms [0.03%]
整合蛋白质工程和化学筛选平台发现蛋白-蛋白互作抑制剂
Timurs Maculins,Javier Garcia-Pardo,Anamarija Skenderovic et al.
Timurs Maculins et al.
Protein-protein interactions (PPIs) govern intracellular life, and identification of PPI inhibitors is challenging. Roadblocks in assay development stemming from weak binding affinities of natural PPIs impede progress in this field. We post...
Strategies for Tuning the Selectivity of Chemical Probes that Target Serine Hydrolases [0.03%]
调节靶向丝氨酸水解酶的化学探针的选择性的策略
Franco Faucher,John M Bennett,Matthew Bogyo et al.
Franco Faucher et al.
Serine hydrolases comprise a large family of enzymes that have diverse roles in key cellular processes, such as lipid metabolism, cell signaling, and regulation of post-translation modifications of proteins. They are also therapeutic target...
Structure-Aided Development of Small-Molecule Inhibitors of ENPP1, the Extracellular Phosphodiesterase of the Immunotransmitter cGAMP [0.03%]
结构辅助的小分子ENPP1抑制剂的开发：ENPP1是免疫信使cGAMP的胞外磷酸二酯酶
Jacqueline A Carozza,Jenifer A Brown,Volker Böhnert et al.
Jacqueline A Carozza et al.
Cancer cells initiate an innate immune response by synthesizing and exporting the small-molecule immunotransmitter cGAMP, which activates the anti-cancer Stimulator of Interferon Genes (STING) pathway in the host. An extracellular enzyme, e...
Mimicry of a Non-ribosomally Produced Antimicrobial, Brevicidine, by Ribosomal Synthesis and Post-translational Modification [0.03%]
由核糖体合成与翻译后修饰模拟产生非核糖体抗微生物剂短肽毒素
Xinghong Zhao,Zhibo Li,Oscar P Kuipers
Xinghong Zhao
The group of bacterial non-ribosomally produced peptides (NRPs) forms a rich source of antibiotics, such as daptomycin, vancomycin, and teixobactin. The difficulty of functionally expressing and engineering the corresponding large biosynthe...
Stephen M Canham,Yuan Wang,Allen Cornett et al.
Stephen M Canham et al.
Chemogenetic libraries, collections of well-defined chemical probes, provide tremendous value to biomedical research but require substantial effort to ensure diversity as well as quality of the contents. We have assembled a chemogenetic lib...
Rational Design of Bioavailable Photosensitizers for Manipulation and Imaging of Biological Systems [0.03%]
用于生物系统操控和成像的可药用光敏剂的理性设计
Thomas C Binns,Anthony X Ayala,Jonathan B Grimm et al.
Thomas C Binns et al.
Light-mediated chemical reactions are powerful methods for manipulating and interrogating biological systems. Photosensitizers, compounds that generate reactive oxygen species upon excitation with light, can be utilized for numerous biologi...