Biochemical investigations using mass spectrometry to monitor JMJD6-catalysed hydroxylation of multi-lysine containing bromodomain-derived substrates [0.03%]
利用质谱监测由JMJD6催化的多赖氨酸衍生底物的羟基化反应的生化研究
Thomas P Corner,Eidarus Salah,Anthony Tumber et al.
Thomas P Corner et al.
Jumonji-C domain-containing protein 6 (JMJD6) is a human 2-oxoglutarate (2OG)/Fe(ii)-dependent oxygenase catalysing post-translational C5 hydroxylation of multiple lysine residues, including in the bromodomain-containing proteins BRD2, BRD3...
Identification of γ-butyrolactone signalling molecules in diverse actinomycetes using resin-assisted isolation and chemoenzymatic synthesis [0.03%]
使用树脂辅助分离和化学酶促合成在多种放线菌中识别γ-丁内酯信号分子
Yuta Kudo,Keiichi Konoki,Mari Yotsu-Yamashita
Yuta Kudo
Actinomycetes are prolific producers of secondary metabolites with diverse bioactivities. Secondary metabolism in actinomycetes is regulated by signalling molecules, often termed "bacterial hormones." In Streptomyces griseus, the γ-butyrol...
Design and application of a fluorescent probe for imaging of endogenous Bruton's tyrosine kinase with preserved enzymatic activity [0.03%]
用于检测具有酶活性的布鲁顿酪氨酸激酶的荧光探针的设计及应用
Anna P Valaka,Hampus Nyström,Liliana Håversen et al.
Anna P Valaka et al.
Fluorophore integration into proteins within living cells is essential for exploring proteins in their natural environment. Bruton's tyrosine kinase (BTK), is a validated oncology target and is crucial for B cell proliferation and activatio...
An activation-based high throughput screen identifies caspase-10 inhibitors [0.03%]
一项基于激活的高通量筛选鉴定出了caspase-10抑制剂
José O Castellón,Constance Yuen,Brandon Han et al.
José O Castellón et al.
Caspases are a family of highly homologous cysteine proteases that play critical roles in inflammation and apoptosis. Small molecule inhibitors are useful tools for studying caspase biology, complementary to genetic approaches. However, ach...
Yoshiki Hashimoto,Sumit Shil,Mitsuki Tsuruta et al.
Yoshiki Hashimoto et al.
Nucleic acids have the potential to form not only duplexes, but also various non-canonical secondary structures in living cells. Non-canonical structures play regulatory functions mainly in the central dogma. Therefore, nucleic acid targeti...
Decoding allosteric landscapes: computational methodologies for enzyme modulation and drug discovery [0.03%]
解码变构景观：酶调控和药物发现的计算方法
Ruidi Zhu,Chengwei Wu,Jinyin Zha et al.
Ruidi Zhu et al.
Allosteric regulation is a fundamental mechanism in enzyme function, enabling dynamic modulation of activity through ligand binding at sites distal to the active site. Allosteric modulators have gained significant attention due to their uni...
Functionalization of a versatile fluorescent sensor for detecting protease activity and temporally gated opioid sensing [0.03%]
多功能荧光传感器的功能化，用于检测蛋白酶活性和时间门控阿片类药物传感
Jennifer Sescil,Hailey Fiel,Steven M Havens et al.
Jennifer Sescil et al.
Genetically encoded fluorescent sensors have been widely applied to detect cell signaling molecules and events. We previously designed a fluorescent sensor motif suitable for detecting protease activity and opioids. In this manuscript, we d...
Cryo-electron microscopy reveals a single domain antibody with a unique binding epitope on fibroblast activation protein alpha [0.03%]
低温电子显微镜揭示了成纤维细胞激活蛋白α上具有独特结合表位的单结构域抗体
Zhen Xu,Akesh Sinha,Darpan N Pandya et al.
Zhen Xu et al.
Fibroblast activation protein alpha (FAP) is a serine protease that is expressed at basal levels in benign tissues but is overexpressed in a variety of pathologies, including cancer. Despite this unique expression profile, designing functio...
Covalent functionalization of G protein-coupled receptors by small molecular probes [0.03%]
小分子探针通过共价作用对G蛋白偶联受体的功能化研究
Bert L H Beerkens,Adriaan P IJzerman,Laura H Heitman et al.
Bert L H Beerkens et al.
Roughly one-third of all marketed drugs act by binding to one or more of the >800 human GPCRs, primarily through activation or inhibition via the orthosteric binding site. In addition, novel strategies to alter GPCR functioning are being de...
Amirhossein Taghavi,Noah A Springer,Patrick R A Zanon et al.
Amirhossein Taghavi et al.
RNA structure plays a role in nearly every disease. Therefore, approaches that identify tractable small molecule chemical matter that targets RNA and affects its function would transform drug discovery. Despite this potential, discovery of ...