53053-08-0Relevant articles and documents
Photoactive chelates for radiolabelling proteins
Eichenberger, Larissa S.,Patra, Malay,Holland, Jason P.
, p. 2257 - 2260 (2019)
Photochemical reactions are an attractive foundation for the synthesis of radiolabelled antibodies, immunoglobulin fragments and other proteins/peptides. The synthesis, 68Ga-radiochemistry and photochemical reactivity of three macrocyclic chela
PHOTOAFFINITY PROBES FOR GIBBERELLIN-BINDING PROTEINS
Beale, Michael H.,Hooley, Richard,Smith, Sally J.,Walker, Robert P.
, p. 1459 - 1464 (1992)
A rational approach to the design, synthesis and radiolabelling, with either 3H or 125I, of gibberellin A4 (GA4) derivatives containing C-17-arylazido functionalities is described.The potential of these compounds as photoaffinity rea
Identification of Pyruvate Carboxylase as the Cellular Target of Natural Bibenzyls with Potent Anticancer Activity against Hepatocellular Carcinoma via Metabolic Reprogramming
Chen, Yuwen,Huang, Yulan,Jiao, Wei,Li, Fu,Li, Suiyan,Li, Wenhua,Lin, Yuan,Liu, Wanli,Ma, Yuling,Sheng, Yuwen,Suksamrarn, Apichart,Wang, Fei,Wang, Jing,Wei, Xiao,Wisanwattana, Wisanee,Wu, Wenbi,Zeng, Zhongqiu,Zhang, Guolin,Zhang, Jichao,Zhu, Qiyu
supporting information, (2022/01/03)
Cancer cell proliferation in some organs often depends on conversion of pyruvate to oxaloacetate via pyruvate carboxylase (PC) for replenishing the tricarboxylic acid cycle to support biomass production. In this study, PC was identified as the cellular target of erianin using the photoaffinity labeling-click chemistry-based probe strategy. Erianin potently inhibited the enzymatic activity of PC, which mediated the anticancer effect of erianin in human hepatocellular carcinoma (HCC). Erianin modulated cancer-related gene expression and induced changes in metabolic intermediates. Moreover, erianin promotes mitochondrial oxidative stress and inhibits glycolysis, leading to insufficient energy required for cell proliferation. Analysis of 14 natural analogs of erianin showed that some compounds exhibited potent inhibitory effects on PC. These results suggest that PC is a cellular target of erianin and reveal the unrecognized function of PC in HCC tumorigenesis; erianin along with its analogs warrants further development as a novel therapeutic strategy for the treatment of HCC.
A Potent Halogen-Bonding Donor Motif for Anion Recognition and Anion Template Mechanical Bond Synthesis
Bunchuay, Thanthapatra,Docker, Andrew,Martinez-Martinez, Antonio J.,Beer, Paul D.
supporting information, p. 13823 - 13827 (2019/08/22)
The covalent attachment of electron deficient perfluoroaryl substituents to a bis-iodotriazole pyridinium group produces a remarkably potent halogen bonding donor motif for anion recognition in aqueous media. Such a motif also establishes halogen bonding anion templation as a highly efficient method for constructing a mechanically interlocked molecule in unprecedented near quantitative yield. The resulting bis-perfluoroaryl substituted iodotriazole pyridinium axle containing halogen bonding [2]rotaxane host exhibits exceptionally strong halide binding affinities in competitive 50 % water containing aqueous media, by a factor of at least three orders of magnitude greater in comparison to a hydrogen bonding rotaxane host analogue. These observations further champion and advance halogen bonding as a powerful tool for recognizing anions in aqueous media.