66640-86-6Relevant articles and documents
Design, synthesis, and biological evaluation of biotinylated colchicine derivatives as potential antitumor agents
Wang, Chao,Zhang, Yujing,Wang, Zeyu,Li, Yuelin,Guan, Qi,Xing, Dongming,Zhang, Weige
, p. 411 - 420 (2021/12/24)
Chemical drug design based on the biochemical characteristics of cancer cells has become an important strategy for discovering new anti-tumour drugs to improve tumour targeting effects and reduce off-target toxicities. Colchicine is one of the most promin
Design and synthesis of biotinylated cardiac glycosides for probing Nur77 protein inducting pathway
Tian, Dan-mei,Qiao, Jia,Bao, Yu-zhou,Liu, Jie,Zhang, Xiao-kun,Sun, Xue-long,Zhang, You-wei,Yao, Xin-sheng,Tang, Jin-shan
supporting information, p. 707 - 712 (2019/01/22)
The orphan nuclear receptor Nur77 (also known as TR3 or nerve growth factor-induced clone B NGFI-B) functions as a nuclear transcription factor in the regulation of target gene expression and plays a critical role in the regulation of differentiation, proliferation, apoptosis, and survival of many different cell types. Recent studies demonstrate that Nur77 also involves many important physiological and pathological processes including cancer, inflammation and immunity, cardiovascular diseases, and bone diseases. Our previous studies showed that cardiac glycosides could induce the expression of Nur77 protein and its translocation from the nucleus to the cytoplasm and subsequent targeting to mitochondria, leading to apoptosis of cancer cells. In order to probe the Nur77 protein inducting pathway, we designed and synthesized a series of novel biotinylated cardiac glycosides from β-Antiarin and α-Antiarin, two typical cardiac glycosides from the plant of Antiaris toxicaria. The induction of Nur77 protein expression of these biotinylated cardiac glycosides and their inhibitory effects on NIH-H460 cancer cell proliferation were evaluated. Results displayed that some biotinylated cardiac glycosides could significantly induce the expression of Nur77 protein comparable with their parent compounds β-Antiarin and α-Antiarin. Also, their streptavidin binding activities were evaluated. Among them, biotinylated cardiac glycosides P4b and P5a exhibited significant effect on the induction of Nur77 expression along with high binding capacity with streptavidin, suggesting that they can be used as probes for probing Nur77 protein inducting pathway.
KAHA ligations that form aspartyl aldehyde residues as synthetic handles for protein modification and purification
Murar, Claudia E.,Thuaud, Frdric,Bode, Jeffrey W.
supporting information, p. 18140 - 18148 (2015/03/04)
Aldehydes are widely recognized as valuable synthetic handles for the chemoselective manipulation of peptides and proteins. In this report, we show that peptides and small proteins containing the aspartic acid semialdehyde (Asa) side chain can be easily p
Heterocyclic acyl-phosphate bioisostere-based inhibitors of Staphylococcus aureus biotin protein ligase
Tieu, William,Jarrad, Angie M.,Paparella, Ashleigh S.,Keeling, Kelly A.,Soares Da Costa, Tatiana P.,Wallace, John C.,Booker, Grant W.,Polyak, Steven W.,Abell, Andrew D.
, p. 4689 - 4693 (2015/01/09)
Inhibitors of Staphylococcus aureus biotin protein ligase (SaBPL) are generated by replacing the acyl phosphate group of biotinyl-5′-AMP with either a 1,2,3-triazole (see 5/10a/10b) or a 1,2,4-oxadiazole (see 7) bioisostere. Importantly, the inhibitors are inactive against the human BPL. The nature of the 5-substituent in the component benzoxazolone of the optimum 1,2,3-triazole series is critical to activity, where this group binds in the ATP binding pocket of the enzyme.
Mechanism-based tumor-targeting drug delivery system. Validation of efficient vitamin receptor-mediated endocytosis and drug release
Chen, Shuyi,Zhao, Xianrui,Chen, Jingyi,Chen, Jin,Kuznetsova, Larisa,Wong, Stanislaus S.,Ojima, Iwao
scheme or table, p. 979 - 987 (2011/02/22)
An efficient mechanism-based tumor-targeting drug delivery system, based on tumor-specific vitamin-receptor mediated endocytosis, has been developed. The tumor-targeting drug delivery system is a conjugate of a tumor-targeting molecule (biotin: vitamin H
