Design, synthesis and biological application of chemical probes for bio-imaging

2010 ◽  
Vol 39 (6) ◽  
pp. 2048 ◽  
Author(s):  
Kazuya Kikuchi
Keyword(s):  
Biological Application ◽  
Chemical Probes ◽  
Design Synthesis ◽  
Bio Imaging

Lipoic acid based core cross-linked micelles for multivalent platforms: design, synthesis and application in bio-imaging and drug delivery

2017 ◽  
Vol 15 (22) ◽  
pp. 4798-4802 ◽  
Author(s):  
Jingsheng Huang ◽  
Fang Wu ◽  
Yunlong Yu ◽  
Haolong Huang ◽  
Shiyong Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Small Molecule ◽  
Lipoic Acid ◽  
Design Synthesis ◽  
Bio Imaging

Natural lipoic acid derived small-molecule amphiphiles self-assemble into micelles in water.

scholarly journals Design, Synthesis, and Biological Application of Novel Photoaffinity Probes of Dihydropyridine Derivatives, BAY R3401

Molecules ◽  
2019 ◽  
Vol 24 (13) ◽  
pp. 2394
Author(s):  
Liying Zhang ◽  
Zhiwei Yan ◽  
Youde Wang ◽  
Chengjun Song ◽  
Guangxin Miao
Keyword(s):  
Hepg2 Cells ◽  
Human Liver ◽  
Molecular Mechanisms ◽  
Biological Application ◽  
Design Synthesis ◽  
Target Proteins ◽  
Promising Tool ◽  
Photoaffinity Probes ◽  
Ic50 Values ◽  
Dihydropyridine Derivatives

To explore the molecular mechanisms of BAY R3401, four types of novel photoaffinity probes bearing different secondary tags were synthesized. Their potency for glycogenolysis was evaluated in primary human liver HL-7702 cells and HepG2 cells. Probe 2d showed the best activity in primary human liver HL-7702 cells and HepG2 cells, with IC50 values of 4.45 μM and 28.49 μM, respectively. Likewise, probe 5d showed IC50 values of 6.46 μM in primary human liver HL-7702 cells and 15.29 μM in HepG2 cells, respectively. Photoaffinity labeling experiments were also performed and protein bands larger than 170 kDa were specifically tagged by probe 2d. The results suggest that the synthesized probe 2d might be a very promising tool for the isolation of the target proteins of BAY R3401.

scholarly journals Design, Synthesis, and Biological Evaluation of Benzo[cd]indol-2(1H)-ones Derivatives as a Lysosome-Targeted Anti-metastatic Agent

2021 ◽  
Vol 11 ◽  
Author(s):  
Jinghua Li ◽  
Shuai Chen ◽  
Yancong Zhao ◽  
Huiyuan Gong ◽  
Tong Wang ◽  
...  
Keyword(s):  
Cancer Metastasis ◽  
Tumor Therapy ◽  
Biological Evaluation ◽  
Imaging Agent ◽  
Design Synthesis ◽  
Dual Functional ◽  
Study Results ◽  
Bio Imaging

Lysosomes have become a hot topic in tumor therapy; targeting the lysosome is therefore a promising strategy in cancer therapy. Based on our previous lysosome-targeted bio-imaging agent, homospermine-benzo[cd]indol-2(1H)-one conjugate (HBC), we further developed three novel series of polyamine- benzo[cd]indol-2(1H)-one conjugates. Among them, compound 15f showed potent inhibitory activity in hepatocellular carcinoma migration both in vitro and in vivo. Our study results showed that compound 15f entered the cancer cells via the polyamine transporter localized in the lysosomes and caused autophagy and apoptosis. The mechanism of action revealed that the crosstalk between autophagy and apoptosis induced by 15f was mutually reinforcing patterns. Besides, 15f also targeted lysosomes and exhibited stronger green fluorescence than HBC, which indicated its potential as an imaging agent. To summarize, compound 15f could be used as a valuable dual-functional lead compound for future development against liver-cancer metastasis and lysosome imaging.

scholarly journals Development and application of ubiquitin-based chemical probes

2020 ◽  
Vol 11 (47) ◽  
pp. 12633-12646 ◽  
Author(s):  
Xin Sui ◽  
Yu Wang ◽  
Yun-Xiang Du ◽  
Lu-Jun Liang ◽  
Qingyun Zheng ◽  
...  
Keyword(s):  
Chemical Probes ◽  
Design Synthesis

This article reviews the design, synthesis, and application of different classes of Ub-based chemical probes.

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