39224-61-8Relevant articles and documents
A bioorthogonal system reveals antitumour immune function of pyroptosis
Ding, Jingjin,Gao, Wenqing,Huang, Huanwei,Liu, Zhibo,Shao, Feng,Wang, Chunhong,Wang, Qinyang,Wang, Yupeng,Zhou, Xuehan
, (2020)
Bioorthogonal chemistry capable of operating in live animals is needed to investigate biological processes such as cell death and immunity. Recent studies have identified a gasdermin family of pore-forming proteins that executes inflammasome-dependent and
Desilylation Induced by Metal Fluoride Nanocrystals Enables Cleavage Chemistry in Vivo
Duan, Dongban,Dong, Hao,Tu, Zhiyu,Wang, Chunhong,Fu, Qunfeng,Chen, Junyi,Zhong, Haipeng,Du, Ping,Sun, Ling-Dong,Liu, Zhibo
, p. 2250 - 2255 (2021)
Metal fluoride nanocrystals are widely used in biomedical studies owing to their unique physicochemical properties. The release of metal ions and fluorides from nanocrystals is intrinsic due to the solubility equilibrium. It used to be considered as a drawback because it is related to the decomposition and defunction of metal fluoride nanocrystals. Many strategies have been developed to stabilize the nanocrystals, and the equilibrium concentrations of fluoride are often 1 mM. Here we make good use of this minimum amount of fluoride and unveil that metal fluoride nanocrystals could effectively induce desilylation cleavage chemistry, enabling controlled release of fluorophores and drug molecules in test tubes, living cells, and tumor-bearing mice. Biocompatible PEG (polyethylene glycol)-coated CaF2 nanocrystals have been prepared to assay the efficiency of desilylation-induced controlled release of functional molecules. We apply the strategy to a prodrug activation of monomethyl auristatin E (MMAE), showing a remarkable anticancer effect, while side effects are almost negligible. In conclusion, this desilylation-induced cleavage chemistry avails the drawback on empowering metal fluoride nanocrystals with a new function of perturbing or activating for further biological applications.
MODULATION OF IMMUNE CELLS
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Paragraph 0049; 00124-00125, (2021/08/06)
Disclosed are immune cell-selective small molecule IMPDH inhibitor compounds and methods of their synthesis and use to treat proliferative disorders.
Looking for new xanthine oxidase inhibitors: 3-Phenylcoumarins versus 2-phenylbenzofurans
Borges, Fernanda,Delogu, Giovanna L.,Era, Benedetta,Fais, Antonella,Gatto, Gianluca,Kumar, Amit,Matos, Maria J.,Pintus, Francesca,Uriarte, Eugenio
, p. 774 - 780 (2020/07/07)
Overproduction of uric acid in the body leads to hyperuricemia, which is also closely related to gout. Uric acid production can be lowered by xanthine oxidase (XO) inhibitors. Inhibition of XO has also been proposed as a mechanism for improving cardiovascular health. Therefore, the search for new efficient XO inhibitors is an interesting topic in drug discovery. 3-Phenylcoumarins and 2-phenylbenzofurans are privileged scaffolds in medicinal chemistry. Their structural similarity makes them interesting molecules for a comparative study. Methoxy and nitro substituents were introduced in both scaffolds. The current study gives some insights into the synthesis and biological activity of these molecules against this important target. For the best compound of the series, the 3-(4-methoxyphenyl)-6-nitrocoumarin (4), the IC50 value, type of inhibition, cytotoxicity on B16F10 cells and ADME theoretical properties, were determined. Docking studies were also performed in order to better understand the interactions of this molecule with the XO binding pocket. This work is a preliminary screening for further design and synthesis of new non-purinergic derivatives as potential compounds involved in the inflammatory suppression, specially related to gout.
