151978-87-9Relevant academic research and scientific papers
Chemical tagging of a drug target using 5-sulfonyl tetrazole
Otsuki, Satsuki,Nishimura, Shinichi,Takabatake, Hisae,Nakajima, Kozue,Takasu, Yasuaki,Yagura, Toru,Sakai, Yuki,Hattori, Akira,Kakeya, Hideaki
, p. 1608 - 1611 (2013/04/10)
Irreversible modification is one of the most promising strategies to identify cellular receptors of bioactive small molecules. Here we report that receptor proteins can be chemically tagged using a 5-sulfonyl tetrazole probe. 5-Sulfonyl tetrazole easily a
Selection of the biological activity of DNJ neoglycoconjugates through click length variation of the side chain
Ardes-Guisot, Nicolas,Alonzi, Dominic S.,Reinkensmeier, Gabriele,Butters, Terry D.,Norez, Caroline,Becq, Frederic,Shimada, Yousuke,Nakagawa, Shinpei,Kato, Atsushi,Bleriot, Yves,Sollogoub, Matthieu,Vauzeilles, Boris
supporting information; experimental part, p. 5373 - 5388 (2011/08/22)
A series of neoglycoconjugates derived from deoxynojirimycin has been prepared by click connection with functionalised adamantanes. They have been assayed as glycosidase inhibitors, as inhibitors of the glycoenzymes relevant to the treatment of Gaucher disease, as well as correctors of the defective ion-transport protein involved in cystic fibrosis. We have demonstrated that it is possible to selectively either strongly inhibit ER-α-glucosidases and ceramide glucosyltransferase or restore the activity of CFTR in CF-KM4 cells by varying the length of the alkyl chain linking DNJ and adamantane.
