Transition state analogue inhibitors of human methylthioadenosine phosphorylase and bacterial methylthioadenosine/S-adenosylhomocysteine nucleosidase incorporating acyclic ribooxacarbenium ion mimics

Several acyclic hydroxy-methylthio-amines with 3 to 5 carbon atoms were prepared and coupled via a methylene link to 9-deazaadenine. The products were tested for inhibition against human MTAP and E. coli and N. meningitidis MTANs and gave K(i) values as low as 0.23 nM. These results were compared to...

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Main Authors: Clinch, Keith, Evans, Gary B., Fröhlich, Richard F. G., Gulab, Shivali A., Gutierrez, Jemy A., Mason, Jennifer M., Schramm, Vern L., Tyler, Peter C., Woolhouse, Anthony D.
Formato: Artigo
Idioma:Inglês
Publicado em: 2012
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3438226/
https://ncbi.nlm.nih.gov/pubmed/22854195
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2012.07.006
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