Entropy-Driven Binding of Picomolar Transition State Analogue Inhibitors to Human 5′-Methylthioadenosine Phosphorylase()

Human 5′-methylthioadenosine phosphorylase (MTAP) links the polyamine biosynthetic and S-adenosyl-L-methionine salvage pathways and is a target for anticancer drugs. p-Cl-PhT-DADMe-ImmA is a 10 pM, slow-onset tight-binding transition state analogue inhibitor of the enzyme. Titration of homotrimeric...

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Main Authors: Guan, Rong, Ho, Meng-Chiao, Brenowitz, Michael, Tyler, Peter C., Evans, Gary B., Almo, Steven C., Schramm, Vern L.
Formato: Artigo
Idioma:Inglês
Publicado: 2011
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC3222737/
https://ncbi.nlm.nih.gov/pubmed/21985704
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/bi201321x
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