8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
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Evans GB, Furneaux RH, Gainsford GJ, Hanson JC, Kicska GA, Sauve AA, Schramm VL, Tyler PC
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
J Med Chem. 2003 Jan 2;46(1):155-60.
- PubMed ID
- 12502369 [ View in PubMed]
- Abstract
The 8-aza-immucillins (8-aza-9-deazapurines linked from C9 to C1 of 1,4-dideoxy-1,4-iminoribitol) have been designed as transition-state analogues of the reactions catalyzed by purine nucleoside phosphorylase and nucleoside hydrolases. Syntheses of the 8-aza-immucillin analogues of inosine and adenosine are described. They are powerful inhibitors of the target enzymes with equilibrium dissociation constants as low as 42 pM.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Forodesine Purine nucleoside phosphorylase Ki (nM) 0.072 N/A N/A Details Immucillin-G Purine nucleoside phosphorylase Ki (nM) 0.029 N/A N/A Details