Picomolar Transition State Analogue Inhibitors of Human 5‘-Methylthioadenosine Phosphorylase and X-ray Structure with MT-Immucillin-A†

Biochemistry ◽  
2004 ◽  
Vol 43 (1) ◽  
pp. 9-18 ◽  
Author(s):  
Vipender Singh ◽  
Wuxian Shi ◽  
Gary B. Evans ◽  
Peter C. Tyler ◽  
Richard H. Furneaux ◽  
...  

2004 ◽  
Vol 47 (12) ◽  
pp. 3275-3281 ◽  
Author(s):  
Gary B. Evans ◽  
Richard H. Furneaux ◽  
Vern L. Schramm ◽  
Vipender Singh ◽  
Peter C. Tyler






2015 ◽  
Vol 69 (2) ◽  
Author(s):  
Marek Baráth ◽  
Chun-Hung Lin ◽  
Igor Tvaroška ◽  
Ján Hirsch

AbstractNew potential transition state analogue inhibitors for N-acetylglucosyltransferases (GnTs) were synthesised. These compounds based on psico- and tagatofuranose (structure) scaffold contained a 2-thiophenyl-1-O-diethylphosphate moiety mimicking the proposed model of the transition state of the enzymatic reaction catalysed by N-acetylglucosyltransferases. The synthesised compounds as well as their precursors were fully characterised by NMR, optical rotation and mass techniques. Anomeric configuration of tagatofuranose derivatives was confirmed by X-ray crystallography. Two types of potential human glycosyltransferase (GnTs) inhibitors representing donor UDP-GlcNAc, assigned for biological assays on human GnTs, were prepared.



2005 ◽  
Vol 48 (14) ◽  
pp. 4679-4689 ◽  
Author(s):  
Gary B. Evans ◽  
Richard H. Furneaux ◽  
Dirk H. Lenz ◽  
Gavin F. Painter ◽  
Vern L. Schramm ◽  
...  


Biochemistry ◽  
2011 ◽  
Vol 50 (47) ◽  
pp. 10408-10417 ◽  
Author(s):  
Rong Guan ◽  
Meng-Chiao Ho ◽  
Michael Brenowitz ◽  
Peter C. Tyler ◽  
Gary B. Evans ◽  
...  




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