Structure-based design of inhibitors of purine nucleoside phosphorylase.
Inhibitors of purine nucleoside phosphorylase may have therapeutic value in the treatment of T-cell proliferative diseases such as T-cell leukemia, in the suppression of host-versus-graft response in organ transplants, and in the treatment of T-cell-mediated autoimmune diseases. Competitive inhibitors of this enzyme have been designed using the three-dimensional structure of the enzyme determined by X-ray crystallography. This approach has resulted in the synthesis of the most potent and membrane-permeable inhibitors of purine nucleoside phosphorylase reported so far.
Babu
Y S
YS
BioCryst Pharmaceuticals, Inc., Birmingham, AL 35244, USA.
Ealick
S E
SE
Bugg
C E
CE
Erion
M D
MD
Guida
W C
WC
Montgomery
J A
JA
Secrist
J A
JA