Structure-based design of inhibitors of purine nucleoside phosphorylase.

Abstract

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.

• Authors: Y S Babu, S E Ealick, C E Bugg, M D Erion, W C Guida, J A Montgomery, J A Secrist 3rd
• Journal: Acta crystallographica. Section D, Biological crystallography (Acta Crystallogr D Biol Crystallogr) Vol. 51 Issue Pt 4 Pg. 529-35 (Jul 01 1995) ISSN: 0907-4449 [Print] United States
• PMID: 15299840 (Publication Type: Journal Article)