title: L-Enantiomers of transition state analogue inhibitors bound to human purine nucleoside phosphorylase.
abstract: Human purine nucleoside phosphorylase (PNP) was crystallized with transition-state analogue inhibitors Immucillin-H and DADMe-Immucillin-H synthesized with ribosyl mimics of l-stereochemistry. The inhibitors demonstrate that major driving forces for tight binding of these analogues are the leaving group interaction and the cationic mimicry of the transition state, even though large geometric changes occur with d-Immucillins and l-Immucillins bound to human PNP.
authors.affiliation: Department of Biochemistry, Albert Einstein College of Medicine, Bronx, New York 10461, USA.
authors.forename: Agnes
authors.initials: A
authors.lastname: Rinaldo-Matthis
authors.forename: Andrew S
authors.initials: AS
authors.lastname: Murkin
authors.forename: Udupi A
authors.initials: UA
authors.lastname: Ramagopal
authors.forename: Keith
authors.initials: K
authors.lastname: Clinch
authors.forename: Simon P H
authors.initials: SP
authors.lastname: Mee
authors.forename: Gary B
authors.initials: GB
authors.lastname: Evans
authors.forename: Peter C
authors.initials: PC
authors.lastname: Tyler
authors.forename: Richard H
authors.initials: RH
authors.lastname: Furneaux
authors.forename: Steven C
authors.initials: SC
authors.lastname: Almo
authors.forename: Vern L
authors.initials: VL
authors.lastname: Schramm
mesh_terms: D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000737:chemistry*; D006801:Humans; D011487:Protein Conformation; D011684:Purine Nucleosides / Q000737:chemistry*; D011683:Purine-Nucleoside Phosphorylase / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D011744:Pyrimidinones / Q000737:chemistry*; D011759:Pyrrolidines / Q000737:chemistry*; D013237:Stereoisomerism; D013379:Substrate Specificity
chemical_list: C508755:DADMe-immucillin H; D004791:Enzyme Inhibitors; D011684:Purine Nucleosides; D011744:Pyrimidinones; D011759:Pyrrolidines; C113101:forodesine; D011683:Purine-Nucleoside Phosphorylase