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Article

Immucillins in custom catalytic-site cavities.

Bioorganic & medicinal chemistry letters - 15 Nov 2008

Murkin Andrew S, Clinch Keith, Mason Jennifer M, Tyler Peter C, Schramm Vern L

Abstract excerpt

Neighboring-group participation in the reaction catalyzed by purine nucleoside phosphorylase involves a compression mode between the 5'- and 4'-ribosyl oxygens, facilitated by His257. The His257Gly mutant opens a space in the catalytic site. Hydrophobic 5'-substituted Immucillins are transition-state analogue inhibitors of this mutant enzyme. Dissociation constants as low as 2pM are achieved, with K(m)/K(d) as...

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Share to Catalytic Domain
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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Source

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Identifiers

PMID: 18778937
DOI: 10.1016/j.bmcl.2008.08.047
PMCID: PMC2614083

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

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