Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases
Card GL, England BP, Suzuki Y, Fong D, Powell B, Lee B, Luu C, Tabrizizad M, Gillette S, Ibrahim PN, Artis DR, Bollag G, Milburn MV, Kim SH, Schlessinger J, Zhang KY. Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases. Structure 2004, 12: 2233-2247. PMID: 15576036, DOI: 10.1016/j.str.2004.10.004.Peer-Reviewed Original ResearchConceptsHigh-resolution crystal structuresInvariant glutamineHydrogen bondingCatalytic domainStructural basisStructural insightsIsoform-selective inhibitorsHydrolysis of cAMPHydrophobic residuesInhibitor bindingActive siteCrystal structureCocrystal structureHydrophobic clampLarge familyDifferent inhibitorsPhosphodiesterasesVariety of diseasesSelective PDE inhibitorsInhibitorsActivity of drugsPDE inhibitorsBondingEnzymeResidues