A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Card GL, Blasdel L, England BP, Zhang C, Suzuki Y, Gillette S, Fong D, Ibrahim PN, Artis DR, Bollag G, Milburn MV, Kim SH, Schlessinger J, Zhang KY. A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design. Nature Biotechnology 2005, 23: 201-207. PMID: 15685167, DOI: 10.1038/nbt1059.Peer-Reviewed Original ResearchConceptsDrug designX-ray crystallographyStructural analysisChemical synthesisDetailed structural analysisScaffold derivativesPyrazole derivativesChemical substitutionPotent PDE4 inhibitorsCarboxylic estersCellular processesDrug candidatesMolecular basisNew inhibitorsCyclic nucleotide phosphodiesterasesCocrystallographyLarge familyCompoundsNucleotide phosphodiesterasesDerivativesPhosphodiesterasesCrystallographyInhibitorsEfficient methodFamily