1999
The design, synthesis, and biological evaluation of analogues of the serine-threonine protein phosphatase 1 and 2A selective inhibitor microcystin LA: rational modifications imparting PP1 selectivity
Aggen J, Humphrey J, Gauss C, Huang H, Nairn A, Chamberlin A. The design, synthesis, and biological evaluation of analogues of the serine-threonine protein phosphatase 1 and 2A selective inhibitor microcystin LA: rational modifications imparting PP1 selectivity. Bioorganic & Medicinal Chemistry 1999, 7: 543-564. PMID: 10220039, DOI: 10.1016/s0968-0896(98)00254-5.Peer-Reviewed Original ResearchConceptsPP1 selectivityProtein phosphatase 1Serine-threonine proteinMicrocystin-LAFirst-generation analogsSmall molecule inhibitorsPhosphatase 1Observed selectivityBiological evaluationMolecular modeling analysisMolecule inhibitorsRational modificationSelectivityStructural modificationsSynthesisAnaloguesInhibition assaysPP1MicrocystinsProteinLaModificationAssaysInhibitors
1995
Three-dimensional structure of the catalytic subunit of protein serine/threonine phosphatase-1
Goldberg J, Huang H, Kwon Y, Greengard P, Nairn A, Kuriyan J. Three-dimensional structure of the catalytic subunit of protein serine/threonine phosphatase-1. Nature 1995, 376: 745-753. PMID: 7651533, DOI: 10.1038/376745a0.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SequenceAnimalsBinding SitesCatalysisCrystallography, X-RayDopamine and cAMP-Regulated Phosphoprotein 32Escherichia coliHumansIntracellular Signaling Peptides and ProteinsMetalsMicrocystinsModels, MolecularMolecular Sequence DataNerve Tissue ProteinsNuclear ProteinsPeptides, CyclicPhosphoprotein PhosphatasesPhosphoproteinsProtein ConformationProtein Phosphatase 1ProteinsRabbitsRecombinant ProteinsRNA-Binding ProteinsSequence Homology, Amino AcidConceptsPhosphatase 1Protein serine/threonine phosphatase-1Serine/threonine phosphatase 1Mammalian protein phosphatase 1Protein phosphatase 1Potential binding sitesThree-dimensional structureCatalytic subunitRegulatory sequencesCatalytic domainCarboxy terminusΒ scaffoldBinding sitesActive siteSurface groovesTerminusSubunitsDomainProteinCrystal structureSitesTyrosineMetalloenzymesSequenceToxin