2021
Modulation of Phosphoprotein Activity by Phosphorylation Targeting Chimeras (PhosTACs)
Chen PH, Hu Z, An E, Okeke I, Zheng S, Luo X, Gong A, Jaime-Figueroa S, Crews CM. Modulation of Phosphoprotein Activity by Phosphorylation Targeting Chimeras (PhosTACs). ACS Chemical Biology 2021, 16: 2808-2815. PMID: 34780684, PMCID: PMC10437008, DOI: 10.1021/acschembio.1c00693.Peer-Reviewed Original ResearchConceptsSer/Thr phosphataseChemical biology approachPP2A holoenzymeProtein dephosphorylationBiology approachProtein substratesTranscriptional activationProtein phosphorylationCatalytic subunitCell biologyReporter geneProtein activityRetinoblastoma proteinOff-target effectsCritical proteinsDephosphorylationTernary complexPhosphorylationKinase inhibitorsFOXO3aPROTACsProteinChimerasPhosphataseDrug resistance
2019
A Conserved Allosteric Pathway in Tyrosine Kinase Regulation
Marsiglia WM, Katigbak J, Zheng S, Mohammadi M, Zhang Y, Traaseth NJ. A Conserved Allosteric Pathway in Tyrosine Kinase Regulation. Structure 2019, 27: 1308-1315.e3. PMID: 31204250, PMCID: PMC6687525, DOI: 10.1016/j.str.2019.05.002.Peer-Reviewed Original ResearchConceptsTyrosine kinaseTyrosine kinase regulationAllosteric control mechanismReceptor tyrosine kinasesTyrosine kinase familyKinase regulationDFG motifActivation loopAllosteric pathwayKinase familyMutational disruptionKinase hingeInactive conformationHydrophobic residuesHuman diseasesKinaseConformational perturbationsCombination of NMREnzyme thermostabilityMutationsSkeletal syndromeActive siteMolecular dynamics simulationsThermostabilityStructural analysis