2024
Development of Ligands and Degraders Targeting MAGE-A3
Li K, Krone M, Butrin A, Bond M, Linhares B, Crews C. Development of Ligands and Degraders Targeting MAGE-A3. Journal Of The American Chemical Society 2024, 146: 24884-24891. PMID: 39190582, DOI: 10.1021/jacs.4c05393.Peer-Reviewed Original ResearchDNA-encoded librariesSmall molecule ligandsDevelopment of ligandsE3 ligase complexCocrystal structureChemical matterLigandPROTAC moleculesSmall moleculesLigase complexTargeted Protein DegradationMAGE-A3Substrate recognition moduleType I MAGEsRING E3 ligasesMoleculesCancer-selective expressionDimer interfaceImprove immunotherapy outcomesIncreased antigen presentationHigh tumor gradeE3 ligaseComplexBiochemical functionsCancer cell surface
2021
Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation
Bond MJ, Crews CM. Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation. RSC Chemical Biology 2021, 2: 725-742. PMID: 34212149, PMCID: PMC8190915, DOI: 10.1039/d1cb00011j.Peer-Reviewed Original Research
2008
Direct Functionalization of Nitrogen Heterocycles via Rh-Catalyzed C−H Bond Activation
Lewis JC, Bergman RG, Ellman JA. Direct Functionalization of Nitrogen Heterocycles via Rh-Catalyzed C−H Bond Activation. Accounts Of Chemical Research 2008, 41: 1013-1025. PMID: 18616300, PMCID: PMC2610463, DOI: 10.1021/ar800042p.Peer-Reviewed Original ResearchConceptsDiverse functional groupsNitrogen heterocyclesCarbene complexesDirect functionalizationBond activationAryl bromidesFunctional groupsH bond functionalization reactionsRh-N-heterocyclic carbene complexesAlkylation of azolesBond functionalization reactionsRh–NHC complexesH bond activationUnique coordination environmentVariety of heterocyclesFunctional group compatibilityNumber of diVariety of substituentsPCy 3Synthetic advancesFragment coordinatesFunctionalization reactionsN-methylbenzimidazoleRobust catalystsDevelopment of ligands
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