Peptidomimetics II


Helix MimicsTopographical MimicsOxopiperazine Helix MimeticsSynthesis of Oxopiperazine Helix MimeticsRecognition of Protein Receptors by Oxopiperazine Helix Mimeticsp53/Mdm2 as a Model System for Ligand DesignIn Silico Design of OHMs to Target PPIsOHMs Targeting the p300/HIF-1a InteractionDevelopment ofHIF-la MimicsHIF OHMs Decrease Expression of Downstream Hypoxia-Induced Genes in Cell CultureHIF-1a OHM Suppresses Tumor Growth In VivoConclusionReferencesHeterocyclic Extended Peptide Surrogates for в-Strand StabilizationIntroductionNative Backbone OrthoticsLactam ConstraintsMacrocyclic TethersAzabicycloalkanesTetrahydropyridazinedionesHeterocyclic Backbone ProstheticsPyrrolinonesDihydropyridinones and DihydropyrazinonesPyrrolesImidazopyridin.esConclusionsReferencesDiketopiperazine-Based Peptide Mimic ScaffoldsIntroductionDiketopiperazines as Rigid Units in Flexible Moleculesjl-Turn MimicsInternal 0-Turnsв-Hairpin Peptidomimetics and ReceptorsExternal в-Turn (Peptide Loops)a- and у-Turn MimicsPeptoid Peptidomimetics Containing DiketopiperazinesDiketopiperazines as Monomers in MacromoleculesDiketopiperazines Assembled via Non-covalent Bonds (Crystal Engineering)Foldamers Containing Multiple Diketopiperazines “Foldamersв-Bend Ribbon MimicsSpiroligomers, Ladder Molecules Containing Multiple DiketopiperazinesDiketopiperazines Involved in Mimicking Enzyme Active SitesScaffolds Containing One DKPScaffolds Containing Several DKPsConclusionReferencesSynthesis of Constrained Peptidomimetics via the Pictet-Spengler ReactionIntroductionPeptidomimeticsThe Pictet-Spengler ReactionSynthesis of Peptidomimetics via the Pictet-Spengler ReactionBi- and Tricyclic PeptidomimeticsPolycyclic PeptidomimeticsSpirocyclic PeptidomimeticsPerspectivesReferencesPeptidomimetics via Iminium Ion Chemistry on Solid Phase: Single, Fused, and Bridged HeterocyclesIntroductionGeneral StrategyApplication to PeptidesSingle HeterocyclesFused HeterocyclesFused Ring System Synthesis Using Five- and Six- Membered Iminium IonsSynthetic Strategies to Access Acyclic PrecursorsRegioselectivity of the Iminium Ion FormationSynthesis of 6,6- and 5,6-Fused Bicyclic SystemsC-Terminal Cyclization with Amino Acid Side Chain NucleophilesCompetition Between Nitrogen and Oxygen NucleophilesBenzoimidazopyrazinone SynthesisFused Ring System Synthesis Using Seven-Membered Iminium IonsFused Ring System Synthesis Using Eight- and Nine- Membered Iminium IonsBridged HeterocyclesBridged Ring System Synthesis Using Six-Membered Iminium Ion IntermediatesBridged Ring System Synthesis Using Seven-Membered Iminium IonsSummaryReferencesSynthesis of Peptidomimetics Through the Disrupted Ugi Reaction with Aziridine Aldehyde DimersMulticomponent ReactionsAmphoteric Molecules in MCRsUgi and Passerini MCRsAziridine AldehydesCyclic Peptide SynthesisConventional CyclizationPeptide Cyclization Through MCRsThe Disrupted Ugi Reaction with Aziridine Aldehyde Dimers and Amino AcidsFour-Component Five-Center Ugi ReactionPiperazinone ChemistryPeptide Macrocycles from Disrupted Ugi Reaction with Aziridine Aldehyde DimersProposed MechanismIncreasing Molecular Complexity Using Functionalized IsocyanidesDownstream Functionalization by Aziridine Ring OpeningSolid-Phase Synthesis Using the Disrupted Ugi ReactionPiperazinone SynthesisOn-Resin Peptide CyclizationSummaryReferencesRecent Studies on Gramicidin S Analog Structure and Antimicrobial ActivityIntroductionGeneralStructure and ConformationMechanism of ActionEffect of CholesterolActivityModifications and ConsequencesRing SizeEffect of N-MethylationExchange of Amino AcidSAA-Based AnalogsGS Dimers and PolymersGS as CatalystSynergistic EffectConclusionsReferencesAnti-amyloidogenic Heterocyclic PeptidesIntroductionAnti-amyloidogenic Heterocyclic PeptidesConformational MimicsCyclic D,L-a-PeptidesSequence MimicsCyclic Modular 0-SheetsCyclic KLVFF DerivativesConformational RestrictorsJanus Cyclic PeptideCyclic Peptide Inhibitors that Interfere with Amyloidogenic Signal TransductionCyclic Peptides Selected by In Vivo ScreeningTransmembrane Neurotrophin p75 Receptor (p75NTR)Protease InhibitorsNatural InhibitorsGramicidin S and DerivativesCyclodepsipeptidesCyclosporinCyclic Peptides as Anti-amyloidogenic Pharmacological ToolsMultivalent ScaffoldsAntibody-Derived Vaccination/Passive ImmunotherapySummaryReferencesLipoylated Peptides and ProteinsLipoic AcidLipoylation: In Vivo Pathways and Naturally Occurring Lipoylated ProteinsIn Vitro Lipoylation: Synthetic Strategies to Obtain Lipoylated PeptidesPreparation of Dihydrolipoylated Peptides and ProteinsUses of Lipoic Acid and Lipoylated MoleculesSummaryReferences
 
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