Jeffrey N. Johnston
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View article: Total Synthesis of Feglymycin Using Umpolung Amide Synthesis
Total Synthesis of Feglymycin Using Umpolung Amide Synthesis Open
The preparation of peptidic molecules is a mainstay of synthesis, creating new tools that advance chemical biology, catalysis, and drug discovery. Despite the wide adoption of methods for amide synthesis based on electrophilic acyl transfe…
View article: Total Synthesis of Feglymycin Using Umpolung Amide Synthesis
Total Synthesis of Feglymycin Using Umpolung Amide Synthesis Open
The preparation of peptidic molecules is a mainstay of synthesis, creating new tools that advance chemical biology, catalysis, and drug discovery. Despite the wide adoption of methods for amide synthesis based on electrophilic acyl transfe…
View article: Performance-Enhancing Asymmetric Catalysis Driven by Achiral Counterion Design
Performance-Enhancing Asymmetric Catalysis Driven by Achiral Counterion Design Open
The development of highly enantioselective reactions often requires the adventitious discovery of a promising chiral catalyst and its resource-intensive optimization to high selectivity and generality. We report an approach less dependent …
View article: End-to-End Backbone Cyclization Enhances Passive Permeability of bRo5 Oligomeric Depsipeptides with Nonlinear Size Dependence
End-to-End Backbone Cyclization Enhances Passive Permeability of bRo5 Oligomeric Depsipeptides with Nonlinear Size Dependence Open
A majority of drugs are small molecules that satisfy Lipinski's Rule-of-Five (Ro5), but efforts to target topologically complex biomolecular interactions have reignited interest in nonconforming molecular therapeutics, dubbed "beyond Ro5 (…
View article: Elucidating Fluorine Steering Effects in Diels‐Alder Reactions Interfaced with Charge‐Enhanced Reactivity
Elucidating Fluorine Steering Effects in Diels‐Alder Reactions Interfaced with Charge‐Enhanced Reactivity Open
Fluorinated molecules are core to contemporary drug discovery programs and critical for advancing innovation in numerous fields. In merging these important chemical themes, fluorinated Diels‐Alder cycloaddition products are a particularly …
View article: Backbone-Determined Antiarrhythmic Structure–Activity Relationships for a Mirror Image, Oligomeric Depsipeptide Natural Product
Backbone-Determined Antiarrhythmic Structure–Activity Relationships for a Mirror Image, Oligomeric Depsipeptide Natural Product Open
Cyclic oligomeric depsipeptides (COD) are a structural class within naturally occurring compounds with a wide range of biological activity. Verticilide is a COD (24-membered ring) that was identified by its inhibition of insect ryanodine r…
View article: CCDC 2287760: Experimental Crystal Structure Determination
CCDC 2287760: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Generality-Driven Catalyst Development: A Universal Catalyst for Enantioselective Nitroalkene Reduction
Generality-Driven Catalyst Development: A Universal Catalyst for Enantioselective Nitroalkene Reduction Open
Cracking the selectivity-generality paradox is among the most pressing challenges in asymmetric catalysis. This obstacle prevents the immediate and successful translation of new methods to diverse small molecules. This is particularly rate…
View article: The backbone constitution drives passive permeability independent of side chains in depsipeptide and peptide macrocycles inspired by <i>ent</i>-verticilide
The backbone constitution drives passive permeability independent of side chains in depsipeptide and peptide macrocycles inspired by <i>ent</i>-verticilide Open
The number of peptide-like scaffolds found in late-stage drug development is increasing, but a critical unanswered question in the field is whether substituents (side chains) or the backbone drive passive permeability.
View article: RyR2 Binding of an Antiarrhythmic Cyclic Depsipeptide Mapped Using Confocal Fluorescence Lifetime Detection of FRET
RyR2 Binding of an Antiarrhythmic Cyclic Depsipeptide Mapped Using Confocal Fluorescence Lifetime Detection of FRET Open
Hyperactivity of cardiac sarcoplasmic reticulum (SR) ryanodine receptor (RyR2) Ca2+-release channels contributes to heart failure and arrhythmias. Reducing the RyR2 activity, particularly during cardiac relaxation (diastole), is a desirabl…
View article: CCDC 2194423: Experimental Crystal Structure Determination
CCDC 2194423: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2194422: Experimental Crystal Structure Determination
CCDC 2194422: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: <i>ent</i>-Verticilide B1 inhibits type 2 ryanodine receptor channels and is antiarrhythmic in Casq2-/- mice
<i>ent</i>-Verticilide B1 inhibits type 2 ryanodine receptor channels and is antiarrhythmic in Casq2-/- mice Open
Ca 2+ leak from cardiac ryanodine receptor (RyR2) is an established mechanism of sudden cardiac death (SCD), whereby dysregulated Ca 2+ handling causes ventricular arrhythmias. We previously discovered the RyR2-selective inhibitor ent- (+)…
View article: RyR2 Binding of an Antiarrhythmic Cyclic Depsipeptide Mapped Using Confocal Fluorescence Lifetime Detection of FRET
RyR2 Binding of an Antiarrhythmic Cyclic Depsipeptide Mapped Using Confocal Fluorescence Lifetime Detection of FRET Open
Hyperactivity of cardiac sarcoplasmic reticulum (SR) ryanodine receptor (RyR2) Ca 2+ -release channels contributes to heart failure and arrhythmias. Reducing RyR2 activity, particularly during cardiac relaxation (diastole), is a desirable …
View article: Supplementary Methods from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Methods from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Methods. Description of additional methods and procedures used in the study.
View article: Supplementary Figure S1 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Figure S1 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Figure S1. The hybrid physiologically-based pharmacokinetic models for (-)-Nutlin-3 and MLN8237 comprising several organ compartments.
View article: Data from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Data from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Therapeutics that induce cancer cell senescence can block cell proliferation and promote immune rejection. However, the risk of tumor relapse due to senescence escape may remain high due to the long lifespan of senescent cells that are not…
View article: Supplementary Figure S2 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Figure S2 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Figure S2. (-)-Nutlin-3 activates p53 in p53WT cells and induces caspase-independent cell death.
View article: Supplementary Figure S1 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Figure S1 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Figure S1. The hybrid physiologically-based pharmacokinetic models for (-)-Nutlin-3 and MLN8237 comprising several organ compartments.
View article: Supplementary Figure S4 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Figure S4 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Figure S4. Combined (-)-Nutlin-3 and MLN8237 treatment induces cell death in mouse B16F0 melanoma cells in vitro and in vivo.
View article: Supplementary Figure S7 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Figure S7 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Figure S7. Results of the flow cytometric analysis of indicated populations of leukocytes in SK-Mel5 tumors grown in BALB/C nu/Foxn1 athymic nude mice.
View article: Supplementary Figure S5 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Figure S5 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Figure S5. (-)-Nutlin-3 treatment affects tumor vasculature in vivo.
View article: Supplementary Figure S7 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Figure S7 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Figure S7. Results of the flow cytometric analysis of indicated populations of leukocytes in SK-Mel5 tumors grown in BALB/C nu/Foxn1 athymic nude mice.
View article: Supplementary Methods from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Methods from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Methods. Description of additional methods and procedures used in the study.
View article: Supplementary Table S1 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Table S1 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Table S1. Parameter estimates and interindividual variability for the (�)�Nutlin�3 pharmacokinetic model.
View article: Supplementary Figure S5 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Figure S5 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Figure S5. (-)-Nutlin-3 treatment affects tumor vasculature in vivo.
View article: Supplementary Table S1 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells
Supplementary Table S1 from Mdm2 and Aurora Kinase A Inhibitors Synergize to Block Melanoma Growth by Driving Apoptosis and Immune Clearance of Tumor Cells Open
Supplementary Table S1. Parameter estimates and interindividual variability for the (�)�Nutlin�3 pharmacokinetic model.