Andrew J. Dannenberg
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View article: Data from Association of a Healthy Lifestyle Index with Risk of Breast Cancer among Women with Normal Body Mass Index in the UK Biobank
Data from Association of a Healthy Lifestyle Index with Risk of Breast Cancer among Women with Normal Body Mass Index in the UK Biobank Open
Background:A high healthy lifestyle index (HLI), a composite score based on good diet quality, low alcohol consumption, no smoking, moderate to high physical activity, and waist circumference 2). Whether the HLI is associated with br…
View article: ApoM-bound S1P acts via endothelial S1PR1 to suppress choroidal neovascularization and vascular leakage
ApoM-bound S1P acts via endothelial S1PR1 to suppress choroidal neovascularization and vascular leakage Open
View article: Table S2 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S2 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
This table provides details on where each cathepsin enzyme was obtained.
View article: Figure S2 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S2 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Shows binding assay performance and differential MetAP2 binding of test compounds.
View article: Figure S1 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S1 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Shows the structures of the PDC, the benzenesulfonate salt form of the physiologically active small molecule, and three test compounds, along with the numbering system utilized for NMR assignment of evexomostat.
View article: Table S7 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S7 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Detailed results from each behavioural measurement conducted in rats to assess potential CNS toxicity of SDX-7320.
View article: Table S1 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S1 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Displays the proton and carbon NMR assignments for evexomostat, including chemical shifts, multiplicities and coupling constants, for evexomostat under the experimental conditions shown based on the numbering system presented in Figure S1.
View article: Table S6 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S6 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Levels of small molecule MetAP2 inhibitors SDX-7539 and TNP-470 in plasma and CSF, used to assess CNS penetration.
View article: Table S3 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S3 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Results of competition for radioligand binding by SDX-9402 at different receptors, to assess the selectivity of the MetAP2 inhibitor against known drug targets.
View article: Table S6 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S6 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Levels of small molecule MetAP2 inhibitors SDX-7539 and TNP-470 in plasma and CSF, used to assess CNS penetration.
View article: Figure S5 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S5 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
This graph displays the exposure-time profile of SDX-7539 in rats after IV administration of SDX-7320 or SDX-7539.
View article: Table S4 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S4 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Results of enzyme assays that assessed the potential inhibitory activity of the MetPA2 inhibitor against various enzymes.
View article: Figure S6 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S6 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Variance in the expression of genes between control and SDX-7320-treated tumor samples is displayed in this graph.
View article: Table S4 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S4 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Results of enzyme assays that assessed the potential inhibitory activity of the MetPA2 inhibitor against various enzymes.
View article: Figure S6 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S6 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Variance in the expression of genes between control and SDX-7320-treated tumor samples is displayed in this graph.
View article: Figure S1 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S1 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Shows the structures of the PDC, the benzenesulfonate salt form of the physiologically active small molecule, and three test compounds, along with the numbering system utilized for NMR assignment of evexomostat.
View article: Figure S4 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S4 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
These results demonstrate the lack of MetAP1 aminopeptidase inhibition by SDX-7539 and TNP-470, and supports the findings regarding selectivity of these compounds for MetAP2.
View article: Data from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Data from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Methionine aminopeptidase type 2 (METAP2) is a ubiquitous, evolutionarily conserved metalloprotease fundamental to protein biosynthesis which catalyzes removal of the N-terminal methionine residue from nascent polypeptides. METAP2 is an at…
View article: Supplementary Data from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Supplementary Data from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Contains methods and results from additional experiments
View article: Table S5 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S5 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Detailed information from the x-ray crystallography of SDX-7539 bound to MetAP2 that enabled determination of the co-crystal’s 3D structure.
View article: Figure S2 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S2 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Shows binding assay performance and differential MetAP2 binding of test compounds.
View article: Figure S4 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S4 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
These results demonstrate the lack of MetAP1 aminopeptidase inhibition by SDX-7539 and TNP-470, and supports the findings regarding selectivity of these compounds for MetAP2.
View article: Supplementary Data from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Supplementary Data from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Contains methods and results from additional experiments
View article: Table S3 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S3 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Results of competition for radioligand binding by SDX-9402 at different receptors, to assess the selectivity of the MetAP2 inhibitor against known drug targets.
View article: Table S5 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S5 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Detailed information from the x-ray crystallography of SDX-7539 bound to MetAP2 that enabled determination of the co-crystal’s 3D structure.
View article: Figure S3 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S3 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Compares the 3D crystal structures of MetAP2 with SDX-7539 bound to that of MetAP2 with TNP-470
View article: Table S2 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S2 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
This table provides details on where each cathepsin enzyme was obtained.
View article: Table S7 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Table S7 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Detailed results from each behavioural measurement conducted in rats to assess potential CNS toxicity of SDX-7320.
View article: Figure S3 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S3 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
Compares the 3D crystal structures of MetAP2 with SDX-7539 bound to that of MetAP2 with TNP-470
View article: Figure S5 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity
Figure S5 from Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity Open
This graph displays the exposure-time profile of SDX-7539 in rats after IV administration of SDX-7320 or SDX-7539.