Richard A. Norman
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View article: SUCCESSFULLY INCREASING DOE-STD-1027 HAZARD CATEGORY 3 (HC-3) THRESHOLD QUANTITIES (TQS)
SUCCESSFULLY INCREASING DOE-STD-1027 HAZARD CATEGORY 3 (HC-3) THRESHOLD QUANTITIES (TQS) Open
View article: Supplementary Tables and Legends from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Supplementary Tables and Legends from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models Open
Supplementary Table 1 contains crystallographic data collection and refinements statistics for AZD9496 binding to the human estrogen receptor α ligand binding domain, Supplementary Table 2 shows the rate constants for association, dissocia…
View article: Supplementary Figure Legends from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Supplementary Figure Legends from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models Open
Legends for Supplementary Figures 1 - 7.
View article: Data from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Data from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models Open
Fulvestrant is an estrogen receptor (ER) antagonist administered to breast cancer patients by monthly intramuscular injection. Given its present limitations of dosing and route of administration, a more flexible orally available compound h…
View article: Supplementary Methods from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Supplementary Methods from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models Open
Methods are given for: the use of SILAC assays to measure the rate of estrogen receptor α peptide degradation over time, the measurement of compound binding affinity of estrogen receptor α ligand binding domain using BIAcore, immunoblottin…
View article: Supplementary Figure Legends from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Supplementary Figure Legends from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models Open
Legends for Supplementary Figures 1 - 7.
View article: Supplementary Figures from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Supplementary Figures from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models Open
Supplementary Figure 1 contains a Western blot showing the amount of estrogen receptor remaining after treatment of MCF-7 cells with AZD9496, fulvestrant and estradiol alongside GAPDH protein levels as an internal gel loading control; Supp…
View article: Data from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Data from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models Open
Fulvestrant is an estrogen receptor (ER) antagonist administered to breast cancer patients by monthly intramuscular injection. Given its present limitations of dosing and route of administration, a more flexible orally available compound h…
View article: Supplementary Methods from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Supplementary Methods from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models Open
Methods are given for: the use of SILAC assays to measure the rate of estrogen receptor α peptide degradation over time, the measurement of compound binding affinity of estrogen receptor α ligand binding domain using BIAcore, immunoblottin…
View article: Supplementary Tables and Legends from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Supplementary Tables and Legends from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models Open
Supplementary Table 1 contains crystallographic data collection and refinements statistics for AZD9496 binding to the human estrogen receptor α ligand binding domain, Supplementary Table 2 shows the rate constants for association, dissocia…
View article: Supplementary Figures from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Supplementary Figures from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models Open
Supplementary Figure 1 contains a Western blot showing the amount of estrogen receptor remaining after treatment of MCF-7 cells with AZD9496, fulvestrant and estradiol alongside GAPDH protein levels as an internal gel loading control; Supp…
View article: Validation of ion mobility spectrometry ‐ mass spectrometry as a screening tool to identify type II kinase inhibitors of FGFR1 kinase
Validation of ion mobility spectrometry ‐ mass spectrometry as a screening tool to identify type II kinase inhibitors of FGFR1 kinase Open
Rationale The protein kinase FGFR1 regulates cellular processes in human development. As over‐activity of FGFR1 is implicated with cancer, effective inhibitors are in demand. Type I inhibitors, which bind to the active form of FGFR1, are l…
View article: Computational approaches to therapeutic antibody design: established methods and emerging trends
Computational approaches to therapeutic antibody design: established methods and emerging trends Open
Antibodies are proteins that recognize the molecular surfaces of potentially noxious molecules to mount an adaptive immune response or, in the case of autoimmune diseases, molecules that are part of healthy cells and tissues. Due to their …
View article: Correction to Investigation of (<i>E</i>)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators
Correction to Investigation of (<i>E</i>)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators Open
ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionNEXTORIGINAL ARTICLEThis notice is a correctionCorrection to Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulato…
View article: Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use
Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use Open
Frequent genetic alterations discovered in FGFRs and evidence implicating some as drivers in diverse tumors has been accompanied by rapid progress in targeting FGFRs for anticancer treatments. Wider assessment of the impact of genetic chan…
View article: Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat Open
A series of tetrahydroisoquinoline phenols was modified to give an estrogen receptor downregulator-antagonist profile. Optimization around the core, alkyl side chain, and pendant aryl ring resulted in compounds with subnanomolar levels of …
View article: Optimization of a Novel Binding Motif to (<i>E</i>)-3-(3,5-Difluoro-4-((1<i>R</i>,3<i>R</i>)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1<i>H</i>-pyrido[3,4-<i>b</i>]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist
Optimization of a Novel Binding Motif to (<i>E</i>)-3-(3,5-Difluoro-4-((1<i>R</i>,3<i>R</i>)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1<i>H</i>-pyrido[3,4-<i>b</i>]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist Open
The discovery of an orally bioavailable selective estrogen receptor downregulator (SERD) with equivalent potency and preclinical pharmacology to the intramuscular SERD fulvestrant is described. A directed screen identified the 1-aryl-2,3,4…
View article: Structural and dynamic insights into the energetics of activation loop rearrangement in FGFR1 kinase
Structural and dynamic insights into the energetics of activation loop rearrangement in FGFR1 kinase Open
View article: Investigation of (<i>E</i>)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators
Investigation of (<i>E</i>)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators Open
A novel estrogen receptor down-regulator, 7-hydroxycoumarin (5, SS5020), has been reported with antitumor effects against chemically induced mammary tumors. Here, we report on our own investigation of 7-hydroxycoumarins as potential select…