Graeme E. Walker
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View article: Supplementary Materials and Methods from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Materials and Methods from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i> Open
PDF - 56KB, Supplementary methods detailing Relative peptide quantification by selected reaction monitoring (SRM)using mass spectrometry
View article: Data from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>
Data from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i> Open
Continued androgen receptor (AR) expression and signaling is a key driver in castration-resistant prostate cancer (CRPC) after classical androgen ablation therapies have failed, and therefore remains a target for the treatment of progressi…
View article: Supplementary Figure Legends from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Figure Legends from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i> Open
PDF - 71KB
View article: Supplementary Materials and Methods from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Materials and Methods from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i> Open
PDF - 56KB, Supplementary methods detailing Relative peptide quantification by selected reaction monitoring (SRM)using mass spectrometry
View article: Supplementary Figures 1 -7 from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Figures 1 -7 from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i> Open
PDF - 464KB, Supplementary Figure 1: Inhibition of AR transcripts with AZD3514 treated LNCaPs in steroid free media and the timecourse of AZD3514 effects in the presence and absence of DHT. Supplementary Figure 2: Effect of AZD3514 on grow…
View article: Data from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>
Data from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i> Open
Continued androgen receptor (AR) expression and signaling is a key driver in castration-resistant prostate cancer (CRPC) after classical androgen ablation therapies have failed, and therefore remains a target for the treatment of progressi…
View article: Supplementary Figures 1 -7 from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Figures 1 -7 from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i> Open
PDF - 464KB, Supplementary Figure 1: Inhibition of AR transcripts with AZD3514 treated LNCaPs in steroid free media and the timecourse of AZD3514 effects in the presence and absence of DHT. Supplementary Figure 2: Effect of AZD3514 on grow…
View article: Supplementary Tables 1-4 from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Tables 1-4 from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i> Open
PDF - 329KB, Supplementary Table 1: TSQ Vantage mass spectrometry instrument settings. Supplementary Table 2: 4000 QTRAP mass spectrometry instrument settings. Supplementary Table 3: The half-life of AR for the first 6 hours following trea…
View article: Supplementary Tables 1-4 from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Tables 1-4 from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i> Open
PDF - 329KB, Supplementary Table 1: TSQ Vantage mass spectrometry instrument settings. Supplementary Table 2: 4000 QTRAP mass spectrometry instrument settings. Supplementary Table 3: The half-life of AR for the first 6 hours following trea…
View article: Supplementary Figure Legends from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Figure Legends from AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i> Open
PDF - 71KB
View article: Supplementary Table from AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies
Supplementary Table from AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies Open
Supplementary Table from AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies
View article: Supplementary Table from AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies
Supplementary Table from AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies Open
Supplementary Table from AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies
View article: Data from AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies
Data from AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies Open
Insights from cell cycle research have led to the hypothesis that tumors may be selectively sensitized to DNA-damaging agents resulting in improved antitumor activity and a wider therapeutic margin. The theory relies on the observation tha…
View article: Data from AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies
Data from AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies Open
Insights from cell cycle research have led to the hypothesis that tumors may be selectively sensitized to DNA-damaging agents resulting in improved antitumor activity and a wider therapeutic margin. The theory relies on the observation tha…
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: 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: 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 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: NMR Molecular Replacement Provides New Insights into Binding Modes to Bromodomains of BRD4 and TRIM24
NMR Molecular Replacement Provides New Insights into Binding Modes to Bromodomains of BRD4 and TRIM24 Open
Structure-based drug discovery (SBDD) largely relies on structural information from X-ray crystallography because traditional NMR structure calculation methods are too time consuming to be aligned with typical drug discovery timelines. The…
View article: A High-Throughput Screening Triage Workflow to Authenticate a Novel Series of PFKFB3 Inhibitors
A High-Throughput Screening Triage Workflow to Authenticate a Novel Series of PFKFB3 Inhibitors Open
A high-throughput screen (HTS) of human 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) resulted in several series of compounds with the potential for further optimization. Informatics was used to identify active chemotypes …
View article: AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies
AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies Open
The bromodomain and extraterminal (BET) protein BRD4 regulates gene expression via recruitment of transcriptional regulatory complexes to acetylated chromatin. Pharmacological targeting of BRD4 bromodomains by small molecule inhibitors has…