azd5153  (AstraZeneca ltd)

Journal: Genes & Diseases

Article Title: Differences between lung adenocarcinoma and lung squamous cell carcinoma: Driver genes, therapeutic targets, and clinical efficacy

doi: 10.1016/j.gendis.2024.101374

Figure Lengend Snippet: Epigenetic targeted therapies for lung adenocarcinoma and lung squamous cell carcinoma.

Article Snippet: , AZD5153 , Malignant solid tumors , Phase I , NCT03205176 , AZD5153 ± olaparib , 49 , Completed , AstraZeneca.

Techniques:

Journal: Cell Reports Medicine

Article Title: Genomic profiling of a multi-lineage and multi-passage patient-derived xenograft biobank reflects heterogeneity of ovarian cancer

doi: 10.1016/j.xcrm.2024.101631

Figure Lengend Snippet: DDR inhibitor drug screening in OC PDX models (A) Tumor volume change curves of OC09_OVPF3 PDX subjected to WEE1i, PARPi, and vehicle treatment ( n = 5 for CON group, n = 6 for WEE1i and PARPi groups). (B) Tumor volume change curves of OC19_OVPF2 PDX subjected to WEE1i, PARPi, and vehicle treatment ( n = 5). (C) Tumor volume change curves of OC13_OVPF3 PDX subjected to WEE1i, PARPi, and vehicle treatment ( n = 6). (D) Tumor volume change curves of OC04_OVPF2 PDX subjected to WEE1i, PARPi, BRD4/BETi, and vehicle treatment ( n = 5 for CON and WEE1i groups, n = 4 for PARPi and BRD4/BETi groups). (E) Tumor volume change curves of OC21_OVPF5 PDX subjected to WEE1i, PARPi, ATMi, and vehicle treatment ( n = 5). (F) Tumor volume change curves of OC27_AFPF3 PDX subjected to WEE1i, PARPi, and vehicle treatment ( n = 5). For (A)–(F), p values were calculated by t test.

Article Snippet: BRD4 inhibitor , MedChemExpress , AZD5153.

Techniques:

Journal: Cell Reports Medicine

Article Title: Genomic profiling of a multi-lineage and multi-passage patient-derived xenograft biobank reflects heterogeneity of ovarian cancer

doi: 10.1016/j.xcrm.2024.101631

Figure Lengend Snippet:

Article Snippet: BRD4 inhibitor , MedChemExpress , AZD5153.

Techniques: Recombinant, Saline, Sequencing, Software

Journal: Cancer cell

Article Title: A deregulated HOX gene axis confers an epigenetic vulnerability in KRAS -mutant lung cancers

doi: 10.1016/j.ccell.2020.03.004

Figure Lengend Snippet: KEY RESOURCES TABLE

Article Snippet: AZD5153 (BETi) , Chemietek , Cat# CT-A5153.

Techniques: Recombinant, Apoptosis Assay, Staining, Microarray, Gene Expression, Plasmid Preparation, Clone Assay, Sequencing, Software

Journal: bioRxiv

Article Title: The BET inhibitors JQ1, AZD5153, and I-BET151 co-opt ubiquitin proteasome system components for altering expression of the BRD4 interactome in a human B cell line

doi: 10.1101/2023.11.09.566482

Figure Lengend Snippet: Venn diagrams showing the combined or individual responses of BET inhibitors on UBQint proteins. The 536 proteins common to JQ1 and AZD5153 treatments was the single largest set, followed by the set of 266 proteins which remain unchanged with BET inhibition. These were mostly housekeeping proteins.

Article Snippet: Compounds and drugs: The BET inhibitors, JQ1 (Catalog No.S7110), AZD5153 (Catalog No.S8344) and I-BET151 (GSK1210151A) (Catalog No.S2780) were purchased from SelleckChem.

Techniques: Inhibition

Journal: bioRxiv

Article Title: The BET inhibitors JQ1, AZD5153, and I-BET151 co-opt ubiquitin proteasome system components for altering expression of the BRD4 interactome in a human B cell line

doi: 10.1101/2023.11.09.566482

Figure Lengend Snippet: Representation of known functions of UBQint proteins. Number of proteins of a specific function identified across all 4 samples (grey bars); commonly and uniquely in JQ1 and AZD5153 (orange bars); over-represented in JQ1 and AZD5153 compared with the average for all 4 samples (green bars); and under-represented in JQ1 and AZD5153 compared with the average for all 4 samples (blue bars).

Article Snippet: Compounds and drugs: The BET inhibitors, JQ1 (Catalog No.S7110), AZD5153 (Catalog No.S8344) and I-BET151 (GSK1210151A) (Catalog No.S2780) were purchased from SelleckChem.

Techniques:

Journal: bioRxiv

Article Title: The BET inhibitors JQ1, AZD5153, and I-BET151 co-opt ubiquitin proteasome system components for altering expression of the BRD4 interactome in a human B cell line

doi: 10.1101/2023.11.09.566482

Figure Lengend Snippet: A chart showing how UBQint proteins common to JQ1 and AZD5153 treatments were segregated into different response zones using the prediction model. The X-axis represents protein candidates, Y-axis shows the per cent ratios of optimized peptide counts for each protein. Proteins mapping to the orange box, yellow box, and green box indicate protein candidates responding to JQ1, AZD5153, and BRD4, respectively.

Article Snippet: Compounds and drugs: The BET inhibitors, JQ1 (Catalog No.S7110), AZD5153 (Catalog No.S8344) and I-BET151 (GSK1210151A) (Catalog No.S2780) were purchased from SelleckChem.

Techniques:

Journal: bioRxiv

Article Title: The BET inhibitors JQ1, AZD5153, and I-BET151 co-opt ubiquitin proteasome system components for altering expression of the BRD4 interactome in a human B cell line

doi: 10.1101/2023.11.09.566482

Figure Lengend Snippet: Representations of proteins known to function in the BAF complex identified in UBQint samples. Blue ovals – identified commonly in all samples, with thecaveat that ARI D1A can switch for ARID1B). Red ovals – Proteins commonly identified in JQ1 and AZD5153 treated samples. Grey oval – protein specific to AZD5153 treatment.

Article Snippet: Compounds and drugs: The BET inhibitors, JQ1 (Catalog No.S7110), AZD5153 (Catalog No.S8344) and I-BET151 (GSK1210151A) (Catalog No.S2780) were purchased from SelleckChem.

Techniques: