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Relevant bibliographies by topics / EGFR-BRD4

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Journal articles
Dissertations / Theses
Conference papers

Academic literature on the topic 'EGFR-BRD4'

Author: Grafiati

Published: 6 September 2023

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Journal articles on the topic "EGFR-BRD4"

1

Lin, Benjamin, Julia Ziebro, Kasey R. Skinner, et al. "Abstract 1125: Elucidating the transcriptomic response to EGFR-targeted therapy in EGFR-driven glioblastoma." Cancer Research 82, no. 12_Supplement (2022): 1125. http://dx.doi.org/10.1158/1538-7445.am2022-1125.

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Abstract Glioblastoma (GBM) is the most common malignant brain tumor in adults with a dismal 15-month median survival. Standard therapy consisting of surgical resection, radiation, and temozolomide has been unsuccessful in meaningfully extending survival and preventing recurrence; thus, novel therapeutics are urgently needed. One proposed targeted treatment strategy for GBM involves using small molecule inhibitors against common genetic mutations. Epidermal growth factor receptor (EGFR) is the most commonly overexpressed oncogene in GBM (~56%). While EGFR tyrosine kinase inhibitors (TKI) have

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2

Wang, Jingyuan, Yi Xiao, Fotios Loupakis, et al. "Genetic variants involved in bromodomain-containing protein 4 (BRD4) regulating pathway to predict outcomes in patients with metastatic colorectal cancer: Results from FIRE3 and MAVERICC trials." Journal of Clinical Oncology 38, no. 4_suppl (2020): 232. http://dx.doi.org/10.1200/jco.2020.38.4_suppl.232.

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232 Background: BRD4 plays an important role in transcription, DNA repair and drug resistance. High expression and polymorphisms of BRD4 regulating pathways were reported to be related to worse prognosis in colorectal cancer. Therefore, we hypothesized that genetic variants in BRD4 regulating pathway may predict first-line treatment outcome in mCRC pts. Methods: The impact on outcome of 22 SNPs in 7 genes involved in BRD4 regulating pathway (BRD4, SIPA1, MYC, 53BP1, H2AX, BATF, CD47) was analyzed through the OncoArray, a customized array manufactured by Illumina, on genomic DNA from blood samp

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Dong, Hang, Hao Yin, Chunlong Zhao, Jiangying Cao, Wenfang Xu, and Yingjie Zhang. "Design, Synthesis and Biological Evaluation of Novel Osimertinib-Based HDAC and EGFR Dual Inhibitors." Molecules 24, no. 13 (2019): 2407. http://dx.doi.org/10.3390/molecules24132407.

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Herein a novel series of histone deacetylases (HDACs) and epidermal growth factor receptor (EGFR) dual inhibitors were designed and synthesized based on the structure of the approved EGFR inhibitor osimertinib (AZD9291). Among them, four compounds 5D, 5E, 9D and 9E exhibited more potent total HDAC inhibition than the approved HDAC inhibitor SAHA. However, these compounds only showed moderate to low inhibitory potency towards EGFR with compounds 5E and 9E possessing IC50 values against EGFRWT and EGFRT790M in the micromolar range. 3-[4,5-dimethyl-2-thiazolyl]-2,5-diphenyl-2H-tetrazolium bromide

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4

Toren, Paul, Amina Zoubeidi, and Jared Allman. "Pre-clinical rationale for combination PI3K and BRD4 inhibition in advanced prostate cancer." Journal of Clinical Oncology 34, no. 2_suppl (2016): 234. http://dx.doi.org/10.1200/jco.2016.34.2_suppl.234.

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234 Background: The PI3K/Akt pathway is frequently activated in aggressive and resistant prostate cancer. Here we detail our pre-clinical evaluation of AZD8186, a novel β and δ selective PI3K small molecule inhibitor. Further, we investigate how increased transcription of the myc oncogene may represent a mechanism of resistance to monotherapy PI3K/Akt inhibition. Therefore, we further evaluated co-targeting strategies against both the PI3K/Akt pathway and the epigenetic reader protein BRD4. Methods: Human prostate cancer cell lines LNCaP and 22RV1 were tested for sensitivity to AZD8186 in vitr

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5

Beaton, Nigel, Jagat Adhikari, Roland Bruderer, et al. "Abstract 2136: Prediction of small molecule-protein binding events for BRD4 and EGFR inhibitors using HR-LiP, a novel structural proteomics approach." Cancer Research 82, no. 12_Supplement (2022): 2136. http://dx.doi.org/10.1158/1538-7445.am2022-2136.

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Abstract Background: Beyond phenotypic efficacy and safety categorization, high resolution profiling of drug-protein interactions and binding mechanisms remains a major hurdle during lead selection and optimization. A key milestone in structure-based drug design is compound binding site identification and characterization. Structure-activity relationship (SAR) studies utilize techniques such as nuclear magnetic resonance (NMR), x-ray crystallography (X-ray), cryo-electron microscopy (cryo-EM) and the mass spectrometry-based hydrogen-deuterium exchange (HDX) to address these hurdles but they ar

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6

Allen, B., S. Mehta, N. Ayad, and S. Schurer. "DD-01 * LIGAND- AND STRUCTURE-BASED VIRTUAL SCREENING TO DISCOVER POLYPHARMACOLOGICAL DUAL EGFR AND BRD4 INHIBITORS." Neuro-Oncology 16, suppl 5 (2014): v60. http://dx.doi.org/10.1093/neuonc/nou246.1.

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7

Wei, Xiuxian, Yi Li, Pengcheng Luo, et al. "Development and Validation of Robust Ferroptosis-Related Genes in Myocardial Ischemia-Reperfusion Injury." Journal of Cardiovascular Development and Disease 10, no. 8 (2023): 344. http://dx.doi.org/10.3390/jcdd10080344.

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(1) Background: Despite the evidence that ferroptosis is involved in myocardial ischemia-reperfusion (MIR), the critical regulator of ferroptosis in MIR remains unclear. (2) Methods: We included three GEO datasets and a set of ferroptosis-related genes with 259 genes. Following the identification of the differentially expressed ferroptosis-related genes (DEFRGs) and hub genes, we performed the functional annotation, protein–protein interaction network, and immune infiltration analysis. The GSE168610 dataset, a cell model, and an animal model were then used to verify key genes. (3) Results: We

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8

Zhang, Chi, Wen Yuan, Ying Wu, Xu Wan, and Yanling Gong. "Co-delivery of EGFR and BRD4 siRNA by cell-penetrating peptides-modified redox-responsive complex in triple negative breast cancer cells." Life Sciences 266 (February 2021): 118886. http://dx.doi.org/10.1016/j.lfs.2020.118886.

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9

Wang, Qiong, Ying Pan, Hongjun Luo, et al. "Novel Approaches for the Solid-Phase Synthesis of Dihydroquinazoline-2(1H)-One Derivatives and Biological Evaluation as Potential Anticancer Agents." Molecules 27, no. 23 (2022): 8577. http://dx.doi.org/10.3390/molecules27238577.

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In the design of antineoplastic drugs, quinazolinone derivatives are often used as small molecule inhibitors for kinases or receptor kinases, such as the EGFR tyrosine kinase inhibitor gefitinib, p38MAP kinase inhibitor DQO-501, and BRD4 protein inhibitor PFI-1. A novel and convenient approach for the solid-phase synthesis of dihydroquinazoline-2(1H)-one derivatives was proposed and 19 different compounds were synthesized. Cytotoxicity tests showed that most of the target compounds had anti-proliferative activity against HepG-2, A2780 and MDA-MB-231 cell lines. Among them, compounds CA1-e and

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10

Jermakowicz, Anna, Vasileios Stathias, Robert Suter, James Duncan, Stephan Schürer, and Nagi Ayad. "GENE-36. INTEGRATING TRANSCRIPTOMICS AND KINOMICS IDENTIFIES SYNERGISTIC DRUG COMBINATIONS FOR GLIOBLASTOMA TREATMENT." Neuro-Oncology 21, Supplement_6 (2019): vi105. http://dx.doi.org/10.1093/neuonc/noz175.438.

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Abstract Glioblastoma (GBM) is the most common and malignant adult brain tumor. Despite years of research, few advancements have been made in its management. One promising avenue of research has been treatment with BRD4 inhibitors, which decrease oncogene expression in GBM cells. However, resistance to these inhibitors is rapidly acquired. Kinome reprogramming is thought to underlie this resistance, suggesting a need for combination therapy with kinase inhibitors. The goal of this study is to determine whether transcriptomic and kinomic profiling of GBM tumors will identify synergistic drug pa

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Dissertations / Theses on the topic "EGFR-BRD4"

1

Mukherjee, Tanushree. "Immunological insights into Epidermal Growth Factor Receptor Signaling: Implications for host-pathogen interactions." Thesis, 2018. http://etd.iisc.ac.in/handle/2005/4340.

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Infectious diseases account for a large proportion of morbidity and mortality worldwide. The major global efforts lie in effectively enhancing the health span of infected individuals and more importantly, curbing infection onset and spread. A multitude of host- and pathogen-derived factors contribute towards coining the outcome of infections. In this regard, the virulence of major successful infectious agents is believed to be determined by their prowess to swivel host immune system to their own benefit. The pathogens effectuate such immune subversions by modulating various host signalling pat

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Conference papers on the topic "EGFR-BRD4"

1

Allen, Bryce, Saurabh Mehta, Nagi Ayad, and Stephan Schürer. "Abstract 3690: Ligand- and structure-based virtual screening to discover dual EGFR and BRD4 inhibitors." In Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1538-7445.am2015-3690.

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