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Pharmacology & Pharmacy
Ying Jiang, Chunhui Huang, Yaqi Huang, Lifan Long, Guowu Wu, Fengqiu Guo, Chuan Huang, Siming Liu, Zhengguang Zhu, Shaoyu Wu, Zhonghuang Li, Jiajie Zhang, Shanhe Wan
Summary: Targeting EGFR with the inhibitor SMUZ106 has shown promising anti-tumor effects for glioblastoma (GBM). In this study, SMUZ106 was found to inhibit the growth and proliferation of GBM cells through various experiments, including MTT, clone formation, and flow cytometry. The selectivity and inhibitory activity of SMUZ106 to EGFR were confirmed using Western blotting, molecular docking, and kinase spectrum screening methods. In vivo experiments demonstrated that SMUZ106 hydrochloride has a high bioavailability and low toxicity, and it significantly inhibited GBM growth.
Review
Immunology
Fenge Li, Huancheng Wu, Xueming Du, Yimo Sun, Barbara Nassif Rausseo, Amjad Talukder, Arjun Katailiha, Lama Elzohary, Yupeng Wang, Zhiyu Wang, Gregory Lizee
Summary: The EGFR gene is frequently overexpressed and mutated in various solid tumors, and peptide vaccines targeting mutated EGFR have shown promising clinical efficacy and safety profiles.
Correction
Biochemistry & Molecular Biology
Jeong-Yub Kim, Hee-Jin Kim, Chan-Woong Jung, Byung-Il Choi, Dae-Hee Lee, Myung-Jin Park
Summary: A correction to this paper has been published.
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Biochemistry & Molecular Biology
Rosemary Lane, Chiara Cilibrasi, Jianing Chen, Kalpit Shah, Eleonora Messuti, Nektarios K. Mazarakis, Justin Stebbing, Giles Critchley, Erwei Song, Thomas Simon, Georgios Giamas
Summary: This study identifies PDGF-R alpha/beta inhibitor CP-673451 as a potential differentiation agent for GBM. In vitro experiments showed that CP-673451 promotes differentiation of GBM cells and GBM stem cells into neural-like cells, while reducing proliferation and invasion. In vivo experiments demonstrated that CP-673451 enhances the anti-tumor effects of temozolomide. Mechanistically, upregulation of phosphatase DUSP1 and downregulation of phosphorylated-p38(MAPK) may underlie the pro-differentiation effect of CP-673451 on GBM cells.
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Oncology
Mengkai Yang, Tao Zhang, Yangfeng Zhang, Xiaojun Ma, Jing Han, Ke Zeng, Yafei Jiang, Zongyi Wang, Zhuoying Wang, Jing Xu, Yingqi Hua, Zhengdong Cai, Wei Sun
Summary: The study revealed that MYLK4 promotes the growth and metastasis of osteosarcoma by activating the EGFR signaling pathway. Additionally, the combination of MYLK4 and EGFR inhibitors showed synergistic effects on the growth and metastasis of OS in vitro and in vivo.
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
(2021)
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Biology
Yongjian Huang, Jana Ognjenovic, Deepti Karandur, Kate Miller, Alan Merk, Sriram Subramaniam, John Kuriyan
Summary: Research has shown that the EGFR receptor can adopt different conformations of the extracellular module when binding to different ligands, with implications for intracellular signaling pathways.
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Oncology
Beomseok Sohn, Kisung Park, Sung Soo Ahn, Yae Won Park, Seung Hong Choi, Seok-Gu Kang, Se Hoon Kim, Jong Hee Chang, Seung-Koo Lee
Summary: A radiomics model based on dynamic contrast-enhanced (DCE) MRI was developed and validated to predict epidermal growth factor receptor (EGFR) amplification in patients with glioblastoma, isocitrate dehydrogenase (IDH) wildtype.
JOURNAL OF NEURO-ONCOLOGY
(2023)
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Oncology
Beomseok Sohn, Kisung Park, Sung Soo Ahn, Yae Won Park, Seung Hong Choi, Seok-Gu Kang, Se Hoon Kim, Jong Hee Chang, Seung-Koo Lee
Summary: The study developed and validated a radiomics model based on dynamic contrast-enhanced (DCE) MRI to predict EGFR amplification in glioblastoma patients. The radiomics model using the K-trans map showed higher accuracy than conventional MRI in predicting EGFR amplification.
JOURNAL OF NEURO-ONCOLOGY
(2023)
Review
Dermatology
Rachel Bierbrier, Megan Lam, Kevin Pehr
Summary: This review summarizes the available data on the use of systemic retinoids for managing acneiform eruptions induced by EGFR inhibitors. The findings suggest that systemic retinoids are a safe and effective therapy, with the majority of patients experiencing moderate to significant improvement after treatment initiation.
DERMATOLOGIC THERAPY
(2022)
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Medicine, Research & Experimental
Satoru Osuka, Dan Zhu, Zhaobin Zhang, Chaoxi Li, Christian T. Stackhouse, Oltea Sampetrean, Jeffrey J. Olson, G. Yancey Gillespie, Hideyuki Saya, Christopher D. Willey, Erwin G. Van Meir
Summary: Glioblastoma is composed of heterogeneous tumor cell populations, including glioma stem cells (GSCs) with stem cell properties. GSCs, which are less radiation sensitive, drive tumor formation and recurrence. Increase in N-cadherin expression enhances radioresistance and stemness in GSCs, while targeting N-cadherin can reverse the radiation resistance phenotype in these cells.
JOURNAL OF CLINICAL INVESTIGATION
(2021)
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Multidisciplinary Sciences
Chun Hu, Carlos A. Leche, Anatoly Kiyatkin, Zhaolong Yu, Steven E. Stayrook, Kathryn M. Ferguson, Mark A. Lemmon
Summary: The epidermal growth factor receptor (EGFR) frequently mutates in human cancer, and is an important therapeutic target. However, EGFR inhibitors have limited effectiveness in glioblastoma multiforme (GBM) due to exclusive mutations in the extracellular region. This study reveals that GBM mutations impair EGFR's ability to distinguish between activating ligands, which may have implications for therapeutic targeting.
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Multidisciplinary Sciences
Brendan Sullivan, Taylor Light, Vinh Vu, Adrian Kapustka, Kalina Hristova, Deborah Leckband
Summary: This study reveals a force-transduction mechanism that connects mechanical perturbations of E-cadherin to the activation of EGFR, a key regulator of cell proliferation. The results demonstrate that E-cadherin and EGFR form complexes at the plasma membrane, which are disrupted by the application of force or the presence of EGF. The findings provide insights into the initial steps of E-cadherin-mediated force transduction and the activation of growth regulatory signaling cascades.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Article
Biochemistry & Molecular Biology
Rosaria Bassi, Michele Dei Cas, Cristina Tringali, Federica Compostella, Rita Paroni, Paola Giussani
Summary: Glioblastoma multiforme (GBM) is the most common and lethal brain tumor. Sphingolipids play important roles in the regulation of GBM cell growth and chemotherapy response. This study demonstrates that overexpression of EGFRvIII in U87MG glioma cells confers resistance to the alkylating agent temozolomide (TMZ), potentially through altered ceramide (Cer) metabolism.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Pharmacology & Pharmacy
Jazlyn P. Borges, Katrina Mekhail, Gregory D. Fairn, Costin N. Antonescu, Benjamin E. Steinberg
Summary: Chronic pain is a major public health issue that is often resistant to conventional analgesics. Recent studies have implicated the epidermal growth factor receptor (EGFR) signaling pathway in chronic pain, suggesting potential therapeutic targets for this devastating condition.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Oncology
Xia Gan, Yonghong Liu, Xueni Wang
Summary: Glioblastomas, a type of brain tumor, have a higher incidence in males compared to females, and this difference may be attributed to the androgen receptor signaling axis. Drug research targeting the androgen receptor for the treatment of glioblastoma has shown that androgen receptor antagonists, in combination with other drugs, can have anti-tumor effects. Additionally, small molecule compounds targeting the androgen receptor have also shown promising results in reducing glioblastoma growth.
CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY
(2023)