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Total 64 results found since Jan 2013.
Napsin A is negatively associated with EMT ‑mediated EGFR‑TKI resistance in lung cancer cells.
Napsin A is negatively associated with EMT‑mediated EGFR‑TKI resistance in lung cancer cells.
Mol Med Rep. 2018 May 25;:
Authors: Zhou L, Lv X, Yang J, Zhu Y, Wang Z, Xu T
Abstract
Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR‑TKI) have been used as a standard therapy for patients with lung cancer with EGFR‑activating mutations. Epithelial‑mesenchymal transition (EMT) has been reported to be associated with the development of EGFR‑TKI resistance, which limits the clinical efficacy of EGFR‑TKI. Therefore, investigating the resistance‑associated mechanism is required i...
Source: Molecular Medicine Reports - June 2, 2018 Category: Molecular Biology Tags: Mol Med Rep Source Type: research
P90-RSK as a synthetic lethal target in pancreatic cancer - molecular characterization and therapeutic inhibition
Objectives Pancreatic cancer continues to be the cancer entity with the worst prognosis among all solid tumors associated with a 5-year survival of 5-8%. Combined chemotherapeutic regimes provide only survival benefits for a few months and are not equally suited for all patients with advanced pancreatic cancer. Targeted approaches have largely failed. A marginal clinical benefit was seen for an EGFR inhibitior, erlotinib, in combination with chemotherapy. Using a kinome-wide small-interfering RNA (siRNA)-based loss of function screen, we recently identified the kinase RPS6KA2, also known as p90 ribosomal S6 kinase RSK3, as...
Source: Pancreatology - June 1, 2018 Category: Gastroenterology Authors: Jan Riedel, Nada Milosevic, Jens von Kries, Marc Nazare, Heidi Griesmann, Patrick Michl Tags: 4. Experimental pancreatitis and cell biology II Source Type: research
Targeting autophagy by small molecule inhibitors of vacuolar protein sorting 34 (Vps34) improves the sensitivity of breast cancer cells to Sunitinib
In this study we systematically screened a library of 306 known anti-cancer drugs for their ability to induce autophagy using a cell-based assay. 114 of the drugs were classified as autophagy inducers; for 16 drugs, the cytotoxicity was potentiated by siRNA-mediated knock-down of Atg7 and Vps34. These drugs were further evaluated in breast cancer cell lines for autophagy induction, and two tyrosine kinase inhibitors, Sunitinib and Erlotinib, were selected for further studies.
Source: Cancer Letters - July 25, 2018 Category: Cancer & Oncology Authors: Matheus Dyczynski, Yasmin Yu, Magdalena Otrocka, Santiago Parpal, Tiago Braga, Aine Brigette Henley, Henric Zazzi, Mikael Lerner, Krister Wennerberg, Jenny Viklund, Jessica Martinsson, Dan Grand ér, Angelo De Milito, Katja Pokrovskaja Tamm Tags: Original Articles Source Type: research
YM155 sensitizes non-small cell lung cancer cells to EGFR-tyrosine kinase inhibitors through the mechanism of autophagy induction
In this study, we showed that YM155 markedly enhanced the sensitivity of erlotinib to EGFR-TKI resistant NSCLC cell lines H1650 (EGFR exon 19 deletion and PTEN loss) and A549 (EGFR wild type and KRAS mutation) through inducing autophagy-dependent apoptosis and autophagic cell death. The effects of YM155 combined with erlotinib on apoptosis and autophagy inductions were more obvious than those of YM155 in combination with survivin knockdown by siRNA transfection, suggesting that YM155 induced autophagy and apoptosis in the NSCLC cells partially depend on survivin downregulation. Meanwhile, we found that the AKT/mTOR pathway...
Source: Biochimica et Biophysica Acta (BBA) Molecular Basis of Disease - October 11, 2018 Category: Molecular Biology Source Type: research
Heterogeneity and Plasticity of Human Breast Cancer Cells in Response to Molecularly-Targeted Drugs
Non-responsive subpopulation of tumor cells, and acquired resistance in initially responsive cells are major challenges for cancer therapy with molecularly-targeted drugs. While point mutations are considered the major contributing factor to acquired resistance, in this study we explored the role of heterogeneity and plasticity of selected human breast cancer cell lines (MDA-MB-231, MDA-MB-468, and AU565) in their initial and adjusted response, respectively, to ruxolitinib, everolimus, and erlotinib. After determination of lethal concentration for 50% cell death (LC50), cells were exposed to selected drugs using three diff...
Source: Frontiers in Oncology - October 14, 2019 Category: Cancer & Oncology Source Type: research
GLI1 activation is a key mechanism of erlotinib resistance in human non-small cell lung cancer.
Authors: Dong Z, Wang Y, Ding V, Yan X, Lv Y, Zhong M, Zhu F, Zhao P, He C, Ding F, Shi H
Abstract
Lung cancer is the leading cause of cancer-associated death worldwide. In recent years, the advancement of epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) targeted therapies has provided clinical benefits for lung cancer patients with EGFR mutations. The response to EGFR-TKI varies in patients with lung cancer, and resistance typically develops during the course of the treatment. Therefore, understanding biomarkers which can predict resistance to EGFR-TKI is important. Overexpression of GLI cause...
Source: Oncology Letters - September 1, 2020 Category: Cancer & Oncology Tags: Oncol Lett Source Type: research
Numb-associated kinases are required for SARS-CoV-2 infection and are cellular targets for antiviral strategies
Antiviral Res. 2022 Jun 20:105367. doi: 10.1016/j.antiviral.2022.105367. Online ahead of print.ABSTRACTThe coronavirus disease 2019 (COVID-19) pandemic caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) continues to pose serious threats to global health. We previously reported that AAK1, BIKE and GAK, members of the Numb-associated kinase family, control intracellular trafficking of multiple RNA viruses during viral entry and assembly/egress. Here, using both genetic and pharmacological approaches, we probe the functional relevance of NAKs for SARS-CoV-2 infection. siRNA-mediated depletion of AAK1, ...
Source: Antiviral Research - June 23, 2022 Category: Virology Authors: Marwah Karim Sirle Saul Luca Ghita Malaya Kumar Sahoo Chengjin Ye Nishank Bhalla Chieh Wen Lo Jing Jin Jun-Gyu Park Bel én Martinez-Gualda Michael Patrick East Gary L Johnson Benjamin A Pinsky Luis Martinez-Sobrido Christopher R M Asquith Aarthi Narayana Source Type: research
Heat shock protein 90 inhibitor 17-AAG down-regulates thymidine phosphorylase expression and potentiates the cytotoxic effect of tamoxifen and erlotinib in human lung squamous carcinoma cells
Biochem Pharmacol. 2022 Aug 9:115207. doi: 10.1016/j.bcp.2022.115207. Online ahead of print.ABSTRACTElevated thymidine phosphorylase (TP) levels, a key enzyme in the pyrimidine nucleoside salvage pathway, in cancer cells, are related to a poor prognosis in a variety of cancers. Heat shock protein 90 (Hsp90) is a ubiquitous molecular chaperone that is involved in the stabilization and maturation of many oncogenic proteins. The aim of this study is to elucidate whether Hsp90 inhibitor 17-AAG could enhance tamoxifen- and erlotinib-induced cytotoxicity in nonsmall cell lung cancer (NSCLC) cells via modulating TP expression in ...
Source: Biochemical Pharmacology - August 12, 2022 Category: Drugs & Pharmacology Authors: Jen-Chung Ko Jyh-Cheng Chen Jou-Min Hsieh Pei-Yu Tseng Chen-Shan Chiang Li-Ling Liu Chin-Cheng Chien I-Hsiang Huang Qiao-Zhen Chang Bo-Cheng Mu Yun-Wei Lin Source Type: research
GSE146975 EGFR activity addiction facilitates anti-ERBB based combination treatment of squamous bladder cancer
Contributors : Michael Rose ; Bernd Denecke ; Nadine T GaisaSeries Type : Expression profiling by arrayOrganism :Recent findings suggested a benefit of anti-EGFR therapy for basal-like muscle invasive bladder cancer (MIBC). However, impact on bladder cancer with substantial squamous differentiated (Sq-BLCA) and especially pure squamous cell carcinoma (SCC) remains unknown. Therefore, we comprehensively characterized pure and mixed Sq-BLCA (n=125) on genetic and protein expression level, and performed functional pathway and drug-response analyses with cell line models and isolated primary SCC (p-SCC) cells of the human urin...
Source: GEO: Gene Expression Omnibus - March 12, 2023 Category: Genetics & Stem Cells Tags: Expression profiling by array Source Type: research
The combination of osimertinib with Raf inhibitor overcomes osimertinib resistance induced by KRAS amplification in EGFR-mutated lung cancer cells
Exp Cell Res. 2023 Jul 11:113722. doi: 10.1016/j.yexcr.2023.113722. Online ahead of print.ABSTRACTOsimertinib is a third-generation epidermal growth factor receptor (EGFR)1 tyrosine kinase inhibitor (TKI) approved for the treatment of EGFR-positive patients exhibiting a T790 M resistance mutation after treatment with an earlier generation of EGFR TKIs. However, resistance to osimertinib inevitably develops despite its efficacy, and the resistance mechanisms are complex and not fully understood. We established cell lines with acquired resistance to osimertinib from gefitinib- or erlotinib-resistant NSCLC cells using a dose-...
Source: Experimental Cell Research - July 13, 2023 Category: Cytology Authors: Tae-Gul Lee Hye-Min Kang Seo Yun Kim Hye-Ryoun Kim Cheol Hyeon Kim Source Type: research
