keyword
MENU ▼
Read by QxMD icon Read
search

Her3

keyword
https://www.readbyqxmd.com/read/28514724/sirna-mediated-inactivation-of-her3-improves-the-antitumour-activity-and-sensitivity-of-gefitinib-in-gastric-cancer-cells
#1
Heng-Heng Yuan, Ying-Nan Yang, Jian-Hua Zhou, Yan-Jing Li, Li-Ying Wang, Jun-Wei Qin, Tao Liu, Zhen-Zhen Li, Qing-Xin Zhou, Xiao-Li Wei, Ting-Ting Zhang, Peng Huang, Wen-Jie Zhang, Lei Liu, Xiao-Xue Du, Yu Han
The human EGFR family consists of four type-1 transmembrane tyrosine kinase receptors: HER1 (EGFR, ErbB1), HER2 (Neu, ErbB2), HER3 (ErbB3), and HER4 (ErbB4). HER3 can dimerize with EGFR, HER2 and even c-Met and likely plays a central role in the response to EGFR-targeted therapy. Because HER3 lacks significant kinase activity and cannot be inhibited by tyrosine kinase inhibitors, neutralizing antibodies and alternative inhibitors of HER3 have been sought as cancer therapeutics. Here, we describe the stable suppression of HER3 mRNA and protein using siRNA...
April 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28507002/neuregulin-1-allosterically-enhances-the-anti-tumor-effects-of-the-non-competing-anti-her3-antibody-9f7-f11-by-increasing-its-binding-to-her3
#2
Christophe Le Clorennec, Hervé Bazin, Olivier Dubreuil, Christel Larbouret, Charline Ogier, Yassamine Lazrek, Veronique Garambois, Marie-Alix Poul, Philippe Mondon, Jean-Marc Barret, Gérard Mathis, Jean-François Prost, André Pèlegrin, Thierry Chardès
Exploratory clinical trials using therapeutic anti-HER3 antibodies strongly suggest that neuregulin (NRG1; HER3 ligand) expression at tumor sites is a predictive biomarker of anti-HER3 antibody efficacy in cancer. We hypothesized that in NRG1-expressing tumors, where the ligand is present before antibody treatment, anti-HER3 antibodies that do not compete with NRG1 for receptor binding have a higher receptor-neutralizing action than antibodies competing with the ligand for binding to HER3. Using time resolved-fluorescence energy transfer (TR-FRET), we demonstrated that in the presence of recombinant NRG1, binding of 9F7-F11 (a non-ligand competing anti-HER3 antibody) to HER3 is increased, whereas that of ligand-competing anti-HER3 antibodies (H4B-121, U3-1287, Ab#6, Mab205...
May 15, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28497320/accelerating-drug-development-by-efficiently-using-emerging-pk-pd-data-from-an-adaptable-entry-into-human-trial-example-of-lumretuzumab
#3
Georgina Meneses-Lorente, Christine McIntyre, Joy C Hsu, Marlene Thomas, Wolfgang Jacob, Celine Adessi, Martin Weisser
PURPOSE: This study aimed at evaluating if pharmacokinetic and pharmacodynamic data from the first few patients treated with an investigational monoclonal antibody in a dose-escalation study can be used to guide the early initiation of potentially more efficacious combination regimens. METHODS: Emerging pharmacokinetic and pharmacodynamic data from the first nine patients treated with lumretuzumab (a glycoengineered anti-HER3 monoclonal antibody) monotherapy at doses from 100 to 400 mg q2w were used along with a pharmacokinetic model that incorporated target-mediated drug disposition to guide the selection of the starting dose for use in combination regimens...
June 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28493933/direct-estrogen-receptor-er-her-family-crosstalk-mediating-sensitivity-to-lumretuzumab-and-pertuzumab-in-er-breast-cancer
#4
Denis Collins, Wolfgang Jacob, Juan Miguel Cejalvo, Maurizio Ceppi, Ian James, Max Hasmann, John Crown, Andrés Cervantes, Martin Weisser, Birgit Bossenmaier
Bidirectional cross talk between members of the human epidermal growth factor family of receptors (HER) and the estrogen receptor (ER) is believed to underlie resistance mechanisms that develop in response to treatment with anti-HER agents and endocrine therapy. We investigated the interaction between HER2, HER3 and the ER in vitro using human embryonic kidney cells transfected with human HER2, HER3, and ERα. We also investigated the additive efficacy of combination regimens consisting of anti-HER3 (lumretuzumab), anti-HER2 (pertuzumab), and endocrine (fulvestrant) therapy in vivo...
2017: PloS One
https://www.readbyqxmd.com/read/28468774/synergy-between-androgen-receptor-antagonism-and-inhibition-of-mtor-and-her2-in-breast-cancer
#5
Michael A Gordon, Nicholas C D'Amato, Haihua Gu, Beatrice Babbs, Julia D Wulfkuhle, Emanuel F Petricoin, Isela Gallagher, Ting Dong, Kathleen Torkko, Bolin Liu, Anthony Elias, Jennifer K Richer
The androgen receptor (AR) is widely expressed in breast cancer (BC) and evidence suggests dependence on AR signaling for growth and survival. AR antagonists such as enzalutamide and seviteronel have shown success in pre-clinical models and clinical trials of prostate cancer, and are currently being evaluated in BC. Reciprocal regulation between AR and the HER2/PI3K/mTOR pathway may contribute to resistance to HER2- and mTOR-targeted therapies; thus, dual inhibition of these pathways may synergistically inhibit BC growth...
May 3, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28460465/functional-characterisation-of-a-novel-ovarian-cancer-cell-line-nuoc-1
#6
Aiste McCormick, Eleanor Earp, Katherine Elliot, Gavin Cuthbert, Rachel O'Donnell, Brian T Wilson, Ruth Sutton, Charlotte Leeson, Huw D Thomas, Helen Blair, Sarah Fordham, John Lunec, James Allan, Richard J Edmondson
BACKGROUND: Cell lines provide a powerful model to study cancer and here we describe a new spontaneously immortalised epithelial ovarian cancer cell line (NUOC-1) derived from the ascites collected at a time of primary debulking surgery for a mixed endometrioid / clear cell / High Grade Serous (HGS) histology. RESULTS: This spontaneously immortalised cell line was found to maintain morphology and epithelial markers throughout long-term culture. NUOC-1 cells grow as an adherent monolayer with a doubling time of 58 hours...
April 18, 2017: Oncotarget
https://www.readbyqxmd.com/read/28454294/mesenchymal-stem-cell-conditioned-medium-promotes-mda-mb-231-cell-migration-and-inhibits-a549-cell-migration-by-regulating-insulin-receptor-and-human-epidermal-growth-factor-receptor-3-phosphorylation
#7
Pengfei Li, Hongwei Zhou, Guohu Di, Jin Liu, Yang Liu, Zhihong Wang, Yinxuan Sun, Haifeng Duan, Junzhong Sun
Various in vitro and in vivo studies have linked mesenchymal stem cells (MSCs) with cancer, but little is known about the effect of MSCs on tumor progression. The present study aimed to analyze the role of the MSCs from different tissues, consisting of human bone marrow, adipose and the umbilical cord tissues, and the heterogeneity of tumors in tumor progression. By collecting the culture supernatants of MSCs as MSC-conditioned media (CMs), the present study found that MSC-CM produces no significant effect on the proliferation of MDA-MB-231 and A549 tumor cells...
March 2017: Oncology Letters
https://www.readbyqxmd.com/read/28454094/proteolytic-cleavages-in-the-extracellular-domain-of-receptor-tyrosine-kinases-by-membrane-associated-serine-proteases
#8
Li-Mei Chen, Karl X Chai
The epithelial extracellular membrane-associated serine proteases matriptase, hepsin, and prostasin are proteolytic modifying enzymes of the extracellular domain (ECD) of the epidermal growth factor receptor (EGFR). Matriptase also cleaves the ECD of the vascular endothelial growth factor receptor 2 (VEGFR2) and the angiopoietin receptor Tie2. In this study we tested the hypothesis that these serine proteases may cleave the ECD of additional receptor tyrosine kinases (RTKs). We co-expressed the proteases in an epithelial cell line with Her2, Her3, Her4, insulin receptor (INSR), insulin-like growth factor I receptor (IGF-1R), the platelet-derived growth factor receptors (PDGFRs) α and β, or nerve growth factor receptor A (TrkA)...
April 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28448604/non-invasive-imaging-assessment-of-the-biodistribution-of-gsk2849330-an-adcc-and-cdc-optimized-anti-her3-mab-and-its-role-in-tumor-macrophage-recruitment-in-human-tumor-bearing-mice
#9
Hasan Alsaid, Tinamarie Skedzielewski, Mary V Rambo, Kristen Hunsinger, Bao Hoang, William Fieles, Edward R Long, James Tunstead, Danielle J Vugts, Matthew Cleveland, Neil Clarke, Christopher Matheny, Beat M Jucker
The purpose of this work was to use various molecular imaging techniques to non-invasively assess GSK2849330 (anti HER3 ADCC and CDC enhanced 'AccretaMab' monoclonal antibody) pharmacokinetics and pharmacodynamics in human xenograft tumor-bearing mice. Immuno-PET biodistribution imaging of radiolabeled 89Zr-GSK2849330 was assessed in mice with HER3 negative (MIA-PaCa-2) and positive (CHL-1) human xenograft tumors. Dose dependency of GSK2849330 disposition was assessed using varying doses of unlabeled GSK2849330 co-injected with 89Zr-GSK2849330...
2017: PloS One
https://www.readbyqxmd.com/read/28440478/overexpression-of-secretory-phospholipase-a2-iia-supports-cancer-stem-cell-phenotype-via-her-erbb-elicited-signaling-in-lung-and-prostate-cancer-cells
#10
Shan Lu, Zhongyun Dong
Resistance to conventional chemotherapies remains a significant clinical challenge in treatment of cancer. The cancer stem cells (CSCs) have properties necessary for tumor initiation, resistance to therapy, and progression. HER/ERBB‑elicited signaling supports CSC properties. Our previous studies revealed that secretory phospholipase A2 group IIa (sPLA2‑IIa) is overexpressed in both prostate and lung cancer cells, leading to an aberrant high level in the interstitial fluid, i.e., tumor microenvironment and blood...
April 19, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28423638/her-inhibitor-promotes-braf-mek-inhibitor-induced-redifferentiation-in-papillary-thyroid-cancer-harboring-brafv600e
#11
Lingxiao Cheng, Yuchen Jin, Min Liu, Maomei Ruan, Libo Chen
Redifferentiation therapy with BRAF/MEK inhibitors to facilitate treatment with radioiodine represents a good choice for radioiodine-refractory differentiated thyroid carcinoma, but recent initial clinical outcomes were modest. MAPK rebound caused by BRAF/MEK inhibitors-induced activation of HER2/HER3 is a resistance mechanism, and combination with HER inhibitor to prevent MAPK rebound may sensitize BRAFV600E-mutant thyroid cancer cells to redifferentiation therapy. To evaluate if inhibiting both BRAF/MEK and HER can produce stronger redifferetiation effect, we tested the effects of BRAF/MEK inhibitor dabrafenib/selumetinib alone or in combination with HER inhibitor lapatinib on the expression and function of iodine- and glucose-handling genes in BRAFV600E-positive BCPAP and K1 cells, using BHP 2-7 cells harboring RET/PTC1 rearrangement as control...
March 21, 2017: Oncotarget
https://www.readbyqxmd.com/read/28421882/inhibition-of-her3-activation-and-tumor-growth-with-a-human-antibody-binding-to-a-conserved-epitope-formed-by-domain-iii-and-iv
#12
Lisa C Schmitt, Alexander Rau, Oliver Seifert, Jonas Honer, Meike Hutt, Simone Schmid, Jonas Zantow, Michael Hust, Stefan Dübel, Monilola A Olayioye, Roland E Kontermann
Human epidermal growth factor receptor 3 (HER3, also known as ErbB3) has emerged as relevant target for antibody-mediated tumor therapy. Here, we describe a novel human antibody, IgG 3-43, recognizing a unique epitope formed by domain III and parts of domain IV of the extracellular region of HER3, conserved between HER3 and mouse ErbB3. An affinity of 11 nM was determined for the monovalent interaction. In the IgG format, the antibody bound recombinant bivalent HER3 with subnanomolar affinity (KD = 220 pM) and HER3-expressing tumor cells with EC50 values in the low picomolar range (27 - 83 pM)...
April 19, 2017: MAbs
https://www.readbyqxmd.com/read/28388240/emerging-treatment-using-tubulin-inhibitors-in-advanced-non-small-cell-lung-cancer
#13
C Hardin, E Shum, A P Singh, R Perez-Soler, H Cheng
Tubulin inhibitors including taxanes and vinca alkaloids are important components of chemotherapy regimens used in advanced non-small cell lung cancer (NSCLC). Despite a treatment paradigm shift due to molecularly-targeted therapies and immunotherapy, a majority of patients will receive chemotherapy during their treatment course. Either used alone or in combination, tubulin inhibitors have demonstrated clinical benefits in different settings of lung cancer management. Areas covered: This review first discusses FDA-approved tubulin inhibitors for NSCLC, such as paclitaxel, docetaxel, vinorelbine, and nab-paclitaxel...
May 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28384967/human-epidermal-growth-factor-receptor-3-mrna-expression-as-a-prognostic-marker-for-invasive-duct-carcinoma-not-otherwise-specified
#14
Ghada Ezat Hammoda, Sally Mohammed El-Hefnawy, Asmaa Gaber Abdou, Rania Abdallah Abdallah
INTRODUCTION: Breast cancer is the most common cancer in women and the Erythroblastosis Oncogene B(ErbB) receptor family holds crucial role in its pathogenesis. Human Epidermal Growth Factor Receptor 3 (HER-3) gene over expression in breast tissue has been associated with aggressive clinical behaviour and bad prognosis. AIM: To evaluate HER-3 mRNA expression level as a prognostic marker for breast cancer and to correlate its level with other established prognostic parameters...
February 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28382169/integration-of-receptor-tyrosine-kinases-determines-sensitivity-to-pi3k%C3%AE-selective-inhibitors-in-breast-cancer
#15
Yi-Chao Xu, Xiang Wang, Yi Chen, Si-Meng Chen, Xin-Ying Yang, Yi-Ming Sun, Mei-Yu Geng, Jian Ding, Ling-Hua Meng
PI3Kα-selective inhibitor BYL719 is currently in phase II/III clinical trial for the treatment of breast cancer, but highly variable response has been observed among patients. We sought to discover predictive biomarker for the efficacy of BYL719 by dissecting the proliferative signaling pathway mediated by PI3K in breast cancer. BYL719 concurrently inhibited the phosphorylation of AKT and ERK in PIK3CA-mutated human breast cancer cells. PI3K-regulated ERK phosphorylation was independent of canonical PDK1/AKT/mTOR pathway, while it was associated with RAF/MEK...
2017: Theranostics
https://www.readbyqxmd.com/read/28377224/piperlongumine-downregulates-the-expression-of-her-family-in-breast-cancer-cells
#16
Hyeon-Ok Jin, Jin-Ah Park, Hyun-Ah Kim, Yoon Hwan Chang, Young Jun Hong, In-Chul Park, Jin Kyung Lee
HER family receptors are frequently deregulated in breast cancer and the deregulation of these receptors is associated with poor prognosis. Thus, these receptors are considered therapeutic targets. In the present study, we found that piperlongumine (PL) downregulates the expression of HER family receptors HER1, HER2, and HER3 in breast cancer cells. Downregulation of these receptors by PL is mediated through the generation of reactive oxygen species (ROS), as N-acetyl-cysteine blocks it. Interestingly, the HER2-overexpressing cell lines BT474 and SkBr3 are somewhat more sensitive to PL than the low HER2-expressing cell line MCF7...
May 13, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28373301/profiling-differential-responses-to-pan-her-inhibition
#17
(no author information available yet)
Findings from the phase II SUMMIT basket trial indicate that among patients with solid cancers harboring HER2/3 mutations, responses to the investigational pan-HER inhibitor neratinib vary by specific alteration and tumor type. Neratinib showed promising single-agent activity in breast, biliary tract, and cervical cancers, but was ineffective against bladder and colorectal cancers; among a small subset of patients with HER3 mutations, no responses were seen.
April 3, 2017: Cancer Discovery
https://www.readbyqxmd.com/read/28369073/her2-signaling-regulates-her2-localization-and-membrane-retention
#18
Jaekwang Jeong, Wonnam Kim, Lark Kyun Kim, Joshua VanHouten, John J Wysolmerski
ErbB2/HER2/Neu is a receptor tyrosine kinase that is overexpressed in 25-30% of human breast cancers, usually associated with amplification of the ERBB2 gene. HER2 has no recognized ligands and heterodimers between HER2 and EGFR (ErbB1/HER1) or HER2 and ErbB3/HER3 are important in breast cancer. Unlike other ErbB family members, HER2 is resistant to internalization and degradation, and remains at the cell surface to signal for prolonged periods after it is activated. Although the mechanisms underlying retention of HER2 at the cell surface are not fully understood, prior studies have shown that, in order to avoid internalization, HER2 must interact with the chaperone, HSP90, and the calcium pump, PMCA2, within specific plasma membrane domains that protrude from the cell surface...
2017: PloS One
https://www.readbyqxmd.com/read/28366103/methods-of-selecting-combination-therapy-for-colorectal-cancer-patients-a-patent-evaluation-of-us20160025730a1
#19
Daniel Plano, Verónica Alcolea, Carmen Sanmartín, Arun K Sharma
Colorectal cancer (CRC) is the fourth most common cancer worldwide. Targeted therapy drugs (TTDs) are a valid treatment, epithelial growth factor receptor (EGFR) inhibitors being one of the most commonly used for CRC patients. However, this treatment is only useful for patients with wild-type KRAS (wtKRAS) and is effective only on about 40 to 60% of this subset due to the high plasticity of ErbB network. Areas covered: The invention proposes the use of ErbB protein levels and ErbB receptor dimer formation as biomarkers for selecting, predicting and monitoring CRC patients showing sensitivity to the action of EGFR inhibitors to benefit from the combination therapy of EGFR and HER2 inhibitors...
May 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28360206/her3-specific-biodistribution-and-tumor-uptake-of-89-zr-msb0010853-visualized-by-real-time-and-non-invasive-pet-imaging
#20
Frank-Jan Warnders, Anton Gt Terwisscha van Scheltinga, Christine Knuehl, Maarten van Roy, Erik F de Vries, Jos G W Kosterink, Elisabeth G E de Vries, Marjolijn N Lub-de Hooge
The human epidermal growth factor receptor (HER)3 is an interesting target for antitumor therapy. For optimal HER3 signaling inhibition a biparatopic Nanobody® construct (MSB0010853) was developed which binds two HER3 epitopes. In addition, MSB0010853 contains a third Nanobody that binds albumin to extend its circulation time. MSB0010853 is cross-reactive with HER3 and albumin of mouse origin. We aimed to gain insight in MSB0010853 biodistribution and tumor uptake by radiolabeling the Nanobody construct with (89)Zr...
March 30, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
keyword
keyword
29571
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"