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Gilotrif (afatinib) Research

22:48 EDT 25th May 2018 | BioPortfolio

Design, synthesis and biological evaluation of 1H-1,2,3-Triazole-Linked-1H‑Dibenzob,hxanthenes as Inductors of ROS-Mediated Apoptosis in the Breast Cancer Cell Line MCF-7.

Low molecular weight 1,2,3-triazoles and naphthoquinones are endowed with various types of biological activity, such as against cancer, HIV and bacteria. However, in some cases, the conjugation of these two nuclei considerably increases their biological activities Objective: In this work, we decided to study the synthesis and screening of bis-naphthoquinones and xanthenes tethered to 1,2,3-triazol...

The PDGFRβ/ERK1/2 pathway regulates CDCP1 expression in triple-negative breast cancer.

CDCP1, a transmembrane protein with tumor pro-metastatic activity, was recently identified as a prognostic marker in TNBC, the most aggressive breast cancer subtype still lacking an effective molecular targeted therapy. The mechanisms driving CDCP1 over-expression are not fully understood, although several stimuli derived from tumor microenvironment, such as factors present in Wound Healing Fluids...

Estimated intraoperative blood loss correlates with postoperative cardiopulmonary complications and length of stay in patients undergoing video-assisted thoracoscopic lung cancer lobectomy: a retrospective cohort study.

The purpose of our study was to estimate the influence of estimated intraoperative blood loss (EIBL) on postoperative cardiopulmonary complications (PCCs) in patients undergoing video-assisted thoracoscopic surgery (VATS) lobectomy for non-small-cell lung cancer (NSCLC).

Involvement of the CB cannabinoid receptor in cell growth inhibition and G0/G1 cell cycle arrest via the cannabinoid agonist WIN 55,212-2 in renal cell carcinoma.

The anti-tumor properties of cannabinoids have been investigated in many in vitro and in vivo studies. Many of these anti-tumor effects are mediated via cannabinoid receptor types 1 and 2 (CB and CB), comprising the endocannabinoid system (ECS). In this study, we investigated the ECS based on CB and CB receptor gene and protein expression in renal cell carcinoma (RCC) cell lines. In view of thei...

Radioligand therapy of metastatic castration-resistant prostate cancer: current approaches.

Prostate Cancer is the forth most common type of cancer. Prostate-specific membrane antigen (PSMA) is anchored in the cell membrane of prostate epithelial cells. PSMA is highly expressed on prostate epithelial cells and strongly up-regulated in prostate cancer. Therefore it is an appropriate target for diagnostic and therapy of prostate cancer and its metastases. This article discusses several art...

Association of serum bilirubin level with lung function decline: a Korean community-based cohort study.

Bilirubin has been reported to be associated with respiratory diseases due to its antioxidant action. We aimed to evaluate the relationship between serum bilirubin concentration and annual lung function decline in the Korean general population.

Safety, tolerability, pharmacokinetics, and pharmacodynamics of GLPG1690, a novel autotaxin inhibitor, to treat idiopathic pulmonary fibrosis (FLORA): a phase 2a randomised placebo-controlled trial.

Idiopathic pulmonary fibrosis (IPF) causes irreversible loss of lung function. People with IPF have increased concentrations of autotaxin in lung tissue and lysophosphatidic acid (LPA) in bronchoalveolar lavage fluid and exhaled condensate. GLPG1690 (Galapagos, Mechelen, Belgium) is a novel, potent, selective autotaxin inhibitor with good oral exposure. We explored the effects of GLPG1690 in patie...

Nanobody-antigen conjugates elicit HPV-specific anti-tumor immune responses.

High-risk human papillomavirus-associated cancers express viral oncoproteins (e.g., E6 and E7) that induce and maintain the malignant phenotype. The viral origin of these proteins makes them attractive targets for development of a therapeutic vaccine. Camelid-derived single-domain antibody fragments (nanobodies or VHHs) that recognize cell surface proteins on antigen-presenting cells (APCs) can se...

BET inhibition overcomes receptor tyrosine kinase-mediated cetuximab resistance in HNSCC.

Cetuximab, the FDA-approved anti-EGFR antibody for head and neck squamous cell carcinoma (HNSCC), has displayed limited efficacy due to the emergence of intrinsic and acquired resistance. We and others have demonstrated that cetuximab resistance in HNSCC is driven by alternative receptor tyrosine kinases (RTK) including HER3, MET, and AXL. In an effort to overcome cetuximab resistance and circumve...

PEDF regulates plasticity of a novel lipid-MTOC axis in prostate cancer associated fibroblasts.

Prostate tumors make metabolic adaptations to ensure adequate energy and amplify cell cycle regulators such as centrosomes to sustain their proliferative capacity. It is not known whether cancer associated fibroblasts (CAFs) undergo metabolic re-programming. We postulated that CAFs augment lipid storage and amplify centrosomal or non-centrosomal microtubule organizing centers (MTOCs) through a pig...

Cell Division Cycle 7-Kinase is a negative regulator of cell-mediated collagen degradation.

Although extensive work has delineated many of the mechanisms of extracellular matrix (ECM) production, far less is known about pathways that regulate ECM degradation. This is particularly true of cellular internalization and degradation of matrix, which play an underappreciated role in ECM metabolism and lung fibrosis. For example, genetic perturbation of this pathway leads to exacerbated fibrosi...

Small Molecule Targeted Recruitment of a Nuclease to RNA.

The choreography between RNA synthesis and degradation is a key determinant in biology. Engineered systems such as CRISPR have been developed to rid a cell of RNAs. Here, we show that a small molecule can recruit a nuclease to a specific transcript, triggering its destruction. A small molecule that selectively binds the oncogenic microRNA(miR)-96 hairpin precursor was appended with a short 2'-5' p...

A systematic understanding of signaling by ErbB2 in cancer using phosphoproteomics.

ErbB2 is an important receptor tyrosine kinase and a member of the ErbB family. Although it does not have a specific ligand, it transmits signals downstream by heterodimerization with other receptors in the family. It plays a major role in a variety of cellular responses like proliferation, differentiation, and adhesion. ErbB2 is amplified at the DNA level in breast cancer (20%-30%) and gastric ca...

Nivolumab for the treatment of colorectal cancer.

Despite a variety of therapies for advanced metastatic colorectal cancer being available, the outcomes in this malignancy remain sub-optimal. Immunotherapy has been slow to impact the management of this patient group. Checkpoint inhibitors, such as nivolumab, have had disappointing results when used broadly. However, for the subset of patients with microsatellite unstable colorectal cancer the use...

Phosphatidylinositol 3-kinase β and δ isoforms play key roles in metastasis of prostate cancer DU145 cells.

Metastasis is the main cause of the lethality of prostate cancer. Class I phosphatidylinositol 3-kinases (PI3Ks), which contain 4 isoforms, α, β, δ, and γ, are known to play important roles in cell growth, migration, invasion, and so on. However, the respective role of each PI3K isoform in cancer cell migration and invasion remains unknown. In a study that aimed to elucidate the respective rol...

Colloid Adenocarcinoma of the Lung: CT and PET/CT Findings in Seven Patients.

We aimed to assess CT and F-FDG PET/CT findings of colloid adenocarcinoma of the lung in seven patients.

High-Resolution CT Findings of Obstructive and Restrictive Phenotypes of Chronic Lung Allograft Dysfunction: More Than Just Bronchiolitis Obliterans Syndrome.

The purpose of this article is to review the high-resolution CT characteristics of individual obstructive and restrictive chronic lung allograft dysfunction (CLAD) phenotypes to aid in making accurate diagnoses and guiding treatment.

In vivo evaluation of Reduction-Responsive Alendronate-Hyaluronan-Curcumin Polymer-Drug Conjugates for Targeted Therapy of Bone Metastatic Breast Cancer.

Many cancers such as human breast cancer and lung cancer easily metastasize to bones, leading to the formation of secondary tumors in advanced stage. Based on the CD44-targeted effect of oHA and bone-targeted effect of ALN, we prepared a reduction-responsive, CD44 receptor-targeting and bone-targeting nano-micelle, called CUR-loaded ALN-oHA-S-S-CUR micelles. In this study, we aimed to evaluate the...

Eradication of Established Tumors by Chemically Self-Assembled Nanoring (CSAN) Targeted T-cells.

Our laboratory has developed chemically self-assembled nanorings (CSANs) as prosthetic antigen receptors (PARs) for the non-genetic modification of T-cell surfaces. PARs have been successfully employed in vitro to activate T cells for the selective killing of leukemia cells. However, PAR efficacy has yet to be evaluated in vivo or against solid tumors. Therefore, we developed bispecific PARs that ...

G1/S Transcription Factor Copy Number Is a Growth-Dependent Determinant of Cell Cycle Commitment in Yeast.

To understand how commitment to cell division in late G1 phase (Start) is controlled by growth and nutrients in budding yeast, we determined the absolute concentrations of the G1/S transcription factors SBF (composed of Swi4 and Swi6) and MBF (composed of Mbp1 and Swi6), the transcriptional repressor Whi5, and the G1 cyclins, Cln1 and Cln2, in single live yeast cells using scanning number and brig...

Lung transplantation in tuberculosis (reply).

Current frontline endocrine treatment options for women with hormone receptor-positive, Human Epidermal Growth Factor Receptor 2 (HER2)-negative advanced-stage breast cancer.

Despite the recent advances in breast cancer early detection and awareness, a significant portion of patients present with an advanced-stage disease and more patients will progress to stage IV despite adequate treatment of their initial early-stage disease. Hormone receptor (HR)-positive, Human Epidermal Growth Factor Receptor-2 (HER2)-negative subtype is the commonest among all breast cancer subt...

The role and mechanism of K3.1 channels in human monocyte migration induced by palmitic acid.

Monocyte migration into diseased tissues contributes to the pathogenesis of diseases. Intermediate-conductance Ca-activated K (K3.1) channels play an important role in cell migration. However, the role of K3.1 channels in mediating monocyte migration induced by palmitic acid (PA) is still unclear. Using cultured THP-1 cells and peripheral blood mononuclear cells from healthy subjects, we investiga...

Is there a survival advantage in diagnosing endometrial cancer in asymptomatic postmenopausal patients? An Israeli Gynecology Oncology Group study.

Incidental ultrasonographic findings in asymptomatic postmenopausal women, such as thickened endometrium or polyps, often lead to invasive procedures and to the occasional diagnosis of endometrial cancer. Data supporting a survival advantage of endometrial cancer diagnosed prior to the onset of postmenopausal bleeding (PMB) are lacking.

The Versatile Hippo Pathway in Oral-maxillofacial Development and Bone Remodeling.

The Hipposignaling pathway is implicated in key aspects of cell proliferation, control of organ size, stem cell functions and tumor suppression. Its functions are primarily mediated either through direct effects on transcription factors to influence target gene expression or through crosstalk with other signaling pathways that regulate multiple physiological activities. Studies are revealing Hippo...

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