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We describe the design of a set of inhibitors to investigate the relationship between cyclin G associated kinase (GAK) and epidermal growth factor receptor (EGFR) in chordoma bone cancers. These compounds were char-acterized both in vitro and using in cell target engagement assays. The most potent chordoma inhibitors were further characterized in a kinome-wide screen demonstrating narrow spectrum profiles. While we observed a direct correlation between EGFR and anti-proliferative effects on chordoma, GAK inhibition appeared to have only a limited effect.
This article was published in the following journal.
Name: Journal of medicinal chemistry
The clinical evidence for the success of tyrosine kinase inhibitors in combination with microtubule targeting agents prompted us to design and to develop single agents which possess both epidermal gro...
Epidermal growth factor receptor (EGFR) mutation status is strongly correlated with leptomeningeal carcinomatosis in non-small cell lung cancer. Historically, patients were treated with radiotherapy, ...
The potential of the positron-emitting zirconium-89 (Zr) (t = 78.4 h) has been recently reported for immune positron emission tomography (immunoPET) radioimmunoconjugates design. In our work, we...
Pancreatic stem/progenitor cells convert from a proliferative to a differentiated fate passing through proliferation cease to a resting state. However, the molecular mechanisms of cell cycle arrest ar...
Administering epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) tyrosine kinase inhibitor (TKI) combined with chemotherapy in patients with non-small cell lung cancer (NSCLC) is a ...
This trial was to explore whether intravenous vitamin C can prolong resistance time of Tyrosine Kinase Inhibitor(TKI) on lung adenocarcinoma patients with Epidermal Growth Factor Receptor(...
In this trial, treatment efficacy and safety of retreatment with 1st generation epidermal growth factor receptor(EGFR) tyrosine kinase inhibitor(TKI)s(Gefitinib/Erlotinib), will be assesse...
RATIONALE: Studying samples of blood and urine in the laboratory from patients with cancer receiving epidermal growth factor receptor inhibitors may help doctors understand the effect of e...
Two thirds or more of breast cancers are dependent on estrogen for growth. We use a number of estrogen-blocking medicines for treatment of metastatic breast cancer. The treatment respons...
This study is conducted to explore the safety and efficacy of anlotinib, a tyrosine kinase inhibitors of Vascular Endothelial Growth Factor Receptor 2（VEGFR）、FGFR（Fibroblast Growth ...
A cell surface receptor involved in regulation of cell growth and differentiation. It is specific for EPIDERMAL GROWTH FACTOR and EGF related peptides including TRANSFORMING GROWTH FACTOR ALPHA, amphiregulin, and heparin-binding EGF-like growth factor. The binding of ligand to the receptor causes activation of its intrinsic tyrosine kinase activity and rapid internalization of the receptor-ligand complex into the cell.
A fibroblast growth factor receptor with specificity for FIBROBLAST GROWTH FACTORS; HEPARAN SULFATE PROTEOGLYCAN; and NEURONAL CELL ADHESION MOLECULES. Several variants of the receptor exist due to multiple ALTERNATIVE SPLICING of its mRNA. Fibroblast growth factor receptor 1 is a tyrosine kinase that transmits signals through the MAP KINASE SIGNALING SYSTEM.
A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. EPIDERMAL GROWTH FACTOR exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and epithelial cells.
A cell surface protein-tyrosine kinase receptor that is specific for NEUREGULINS. It has extensive homology to and can heterodimerize with the EGF Receptor (RECEPTOR, EPIDERMAL GROWTH FACTOR) and the erbB-2 receptor (RECEPTOR, ERBB-2). Overexpression of the erbB-3 receptor is associated with tumorigenesis.
A cell surface protein-tyrosine kinase receptor that is found to be overexpressed in a significant number of adenocarcinomas. It has extensive homology to and can heterodimerize with the EGF receptor (RECEPTOR, EPIDERMAL GROWTH FACTOR), the erbB-3 receptor (RECEPTOR, ERBB-3) and the erbB-4 receptor. Activation of the erbB-2 receptor occurs during heterodimer formation with a ligand-bound erbB receptor family members.
Osteoporosis is a disease in which the bones become extremely porous, are subject to fracture, and heal slowly, occurring especially in women following menopause and often leading to curvature of the spine from vertebral collapse. Follow and track&n...
Immunoassay - ELISA
Immunoassays are quick and accurate tests to detect specific molecules. Immunoassays rely on an antibody to bind to the specific structure of a molecule. Antibodies are proteins generated by animals in response to the invasion of a foreign molecule (anti...