• The platelet-derived growth factor receptor (PDGFR) has an important role in tumorigenesis and tumor progression. (nih.gov)
  • Platelet-derived growth factor receptor β (PDGFRβ) and platelet-derived growth factor receptor α (PDGFRα) have previously been recognized as markers of cells involved in muscle fibroadipogenesis. (nih.gov)
  • Here we report a prospective cohort study of extremely preterm neonates wherein infants diagnosed with severe BPD expressed increased airway miR-219-5p and decreased platelet derived growth factor receptor alpha (PDGFR-α), a target of mir-219-5p and a key regulator of alveolarization, compared to post-conception age-matched term infants. (biomedcentral.com)
  • PDGF-AA binds only to PDGFR-αα, while PDGF-BB is the only PDGF that can bind all three receptor combinations with high affinity. (wikipedia.org)
  • Expression of both receptors and each of the four PDGFs is under independent control, giving the PDGF/PDGFR system a high flexibility. (wikipedia.org)
  • PDGFR alpha is membrane protein, so enrichment of membrane could help increasing the detection level of PDGFR alpha. (abcam.com)
  • 15. The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders. (nih.gov)
  • 16. Platelet-derived growth factor receptor/platelet-derived growth factor (PDGFR/PDGF) system is a prognostic and treatment response biomarker with multifarious therapeutic targets in cancers. (nih.gov)
  • Lartruvo is a platelet-derived growth factor receptor alpha (PDGFR-α) blocking antibody that specifically binds PDGFR-α and prevents receptor activation. (pharmaphorum.com)
  • the platelet derived growth factor receptor alpha (PDGFRα), KIT, and RET. (drugbank.com)
  • Platelet-derived growth factor receptor-β (PDGFR-β) is highly expressed on EWS cells. (tau.ac.il)
  • Specific PDGFR-β silencing in EWS cells enhanced the effects of TRAIL, possibly through an increase in the expression of death receptors 4 and 5. (tau.ac.il)
  • The PDGFRA gene provides instructions for making a protein called platelet-derived growth factor receptor alpha (PDGFRA), which is part of a family of proteins called receptor tyrosine kinases (RTKs). (nih.gov)
  • The PDGFRA protein is found in the cell membrane of certain cell types where a specific protein, called platelet-derived growth factor, attaches (binds) to it. (nih.gov)
  • The signaling pathways stimulated by the PDGFRA protein control many important cellular processes such as cell growth and division (proliferation) and cell survival. (nih.gov)
  • However, unlike the normal PDGFRA protein, the fusion protein does not require binding of the platelet-derived growth factor protein to be activated. (nih.gov)
  • When the FIP1L1-PDGFRA fusion gene mutation or point mutations in the PDGFRA gene occur in early blood cells, the growth of eosinophils (and occasionally other blood cells) is poorly controlled, leading to PDGFRA -associated chronic eosinophilic leukemia. (nih.gov)
  • PDGFRA gene mutations associated with GISTs create a protein that no longer requires binding of the platelet-derived growth factor protein to be activated. (nih.gov)
  • Today, the U.S. Food and Drug Administration approved Ayvakit (avapritinib) for the treatment of adults with unresectable (unable to be removed with surgery) or metastatic (when cancer cells spread to other parts of the body) gastrointestinal stromal tumor (GIST) - a type of tumor that occurs in the gastrointestinal tract, most commonly in the stomach or small intestine - harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation. (fda.gov)
  • Another tyrosine kinase mutation that is occasionally seen in KIT mutation-negative GIST tumours is the platelet-derived growth factor receptor alpha (PDGFRA). (rgare.com)
  • SNPs in the platelet-derived growth factor receptor (PDGFRA) and integrins were also selected based on their role in binding gB. (biomedcentral.com)
  • Avapritinib, another tyrosine kinase inhibitor, should be used as first-line therapy for patients with a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations. (msdmanuals.com)
  • Mus musculus platelet derived growth factor receptor, alpha polypeptide (Pdgfra), transcript variant 4, mRNA. (mousebrain.org)
  • The FDA approved avapritinib (Ayvakit, Blueprint Medicines Corp) on 1/9/20 for the treatment of unresectable or metastatic gastrointestinal stromal tumors (GIST) that harbor a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation. (prescriberight.com)
  • J. Merla and S. Goel, "Novel Drugs Targeting the Epidermal Growth Factor Receptor and Its Downstream Pathways in the Treatment of Colorectal Cancer: A Systematic Review," Chemotherapy Research and Practice, Vol. 1, 2012, pp. 225-235. (scirp.org)
  • Nickel nanoparticles enhance platelet-derived growth factor-induced chemokine expression by mesothelial cells via prolonged mitogen-activated protein kinase activation. (nih.gov)
  • NiNPs prolonged PDGF-induced phosphorylation of the mitogen-activated protein kinase family termed extracellular signal-regulated kinases (ERK)-1 and -2 for up to 24 hours, and NiNPs also synergistically increased PDGF-induced hypoxia-inducible factor (HIF)-1ýý protein levels in NRM2 cells. (nih.gov)
  • Description: A sandwich quantitative ELISA assay kit for detection of Human Platelet Derived Growth Factor Receptor Beta (PDGFRb) in samples from tissue homogenates, cell lysates or other biological fluids. (clinical-trial-logistics.com)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human Platelet Derived Growth Factor Receptor Beta (PDGFRb) in tissue homogenates, cell lysates and other biological fluids. (clinical-trial-logistics.com)
  • Description: Enzyme-linked immunosorbent assay based on the Double-antibody Sandwich method for detection of Human Platelet Derived Growth Factor Receptor Beta (PDGFRb) in samples from tissue homogenates, cell lysates and other biological fluids with no significant corss-reactivity with analogues from other species. (clinical-trial-logistics.com)
  • Stimulation with TGF-beta 1 revealed decreased PDGF alpha-receptor mRNA expression in normal mesothelial cells. (nih.gov)
  • The combination of imatinib mesylate and TRAIL significantly inhibited the growth of primary tumors and decreased the incidence of spontaneous EWS pulmonary metastasis compared with either drug alone. (tau.ac.il)
  • Gastrointestinal stromal tumors are tumors of the gastrointestinal tract derived from mesenchymal precursor cells in the gut wall. (msdmanuals.com)
  • Gastrointestinal stromal tumors are KIT-expressing and KIT (tyrosine kinase receptor - CD117)-signaling driven mesenchymal tumors. (biomedcentral.com)
  • Platelet-derived growth factor receptors (PDGF-R) are cell surface tyrosine kinase receptors for members of the platelet-derived growth factor (PDGF) family. (wikipedia.org)
  • The PDGFs bind to the protein tyrosine kinase receptors PDGF receptor-α and -β. (wikipedia.org)
  • The extracellular region of the receptor consists of five immunoglobulin-like domains while the intracellular part is a tyrosine kinase domain. (wikipedia.org)
  • Kinase activation is visualized as tyrosine phosphorylation of the receptor molecules, which occurs between the dimerized receptor molecules (transphosphorylation). (wikipedia.org)
  • In conjunction with dimerization and kinase activation, the receptor molecules undergo conformational changes, which allow a basal kinase activity to phosphorylate a critical tyrosine residue, thereby "unlocking" the kinase, leading to full enzymatic activity directed toward other tyrosine residues in the receptor molecules as well as other substrates for the kinase. (wikipedia.org)
  • Tyrosine phosphorylation sites in growth factor receptors serve two major purposes-to control the state of activity of the kinase and to create binding sites for downstream signal transduction molecules, which in many cases also are substrates for the kinase. (wikipedia.org)
  • The second part of the tyrosine kinase domain in the PDGFβ receptor is phosphorylated at Tyr-857, and mutant receptors carrying phenylalanine at this position have reduced kinase activity. (wikipedia.org)
  • Sites of tyrosine phosphorylation involved in binding signal transduction molecules have been identified in the juxtamembrane domain, the kinase insert, and in the C-terminal tail in the PDGFβ receptor. (wikipedia.org)
  • RAHWAY, N.J. & NUTLEY, N.J.--(BUSINESS WIRE)-- Merck (NYSE: MRK), known as MSD outside of the United States and Canada, and Eisai today provided updates on two Phase 3 trials, LEAP-003 and LEAP-017 investigating KEYTRUDA, Merck's anti-PD-1 therapy, plus LENVIMA, the orally available multiple receptor tyrosine kinase inhibitor discovered by Eisai. (merck.com)
  • 1989) "Mutations of the Platelet-Derived Growth Factor Receptor That Cause a Loss of Ligand-Induced Conformational Change, Subtle Changes in Kinase Activity, and Impaired Ability To Stimulate DNA Synthesis" Mol. (everypatent.com)
  • Lenvatinib is a receptor tyrosine kinase inhibitor used for the treatment of metastatic thyroid cancer, advanced renal cell carcinoma in combination with everolimus, and unresectable hepatocellular carcinoma. (drugbank.com)
  • Lenvatinib is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). (drugbank.com)
  • Specific SNPs in TLR7 and IKBKE (inhibitor of nuclear factor kappa-B kinase subunit epsilon) were associated with antibody responses to gB vaccine. (biomedcentral.com)
  • Activation of Neu (ErbB-2) mediated by disulfide bond-induced dimerization reveals a receptor tyrosine kinase dimer interface. (xenbase.org)
  • A stereochemical model for tyrosine kinase receptor activation. (xenbase.org)
  • Our recent mutagenesis screening of the medaka identified headfish ( hdf ), a null mutant for fgf receptor 1 ( fgfr1 ),which fails to develop structures in the trunk and tail. (biologists.com)
  • Despite its crucial role in early development, the functions of Fgfr1-mediated signaling have not yet been well characterized due to the complexity of the underlying ligand-receptor interactions. (biologists.com)
  • A PDGF receptor that binds specifically to both PDGF-A chains and PDGF-B chains. (bvsalud.org)
  • In this paper we studied regulation of this differential PDGF receptor mRNA expression. (nih.gov)
  • Transforming growth factor beta-1 (TGF-beta 1), which is being produced in active form by mesothelial cells was evaluated for its potential role in regulation of the differential PDGF receptor expression in these cells. (nih.gov)
  • Although the TGF-beta 1 effect cannot entirely explain the differential PDGF receptor expression pattern, TGF-beta 1 may nevertheless play a role in downregulation of an (already) low PDGF alpha-receptor mRNA level in malignant mesothelioma cell lines. (nih.gov)
  • 2. The PDGF receptor alpha subunit activates p21ras and triggers DNA synthesis without interacting with rasGAP. (nih.gov)
  • 11. Increased mitogenicity of an alphabeta heterodimeric PDGF receptor complex correlates with lack of RasGAP binding. (nih.gov)
  • 1988), "A Common PDGF Receptor is Activated by Homodimeric A and B Forms of PDGF" Science 240:1532-1534. (everypatent.com)
  • 1988) "Two Classes of PDGF Receptor Recognize Different Isoforms of PDGF" Science 240:1529-1531. (everypatent.com)
  • 1988) "cDNA Cloning and Expression of a Human Platelet-Derived Growth Factor (PDGF) Receptor Specific for B-Chain-Containing PDGF Molecules" Mol. (everypatent.com)
  • TrkA immunoglobulin-like ligand binding domains inhibit spontaneous activation of the receptor. (xenbase.org)
  • Platelet-derived growth factors (PDGFs) are known to be associated with tumor growth and angiogenesis through their activation of the receptor tyrosine kinases, PDGF receptors alpha and beta. (scirp.org)
  • Extracellular region domain structures are identified and modifications and combinatorial rearrangements of the receptor segments are provided. (everypatent.com)
  • 1988), "Structural and Functional Model of the Platelet Derived Growth Factor Receptor Extracellular Domain," Journal of Cellular Biochemistry, 12:98. (everypatent.com)
  • We suggest that OC regulates prostate cancer growth depending on the γ-carboxylation, in part by triggering reduced phosphorylation of receptor tyrosine kinases. (jcancer.org)
  • Application of NGF to TrkA receptor-expressing oocytes promoted tyrosine phosphorylation and activated an oscillating transmembrane inward current, indicating that the TrkA receptors were functional. (xenbase.org)
  • The appearance of these particles in the plasma membrane correlated with responsiveness to NGF as detected by electrophysiological analysis and receptor phosphorylation, indicating that these novel P-face particles were TrkA receptors. (xenbase.org)
  • PDGF subunits -A and -B are important factors regulating cell proliferation, cellular differentiation, cell growth, development and many diseases including cancer. (wikipedia.org)
  • 1988) "Platelet-Derived Growth Factor Receptors Expressed by cDNA Transfection Couple to a Diverse Group of Cellular Responses Associated with Cell Proliferation" J. Biol. (everypatent.com)
  • Williams (1988) "Stimulation of Paracrine and Autocrine Pathways of Cell Proliferation by Platelet-Derived Growth Factor" Clinical Research 36:5-10. (everypatent.com)
  • Different external stimuli such as inflammation, embryonic development or differentiation modulate cellular receptor expression allowing binding of some PDGFs but not others. (wikipedia.org)
  • Nerve growth factor ( NGF ) promotes neuronal survival and differentiation by activating TrkA receptors. (xenbase.org)
  • In earlier studies we showed that the expression of patterns of platelet-derived growth factor (PDGF) alpha- and beta-receptors differ between normal and malignant mesothelial cell lines. (nih.gov)
  • However, the fact that PDGF alpha-receptor mRNA could not be detected by Northern blot analysis, even after cycloheximide treatment, suggests a difference in steady-state PDGF alpha-receptor mRNA expression levels between normal and malignant mesothelial cell lines, which is likely to be caused by a post-transcriptional mechanism. (nih.gov)
  • In the majority of malignant mesothelioma cell lines clear PDGF beta-receptor mRNA expression was seen. (nih.gov)
  • 9. Expression of platelet-derived growth factor-beta receptors on human fibroblasts. (nih.gov)
  • 1988), "Expression and Characterization of the Extracytoplasmic Portion of the Mouse Platelet Derived Growth Factor Receptor," Journal of Cellular Biochemistry, 12:110. (everypatent.com)
  • 1988) "Cloning and expression of a cDNA coding for the human platelet-derived growth factor receptor: Evidence for more than one receptor class" Proc. (everypatent.com)
  • Expression of death receptors was measured by fluorescence-activated cell-sorting (FACS) analysis, and caspase 8 activity was evaluated by Western blot analysis. (tau.ac.il)
  • In our experiments, platelet-derived growth factor B (PDGF-B) retention motif knockout (PDGF-B ret/ret ) mice and adeno-associated virus PDGF-B were employed to show the involvement of pericyte deficiency and PDGF-B expression. (biomedcentral.com)
  • S. Yamauchi, S. Iida, M. Ishiguro, T. Ishikawa, H. Uetake and K. Sugihara, "Clinical Significance of Platelet-Derived Growth Factor-C Expression in Colorectal Cancer," Journal of Cancer Therapy , Vol. 5 No. 1, 2014, pp. 11-20. (scirp.org)
  • 5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyro. (idrblab.net)
  • K. Forsberg, I. Valyi-Nagy, C. H. Heldin, M. Herlyn and B. Westermark, "Platelet-Derived Growth Factor (PDGF) in Oncogenesis: Development of a Vascular Connective Tissue Stroma in Xenotransplanted Human Melanoma Producing PDGF-BB," Proceedings of the National Academy of Sciences of the United States of America, Vol. 90, 1993, pp. 393-397. (scirp.org)
  • Normal mesothelial cells predominantly express PDGF alpha-receptor mRNA and protein, whereas most malignant mesothelioma cell lines produce PDGF beta-receptor mRNA and protein. (nih.gov)
  • In normal mesothelial cells a half-life of more than 6 h was observed for PDGF alpha-receptor mRNA. (nih.gov)
  • In contrast, hardly any PDGF beta-receptor transcription was observed in run off assays in normal mesothelial cells, suggesting that differences in beta-receptor transcriptional initiation most probably account for the inability to clearly detect PDGF beta-receptor transcripts in these cells. (nih.gov)
  • Such an analysis is of importance in view of the suggested PDGF autocrine activity involving the PDGF beta-receptor mesothelioma cells. (nih.gov)
  • The results obtained in this study demonstrate that malignant mesothelioma cell lines are not only capable of PDGF beta-receptor transcription but of alpha-receptor transcription as well, as evidenced from run off analysis and RT-PCR using alpha-receptor specific primers. (nih.gov)
  • The half-life of the PDGF beta-receptor transcript was at least 6 h in these cells. (nih.gov)
  • The effect on PDGF beta-receptor mRNA in the malignant mesothelioma cell lines was variable. (nih.gov)
  • 3. PDGF-D is a specific, protease-activated ligand for the PDGF beta-receptor. (nih.gov)
  • 1988) "Different effects of homo-and heterodimers of platelet-derived growth factor A and B chains on human and mouse fibroblasts" EMBO J. 7:3727-3735. (everypatent.com)
  • In response to cytokines and growth factors, STAT family members are phosphorylated by the receptor associated kinases, and then form homo- or heterodimers that translocate to the cell nucleus where they act as transcription activators. (ximbio.com)
  • 19. Structural and functional aspects of the receptors for platelet-derived growth factor. (nih.gov)
  • 1986) "PDGF receptors: Structural and Functional Studies" Miami Winter Symposium 1986. (everypatent.com)
  • To study this process, we expressed TrkA receptors in Xenopus laevis oocytes and analyzed their response to NGF by using a combination of functional, biochemical, and structural approaches. (xenbase.org)
  • Structural and functional properties of the TRK family of neurotrophin receptors. (xenbase.org)
  • Mature PDGF dimers bind and induce the homo- or hetero-dimerization of two receptor tyrosine kinases (PDGF R alpha and R beta). (rndsystems.com)
  • Similar to other receptor tyrosine kinases, ligand-induced dimerization is thought to be required for TrkA receptor activation. (xenbase.org)
  • Demonstration of epidermal growth factor-induced receptor dimerization in living cells using a chemical covalent cross-linking agent. (xenbase.org)
  • A new case of Carney triad: gastrointestinal stromal tumours and leiomyoma of the oesophagus do not show activating mutations of KIT and platelet-derived growth factor receptor alpha. (medscape.com)
  • Tumor-Driven Paracrine Platelet-Derived Growth Factor Receptor Alpha Signaling Is a Key Determinant of Stromal Cell Recruitment in a Model of Human Lung Carcinoma," Clinical Cancer Research, Vol. 12, 2006, pp. 2676-2688. (scirp.org)
  • After demyelination, oligodendrocytes derived from these newly-formed progenitors provide functional remyelination, restoring normal conduction. (elifesciences.org)
  • METHODS: The effect of combined imatinib mesylate (Gleevec) and TRAIL on EWS cell growth and apoptosis was tested in vitro. (tau.ac.il)
  • An orthotopic human xenograft model of EWS growth and spontaneous metastasis in nude mice was used to assess the in vivo affect of combined imatinib mesylate and TRAIL. (tau.ac.il)
  • These outcomes were accompanied by higher expressions of self-renewal genes or proteins or both, including OCT4, SOX2, NANOG, and cytokine receptor IL6ST, as well as pluripotency and the cell fate regulator cyclin D1. (nih.gov)
  • Regulation of growth cone morphology by nerve growth factor: a comparative study by scanning electron microscopy. (xenbase.org)
  • These results indicate that in Xenopus oocytes, NGF activates signaling via pre-formed TrkA receptor oligomers. (xenbase.org)
  • These growth factors are mitogens for cells of mesenchymal origin. (caslab.com)
  • Moreover, the neural crest (NC)-mesenchymal ectoderm-derived component contributes to from the corneal stroma and endothelium, ciliary body, and melanocytes [ 7 ]. (biomedcentral.com)
  • The ligand-binding sites of the receptors are located to the three first immunoglobulin-like domains. (wikipedia.org)
  • Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) induces apoptosis in EWS cells in vitro. (tau.ac.il)
  • In turn, MAPK10/JNK3 phosphorylates a number of transcription factors, primarily components of AP-1 such as JUN and ATF2 and thus regulates AP-1 transcriptional activity. (idrblab.net)
  • The signals ultimately converge in the nucleus, influencing transcription of oncogenic proteins including, but not limited to, NF-κB), hypoxia-induced factor 1 alpha unit (HIF1α), TGFβ, VEGF, and FGF. (aacrjournals.org)
  • Interestingly, the host hybrid fish recovered their fertility and produced donor-derived mutant progeny. (biologists.com)
  • Nerve growth factor signals via preexisting TrkA receptor oligomers. (xenbase.org)
  • TrkA receptor protein was detected in the membrane fraction of oocytes injected with TrkA receptor cRNA, but not in uninjected or mock-injected oocytes. (xenbase.org)
  • The dimensions of these particles (8.6 x 10 nm) were too large to be accounted for by TrkA monomers, suggesting the formation of TrkA receptor oligomers. (xenbase.org)
  • Application of NGF did not lead to a discernible change in the size or shape of these TrkA receptor particles during an active response. (xenbase.org)
  • TrkA cross-linking mimics neuronal responses to nerve growth factor. (xenbase.org)
  • 14. Biology of platelet-derived growth factors in development. (nih.gov)