• The activity of this kinase first appears in mid-G1 phase, which is controlled by the regulatory subunits including D-type cyclins and members of INK4 family of CDK inhibitors. (cancerindex.org)
  • My research interests are focusing on the activity of tyrosine kinases, targeted inhibitors, effects of ascitic fluid ,and anti-tumour properties of natural food compounds in the progression of advanced ovarian cancer. (otago.ac.nz)
  • Tyrosine kinase inhibitors (TKIs) are frequently used in combined therapy to enhance treatment efficacy and overcome drug resistance. (muni.cz)
  • Lung cancer with epidermal growth factor receptor (EGFR)-activating mutations responds favorably to the EGFR tyrosine kinase inhibitors gefitinib and erlotinib. (aacrjournals.org)
  • Treatments with pertussis-toxin, inhibition of phospholipase C and protein kinase C inhibitors and chelation of free cytosolic calcium did not change the bradykinin-induced inhibition of phosphotyrosine kinase. (nih.gov)
  • The treatment paradigm of AML patients harboring FLT3 mutations (30%) has been modified by the discovery of tyrosine kinase inhibitors. (dovepress.com)
  • Activity of these inhibitors depends on their mechanism of receptor binding (active vs inactive conformation) and efficacy against the FLT3-ITD and -TKD mutations (type 1 inhibitors are active both on FLT3 -ITD and TKD, whereas type 2 inhibitors are active only on FLT3 -ITD). (dovepress.com)
  • Mulitkinase inhibitor that targets several tyrosine kinase inhibitors implicated in tumor growth, pathologic angiogenesis, and metastatic progression. (medscape.com)
  • Covalent inhibitors of Bruton tyrosine kinase (BTK) have transformed the therapy of chronic lymphocytic leukemia (CLL), but continuous therapy has been complicated by the development of resistance. (lu.se)
  • Epidermal growth factor receptor (EGFR) inhibitors are part of an emerging class of anticancer medicines known as "targeted therapy," which target pathways more specific to neoplastic proliferation than traditional chemotherapeutic agents. (medscape.com)
  • There are several different types of EGFRIs, including small molecule tyrosine kinase inhibitors, monoclonal antibodies, and multikinase inhibitors. (medscape.com)
  • Small molecule tyrosine kinase inhibitors, such as gefitinib and erlotinib, selectively bind the adenosine triphosphate (ATP)-binding site of the EGFR tyrosine kinase receptor, inhibiting the receptor's intracellular domain via preventing phosphorylation. (medscape.com)
  • both EGFR and c-Src kinase activities. (123dok.org)
  • This gene encodes a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases. (nih.gov)
  • Although a number of studies have shown that patients with activating mutations in exons 18-21 of the epidermal growth factor receptor (EGFR) gene respond particularly well to gefitinib and erlotinib, a prospective, randomised study was needed to differentiate between the prognostic and predictive value of EGFR mutations. (ersjournals.com)
  • This review considers the current evidence linking biomarker profile to efficacy of epidermal growth factor receptor (EGFR)-targeted therapy in advanced nonsmall cell lung cancer (NSCLC) and the clinical implications of recent findings. (ersjournals.com)
  • Receptor tyrosine kinases including EGFR, HER-2 and c-Met and non receptor tyrosine kinase including Jaks are selectively expressed in primary tissue and metastatic tumour of advanced ovarian cancer cells. (otago.ac.nz)
  • PURPOSE: Vascular endothelial growth factor receptor (VEGFR) and epidermal growth factor receptor (EGFR) play a significant role in glioblastoma angiogenesis and proliferation, making tyrosine kinase (TK) receptors logical targets for treatment. (duke.edu)
  • The small molecule compound, Erlotinib is a receptor tyrosine kinase inhibitor (EGFR antagonist) and belongs to molecular targeted therapy Drugs. (lookchem.com)
  • It can inhibit the phosphorylation reaction through competing with adenosine triphosphate to bind to the catalytic region of the receptor tyrosine kinase, thereby blocking the down-proliferation signaling and inhibiting the activity of the tumor cell ligand-dependent HER-1/EGFR, thus achieving the inhibition of the proliferation of tumor cells. (lookchem.com)
  • Here, we showed that hepatocyte growth factor (HGF), a ligand of MET oncoprotein, induces gefitinib resistance of lung adenocarcinoma cells with EGFR -activating mutations by restoring the phosphatidylinositol 3-kinase/Akt signaling pathway via phosphorylation of MET, but not EGFR or ErbB3. (aacrjournals.org)
  • However, this study, conducted by a team of researchers based at the Division of Biomimetics, Faculty of Dentistry & Graduate School of Medical and Dental Sciences, Niigata University, Japan, highlights the significant involvement of the epidermal growth factor/epidermal growth factor receptor (EGF/EGFR) axis and its downstream signaling cascade, particularly Src/PI3K/Akt/mTOR, in the modulation of oral keratinocyte cell motility and proliferative capacity. (news-medical.net)
  • The epidermal growth factor receptor (EGFR) is expressed in epithelial tissues as well as hair follicles. (medscape.com)
  • In contrast, monoclonal antibodies that target EGFR, such as cetuximab and panitumumab, bind to its extracellular domain and competitively inhibit endogenous ligand binding to the receptor. (medscape.com)
  • There are also combination therapies that affect multiple receptors such as lapatinib (approved for human epidermal growth factor receptor 2-positive [HER2+] breast cancer) and afatinib (approved for non-small cell lung cancer), which inhibit both the EGFR and HER2 receptors, and vandetanib (approved for advanced medullary thyroid cancer), which inhibits EGFR, vascular endothelial growth factor (VEGFR), and rearranged during transfection (RET) activities. (medscape.com)
  • Scholars@Duke publication: Phase I study of AEE788, a novel multitarget inhibitor of ErbB- and VEGF-receptor-family tyrosine kinases, in recurrent glioblastoma patients. (duke.edu)
  • c-FMS inhibitor is a potent, orally active and small-molecule inhibitor of FMS kinase with IC50 value of 0.8 nM. (adooq.com)
  • PLX647 is a highly specific dual FMS/KIT kinase inhibitor with IC50 of 28/16 nM respectively. (adooq.com)
  • cFMS-IN-2 is a FMS kinase inhibitor with an IC50 of 0.024 μM. (adooq.com)
  • BUN60856, also known as cFMS Receptor Inhibitor II, is a cFMS inhibitor. (adooq.com)
  • c-Fms-IN-8 (compound 4a) is a colony stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor, with an IC50 of 9.1 nM. (adooq.com)
  • c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, an kinase inhibitor of FMS (Colony stimulating factor-1 receptor, CSF-1R) with IC50 of 2 nM. (adooq.com)
  • Like sorafenib, lapatinib is a protein kinase inhibitor shown to decrease tumor-causing breast cancer stem cells. (hmdb.ca)
  • Entrectinib is a selective tyrosine kinase inhibitor designed to inhibit the kinase activity of the tropomyosin receptor kinase (TRK) A/B/C and ROS1 proteins. (medscape.com)
  • Imatinib mesylate (Gleevec), a 2-phenylaminopyridine that functions as a tyrosine kinase inhibitor, targets the c-kit domain expressed by some GISTs . (medscape.com)
  • RON is a 180-kDa heterodimeric protein composed of a 40-kDa α-chain and a 150-kDa transmembrane β-chain with intrinsic tyrosine kinase activity. (spandidos-publications.com)
  • Maturation occurs in the cell membrane resulting in a 180-kDa heterodimeric protein composed of a 40-kDa α-chain and a 150-kDa transmembrane β-chain with intrinsic tyrosine kinase activity ( 5 , 6 ). (spandidos-publications.com)
  • and transmembrane receptor protein tyrosine kinase signaling pathway. (nih.gov)
  • Tyrosine kinase of the non-receptor type, involved in the interleukin-2 and interleukin-4 signaling pathway. (lu.se)
  • Amplification of the human epidermal growth factor receptor 2 ( HER2 ) gene and overexpression of the HER2 protein is found in 15%-20% of patients with gastric and gastroesophageal junction cancer. (wjgnet.com)
  • Clinically relevant improvements in survival have been attained by administering targeted therapy to the appropriate patient population: for example, the addition of trastuzumab to standard first-line chemotherapy in patients with human epidermal growth factor receptor-positive (HER2+) metastatic breast cancer 3 . (ersjournals.com)
  • Specifically designed to inhibit tyrosine kinase activity of bcr-abl kinase in GISTs. (medscape.com)
  • We have previously shown that VWF itself regulates angiogenesis, raising the hypothesis that some of the angiogenic activity of VWF may be mediated by its interaction with Angpt-2. (imperial.ac.uk)
  • Integrin engagement by ECM can modulate growth factor signaling pathways, increasing the activity of growth factor RTKs (7, 8) and their downstream intracellular mediators (9, 10). (123dok.org)
  • Recent data suggest that integrin association with RTKs might also protect the latter against the activity of phosphatases (17, 19) and/or ensure the correct subcellular juxtaposition of cytoplasmic tails of dimer-ized growth factor receptors (17). (123dok.org)
  • In particular, drugs targeting receptor tyrosine kinases (RTKs) have been successful. (europa.eu)
  • AXL receptor tyrosine kinase belongs to the TAM subfamily of receptor tyrosine kinases (RTKs) and overexpression has been detected in various cancers. (justia.com)
  • This kinase, as well as CDK4, has been shown to phosphorylate, and thus regulate the activity of, tumor suppressor protein Rb. (cancerindex.org)
  • NK cells contribute to cancer immune surveillance not only by their direct natural cytotoxicity which is triggered rapidly upon stimulation through germline-encoded cell surface receptors, but also by modulating T-cell mediated antitumor immune responses through maintaining the quality of dendritic cells and enhancing the presentation of tumor antigens. (frontiersin.org)
  • When unregulated, members of this family and their receptors are known to be involved in tumor formation. (rndsystems.com)
  • c-Fms-IN-10 has anti-tumor activity. (adooq.com)
  • Distinct roles of the two tumor necrosis factor (TNF) receptors in modulating TNF and lymphotoxin alpha effects. (aaem.pl)
  • Engelmann H, Holtmann H, Brakebusch C, Avni YS, Sarov I, Nophar Y, Hadas E, Leitner O, Wallach D. Antibodies to a soluble form of a tumor necrosis factor (TNF) receptor have TNF-like activity. (aaem.pl)
  • Aderka D, Engelmann H, Maor Y, Brakebusch C, Wallach D. Stabilization of the bioactivity of tumor necrosis factor by its soluble receptors. (aaem.pl)
  • Chegini N. An inverse relation between the expression of tumor necrosis factor alpha (TNF-alpha) and TNF-alpha receptor in human endometrium. (aaem.pl)
  • Onsrud M, Shabana A, Austgulen R, Nustad K. Comparison between soluble tumor necrosis factor receptors and CA125 in peritoneal fluids as a marker for epithelial ovarian cancer. (aaem.pl)
  • In addition to plexins, various other proteins have been implicated either as receptors for semaphorins or as components of the semaphorin receptor complex ( Pasterkamp and Kolodkin, 2003 ). (rupress.org)
  • The present invention relates to antigen-binding proteins, or antigen-binding fragments thereof that bind to a glycan on the AXL receptor tyrosine kinase. (justia.com)
  • The present invention also relates to antigen-binding proteins, or antigen-binding fragment conjugated to a radioisotope or cytotoxin, and wherein said antigen-binding proteins, or antigen-binding fragment is internalised into a cell upon binding to AXL receptor tyrosine kinase. (justia.com)
  • Among the range of proteins shown to co-localize to WPB is angiopoietin-2 (Angpt-2), a ligand of the receptor tyrosine kinase Tie-2. (imperial.ac.uk)
  • Olsson I, Gatanaga T, Gullberg U, Lantz M, Granger GA. Tumour necrosis factor (TNF) binding proteins (soluble TNF receptor forms) with possible roles in inflammation and malignancy. (aaem.pl)
  • Finally, we found that phospho-DARPP-32 inhibited the activity of the focal adhesion kinase (FAK) in MCF-7 breast cancer cells, and that MCF-7 cells expressing phospho-DARPP-32 displayed less filopodia formation. (lu.se)
  • These agents inhibit the signal transduction pathway regulated by receptor tyrosine kinase. (medscape.com)
  • Moreover, Wnt-5a is known to inhibit migration of breast epithelial cells in culture and expression of Wnt-5a potentiates activation of the receptor tyrosine kinase DDR1, a collagen receptor implicated in cell adhesion and migration. (lu.se)
  • Despite the cited progress in this area of research, the molecular mechanisms underlying growth factor receptor activation by integrins remain to be defined. (123dok.org)
  • Despite wealth information of these tyrosine kinase expressions and activation, little is known about the biological activity of tyrosine kinases in ovarian cancer cells are present in ascitic fluid. (otago.ac.nz)
  • This project is investigating the expression and activation of tyrosine kinases in ovarian cancer cells isolated from ascitic fluid. (otago.ac.nz)
  • Nevertheless, ex vivo activation with cytokines can restore cytolytic activity of NK cells against GB, indicating that NK cells have potential for adoptive immunotherapy of GB if potent cytotoxicity can be maintained in vivo . (frontiersin.org)
  • The activation of Src, a non-receptor tyrosine kinase, appeared to transduce signals from various receptors to internal signaling pathways, affecting cellular events such as survival, adhesion, proliferation, and migration. (news-medical.net)
  • GISTs are characterized by expression of the product of the proto-oncogene c-kit and often harbor gain-of-function kit mutations, leading to ligand-independent kinase activation. (medscape.com)
  • Activation of the protein-tyrosine kinase activity of the receptors occurs by ligand-induced dimerization or heterodimerization of PDGF receptor types. (bvsalud.org)
  • Signalling pathways activated downstream of AXL include PI3K-AKT-mTOR, MEKERK, NF-κB, and JAK/STAT. This receptor can also mediate cell aggregation by homophilic binding. (wikipedia.org)
  • This finding challenges previous studies that reported the motogenic and mitogenic activity of these pathways in normal epithelial cells. (news-medical.net)
  • FMS-like tyrosine kinase 3 ( FLT3 ) is one of the most frequently mutated genes in acute myeloid leukemia (AML). (dovepress.com)
  • Approximately 30% of the adult cases harbor an internal tandem duplication ( FLT3 -ITD) and 5- 10% a tyrosine kinase domain (TKD) amino acid substitution ( FLT3-TKD ). (dovepress.com)
  • Among the most mutated driver genes in AML is FMS-like tyrosine kinase 3 ( FLT3 ). (dovepress.com)
  • This kinase is a catalytic subunit of the protein kinase complex that is important for cell cycle G1 phase progression and G1/S transition. (cancerindex.org)
  • The receptors are ligand binding factors of type 1, 2 or 3 and protein-molecules that receive chemical-signals from outside a cell. (gentaur.com)
  • In this sense, am olfactory receptor is a protein-molecule that recognizes and responds to endogenous-chemical signals, chemokinesor cytokines e.g. an acetylcholine-receptor recognizes and responds to its endogenous-ligand, acetylcholine. (gentaur.com)
  • However, it is unclear how the activity of plexin-B1 and its downstream effectors is regulated by its ligand Sema4D. (rupress.org)
  • b ) receptors that associate with other tyrosine kinases, and ( c ) tyrosine-kinase-associated receptors with the ligand-binding subunit membrane anchored by a glycolipid, such as that for ciliary neurotrophic factor. (aspetjournals.org)
  • The AXL protein is characterized by an extracellular structure consisting of two fibronectin type 3-like repeats and two immunoglobulin-like repeats along with its intracellular tyrosine kinase domain. (wikipedia.org)
  • In vivo, tumour cells are simultaneously exposed to signals initiated by a variety of oncogenes, cytokine receptors and adhesion molecules, and it is the integrated signals that determine the cellular phenotype. (europa.eu)
  • Resveratrol shows anti-tumour activities in an in vitro in various tumour types including ovarian cancer. (otago.ac.nz)
  • Opala T, Rzymski P, Wilczak M, Woźniak J. Evaluation of soluble tumour necrosis factor alpha receptors p55 and p75 in ovarian cancer patients. (aaem.pl)
  • Interleukin 35 (IL35) may presumably signal via a complex that includes Tyrosine protein kinase JAK1 (JAK1) and JAK2 associated with Interleukin 6 receptor beta subunit (IL6ST) and Interleukin 12 receptor beta 2 subunit (IL12RB2) (Collison et al. (reactome.org)
  • Pirtobrutinib is a highly selective, noncovalent BTKi with substantial clinical activity in patients whose disease has progressed on covalent BTKi, regardless of BTK mutation status. (lu.se)
  • [ 2 ] They are often CD34 immunoreactive and express tyrosine kinase c-kit (CD117) receptor activity, in contrast to leiomyosarcomas. (medscape.com)
  • 19 normal healthy in- receptor protein (CD117) that is structurally dividuals were recruited as a control group. (who.int)
  • When such chemical-signals couple or bind to a receptor, they cause some form of cellular/tissue-response, e.g. a change in the electrical-activity of a cell. (gentaur.com)
  • Neurotrophins bind two classes of receptors, the receptor tyrosine kinase family of Trk (A, B, and C) receptors and the p75 neurotrophin receptor (NTR). (jneurosci.org)
  • La activación de la actividad proteín-tirosina cinasa de los receptores tiene lugar por dimerización o heterodimerización de los tipos de receptor de PDGF inducida por ligandos. (bvsalud.org)
  • An oral sphingosine 1-phosphate receptor 1 (S1P(1)) antagonist prodrug with efficacy in vivo: discovery, synthesis, and evaluation. (novartis.com)
  • [ 3 ] Mutations in the c-kit receptor are linked to the neoplastic development. (medscape.com)
  • A monoclonal antibody targeting AXL (YW327.6S2) and an AXL decoy receptor (GL2I.T) are currently in preclinical development. (wikipedia.org)
  • After blocking endogenous peroxidase activity and nonspecific protein binding, 1:100 dilution of mouse monoclonal antibody against c-kit human oncoprotein was applied to tissues. (scielo.br)
  • Recent investigations have shown that the RON receptor is expressed in various cell types including epithelial cells (23) and that MSP-mediated effects on epithelial cells are integrin-dependent (23, 24). (123dok.org)
  • Recepteur d'origine nantais (RON) is a receptor tyrosine kinase (RTK) normally expressed at low levels in epithelial cells. (spandidos-publications.com)
  • by normal individuals cause broncho-constriction in Cytokines often have overlapping biological activities, patients with asthma. (cdc.gov)
  • Simultaneous administration of the drugs consistently resulted in synergistic and/or additive activities against the cell lines derived from the most frequent types of pediatric solid tumors. (muni.cz)
  • the change in enzyme activity as a result of the enzyme-antibody-antigen reaction is proportional to the concentration of the antigen and can be measured spectrophotometrically or with the naked eye. (gentaur.com)
  • Such therapy functions through mediating alterations in antigen or receptor function, modulating the immune system or delivering a specific drug that is conjugated to an antibody that targets a specific antigen. (justia.com)
  • In one aspect, there is provided an antigen-binding protein, or an antigen-binding fragment thereof that competes with the antigen binding protein as defined herein for binding to AXL receptor tyrosine kinase. (justia.com)
  • Furthermore, similar to T cells, specific recognition and elimination of cancer cells by NK cells can be markedly enhanced through expression of chimeric antigen receptors (CARs), which provides an opportunity to generate NK-cell therapeutics of defined specificity for cancer immunotherapy. (frontiersin.org)
  • The AXL receptor transduces signals from the extracellular matrix into the cytoplasm by binding growth factors like vitamin K-dependent protein growth-arrest-specific gene 6 (GAS6). (wikipedia.org)
  • AXL is a cell surface receptor tyrosine kinase, part of the TAM family of kinases including TYRO3 and MERTK. (wikipedia.org)
  • The function of activated AXL in normal tissues includes the efficient clearance of apoptotic material and the dampening of TLR-dependent inflammatory responses and natural killer cell activity. (wikipedia.org)
  • As to the basis for their collaboration, integrins and growth factor receptors may form macromolecular complexes on the cell membrane (7, 8, 13, 16 -18). (123dok.org)
  • To understand these factors, I am using three dimensional (3D) cell cultures, chicken embryos and a syngeneic mouse model to investigate the biological activity in ovarian cancer. (otago.ac.nz)
  • We demonstrated that bradykinin (BK), through the B2 receptor, induced a dose-dependent inhibition of mesangial cell proliferation stimulated by fetal calf serum. (nih.gov)
  • Taken together, these data suggest for the first time that, in proliferating rat mesangial cells, B2 receptor stimulation is able to induce, via a pertussis insensitive pathway, the inhibition of tyrosine kinase activity and mesangial cell proliferation. (nih.gov)
  • Specific receptors on cell membranes that react with PLATELET-DERIVED GROWTH FACTOR, its analogs, or antagonists. (bvsalud.org)
  • Using in vitro ibrutinib-resistant models and cells from patients with CLL, we show that pirtobrutinib potently inhibits BTK-mediated functions including B-cell receptor. (lu.se)
  • Using in vitro ibrutinib-resistant models and cells from patients with CLL, we show that pirtobrutinib potently inhibits BTK-mediated functions including B-cell receptor (BCR) signaling, cell viability, and CCL3/CCL4 chemokine production in both BTK wild-type and C481S mutant CLL cells. (lu.se)
  • Furthermore, p75 NTR regulates RhoA activity to mediate filopodial dynamics. (jneurosci.org)
  • BDNF treatment of retinal neurons results in reduced RhoA activity. (jneurosci.org)
  • Growth cone behaviors were not investigated in previous studies, and it is unknown whether neurotrophin-p75 NTR interactions regulate RhoA activity in growth cones. (jneurosci.org)
  • Additionally, we found that neurotrophin binding to p75 NTR reduces RhoA activity. (jneurosci.org)
  • The Abl-related gene (Arg) requires its F-actin-microtubule cross-linking activity to regulate lamellipodial dynamics during fibroblast adhesion. (nih.gov)
  • Tyrosine-protein kinase receptor UFO is an enzyme that in humans is encoded by the AXL gene. (wikipedia.org)
  • Molecular targets acted on by products in development for blood pressure disorders include angiotensin receptors, tyrosine protein kinases and phosphodiesterases. (openpr.com)
  • Proteolytic cleavage of the AXL extracellular domain by the metalloproteinases ADAM10 and ADAM17 can downregulate this signalling activity. (wikipedia.org)
  • This membrane-bound protein has a neuregulin binding domain but not an active kinase domain. (nih.gov)
  • Regulation of MT dynamics via direct binding of an Abl family kinase. (nih.gov)
  • However, it does form heterodimers with other EGF receptor family members which do have kinase activity. (nih.gov)
  • In recent years, a few studies have started to investigate the biological activity of ascitic fluid,which is believed to influence behavior of ovarian cancer cells. (otago.ac.nz)
  • I am interested in the biological activity of resveratrol and its derivatives. (otago.ac.nz)
  • The biological effects of TNF-alpha are mediated by two receptors, p55 and p75. (aaem.pl)