tyrphostins

Summary

Summary: A family of synthetic protein tyrosine kinase inhibitors. They selectively inhibit receptor autophosphorylation and are used to study receptor function.

Top Publications

  1. ncbi Inhibition of STAT3 signaling induces apoptosis and decreases survivin expression in primary effusion lymphoma
    Yoshiyasu Aoki
    Experimental Transplantation and Immunology Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA
    Blood 101:1535-42. 2003
  2. ncbi Signal transducer and activator of transcription 3 (STAT3) activation in prostate cancer: Direct STAT3 inhibition induces apoptosis in prostate cancer lines
    Beverly E Barton
    Department of Surgery, New Jersey Medical School, University of Medicine and Dentistry of New Jersey, Newark, NJ 07103, USA
    Mol Cancer Ther 3:11-20. 2004
  3. ncbi Ischaemic postconditioning protects against reperfusion injury via the SAFE pathway
    Lydia Lacerda
    Hatter Cardiovascular Research Institute, Cardioprotection Group, Department of Medicine, Faculty of Health Sciences, University of Cape Town, Observatory 7925, Cape Town, South Africa
    Cardiovasc Res 84:201-8. 2009
  4. ncbi Insulin-like growth factor receptor I mediates resistance to anti-epidermal growth factor receptor therapy in primary human glioblastoma cells through continued activation of phosphoinositide 3-kinase signaling
    Arnab Chakravarti
    Department of Radiation Oncology, Massachusetts General Hospital Harvard Medical School, Charlestown, Massachusetts 02129, USA
    Cancer Res 62:200-7. 2002
  5. pmc A novel inhibitor of signal transducers and activators of transcription 3 activation is efficacious against established central nervous system melanoma and inhibits regulatory T cells
    Ling Yuan Kong
    Department of Neurosurgery, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Clin Cancer Res 14:5759-68. 2008
  6. ncbi Tyrphostins and other tyrosine kinase inhibitors
    Alexander Levitzki
    The Silberman Institute for Life Sciences, Department of Biological Chemistry, The Hebrew University, Givat Ram Campus, Jerusalem 91904, Israel
    Annu Rev Biochem 75:93-109. 2006
  7. ncbi Tyrphostin A23 inhibits internalization of the transferrin receptor by perturbing the interaction between tyrosine motifs and the medium chain subunit of the AP-2 adaptor complex
    David N Banbury
    Department of Biochemistry, School of Medical Sciences, University of Bristol, Bristol BS8 1TD, United Kingdom
    J Biol Chem 278:12022-8. 2003
  8. ncbi Inhibition of HER2/neu (erbB-2) and mitogen-activated protein kinases enhances tamoxifen action against HER2-overexpressing, tamoxifen-resistant breast cancer cells
    H Kurokawa
    Department of Medicine, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    Cancer Res 60:5887-94. 2000
  9. pmc Jak2 inhibition deactivates Lyn kinase through the SET-PP2A-SHP1 pathway, causing apoptosis in drug-resistant cells from chronic myelogenous leukemia patients
    A K Samanta
    Department of Molecular Pathology, University of Texas MD Anderson Cancer Center, Houston, TX 77054, USA
    Oncogene 28:1669-81. 2009
  10. pmc AG490 influences UCN-01-induced cytotoxicity in glioma cells in a p53-dependent fashion, correlating with effects on BAX cleavage and BAD phosphorylation
    Esther P Jane
    Department of Neurosurgery, Children s Hospital of Pittsburgh, University of Pittsburgh School of Medicine, Pittsburgh, PA 15213, USA
    Cancer Lett 257:36-46. 2007

Detail Information

Publications224 found, 100 shown here

  1. ncbi Inhibition of STAT3 signaling induces apoptosis and decreases survivin expression in primary effusion lymphoma
    Yoshiyasu Aoki
    Experimental Transplantation and Immunology Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA
    Blood 101:1535-42. 2003
    ..Since constitutive STAT3 activation and survivin expression have been widely documented in different types of cancers, their linkage may extend to many malignancies and be critical to their pathogenesis...
  2. ncbi Signal transducer and activator of transcription 3 (STAT3) activation in prostate cancer: Direct STAT3 inhibition induces apoptosis in prostate cancer lines
    Beverly E Barton
    Department of Surgery, New Jersey Medical School, University of Medicine and Dentistry of New Jersey, Newark, NJ 07103, USA
    Mol Cancer Ther 3:11-20. 2004
    ....
  3. ncbi Ischaemic postconditioning protects against reperfusion injury via the SAFE pathway
    Lydia Lacerda
    Hatter Cardiovascular Research Institute, Cardioprotection Group, Department of Medicine, Faculty of Health Sciences, University of Cape Town, Observatory 7925, Cape Town, South Africa
    Cardiovasc Res 84:201-8. 2009
    ....
  4. ncbi Insulin-like growth factor receptor I mediates resistance to anti-epidermal growth factor receptor therapy in primary human glioblastoma cells through continued activation of phosphoinositide 3-kinase signaling
    Arnab Chakravarti
    Department of Radiation Oncology, Massachusetts General Hospital Harvard Medical School, Charlestown, Massachusetts 02129, USA
    Cancer Res 62:200-7. 2002
    ..These findings suggest that IGFR-I signaling through phosphoinositide 3-kinase may represent a novel and potentially important mechanism of resistance to anti-EGFR therapy...
  5. pmc A novel inhibitor of signal transducers and activators of transcription 3 activation is efficacious against established central nervous system melanoma and inhibits regulatory T cells
    Ling Yuan Kong
    Department of Neurosurgery, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Clin Cancer Res 14:5759-68. 2008
    ..We hypothesized that WP1066, a novel STAT3 blockade agent, has marked antitumor activity, even against the melanoma metastasis to brain, a site typically refractory to therapies...
  6. ncbi Tyrphostins and other tyrosine kinase inhibitors
    Alexander Levitzki
    The Silberman Institute for Life Sciences, Department of Biological Chemistry, The Hebrew University, Givat Ram Campus, Jerusalem 91904, Israel
    Annu Rev Biochem 75:93-109. 2006
    ..apoptosis-the best way to induce the demise of the cancer cell, and (d) the potential to utilize PTK inhibitors/tyrphostins to attenuate nonmalignant pathological conditions, such as immune disorders, tissue rejection, and restenosis.
  7. ncbi Tyrphostin A23 inhibits internalization of the transferrin receptor by perturbing the interaction between tyrosine motifs and the medium chain subunit of the AP-2 adaptor complex
    David N Banbury
    Department of Biochemistry, School of Medical Sciences, University of Bristol, Bristol BS8 1TD, United Kingdom
    J Biol Chem 278:12022-8. 2003
    ..The YXXPhi motif is similar to motifs in which the tyrosine residue is phosphorylated by tyrosine kinases. Tyrphostins (structural analogs of tyrosine) are inhibitors of tyrosine kinases and function by binding to the active sites ..
  8. ncbi Inhibition of HER2/neu (erbB-2) and mitogen-activated protein kinases enhances tamoxifen action against HER2-overexpressing, tamoxifen-resistant breast cancer cells
    H Kurokawa
    Department of Medicine, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    Cancer Res 60:5887-94. 2000
    ..Thus, blockade of HER2 and MAPK signaling may enhance tamoxifen action and abrogate antiestrogen resistance in human breast cancer...
  9. pmc Jak2 inhibition deactivates Lyn kinase through the SET-PP2A-SHP1 pathway, causing apoptosis in drug-resistant cells from chronic myelogenous leukemia patients
    A K Samanta
    Department of Molecular Pathology, University of Texas MD Anderson Cancer Center, Houston, TX 77054, USA
    Oncogene 28:1669-81. 2009
    ..These results indicate that Lyn is downstream of Jak2, and Jak2 maintains activated Lyn kinase in CML through the SET-PP2A-Shp1 pathway...
  10. pmc AG490 influences UCN-01-induced cytotoxicity in glioma cells in a p53-dependent fashion, correlating with effects on BAX cleavage and BAD phosphorylation
    Esther P Jane
    Department of Neurosurgery, Children s Hospital of Pittsburgh, University of Pittsburgh School of Medicine, Pittsburgh, PA 15213, USA
    Cancer Lett 257:36-46. 2007
    ....
  11. ncbi Epidermal growth factor receptor inhibitors promote CNS axon growth through off-target effects on glia
    Zubair Ahmed
    Molecular Neuroscience Group, School of Clinical and Experimental Medicine, College of Medical and Dental Sciences, University of Birmingham, Institute of Biomedical Research West, Edgbaston, Birmingham B15 2TT, UK
    Neurobiol Dis 36:142-50. 2009
    ..Accordingly, we suggest that chemical EGFR inhibitors act independently of EGFR, inducing glia and neurons to secrete NT and raising cAMP levels in DRG cultures, leading to Trk-dependent disinhibited DRGN neurite outgrowth...
  12. pmc Inhibition of STAT3 expression and signaling in resveratrol-differentiated medulloblastoma cells
    Li Jun Yu
    Liaoning Laboratory of Cancer Genomics and Department of Cell Biology, College of Basic Medical Sciences, Dalian Medical University, 116044 Dalian, PR China
    Neoplasia 10:736-44. 2008
    ..This signaling may be the major target of resveratrol. Enhanced leukemia inhibitory factor and Bcl-2 expressions in resveratrol-treated cells might reflect a compensatory response to the loss of STAT3 function...
  13. ncbi Inhibition of protein kinase CK2 by flavonoids and tyrphostins. A structural insight
    Graziano Lolli
    Venetian Institute of Molecular Medicine VIMM, Padova, Italy, Via G Orus 2 35129 Padova, Italy
    Biochemistry 51:6097-107. 2012
    ..As in the case of luteolin, the pyrocatechol group of AG99 is critical for binding, interacting with the positive area in the deepest part of the CK2 active site...
  14. ncbi AG490 prevents cell death after exposure of rat astrocytes to hydrogen peroxide or proinflammatory cytokines: involvement of the Jak2/STAT pathway
    Roser Gorina
    Departament de Farmacologia i Toxicologia, IIBB CSIC, IDIBAPS, Rossello 161, Planta 6, 08036 Barcelona, Spain
    J Neurochem 92:505-18. 2005
    ....
  15. ncbi Uridine adenosine tetraphosphate (Up4A) is a strong inductor of smooth muscle cell migration via activation of the P2Y2 receptor and cross-communication to the PDGF receptor
    Annette Wiedon
    Charite Universitatsmedizin Berlin, CharitéCentrum, Department of Nephrology, Campus Benjamin Franklin, Germany
    Biochem Biophys Res Commun 417:1035-40. 2012
    ..We further suggest that the initiation of the migration process occurs predominant through direct activation of the P2Y(2) by Up(4)A and via transactivation of the PDGFR...
  16. pmc leptin-induced growth stimulation of breast cancer cells involves recruitment of histone acetyltransferases and mediator complex to CYCLIN D1 promoter via activation of Stat3
    Neeraj K Saxena
    Division of Digestive Diseases, Department of Medicine, Emory University School of Medicine, Atlanta, Georgia 30322, USA
    J Biol Chem 282:13316-25. 2007
    ..Our data suggest that CYCLIN D1 may be a target gene for leptin mediated growth stimulation of breast cancer cells and molecular mechanisms involve activated Stat3-mediated recruitment of distinct coactivator complexes...
  17. ncbi Mechanisms of endothelial cell protection by blockade of the JAK2 pathway
    Fernando Neria
    Laboratorio de Nefrologia Hipertension, Fundacion Jimenez Diaz, Universidad Autonoma, Avda Reyes Catolicos 2, 28040 Madrid, Spain
    Am J Physiol Cell Physiol 292:C1123-31. 2007
    ..These applications affect not only EC in the monolayer but also circulating detached cells and involve mechanistic interactions not previously described...
  18. ncbi Constitutive activation of Stat3 signaling confers resistance to apoptosis in human U266 myeloma cells
    R Catlett-Falcone
    H Lee Moffitt Cancer Center and Research Institute, University of South Florida College of Medicine, Tampa 33612, USA
    Immunity 10:105-15. 1999
    ..These findings provide evidence that constitutively activated Stat3 signaling contributes to the pathogenesis of multiple myeloma by preventing apoptosis...
  19. ncbi Hexose transporter GLUT1 harbors several distinct regulatory binding sites for flavones and tyrphostins
    Alejandra Perez
    Instituto de Bioquímica y Microbiología, Facultad de Ciencias, Campus Isla Teja s n, Universidad Austral de Chile, Casilla 567, Valdivia, Chile
    Biochemistry 50:8834-45. 2011
    ..inhibitors that include natural products such as flavones and isoflavones and synthetic compounds such as tyrphostins, molecules that are structurally unrelated to the transported substrates [Vera, et al...
  20. ncbi Preclinical analysis of the analinoquinazoline AG1478, a specific small molecule inhibitor of EGF receptor tyrosine kinase
    A G Ellis
    Pharmacology and Developmental Therapeutics Unit, Trescowthick Research Laboratories, Peter MacCallum Cancer Centre, Melbourne, Vic, Australia
    Biochem Pharmacol 71:1422-34. 2006
    ..Taken together, these experiments provide essential data to assess the anti-tumour efficacy of AG1478 and will assist in the rational design of dose regimens for clinical studies...
  21. ncbi Role of JAK/STAT pathway in IL-6-induced activation of vascular smooth muscle cells
    Susumu Watanabe
    Baylor College of Medicine, Houston, Tex, USA
    Am J Nephrol 24:387-92. 2004
    ..We hypothesized that this stimulation occurs via the JAK (janus-activated kinase)/STAT (signal and transducers and activators of transcription) signaling pathway...
  22. pmc A VEGF/JAK2/STAT5 axis may partially mediate endothelial cell tolerance to hypoxia
    Andrew C Dudley
    Department of Medicine, St Vincent s Hospital, University of Melbourne, Corner of Princes and Regent Streets, Fitzroy, Vic, 3065, Australia
    Biochem J 390:427-36. 2005
    ....
  23. ncbi Elevated interleukin-6 and G-CSF in human pancreatic cancer cell conditioned medium suppress dendritic cell differentiation and activation
    Uddalak Bharadwaj
    Molecular Surgeon Research Center, Michael E DeBakey Department of Surgery, Baylor College of Medicine, Houston, Texas 77030, USA
    Cancer Res 67:5479-88. 2007
    ....
  24. ncbi Extracellular matrix proteins protect small cell lung cancer cells against apoptosis: a mechanism for small cell lung cancer growth and drug resistance in vivo
    T Sethi
    Respiratory Medicine Unit, Rayne Laboratory, University of Edinburgh Medical School, Scotland, UK
    Nat Med 5:662-8. 1999
    ..Strategies based on blocking beta1 integrin-mediated survival signals may represent a new therapeutic approach to improve the response to chemotherapy in SCLC...
  25. ncbi Exposure of glia to pro-oxidant agents revealed selective Stat1 activation by H2O2 and Jak2-independent antioxidant features of the Jak2 inhibitor AG490
    Roser Gorina
    Department of Brain Ischemia and Neurodegeneration, Institut d Investigacions Biomèdiques de Barcelona IIBB Consejo Superior de Investigaciones Científicas CSIC, Barcelona, Spain
    Glia 55:1313-24. 2007
    ..These findings reveal previously unrecognized Jak2-independent antioxidant properties of AG490, and show that Jak2-dependent Stat1 activation by peroxide is dissociated from ROS generation...
  26. ncbi JAK/STAT signaling is associated with cardiac dysfunction during ischemia and reperfusion
    E Mascareno
    Center for Cardiovascular and Muscle Research, Department of Anatomy and Cell Biology, State University of New York Health Science Center Brooklyn, Brooklyn, NY, USA
    Circulation 104:325-9. 2001
    ....
  27. ncbi The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells
    Agnieszka Bojko
    Department of General Biochemistry, Faculty of Biochemistry, Biophysics and Biotechnology, Jagiellonian University, Krakow, Poland
    Folia Histochem Cytobiol 50:186-95. 2012
    ..Both tested tyrphostins significantly inhibited autocrine growth of the investigated cell lines...
  28. ncbi JAK/STAT pathway mediates retinal ganglion cell survival after acute ocular hypertension but not under normal conditions
    Yao Huang
    Department of Ophthalmology and Visual Sciences, The Chinese University of Hong Kong, 147K Argyle Street, Kowloon, Hong Kong, P R China
    Exp Eye Res 85:684-95. 2007
    ..This study thus shows that (1) acute IOP elevation activates JAK/STAT pathway in RGCs, and (2) JAK/STAT pathway mediates RGC survival following IOP elevation but not under normal condition...
  29. ncbi Tyrphostins as potential therapeutic agents for acute kidney injury
    S Goncalves
    Hospital de Santa Maria, CHLN, EPE, Lisbon, Portugal
    Curr Med Chem 17:974-86. 2010
    ..b>Tyrphostins are a family of compounds originally designed as protein tyrosine kinase inhibitors...
  30. ncbi Inhibition of STAT3 activity with AG490 decreases the invasion of human pancreatic cancer cells in vitro
    Chen Huang
    Department of General Surgery, Affiliated First People s Hospital, Shanghai Jiao Tong University, Shanghai 200080, China
    Cancer Sci 97:1417-23. 2006
    ....
  31. ncbi Small molecule inhibitors of dynamin I GTPase activity: development of dimeric tyrphostins
    Timothy Hill
    Discipline of Chemistry, Chemistry Building, School of Environmental and Life Sciences, The University of Newcastle, Callaghan, NSW 2308, Australia
    J Med Chem 48:7781-8. 2005
    ..Screening of a library of tyrphostins, in our laboratory, against the GTPase activity of dynamin I gave rise to a microM potent lead, 2-cyano-3-(3,4-..
  32. ncbi STAT3, but not ERKs, mediates the IL-6-induced proliferation of renal cancer cells, ACHN and 769P
    Akio Horiguchi
    Department of Urology, Keio University School of Medicine, 35 Shinanomachi, Shinjuku ku, Tokyo 160 8582, Japan
    Kidney Int 61:926-38. 2002
    ..The aim of this study was to characterize the signaling cascades mediating IL-6-induced proliferation and to investigate the use of effective novel interventions to block the IL-6-induced autocrine growth of renal cancer cells...
  33. pmc Heparin-binding epidermal growth factor-like growth factor is a potent regulator of invasion activity in oral squamous cell carcinoma
    Yuichi Ohnishi
    Second Department of Oral and Maxillofacial Surgery, Osaka Dental University, Chuo Ku, Osaka 540 0008, Japan
    Oncol Rep 27:954-8. 2012
    ..These data indicate that HB-EGF released from HSC3 cells by TACE stimulates EGFR in an autocrine manner, which in turn activates invasion activity via MMP-9 upregulation...
  34. ncbi Involvement of epidermal growth factor receptor in chemically induced mouse bladder tumour progression
    A el-Marjou
    UMR 144, CNRS, Institut Curie, 26 Rue d Ulm, 75248 Paris Cedex 05, France
    Carcinogenesis 21:2211-8. 2000
    ..These results suggest that EGFR plays a critical role in bladder tumour progression...
  35. ncbi Acute stimulation of glucose uptake by leptin in l6 muscle cells
    S H Bates
    School of Life and Health Sciences, Aston University, Birmingham, UK
    Horm Metab Res 34:111-5. 2002
    ..The results suggest that leptin can act directly on L6 muscle cellsvia a short leptin receptor isoform to acutely stimulate basal (but not insulin-stimulated) glucose uptake via a PI3K-dependent pathway...
  36. ncbi Angiotensin II triggers EGFR tyrosine kinase-dependent Ca2+ influx in afferent arterioles
    Qi Che
    Department of Physiology and Biophysics, University of Nebraska College of Medicine, Omaha, Neb 68198 4575, USA
    Hypertension 40:700-6. 2002
    ..We conclude that epidermal growth factor receptor tyrosine kinase activity contributes to the afferent arteriolar intracellular [Ca2+] response to angiotensin II and that this process involves promotion of Ca2+ influx...
  37. ncbi Tyrphostins protect neuronal cells from oxidative stress
    Yutaka Sagara
    Department of Neurosciences, University of California, San Diego, La Jolla, California 92093 0624, USA
    J Biol Chem 277:36204-15. 2002
    b>Tyrphostins are a family of tyrosine kinase inhibitors originally synthesized as potential anticarcinogenic compounds...
  38. ncbi Role of insulin-like growth factor 1 receptor and c-Src in endothelin-1- and angiotensin II-induced PKB phosphorylation, and hypertrophic and proliferative responses in vascular smooth muscle cells
    Ali Bouallegue
    Laboratory of Cell Signaling, Montreal Diabetes Research Centre, Centre de Recherche, Centre hospitalier de l Université de Montréal CRCHUM, Technopole Angus Campus, and Department of Medicine, University of Montreal, Montreal, Quebec, Canada
    Can J Physiol Pharmacol 87:1009-18. 2009
    ..In conclusion, these data suggest that IGF-1R PTK and c-Src PTK play a critical role in mediating PKB phosphorylation as well as hypertrophic and proliferative responses induced by ET-1 and Ang II in A10 VSMC...
  39. pmc IL-6 signaling by STAT3 participates in the change from hyperplasia to neoplasia in NRP-152 and NRP-154 rat prostatic epithelial cells
    B E Barton
    Division of General Surgery, Department of Surgery, UMDNJ NJMS, 185 S Orange Ave, Newark, NJ 07103, USA
    BMC Cancer 1:19. 2001
    ..These lines are believed to represent 2 of the stages in the development of prostate cancer, hyperplasia and neoplasia. Differences in signaling pathways should play a role in the 2 phenotypes, hyperplastic and neoplastic...
  40. ncbi Inhibition of experimental autoimmune encephalomyelitis by a tyrosine kinase inhibitor
    G Constantin
    Department of Pathology, Digestive Disease Center, Stanford University School of Medicine, CA 95305, USA
    J Immunol 162:1144-9. 1999
    ..Our results suggest that inhibition of signaling pathways involved in lymphocyte adhesion may represent a novel therapeutic approach for demyelinating diseases...
  41. pmc Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells
    B Wen
    , Institut Gustave Roussy, , France
    Br J Cancer 85:2017-21. 2001
    ..These results suggest that Tyrphostin AG 1024 could be used as a potential therapeutic agent in combination with irradiation...
  42. ncbi Metalloprotease disintegrin-mediated ectodomain shedding of EGFR ligands promotes intestinal epithelial restitution
    Gennett M Myhre
    Gastroenterology Research Unit, Mayo Clinic, 200 First St SW, Rochester, MN 55905, USA
    Am J Physiol Gastrointest Liver Physiol 287:G1213-9. 2004
    ..Therefore, activation of the TACE-EGFR system might promote the healing of intestinal tract ulcers in patients...
  43. ncbi Role of the STAT1 pathway in apoptosis induced by fludarabine and JAK kinase inhibitors in B-cell chronic lymphocytic leukemia
    Luis Martinez-Lostao
    Immunology Department, Hospital de Sant Pau, Universitat Autonoma de Barcelona, Spain
    Leuk Lymphoma 46:435-42. 2005
    ..In conclusion, our data show that JAK kinase inhibitors, such as AG490 and WHI-P131 are able to inhibit the STAT1 pathway on B-CLL cells and are strong inductors of apoptosis on these cells...
  44. ncbi Functional uncoupling of the Janus kinase 3-Stat5 pathway in malignant growth of human T cell leukemia virus type 1-transformed human T cells
    R A Kirken
    Department of Integrative Biology and Pharmacology, University of Texas Health Science Center, Houston, TX 77030, USA
    J Immunol 165:5097-104. 2000
    ..Reversal of this functional uncoupling may be required before Jak3/Stat5 inhibitors will be useful in the treatment of this malignancy...
  45. ncbi Effects of AG490 on lens epithelial cell death induced by H(2)O(2)
    Ungsoo Samuel Kim
    Department of Ophthalmology, Kim s Eye Hospital, Myung Gok Eye Research Institute, Konyang University College of Medicine, Seoul, Korea
    Jpn J Ophthalmol 54:151-5. 2010
    ....
  46. ncbi Concomitant inhibition of Janus kinase 3 and calcineurin-dependent signaling pathways synergistically prolongs the survival of rat heart allografts
    F Behbod
    Department of Integrative Biology and Pharmacology, University of Texas Medical School, Houston, TX 77030, USA
    J Immunol 166:3724-32. 2001
    ..Thus, inhibition of Jak3 prolongs allograft survival and also potentiates the immunosuppressive effects of cyclosporin A, but not rapamycin...
  47. ncbi Inhibition of JAK2/STAT3 signalling induces colorectal cancer cell apoptosis via mitochondrial pathway
    Wan Du
    GI Division, Shanghai Jiao Tong University School of Medicine Renji Hospital, Shanghai Institution of Digestive Disease, Key Laboratory of Gastroenterology and Hepatology, Shanghai, China
    J Cell Mol Med 16:1878-88. 2012
    ..Therefore, JAK2/STAT3 signalling may be a potential target for therapy of CRC...
  48. ncbi Pyridone 6, a pan-Janus-activated kinase inhibitor, induces growth inhibition of multiple myeloma cells
    Laura Pedranzini
    Department of Medicine, Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA
    Cancer Res 66:9714-21. 2006
    ..Thus, P6 is a more sensitive and specific inhibitor of JAK-STAT3 activity compared with AG490 and potently inhibited the growth of primary myeloma cells and myeloma-derived cell lines grown on BMSCs...
  49. ncbi Inhibition of constitutively active Stat3 suppresses proliferation and induces apoptosis in glioblastoma multiforme cells
    Shaik Ohidar Rahaman
    Department of Cancer Biology, Lerner Research Institute, Cleveland Clinic Foundation, 9500 Euclid Avenue, Cleveland, Ohio, OH 44195, USA
    Oncogene 21:8404-13. 2002
    ..Therefore, targeting Stat3 signaling may provide a potential therapeutic intervention for GBM...
  50. ncbi Epidermal growth factor receptor activation by protein kinase C is necessary for FSH-induced meiotic resumption in porcine cumulus-oocyte complexes
    Xiufen Chen
    State Key Laboratory for Agrobiotechnology, College of Biological Sciences, China Agricultural University, Beijing 100094, People s Republic of China
    J Endocrinol 197:409-19. 2008
    ..These data together suggested that EGFR activation, by PKC signal pathway, participates in FSH-induced porcine oocyte meiotic resumption...
  51. pmc HER2 oncogenic function escapes EGFR tyrosine kinase inhibitors via activation of alternative HER receptors in breast cancer cells
    Anthony Kong
    Cell Biophysics Laboratory, Lincoln s Inn Fields Laboratories, London Research Institute, Cancer Research UK, London, United Kingdom
    PLoS ONE 3:e2881. 2008
    ..Furthermore, although TKIs suppress the growth of HER2-overexpressing breast tumor cells, they do not fully inhibit HER2 oncogenic function at physiological doses...
  52. ncbi The JAK2 inhibitor AG490 predominantly abrogates the growth of human B-precursor leukemic cells with 11q23 translocation or Philadelphia chromosome
    N Miyamoto
    Department of Pediatrics, Yamanashi Medical University, Japan
    Leukemia 15:1758-68. 2001
    ..B-precursor leukemic cell line was potently inhibited in its proliferation by one of synthetic PTK inhibitors (tyrphostins), AG490, via anti-JAK2 activity. However, no extensive studies about it have been performed...
  53. ncbi Conditioning injury-induced spinal axon regeneration requires signal transducer and activator of transcription 3 activation
    Jin Qiu
    Wolfson Centre for Age Related Diseases, Guy s, King s, and St Thomas s School of Biomedical Science, King s College London, London SE1 1UL, United Kingdom
    J Neurosci 25:1645-53. 2005
    ..We conclude that STAT3 activation is necessary for increased growth ability of DRG neurons and improved axonal regeneration in the spinal cord after a conditioning injury...
  54. ncbi Combined inhibition of epidermal growth factor receptor and JAK/STAT pathways results in greater growth inhibition in vitro than single agent therapy
    Afshin Dowlati
    Division of Hematology Oncology, Department of Medicine, Case Western Reserve University and University Hospitals of Cleveland, Cleveland, OH 44016, USA
    Mol Cancer Ther 3:459-63. 2004
    ..We conclude that targeting multiple pathways (EGFR and JAK/STAT pathways) in EGF-driven tumors may result in greater antiproliferative activity than blocking EGFR alone...
  55. ncbi Synergy of epidermal growth factor receptor kinase inhibitor AG1478 and ErbB2 kinase inhibitor AG879 in human colon carcinoma cells is associated with induction of apoptosis
    Yunfei Zhou
    Department of Pharmacology and Therapeutics, Roswell Park Cancer Institute, Buffalo, New York 14263, USA
    Cancer Res 65:5848-56. 2005
    ..These data suggest that the strategy to target both EGFR and ErbB2 simultaneously might result in more efficient inhibition of tumor growth than to target single receptor alone...
  56. ncbi The relative role of ErbB1-4 receptor tyrosine kinases in radiation signal transduction responses of human carcinoma cells
    G Bowers
    Department of Radiation Oncology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia, VA23298-0058, USA
    Oncogene 20:1388-97. 2001
    ..Inhibiting ErbB2 caused an enhanced MAPK response simulating an amplified ErbB1 (or 4) response. Thus ErbB2 is a modulator of ErbB1 (or 4) function leading to different MAPK response profiles to GF or radiation exposure...
  57. ncbi Proximal events in signaling by plasma membrane estrogen receptors
    Mahnaz Razandi
    Division of Endocrinology, Veterans Affairs Medical Center, Long Beach, California 90822, USA
    J Biol Chem 278:2701-12. 2003
    ..The E domain is sufficient to enact these events, defining additional details of the important cross-talk between membrane ER and EGFR in breast cancer...
  58. ncbi Differential roles of WAVE1 and WAVE2 in dorsal and peripheral ruffle formation for fibroblast cell migration
    Shiro Suetsugu
    Department of Biochemistry, Institute of Medical Science, University of Tokyo, Tokyo, 108 8639, Japan
    Dev Cell 5:595-609. 2003
    ..Thus, WAVE2 is essential for leading edge extension for directed migration in general and WAVE1 is essential in MMP-dependent migration in ECM...
  59. ncbi Carbachol-stimulated transactivation of epidermal growth factor receptor and mitogen-activated protein kinase in T(84) cells is mediated by intracellular Ca2+, PYK-2, and p60(src)
    S J Keely
    Department of Medicine, University of California, San Diego, School of Medicine, San Diego, California 92103, USA
    J Biol Chem 275:12619-25. 2000
    ..This pathway represents a mechanism that limits CCh-stimulated chloride secretion across intestinal epithelia...
  60. pmc Regulating RISK: a role for JAK-STAT signaling in postconditioning?
    Michael D Goodman
    Department of Surgery, University of Cincinnati, Cincinnati, Ohio 45267, USA
    Am J Physiol Heart Circ Physiol 295:H1649-56. 2008
    ..POC induces myocardial functional protection by activating the RISK pathway. JAK-STAT signaling, however, is insufficient for effective POC without PI3K-Akt activation...
  61. ncbi STAT3 mediates the survival signal in oncogenic ras-transfected intestinal epithelial cells
    S Zushi
    Second Department of Internal Medicine, Osaka University Medical School, Suita, Japan
    Int J Cancer 78:326-30. 1998
    ..Moreover, the expression of Bcl-2 and Bcl-xL, apoptosis-suppressive proteins, is reduced in dominant-negative STAT3-transfected cells. Thus, STAT3 appears to be an important mediator of the antiapoptotic signal in IEC-ras cells...
  62. ncbi A novel small molecule inhibitor of signal transducers and activators of transcription 3 reverses immune tolerance in malignant glioma patients
    S Farzana Hussain
    Department of Neurosurgery, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Cancer Res 67:9630-6. 2007
    ....
  63. ncbi Simultaneously targeting epidermal growth factor receptor tyrosine kinase and cyclooxygenase-2, an efficient approach to inhibition of squamous cell carcinoma of the head and neck
    Zhuo Chen
    Department of Hematology Oncology, Winship Cancer Institute, Emory University, Atlanta, Georgia, USA
    Clin Cancer Res 10:5930-9. 2004
    ..Simultaneously blocking both EGFR and Cox-2-mediated pathways may be an efficient means of inhibiting cancer cell growth in SCCHN...
  64. ncbi Janus kinase 2 is involved in stromal cell-derived factor-1alpha-induced tyrosine phosphorylation of focal adhesion proteins and migration of hematopoietic progenitor cells
    X F Zhang
    Division of Experimental Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, 4 Blackfan Circle, Boston, MA 02115, USA
    Blood 97:3342-8. 2001
    ..Hence, these results suggest that JAK2 is required for CXCR4 receptor-mediated signaling that regulates cytoskeletal proteins and cell migration through PI3-kinase pathways in hematopoietic progenitor cells. (Blood. 2001;97:3342-3348)..
  65. pmc Inhibition of JAK1, 2/STAT3 signaling induces apoptosis, cell cycle arrest, and reduces tumor cell invasion in colorectal cancer cells
    Hua Xiong
    Department of Gastroenterology, Shanghai Jiao Tong University School of Medicine, Ren Ji Hospital, Shanghai Institute of Digestive Disease, Shanghai, 200001, China
    Neoplasia 10:287-97. 2008
    ..Therefore, our findings illustrate the biologic significance of JAK1, 2/STAT3 signaling in CRC progression and provide novel evidence that the JAK/STAT3 pathway may be a new potential target for therapy of CRC...
  66. ncbi WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells
    Alessandra Ferrajoli
    Department of Leukemia, The University of Texas M D Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, USA
    Cancer Res 67:11291-9. 2007
    ..Thus, WP1066 is a potent JAK2 inhibitor whose effects in AML and other hematologic malignancies merit further investigation...
  67. ncbi BCR-ABL down-regulates the DNA repair protein DNA-PKcs
    E Deutsch
    , Institut Gustave Roussy, Villejuif, France
    Blood 97:2084-90. 2001
    ..The down-regulation of DNA-PKcs was reversible in CD34(+) CML cells suggesting that this approach might offer a novel and powerful therapeutic strategy in this disease, especially to delay the blast crisis. (Blood. 2001;97:2084-2090)..
  68. ncbi Inhibition of the Jak/STAT signaling pathway prevents the high glucose-induced increase in tgf-beta and fibronectin synthesis in mesangial cells
    Xiaodan Wang
    Vascular Biology Center, Medical College of Georgia, Augusta, GA 30912 2500, USA
    Diabetes 51:3505-9. 2002
    ..These results provide direct evidence for linkages between JAK2, STAT1, and the glucose-induced overproduction of TGF-beta and fibronectin in GMC...
  69. ncbi EGFR activation mediates inhibition of axon regeneration by myelin and chondroitin sulfate proteoglycans
    Vuk Koprivica
    Division of Neuroscience, Children s Hospital, Boston, MA 02115, USA
    Science 310:106-10. 2005
    ..Local administration of EGFR inhibitors promotes significant regeneration of injured optic nerve fibers, pointing to a promising therapeutic avenue for enhancing axon regeneration after CNS injury...
  70. ncbi Involvement of JAK2 and Src kinase tyrosine phosphorylation in human growth hormone-stimulated increases in cytosolic free Ca2+ and insulin secretion
    Fan Zhang
    Research Center, Karolinska Institute, Stockholm South Hospital, SE 11883 Stockholm, Sweden
    Am J Physiol Cell Physiol 291:C466-75. 2006
    ..Our study indicates that hGH stimulates rise in [Ca(2+)](i) and insulin secretion mainly through activation of the prolactin receptor and JAK2 and Src kinases in rat insulin-secreting cells...
  71. pmc Stable expression of constitutively-activated STAT3 in benign prostatic epithelial cells changes their phenotype to that resembling malignant cells
    Hosea F Huang
    Division of Urology, Department of Surgery, UMDNJ New Jersey Medical School, 185 S, Orange, Ave, Newark 07103, USA
    Mol Cancer 4:2. 2005
    ....
  72. ncbi A novel inhibitor of the STAT3 pathway induces apoptosis in malignant glioma cells both in vitro and in vivo
    A Iwamaru
    Department of Neurosurgery, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA
    Oncogene 26:2435-44. 2007
    ..We conclude that WP1066 holds promise as a therapeutic agent against malignant gliomas...
  73. ncbi WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation
    Srdan Verstovsek
    Department of Leukemia, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Clin Cancer Res 14:788-96. 2008
    ..However, no effective JAK2 inhibitors are currently available for clinical use...
  74. ncbi STAT3 attenuates EGFR-mediated ERK activation and cell survival during oxidant stress in mouse proximal tubular cells
    I Arany
    Department of Internal Medicine, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, USA
    Kidney Int 70:669-74. 2006
    ..These data suggest that the STAT3 pathway might represent a new target for improved survival of proximal tubule cells exposed to severe oxidant injury...
  75. pmc Epidermal growth factor differentially augments G(i)-mediated stimulation of c-Jun N-terminal kinase activity
    Anthony S L Chan
    Department of Biochemistry, The Biotechnology Research Institute, and the Molecular Neuroscience Center, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong
    Br J Pharmacol 142:635-46. 2004
    ..6. Our results support a mechanistic model where EGF signaling may differentially regulate the JNK activities triggered by GPCRs of different coupling specificities...
  76. ncbi Tethering of the platelet-derived growth factor beta receptor to G-protein-coupled receptors. A novel platform for integrative signaling by these receptor classes in mammalian cells
    F Alderton
    Department of Physiology and Pharmacology, Strathclyde Institute for Biomedical Sciences, University of Strathclyde, 27 Taylor St, Glasgow, G4 0NR, Scotland, United Kingdom
    J Biol Chem 276:28578-85. 2001
    ..These results provide a model that may account for the co-mitogenic effect of certain G-protein-coupled receptor agonists with platelet-derived growth factor on DNA synthesis...
  77. ncbi Tyrosine kinases as targets for cancer therapy
    Alexander Levitzki
    Unit of Cellular Signaling, Department of Biological Chemistry, The Silverman Institute for Life Sciences, The Hebrew University of Jerusalem, Jerusalem 91904, Israel
    Eur J Cancer 38:S11-8. 2002
    ..in the treatment of cancer led to the systematic synthesis of selective tyrosine phosphorylation inhibitors (tyrphostins) that show in vitro and in vivo anticancer activity...
  78. pmc Role of the tyrosine kinase pyk2 in the integrin-dependent activation of human neutrophils by TNF
    M Fuortes
    Department of Cell Biology, Department of Microbiology and Immunology, Weill Medical College of Cornell University, New York 10021, USA
    J Clin Invest 104:327-35. 1999
    ..Thus, pyk2 appears to play an essential role in the ability of neutrophils to integrate signals from beta(2) integrins and TNF receptors...
  79. ncbi Group I mGluRs coupled to G proteins are regulated by tyrosine kinase in dopamine neurons of the rat midbrain
    A Tozzi
    Istituto di Ricovero e Cura a Carattere Scientifico Fondazione S. Lucia, 00179 Rome, Italy
    J Neurophysiol 85:2490-7. 2001
    ..Thus our results indicate that the responses, mainly mediated by mGluRs1 in dopamine neurons, are activated by intracellular mechanisms coupled to G proteins and regulated by tyrosine kinases...
  80. ncbi Evidence that tyrphostins AG10 and AG18 are mitochondrial uncouplers that alter phosphorylation-dependent cell signaling
    Stephen P Soltoff
    Beth Israel Deaconess Medical Center, Division of Signal Transduction, Boston, Massachusetts 02215, USA
    J Biol Chem 279:10910-8. 2004
    ..However, like the mitochondrial uncoupler carbonyl cyanide p-trifluoromethoxyphenyl hydrazone, tyrphostins AG10 and AG18 increased the rate of oxygen consumption and reduced cellular ATP by approximately 90% in the ..
  81. ncbi Unliganded epidermal growth factor receptor dimerization induced by direct interaction of quinazolines with the ATP binding site
    C L Arteaga
    Department of Medicine, Vanderbilt University School of Medicine, Vanderbilt Cancer Center, Nashville, Tennessee 37232 5536, USA
    J Biol Chem 272:23247-54. 1997
    ....
  82. ncbi Platelet-derived growth factor-BB-induced human smooth muscle cell proliferation depends on basic FGF release and FGFR-1 activation
    Esther Millette
    University of Washington School of Medicine, Department of Surgery, Box 356410, 1959 NE Pacific St, Seattle, WA 98195 6410, USA
    Circ Res 96:172-9. 2005
    ..Our results provide support for a novel mechanism by which PDGF-BB induces the release of bFGF and activation of FGFR-1 followed by the sustained activation of ERK and proliferation of human SMCs...
  83. pmc Inhibition of STAT3 signaling leads to apoptosis of leukemic large granular lymphocytes and decreased Mcl-1 expression
    P K Epling-Burnette
    Hematologic Malignancy Program, H Lee Moffitt Cancer Center and Research Institute, 12902 Magnolia Drive, MRC, Room 2068 f and g, Tampa, Florida 33612, USA
    J Clin Invest 107:351-62. 2001
    ..We conclude that STAT3 activation contributed to accumulation of the leukemic LGL clones. These findings suggest that investigation should focus on novel strategies targeting STAT3 in the treatment of LGL leukemia...
  84. ncbi Tyrphostins are inhibitors of guanylyl and adenylyl cyclases
    Mahaboobi Jaleel
    Department of Molecular Reproduction, Development, and Genetics, Indian Institute of Science, Bangalore 560012, India
    Biochemistry 43:8247-55. 2004
    ..this study, we have tested the effect of several protein kinase inhibitors on GC-C activity and find that the tyrphostins, known to be tyrosine kinase inhibitors, could inhibit GC-C activity in vitro...
  85. ncbi Pervanadate inhibits volume-sensitive chloride current in bovine chromaffin cells
    P Doroshenko
    Loeb Research Institute, 1053 Carling Avenue, Ottawa, Ontario, K1Y 4E9, Canada
    Pflugers Arch 435:303-9. 1998
    ..The possibility of pervanadate acting via a pathway unrelated to protein phosphorylation is also discussed...
  86. ncbi Independent role of phosphoinositol-3-kinase (PI3K) and casein kinase II (CK-2) in EGFR and Her-2-mediated constitutive NF-kappaB activation in prostate cancer cells
    Cécile Le Page
    Centre de recherche du Centre Hospitalier de l Université de Montréal CR CHUM, 1560 rue Sherbrooke Est, Montreal, Quebec, Canada
    Prostate 65:306-15. 2005
    ....
  87. ncbi Extracellular calcium-sensing receptor transactivates the epidermal growth factor receptor by a triple-membrane-spanning signaling mechanism
    R John Macleod
    Endocrine Hypertension Division and Membrane Biology Program, Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
    Biochem Biophys Res Commun 320:455-60. 2004
    ..Proximal and distal signal transduction cascades activated by the CaR may reflect transactivation of the EGFR by the extracellular calcium-sensing receptor...
  88. ncbi Signal transduction through substance P receptor in human glioblastoma cells: roles for Src and PKCdelta
    Keisuke Yamaguchi
    Department of Anesthesiology and Pain Medicine, Juntendo University School of Medicine, Tokyo, Japan
    Cancer Chemother Pharmacol 56:585-93. 2005
    ..Finally, rottlerin and PP2 were both found to inhibit the growth of several glioblastoma cell lines, underscoring the potential of these agents to block glioblastoma growth...
  89. pmc AP-2alpha: a regulator of EGF receptor signaling and proliferation in skin epidermis
    Xuan Wang
    The Howard Hughes Medical Institute, Rockefeller University, New York, NY 10021, USA
    J Cell Biol 172:409-21. 2006
    ..These results provide insights into why elevated AP-2alpha levels are often associated with terminal differentiation and why tumor cells often display reduced AP-2alpha and elevated EGFR proteins...
  90. ncbi Evidence that basal activity, but not transactivation, of the epidermal growth factor receptor tyrosine kinase is required for insulin-like growth factor I-induced activation of extracellular signal-regulated kinase in oral carcinoma cells
    Ami Kuribayashi
    Molecular Diagnosis and Therapeutics, Department of Oral Restitution, Graduate School, Tokyo Medical and Dental University, 1 5 45 Yushima, Bunkyo ku, Tokyo 113 8549, Japan
    Endocrinology 145:4976-84. 2004
    ..The elucidation of such a unique mechanism involving cross-talk between EGFR and heterologous receptors may shed additional light on the clinical use of EGFR-TK inhibitors in antitumor therapies...
  91. ncbi PGE2 up-regulates vascular endothelial growth factor expression in MKN28 gastric cancer cells via epidermal growth factor receptor signaling system
    Yan bing Ding
    Department of Gastroenterology and Oncology, Yangzhou First Municipal Hospital, Yangzhou University, Yangzhou 225001, Jiangsu Province, China
    Exp Oncol 27:108-13. 2005
    ....
  92. ncbi Dominant-negative Notch3 receptor inhibits mitogen-activated protein kinase pathway and the growth of human lung cancers
    Nobuhiro Haruki
    Division of Hematology, Allergy Pulmonary and Critical Care Medicine, Vanderbilt University Medical Center, Nashville, Tennessee 37232, USA
    Cancer Res 65:3555-61. 2005
    ..These observations support a role for Notch3 signaling in lung cancer, and one potential mechanism of maintaining the neoplastic phenotype is through the modulation of the EGF pathway...
  93. ncbi Angiotensin II stimulates Pax-2 in rat kidney proximal tubular cells: impact on proliferation and apoptosis
    Shao Ling Zhang
    Pediatric Nephrology Unit, Harvard Medical School, Massachusetts General Hospital, Boston, Massachusetts 02114 3117, USA
    Kidney Int 66:2181-92. 2004
    ..The present investigation hypothesized that AT2R activation would stimulate Pax-2 gene expression in immortalized rat renal proximal tubular cells (IRPTC), as we have found in fetal cells...
  94. ncbi Src tyrosine kinase inhibitor PP2 suppresses ERK1/2 activation and epidermal growth factor receptor transactivation by X-irradiation
    Zhiping Li
    Department of Radiation Research, Faculty of Medicine, University of Tokyo, Tokyo 113 0033, Japan
    Biochem Biophys Res Commun 341:363-8. 2006
    ..These data suggest that IR-induced ERK1/2 activation involves EGFR through a Src-dependent pathway that is distinct from EGFR ligand activation...
  95. ncbi Mechanical stretch stimulates protein kinase B/Akt phosphorylation in epidermal cells via angiotensin II type 1 receptor and epidermal growth factor receptor
    Stefan Kippenberger
    Department of Dermatology, University of Frankfurt Medical School, D 60596 FrankfurtMain, Germany
    J Biol Chem 280:3060-7. 2005
    ..Evidence is provided that stretch-induced activation of PKB/Akt protects cells against induced apoptosis...
  96. pmc Combining RNA interference and kinase inhibitors against cell signalling components involved in cancer
    Michael O'Grady
    Invitrogen Corporation, Madison, WI 53719, USA
    BMC Cancer 5:125. 2005
    ....
  97. ncbi Toluene diisocyanate (TDI) induces production of inflammatory cytokines and chemokines by bronchial epithelial cells via the epidermal growth factor receptor and p38 mitogen-activated protein kinase pathways
    Hirohisa Ogawa
    Department of Clinical Investigation, National Hospital Organization National Kochi Hospital, Kochi City, Japan
    Exp Lung Res 32:245-62. 2006
    ..Thus, TDI was shown to have a stimulatory effect on bronchial epithelial cells, suggesting the potent role of bronchial epithelial cells in TDI-induced asthma...
  98. ncbi beta-Arrestin 2 expression determines the transcriptional response to lysophosphatidic acid stimulation in murine embryo fibroblasts
    Diane Gesty-Palmer
    Department of Medicine, Duke University Medical Center, Durham, North Carolina 27710, USA
    J Biol Chem 280:32157-67. 2005
    ..These data indicate that beta-arrestin 2 functions both to attenuate EGF receptor transactivation-dependent signaling and to promote a distinct subset of ERK1/2-mediated responses to LPA receptor activation...
  99. ncbi Bronchial epithelial compression regulates epidermal growth factor receptor family ligand expression in an autocrine manner
    Eric K Chu
    Department of Pulmonary and Critical Care Medicine, Brigham and Women s Hospital, 75 Francis Street, Boston, MA 02115, USA
    Am J Respir Cell Mol Biol 32:373-80. 2005
    ..The response of all three EGFR ligands persisted long after the mechanical stimulus was removed. Taken together, these data suggest the possibility of a mechanically activated EGFR autocrine feedback loop involving selected EGFR ligands...
  100. ncbi A FRET-based probe for epidermal growth factor receptor bound non-covalently to a pair of synthetic amphipathic helixes
    Reina E Itoh
    Department of Tumor Virology, Research Institute for Microbial Diseases, Osaka University, Yamadaoka, Suita Shi, Osaka 565 0871, Japan
    Exp Cell Res 307:142-52. 2005
    ....
  101. ncbi EGFR-induced cell migration is mediated predominantly by the JAK-STAT pathway in primary esophageal keratinocytes
    Claudia D Andl
    Gastroenterology Division, Department of Medicine, Abramson Cancer Center and Family Cancer Research Institute, University of Pennsylvania, 415 Curie Blvd, Philadelphia, PA 19104, USA
    Am J Physiol Gastrointest Liver Physiol 287:G1227-37. 2004
    ..Taken together, we find that the recruitment of the STAT-JAK complex by EGFR is responsible for keratinocyte migration that, in turn, might be mediated by MMP-1 activation...

Research Grants40

  1. Preclinical Evaluation of Bcr/Abl-Directed Tyrphostins
    Scott Kaufmann; Fiscal Year: 2007
    ..abstract_text> ..
  2. Novel cancer therapy by EGFR targeted transfection of synthetic dsRNA
    Alexander Levitzki; Fiscal Year: 2009
    ..Our preliminary results (shown here) support our contention. If successful, this form of therapy could benefit or even cure many cancer patients, without the need for lengthy and expensive procedures. ..
  3. Dedifferentiation Following Renal Cell Injury
    Shougang Zhuang; Fiscal Year: 2009
    ..These studies will increase our knowledge of the mechanisms of RPTC dedifferentiation after injury and may contribute to the development of novel treatment for patients with ARF. ..
  4. Cell-targeting peptide nucleic acids for hormone-refractory prostate cancer
    Beverly Barton; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  5. Role of ghrelin in intestinal inflammation
    Dezheng Zhao; Fiscal Year: 2008
    ....
  6. Role of ErbB/Stat3 in the establishment and progression of pancreatic cancer
    James Freeman; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  7. A Request for support of 25th SPRSM Meeting
    James Wang; Fiscal Year: 2006
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  8. Role of Acetaldehyde in Alcoholic Cardiomyopathy
    Jun Ren; Fiscal Year: 2008
    ..Our long-term goal is to establish the toxic mechanism of acetaldehyde in the development of alcoholic cardiomyopathy so that prevention and treatment can be optimized [unreadable] [unreadable]..
  9. DEVELOPING A POTENT INHIBITOR OF HIV-I INTEGRASE
    Naijie Jing; Fiscal Year: 2001
    ....
  10. The Role of Tuberin in Smooth Muscle Cell Proliferation
    Geraldine Finlay; Fiscal Year: 2007
    ..abstract_text> ..
  11. Akt1 and erbB2 - New Molecular Targets for Hormone Resistance in Breast Cancer
    Adriana Stoica; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  12. Probiotics regulate intestinal epithelial cell homeostasis
    Fang Yan; Fiscal Year: 2008
    ..Genes regulated by LGG in colon cells will be identified using DNA microarray. These findings will have significant relevance to further understanding the probiotic regulation of intestinal health. ..
  13. Translational Assess. of Kinase Targets in Lung Cancer
    Afshin Dowlati; Fiscal Year: 2008
    ..Based on our preclinical data targeting EGFR and ErbB2 results in superior anti-tumor activity as compared to EGFR blockade alone. ..
  14. Human Hematopoietic Cell Transformation by BCR/ABL
    Ravi Bhatia; Fiscal Year: 2008
    ..These studies are expected to result in improved understanding of mechanisms critical for human progenitor transformation in CML and guide rational development of additional mechanism-based therapies. ..
  15. Defects of Neurotransmission in Ischemia and Reperfusion
    ALEXANDER MONGIN; Fiscal Year: 2008
    ..abstract_text> ..
  16. An interdisciplinary and integrative study of tendinopathy
    James H C Wang; Fiscal Year: 2010
    ....
  17. SIGNALING BY VASOPRESSIN--ARTERIAL SMOOTH MUSCLE CELLS
    KENNETH BYRON; Fiscal Year: 2002
    ..Finally, the effects of AVP and other hormones on [Ca2+]i and membrane currents will be examined in freshly isolated smooth muscle cells from rat mesenteric arteries. ..
  18. INVESTIGATING THE MECHANISMS OF PRB TUMOR SUPPRESSION
    Arnab Chakravarti; Fiscal Year: 2003
    ..Specific Aim number 3: To determine whether the deregulation of E2F dependent transcription is correlated with the tumorigenic potential of RB -/- cells in-vivo. ..
  19. A Novel Inhibitor of Stat3 for Prostate Cancer Therapy
    Naijie Jing; Fiscal Year: 2009
    ..abstract_text> ..
  20. Silibinin in Prostate Cancer Chemoprevention & Treatment
    Michael Pollak; Fiscal Year: 2004
    ..The work is justified by the favorable toxicity profile of silibinin, together with prior positive laboratory studies reported by our group and other investigators. ..
  21. PHASE I TRIAL OF A PEPTIDE VACCINE AGAINST EGFRVIII
    Bruce Montgomery; Fiscal Year: 2005
    ..To characterize effects of human anti-EGFRvIII antibodies on EGFRvIII signaling. 4. To determine the level of EGFR specific T cell response after immunization with EGFRvIII peptide. ..
  22. ENDOTHELIAL GROWTH FACTOR IN PROSTATE CANCER METASTASIS
    Dan Theodorescu; Fiscal Year: 2005
    ..abstract_text> ..
  23. Chemical Genetic Analysis of Platelet Granule Secretion
    Robert Flaumenhaft; Fiscal Year: 2008
    ..Once identified, compounds will be tested in a previously established battery of platelet function tests and evaluated for antithrombotic potential in an in vivo murine model of thrombus formation. [unreadable] [unreadable] [unreadable]..
  24. Role of Wnt signaling in Cervical Cancer Pathogenesis
    Aykut Uren; Fiscal Year: 2010
    ..Aykut The name of the principal investigator/program director must be provided at the top of each printed page and each continuation page. RESEARCH GRANT TABLE OF CONTENTS Page Numbers Face Page 1 Description, ..
  25. Abnormalities in gene expression in therapy-related MDS
    Ravi Bhatia; Fiscal Year: 2008
    ..These studies may also allow identification of markers of susceptibility to t-MDS allowing early detection of patients at risk for this complication. ..
  26. Micellar VIP Nanoparticles for Rheumatoid Arthritis
    Israel Rubinstein; Fiscal Year: 2007
    ..abstract_text> ..
  27. IGF-1, Oxidative Stress and Cardiovascular Aging
    Jun Ren; Fiscal Year: 2002
    ..Our long-term goal is to establish the causal link among IGF-1 deficiency, enhanced oxidative damage and ventricular dysfunction in the progression of cardiovascular aging so that hormonal or antioxidant therapy can be optimized...
  28. REGULATION OF THE STEROIDOGENIC ACUTE REGULATORY PROTEIN
    Barbara Clark; Fiscal Year: 2005
    ..This will ultimately lead to a better understanding of potential developmental or disease states that result from aberrant over- or under-expression of StAR in a cell-specific manner. ..
  29. Calcium entry and vascular smooth muscle excitation
    KENNETH BYRON; Fiscal Year: 2006
    ..abstract_text> ..
  30. PROTOCOLS FOR MATURING AND FREEZING MONKEY OOCYTES
    Catherine VandeVoort; Fiscal Year: 2006
    ..abstract_text> ..
  31. SNARE PROTEINS IN PLATELET ALPHA-GRANULE SECRETION
    Robert Flaumenhaft; Fiscal Year: 2007
    ..abstract_text> ..
  32. Binge Ethanol and Oocyte Quality
    Catherine A Vandevoort; Fiscal Year: 2010
    ..The outcome of this project will have direct relevance to the effects of binge drinking in women. ..
  33. Regulation of Interleukin-5 Receptor Signaling
    MAGARITA MARTINEZ MOCZYGEMBA; Fiscal Year: 2003
    ..In addition, eosinophils from IL-5 transgenic mice will be isolated and analyzed for their ability to be further stimulated by GM-CSF or IL-3 in vitro. ..
  34. Effects of Fetal Bisphenol A Exposure on Oogenesis in Primates
    CATHERINE A contact VANDEVOORT; Fiscal Year: 2010
    ..Because the dose used will be similar to current human blood levels of BPA, the results should have direct relevance to human health. ..
  35. Dopamine Transporter Regulation in Rat Brain
    BRIAN HOOVER; Fiscal Year: 2004
    ..These studies will help elucidate the biochemical mechanisms underlying DAT regulation in brain under both physiological and drug-exposed conditions. ..
  36. Regulation of Mammalian Oocyte Maturation
    Stephen Downs; Fiscal Year: 2007
    ..Furthermore, these studies will benefit the development of in vitro systems where either meiotic arrest or completion of meiotic maturation is the desired endpoint. ..
  37. LIPID/LIPOPROTEIN METABOLISM AND CARDIOVASCULAR DISEASES
    KAFAIT MALIK; Fiscal Year: 2007
    ..It is also our intention to provide postdoctoral trainees some experience in grant writing. ..
  38. Tissue Transglutaminase in Neurologic Injury
    THUNG SHEN LAI; Fiscal Year: 2007
    ..The inhibitors will be used to investigate the role of TTG in the pathogenesis of expanded polyQ diseases. Current proposal will lead to new therapy for HD and other neurologic disorders. [unreadable] [unreadable] [unreadable]..