Targeting multiple signal transduction pathways through inhibition of Hsp90

[1]  D. Auclair,et al.  BAY 43-9006 Exhibits Broad Spectrum Oral Antitumor Activity and Targets the RAF/MEK/ERK Pathway and Receptor Tyrosine Kinases Involved in Tumor Progression and Angiogenesis , 2004, Cancer Research.

[2]  W. Hiddemann,et al.  Mutations in the tyrosine kinase domain of FLT3 define a new molecular mechanism of acquired drug resistance to PTK inhibitors in FLT3-ITD-transformed hematopoietic cells. , 2004, Blood.

[3]  Yosef Yarden,et al.  The Achilles Heel of ErbB-2/HER2: Regulation by the Hsp90 Chaperone Machine and Potential for Pharmacological Intervention , 2004, Cell cycle.

[4]  L. Neckers,et al.  Heat shock protein 90 , 2003, Current opinion in oncology.

[5]  John H Kersey,et al.  FLT3 expressing leukemias are selectively sensitive to inhibitors of the molecular chaperone heat shock protein 90 through destabilization of signal transduction-associated kinases. , 2003, Clinical cancer research : an official journal of the American Association for Cancer Research.

[6]  E. Sausville,et al.  Clinical development of 17-allylamino, 17-demethoxygeldanamycin. , 2003, Current cancer drug targets.

[7]  L. Pearl,et al.  Structure and functional relationships of Hsp90. , 2003, Current cancer drug targets.

[8]  L. Fritz,et al.  A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors , 2003, Nature.

[9]  J. Radich,et al.  The role of FLT3 in haematopoietic malignancies , 2003, Nature Reviews Cancer.

[10]  I. Bernstein,et al.  Activating mutations of RTK/ras signal transduction pathway in pediatric acute myeloid leukemia. , 2003, Blood.

[11]  Shile Huang,et al.  Targeting mTOR signaling for cancer therapy. , 2003, Current opinion in pharmacology.

[12]  G. Mills,et al.  Loss of PTEN/MMAC1/TEP in EGF receptor-expressing tumor cells counteracts the antitumor action of EGFR tyrosine kinase inhibitors , 2003, Oncogene.

[13]  A. Olshen,et al.  Inhibition of heat shock protein 90 function down-regulates Akt kinase and sensitizes tumors to Taxol. , 2003, Cancer research.

[14]  L. Neckers Development of small molecule Hsp90 inhibitors: utilizing both forward and reverse chemical genomics for drug identification. , 2003, Current medicinal chemistry.

[15]  J. Marshall,et al.  Activity of the Raf kinase inhibitor BAY 43-9006 in patients with advanced solid tumors. , 2003, Clinical colorectal cancer.

[16]  P. Ladenson,et al.  BRAF mutation in papillary thyroid carcinoma. , 2003, Journal of the National Cancer Institute.

[17]  S. Silberman,et al.  Imatinib: a targeted clinical drug development. , 2003, Seminars in hematology.

[18]  C. Arteaga Inhibiting Tyrosine Kinases: Successes and Limitations , 2003, Cancer biology & therapy.

[19]  H. Fuse,et al.  Involvement of heat-shock protein 90 in the interleukin-6-mediated signaling pathway through STAT3. , 2003, Biochemical and biophysical research communications.

[20]  N. Rosen,et al.  Development of a purine-scaffold novel class of Hsp90 binders that inhibit the proliferation of cancer cells and induce the degradation of Her2 tyrosine kinase. , 2002, Bioorganic & medicinal chemistry.

[21]  S. Wilhelm,et al.  BAY 43-9006: preclinical data. , 2002, Current pharmaceutical design.

[22]  N. Rosen,et al.  Akt Forms an Intracellular Complex with Heat Shock Protein 90 (Hsp90) and Cdc37 and Is Destabilized by Inhibitors of Hsp90 Function* , 2002, The Journal of Biological Chemistry.

[23]  R. Jove,et al.  Molecular characterization and sensitivity of STI-571 (imatinib mesylate, Gleevec)-resistant, Bcr-Abl-positive, human acute leukemia cells to SRC kinase inhibitor PD180970 and 17-allylamino-17-demethoxygeldanamycin. , 2002, Cancer research.

[24]  Gabriela Chiosis,et al.  BCR-ABL point mutants isolated from patients with imatinib mesylate-resistant chronic myeloid leukemia remain sensitive to inhibitors of the BCR-ABL chaperone heat shock protein 90. , 2002, Blood.

[25]  K. Gibson,et al.  ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. , 2002, Cancer research.

[26]  J. Dancey Clinical development of mammalian target of rapamycin inhibitors. , 2002, Hematology/oncology clinics of North America.

[27]  P. Chène,et al.  ATPases as drug targets: learning from their structure , 2002, Nature Reviews Drug Discovery.

[28]  R. Bookstein,et al.  Mutations to CCI-779 PTEN Enhanced Sensitivity of Multiple Myeloma Cells Containing Updated Version , 2002 .

[29]  C. Sawyers,et al.  The phosphatidylinositol 3-Kinase–AKT pathway in human cancer , 2002, Nature Reviews Cancer.

[30]  A. Nicholson,et al.  Mutations of the BRAF gene in human cancer , 2002, Nature.

[31]  A. Ishida,et al.  Involvement of Hsp90 in Signaling and Stability of 3-Phosphoinositide-dependent Kinase-1* , 2002, The Journal of Biological Chemistry.

[32]  P. Csermely,et al.  A Nucleotide-dependent Molecular Switch Controls Atp Binding at the C-terminal Domain of Hsp90 N-terminal Nucleotide Binding Unmasks a C-terminal Binding Pocket* , 2022 .

[33]  N. Rosen,et al.  Ansamycin antibiotics inhibit Akt activation and cyclin D expression in breast cancer cells that overexpress HER2 , 2002, Oncogene.

[34]  D. Goeddel,et al.  TNF-induced recruitment and activation of the IKK complex require Cdc37 and Hsp90. , 2002, Molecular cell.

[35]  P. Workman,et al.  HSP90 as a new therapeutic target for cancer therapy: the story unfolds , 2002, Expert opinion on biological therapy.

[36]  M. Shimizu,et al.  Stereospecific antitumor activity of radicicol oxime derivatives , 2001, Cancer Chemotherapy and Pharmacology.

[37]  R. Gaynor,et al.  Regulation of β-Catenin Function by the IκB Kinases* , 2001, The Journal of Biological Chemistry.

[38]  G. Bollag,et al.  Discovery of a novel Raf kinase inhibitor. , 2001, Endocrine-related cancer.

[39]  D. Schrump,et al.  Enhancement of paclitaxel-mediated cytotoxicity in lung cancer cells by 17-allylamino geldanamycin: in vitro and in vivo analysis. , 2001, The Annals of thoracic surgery.

[40]  T. Naoe,et al.  FLT3 tyrosine kinase as a target molecule for selective antileukemia therapy , 2001, Cancer Chemotherapy and Pharmacology.

[41]  P. N. Rao,et al.  Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or Amplification , 2001, Science.

[42]  K. Bhalla,et al.  Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts. , 2001, Cancer research.

[43]  N. Rosen,et al.  A small molecule designed to bind to the adenine nucleotide pocket of Hsp90 causes Her2 degradation and the growth arrest and differentiation of breast cancer cells. , 2001, Chemistry & biology.

[44]  Y. Yarden,et al.  Sensitivity of Mature ErbB2 to Geldanamycin Is Conferred by Its Kinase Domain and Is Mediated by the Chaperone Protein Hsp90* , 2001, The Journal of Biological Chemistry.

[45]  J. Turkson,et al.  Inhibition of STAT3 signaling leads to apoptosis of leukemic large granular lymphocytes and decreased Mcl-1 expression. , 2001, The Journal of clinical investigation.

[46]  L. Neckers,et al.  The Heat Shock Protein 90 Antagonist Novobiocin Interacts with a Previously Unrecognized ATP-binding Domain in the Carboxyl Terminus of the Chaperone* , 2000, The Journal of Biological Chemistry.

[47]  T. Tsuruo,et al.  Modulation of Akt kinase activity by binding to Hsp90. , 2000, Proceedings of the National Academy of Sciences of the United States of America.

[48]  L. Neckers,et al.  Novel oxime derivatives of radicicol induce erythroid differentiation associated with preferential G1 phase accumulation against chronic myelogenous leukemia cells through destabilization of Bcr-Abl with Hsp90 complex , 2000 .

[49]  P. Polakis Wnt signaling and cancer. , 2000, Genes & development.

[50]  Roy Garcia,et al.  STATs in oncogenesis , 2000, Oncogene.

[51]  L. Neckers,et al.  Novobiocin and related coumarins and depletion of heat shock protein 90-dependent signaling proteins. , 2000, Journal of the National Cancer Institute.

[52]  Michael Karin,et al.  The IκB kinase (IKK) and NF-κB: key elements of proinflammatory signalling , 2000 .

[53]  H. Itoh,et al.  A novel chaperone-activity-reducing mechanism of the 90-kDa molecular chaperone HSP90. , 1999, The Biochemical journal.

[54]  Sreenath V. Sharma,et al.  Interaction of radicicol with members of the heat shock protein 90 family of molecular chaperones. , 1999, Molecular endocrinology.

[55]  M. Sliwkowski,et al.  Nonclinical studies addressing the mechanism of action of trastuzumab (Herceptin). , 1999, Seminars in oncology.

[56]  L. Neckers,et al.  KF25706, a novel oxime derivative of radicicol, exhibits in vivo antitumor activity via selective depletion of Hsp90 binding signaling molecules. , 1999, Cancer research.

[57]  L. Pearl,et al.  Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin. , 1999, Journal of medicinal chemistry.

[58]  B. Geiger,et al.  Differential molecular interactions of beta-catenin and plakoglobin in adhesion, signaling and cancer. , 1998, Current opinion in cell biology.

[59]  L. Neckers,et al.  Antibiotic radicicol binds to the N-terminal domain of Hsp90 and shares important biologic activities with geldanamycin. , 1998, Cell stress & chaperones.

[60]  Sreenath V. Sharma,et al.  Targeting of the protein chaperone, HSP90, by the transformation suppressing agent, radicicol , 1998, Oncogene.

[61]  L. Pearl,et al.  Identification and Structural Characterization of the ATP/ADP-Binding Site in the Hsp90 Molecular Chaperone , 1997, Cell.

[62]  M. Zalutsky Growth factor receptors as molecular targets for cancer diagnosis and therapy. , 1997, The quarterly journal of nuclear medicine : official publication of the Italian Association of Nuclear Medicine (AIMN) [and] the International Association of Radiopharmacology.

[63]  Neal Rosen,et al.  Crystal Structure of an Hsp90–Geldanamycin Complex: Targeting of a Protein Chaperone by an Antitumor Agent , 1997, Cell.

[64]  L. Neckers,et al.  Destabilization of Raf-1 by geldanamycin leads to disruption of the Raf-1-MEK-mitogen-activated protein kinase signalling pathway , 1996, Molecular and cellular biology.

[65]  W. Kolch,et al.  Nerve Growth Factor-mediated Activation of the Mitogen-activated Protein (MAP) Kinase Cascade Involves a Signaling Complex Containing B-Raf and HSP90* , 1996, The Journal of Biological Chemistry.

[66]  D. Birnbaum,et al.  Human FLT3/FLK2 receptor tyrosine kinase is expressed at the surface of normal and malignant hematopoietic cells. , 1996, Leukemia.

[67]  M. Borowitz,et al.  Expression of the hematopoietic growth factor receptor FLT3 (STK-1/Flk2) in human leukemias. , 1996, Blood.

[68]  Mikhail V. Blagosklonny,et al.  Disruption of the Raf-1-Hsp90 Molecular Complex Results in Destabilization of Raf-1 and Loss of Raf-1-Ras Association (*) , 1995, The Journal of Biological Chemistry.

[69]  H. Nakano,et al.  Suppression of RAS and MOS transformation by radicicol. , 1995, Oncogene.

[70]  P. McCrea,et al.  Overexpression of cadherins and underexpression of β-catenin inhibit dorsal mesoderm induction in early Xenopus embryos , 1994, Cell.

[71]  L. Neckers,et al.  Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation. , 1994, Proceedings of the National Academy of Sciences of the United States of America.

[72]  G. Carpenter,et al.  Differential heat stress stability of epidermal growth factor receptor and erbB‐2 receptor tyrosine kinase activities , 1993, Journal of cellular physiology.

[73]  H. Kwon,et al.  Radicicol, an agent inducing the reversal of transformed phenotypes of src-transformed fibroblasts. , 1992, Bioscience, biotechnology, and biochemistry.

[74]  H Umezawa,et al.  Phenotypic change from transformed to normal induced by benzoquinonoid ansamycins accompanies inactivation of p60src in rat kidney cells infected with Rous sarcoma virus , 1986, Molecular and cellular biology.

[75]  C. Deboer,et al.  Geldanamycin, a new antibiotic. , 1970, The Journal of antibiotics.

[76]  Brian Dymock,et al.  Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures. , 2004, Bioorganic & medicinal chemistry letters.

[77]  Oliver Hantschel,et al.  Regulation of the c-Abl and Bcr–Abl tyrosine kinases , 2004, Nature Reviews Molecular Cell Biology.

[78]  B. Mellado,et al.  Mechanism of action of anti-HER2 monoclonal antibodies: scientific update on trastuzumab and 2C4. , 2003, Advances in experimental medicine and biology.

[79]  R. Gaynor,et al.  Regulation of beta-catenin function by the IkappaB kinases. , 2001, The Journal of biological chemistry.

[80]  M. Campiglio,et al.  HER2 overexpression in various tumor types, focussing on its relationship to the development of invasive breast cancer. , 2001, Annals of oncology : official journal of the European Society for Medical Oncology.

[81]  M. Karin,et al.  Phosphorylation meets ubiquitination: the control of NF-[kappa]B activity. , 2000, Annual review of immunology.

[82]  M. Karin,et al.  The I kappa B kinase (IKK) and NF-kappa B: key elements of proinflammatory signalling. , 2000, Seminars in immunology.

[83]  L. Neckers,et al.  Novel oxime derivatives of radicicol induce erythroid differentiation associated with preferential G(1) phase accumulation against chronic myelogenous leukemia cells through destabilization of Bcr-Abl with Hsp90 complex. , 2000, Blood.

[84]  L. Neckers,et al.  The benzoquinone ansamycin 17-allylamino-17-demethoxygeldanamycin binds to HSP90 and shares important biologic activities with geldanamycin , 1998, Cancer Chemotherapy and Pharmacology.