Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
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James R. Porter | J. Sydor | J. Adams | V. Palombella | M. Dembski | Yun Gao | J. Tong | J. Patterson | L. Grenier | J. Ge | J. R. Porter | E. Normant | J. Ali | A. T. Georges | R. Pak | T. Tibbitts | Asimina T. Georges
[1] B. Blagg,et al. Radanamycin, a macrocyclic chimera of radicicol and geldanamycin. , 2006, Bioorganic & medicinal chemistry letters.
[2] S. Jagannath,et al. Update on Phase I Clinical Trial of IPI-504, a Novel, Water-Soluble Hsp90 Inhibitor, in Patients with Relapsed/Refractory Multiple Myeloma (MM). , 2005 .
[3] Yves L Janin,et al. Heat shock protein 90 inhibitors. A text book example of medicinal chemistry? , 2005, Journal of medicinal chemistry.
[4] David Siegel,et al. Formation of 17-allylamino-demethoxygeldanamycin (17-AAG) hydroquinone by NAD(P)H:quinone oxidoreductase 1: role of 17-AAG hydroquinone in heat shock protein 90 inhibition. , 2005, Cancer research.
[5] R. Immormino,et al. Structure of Unliganded GRP94, the Endoplasmic Reticulum Hsp90 , 2005, Journal of Biological Chemistry.
[6] A. Lowell,et al. Epidermal growth factor receptors harboring kinase domain mutations associate with the heat shock protein 90 chaperone and are destabilized following exposure to geldanamycins. , 2005, Cancer research.
[7] S. Lakhani,et al. Phase I pharmacokinetic and pharmacodynamic study of 17-allylamino, 17-demethoxygeldanamycin in patients with advanced malignancies. , 2005, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[8] Xavier Barril,et al. Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. , 2005, Journal of medicinal chemistry.
[9] P. Richardson,et al. Dose escalating trial of 17-AAG with bortezomib (BZ) in patients with relapsed refractory multiple myeloma (MM) , 2005 .
[10] Kedar Patel,et al. Engineered biosynthesis of geldanamycin analogs for Hsp90 inhibition. , 2004, Chemistry & biology.
[11] S. Jackson,et al. Independent ATPase activity of Hsp90 subunits creates a flexible assembly platform. , 2004, Journal of molecular biology.
[12] R. Immormino,et al. Ligand-induced Conformational Shift in the N-terminal Domain of GRP94, an Hsp90 Chaperone* , 2004, Journal of Biological Chemistry.
[13] D. Solit,et al. Hsp90: the vulnerable chaperone. , 2004, Drug discovery today.
[14] Yaoquan Liu,et al. Synthesis and biological activities of novel 17-aminogeldanamycin derivatives. , 2004, Bioorganic & medicinal chemistry.
[15] T. Isobe,et al. IC101 Induces Apoptosis by Akt Dephosphorylation via an Inhibition of Heat Shock Protein 90-ATP Binding Activity Accompanied by Preventing the Interaction with Akt in L1210 Cells , 2004, Journal of Pharmacology and Experimental Therapeutics.
[16] N. Rosen,et al. Development of a Fluorescence Polarization Assay for the Molecular Chaperone Hsp90 , 2004, Journal of biomolecular screening.
[17] L. Whitesell,et al. Altered Hsp90 function in cancer: a unique therapeutic opportunity. , 2004, Molecular cancer therapeutics.
[18] A. Kamal,et al. Synthesis and biological evaluation of a new class of geldanamycin derivatives as potent inhibitors of Hsp90. , 2004, Journal of Medicinal Chemistry.
[19] S. Larson,et al. Phase 1 pharmacokinetic and pharmacodynamic trial of docetaxel and 17AAG (17-allylamino-17-demethoxygeldanamycin). , 2004, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[20] L. Neckers,et al. Quantum chemical calculations and mutational analysis suggest heat shock protein 90 catalyzes trans-cis isomerization of geldanamycin. , 2004, Chemistry & biology.
[21] N. Rosen,et al. Targeting wide-range oncogenic transformation via PU24FCl, a specific inhibitor of tumor Hsp90. , 2004, Chemistry & biology.
[22] P. Workman. Combinatorial attack on multistep oncogenesis by inhibiting the Hsp90 molecular chaperone. , 2004, Cancer letters.
[23] P. Csermely,et al. Inhibition of Hsp90: a new strategy for inhibiting protein kinases. , 2004, Biochimica et biophysica acta.
[24] W. Stolz,et al. Induction of Hsp90 protein expression in malignant melanomas and melanoma metastases , 2004, Experimental dermatology.
[25] L. Müller,et al. Hsp70 and Hsp90--a relay team for protein folding. , 2004, Reviews of physiology, biochemistry and pharmacology.
[26] C. Nicchitta,et al. Structure of the N-terminal Domain of GRP94 , 2003, Journal of Biological Chemistry.
[27] N. Rosen,et al. Synthesis of novel fluorescent probes for the molecular chaperone Hsp90. , 2003, Bioorganic & medicinal chemistry letters.
[28] L. Fritz,et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors , 2003, Nature.
[29] L. Neckers,et al. Cancer: The rules of attraction , 2003, Nature.
[30] Andreas Schirmer,et al. Filter binding assay for the geldanamycin-heat shock protein 90 interaction. , 2003, Analytical biochemistry.
[31] Giulio Rastelli,et al. Crystal structure and molecular modeling of 17-DMAG in complex with human Hsp90. , 2003, Chemistry & biology.
[32] L. Neckers,et al. Heat shock protein 90 as a molecular target for cancer therapeutics. , 2003, Cancer cell.
[33] 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.
[34] N. Rosen,et al. Degradation of HER2 by ansamycins induces growth arrest and apoptosis in cells with HER2 overexpression via a HER3, phosphatidylinositol 3'-kinase-AKT-dependent pathway. , 2002, Cancer research.
[35] Sung Gyoo Park,et al. Proteome analysis of hepatocellular carcinoma. , 2002, Biochemical and biophysical research communications.
[36] B. Seed,et al. Endoplasmic reticulum chaperone gp96 is required for innate immunity but not cell viability , 2001, Nature Cell Biology.
[37] 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.
[38] 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.
[39] J. Peyrat,et al. Proteomic detection of changes in protein synthesis induced by fibroblast growth factor-2 in MCF-7 human breast cancer cells. , 2001, Experimental cell research.
[40] P. Sale,et al. Heat shock protein-90, IL-6 and IL-10 in bladder cancer. , 2000, Anticancer Research.
[41] C. Nicchitta,et al. Ligand Interactions in the Adenosine Nucleotide-binding Domain of the Hsp90 Chaperone, GRP94 , 2000, The Journal of Biological Chemistry.
[42] L. Neckers,et al. The heat shock protein 90 antagonist geldanamycin alters chaperone association with p210bcr-abl and v-src proteins before their degradation by the proteasome. , 2000, Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research.
[43] Y. Moriyama,et al. Overexpression and localization of heat shock proteins mRNA in pancreatic carcinoma. , 2000, Journal of Nippon Medical School = Nippon Ika Daigaku zasshi.
[44] 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.
[45] M. Egorin,et al. Metabolism of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) by murine and human hepatic preparations. , 1998, Cancer research.
[46] M. Galigniana,et al. The Role of DnaJ-like Proteins in Glucocorticoid Receptor·hsp90 Heterocomplex Assembly by the Reconstituted hsp90·p60·hsp70 Foldosome Complex* , 1998, The Journal of Biological Chemistry.
[47] L. Neckers,et al. Geldanamycin-induced destabilization of Raf-1 involves the proteasome. , 1997, Biochemical and biophysical research communications.
[48] L. Pearl,et al. Identification and Structural Characterization of the ATP/ADP-Binding Site in the Hsp90 Molecular Chaperone , 1997, Cell.
[49] P. Sutphin,et al. Geldanamycin-stimulated destabilization of mutated p53 is mediated by the proteasome in vivo , 1997, Oncogene.
[50] Neal Rosen,et al. Crystal Structure of an Hsp90–Geldanamycin Complex: Targeting of a Protein Chaperone by an Antitumor Agent , 1997, Cell.
[51] E. Alnemri,et al. Nucleotides and Two Functional States of hsp90* , 1997, The Journal of Biological Chemistry.
[52] P. Miller,et al. erbB-2 oncogene inhibition by geldanamycin derivatives: synthesis, mechanism of action, and structure-activity relationships. , 1995, Journal of medicinal chemistry.
[53] C. Diorio,et al. Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives. , 1995, Journal of medicinal chemistry.
[54] P. Rose,et al. Analysis of heat‐shock protein expression in myeloid leukaemia cells by flow cytometry , 1995, British journal of haematology.
[55] 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.
[56] M. Ferrarini,et al. Unusual expression and localization of heat‐shock proteins in human tumor cells , 1992, International journal of cancer.
[57] H. Nawata,et al. High constitutive expression of heat shock protein 90α in human acute leukemia cells , 1992 .
[58] R. Coombes,et al. Clinical and biological significance of HSP89 alpha in human breast cancer , 1992, International journal of cancer.
[59] B. Lai,et al. Quantitation and intracellular localization of the 85K heat shock protein by using monoclonal and polyclonal antibodies , 1984, Molecular and cellular biology.
[60] M. Muroi,et al. Macbecins I and II, new antitumor antibiotics. II. Isolation and characterization. , 1980, The Journal of antibiotics.