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The Gabriela Chiosis Lab: Publications

Visit PubMed for a full listing of Gabriela Chiosis’ journal articles

Pubmed is an online index of biomedical articles maintained by the U.S. National Library of Medicine and the National Institutes of Health.

  1. Guo, A.; Lu, P.; Lee, J.; Zhen, C.; Chiosis, G.; Wang, Y. L., HSP90 stabilizes B-cell receptor kinases in a multi-client interactome: PU-H71 induces CLL apoptosis in a cytoprotective microenvironment. Oncogene 2017.
  2. Tai, W.; Guzman, M. L.; Chiosis, G., The epichaperome: the power of many as the power of one. Oncoscience 2016, 3 (9-10), 266-267.
  3. Rodina, A.*; Wang, T.*; Yan, P.*; Gomes, E. D.*; Dunphy, M. P.*; Pillarsetty, N.; Koren, J.; Gerecitano, J. F.; Taldone, T.; Zong, H.; Caldas-Lopes, E.; Alpaugh, M.; Corben, A.; Riolo, M.; Beattie, B.; Pressl, C.; Peter, R. I.; Xu, C.; Trondl, R.; Patel, H. J.; Shimizu, F.; Bolaender, A.; Yang, C.; Panchal, P.; Farooq, M. F.; Kishinevsky, S.; Modi, S.; Lin, O.; Chu, F.; Patil, S.; Erdjument-Bromage, H.; Zanzonico, P.; Hudis, C.; Studer, L.; Roboz, G. J.; Cesarman, E.; Cerchietti, L.; Levine, R.; Melnick, A.; Larson, S. M.; Lewis, J. S.; Guzman, M. L.; Chiosis, G., The epichaperome is an integrated chaperome network that facilitates tumour survival. Nature 2016, 538 (7625), 397-401.
  4. Taldone, T.; Zatorska, D.; Ochiana, S. O.; Smith-Jones, P.; Koziorowski, J.; Dunphy, M. P.; Zanzonico, P.; Bolaender, A.; Lewis, J. S.; Larson, S. M.; Chiosis, G.; Pillarsetty, N. V., Radiosynthesis of the iodine-124 labeled Hsp90 inhibitor PU-H71. J Labelled Comp Radiopharm 2016, 59 (3), 129-32.
  5.  Shrestha, L.; Patel, H. J.; Chiosis, G., Chemical Tools to Investigate Mechanisms Associated with HSP90 and HSP70 in Disease. Cell Chem Biol 2016, 23 (1), 158-72.
  6.  Patel, M. R.; Kozuch, S. D.; Cultrara, C. N.; Yadav, R.; Huang, S.; Samuni, U.; Koren, J., 3rd; Chiosis, G.; Sabatino, D., RNAi Screening of the Glucose-Regulated Chaperones in Cancer with Self-Assembled siRNA Nanostructures. Nano Lett 2016.
  7.  Culjkovic-Kraljacic, B.; Fernando, T. M.; Marullo, R.; Calvo-Vidal, N.; Verma, A.; Yang, S.; Tabbo, F.; Gaudiano, M.; Zahreddine, H.; Goldstein, R. L.; Patel, J.; Taldone, T.; Chiosis, G.; Ladetto, M.; Ghione, P.; Machiorlatti, R.; Elemento, O.; Inghirami, G.; Melnick, A.; Borden, K. L.; Cerchietti, L., Combinatorial targeting of nuclear export and translation of RNA inhibits aggressive B-cell lymphomas. Blood 2016, 127 (7), 858-68.
  8.  Chiosis, G., Editorial (Thematic Issue: Heat Shock Proteins in Disease - From Molecular Mechanisms to Therapeutics). Curr Top Med Chem 2016, 16 (25), 2727-8.
  9.  Carney, B.; Carlucci, G.; Salinas, B.; Di Gialleonardo, V.; Kossatz, S.; Vansteene, A.; Longo, V. A.; Bolaender, A.; Chiosis, G.; Keshari, K. R.; Weber, W. A.; Reiner, T., Non-invasive PET Imaging of PARP1 Expression in Glioblastoma Models. Mol Imaging Biol 2016, 18 (3), 386-92.
  10.  Ansa-Addo, E. A.; Thaxton, J.; Hong, F.; Wu, B. X.; Zhang, Y.; Fugle, C. W.; Metelli, A.; Riesenberg, B.; Williams, K.; Gewirth, D. T.; Chiosis, G.; Liu, B.; Li, Z., Clients and Oncogenic Roles of Molecular Chaperone gp96/grp94. Curr Top Med Chem 2016, 16 (25), 2765-78.
  11.  Zong, H.; Gozman, A.; Caldas-Lopes, E.; Taldone, T.; Sturgill, E.; Brennan, S.; Ochiana, S. O.; Gomes-DaGama, E. M.; Sen, S.; Rodina, A.; Koren, J., 3rd; Becker, M. W.; Rudin, C. M.; Melnick, A.; Levine, R. L.; Roboz, G. J.; Nimer, S. D.; Chiosis, G.; Guzman, M. L., A Hyperactive Signalosome in Acute Myeloid Leukemia Drives Addiction to a Tumor-Specific Hsp90 Species. Cell Rep 2015, 13 (10), 2159-73.
  12.  Salinas, B.; Irwin, C. P.; Kossatz, S.; Bolaender, A.; Chiosis, G.; Pillarsetty, N.; Weber, W. A.; Reiner, T., Radioiodinated PARP1 tracers for glioblastoma imaging. EJNMMI Res 2015, 5 (1), 123.
  13.  Rachidi, S.; Sun, S.; Wu, B. X.; Jones, E.; Drake, R. R.; Ogretmen, B.; Cowart, L. A.; Clarke, C. J.; Hannun, Y. A.; Chiosis, G.; Liu, B.; Li, Z., Endoplasmic reticulum heat shock protein gp96 maintains liver homeostasis and promotes hepatocellular carcinogenesis. J Hepatol 2015, 62 (4), 879-88.
  14.  Patel, H. J.; Patel, P. D.; Ochiana, S. O.; Yan, P.; Sun, W.; Patel, M. R.; Shah, S. K.; Tramentozzi, E.; Brooks, J.; Bolaender, A.; Shrestha, L.; Stephani, R.; Finotti, P.; Leifer, C.; Li, Z.; Gewirth, D. T.; Taldone, T.; Chiosis, G., Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94. J Med Chem 2015, 58 (9), 3922-43.
  15.  Needham, P. G.; Patel, H. J.; Chiosis, G.; Thibodeau, P. H.; Brodsky, J. L., Mutations in the Yeast Hsp70, Ssa1, at P417 Alter ATP Cycling, Interdomain Coupling, and Specific Chaperone Functions. J Mol Biol 2015, 427 (18), 2948-65.
  16.  Kucine, N.; Marubayashi, S.; Bhagwat, N.; Papalexi, E.; Koppikar, P.; Sanchez Martin, M.; Dong, L.; Tallman, M. S.; Paietta, E.; Wang, K.; He, J.; Lipson, D.; Stephens, P.; Miller, V.; Rowe, J. M.; Teruya-Feldstein, J.; Mullighan, C. G.; Ferrando, A. A.; Krivtsov, A.; Armstrong, S.; Leung, L.; Ochiana, S. O.; Chiosis, G.; Levine, R. L.; Kleppe, M., Tumor-specific HSP90 inhibition as a therapeutic approach in JAK-mutant acute lymphoblastic leukemias. Blood 2015, 126 (22), 2479-83.
  17.  Kaittanis, C.; Shaffer, T. M.; Bolaender, A.; Appelbaum, Z.; Appelbaum, J.; Chiosis, G.; Grimm, J., Multifunctional MRI/PET Nanobeacons Derived from the in Situ Self-Assembly of Translational Polymers and Clinical Cargo through Coalescent Intermolecular Forces. Nano Lett 2015, 15 (12), 8032-43.
  18.  Goldstein, R. L.; Yang, S. N.; Taldone, T.; Chang, B.; Gerecitano, J.; Elenitoba-Johnson, K.; Shaknovich, R.; Tam, W.; Leonard, J. P.; Chiosis, G.; Cerchietti, L.; Melnick, A., Pharmacoproteomics identifies combinatorial therapy targets for diffuse large B cell lymphoma. J Clin Invest 2015, 125 (12), 4559-71.
  19.  Taldone, T.; Patel, H. J.; Bolaender, A.; Patel, M. R.; Chiosis, G., Protein chaperones: a composition of matter review (2008 - 2013). Expert Opin Ther Pat 2014, 24 (5), 501-18.
  20.  Taldone, T.; Ochiana, S. O.; Patel, P. D.; Chiosis, G., Selective targeting of the stress chaperome as a therapeutic strategy. Trends Pharmacol Sci 2014, 35 (11), 592-603.
  21.  Taldone, T.; Kang, Y.; Patel, H. J.; Patel, M. R.; Patel, P. D.; Rodina, A.; Patel, Y.; Gozman, A.; Maharaj, R.; Clement, C. C.; Lu, A.; Young, J. C.; Chiosis, G., Heat shock protein 70 inhibitors. 2. 2,5’-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70. J Med Chem 2014, 57 (4), 1208-24.
  22.  Rodina, A.; Taldone, T.; Kang, Y.; Patel, P. D.; Koren, J., 3rd; Yan, P.; DaGama Gomes, E. M.; Yang, C.; Patel, M. R.; Shrestha, L.; Ochiana, S. O.; Santarossa, C.; Maharaj, R.; Gozman, A.; Cox, M. B.; Erdjument-Bromage, H.; Hendrickson, R. C.; Cerchietti, L.; Melnick, A.; Guzman, M. L.; Chiosis, G., Affinity purification probes of potential use to investigate the endogenous Hsp70 interactome in cancer. ACS Chem Biol 2014, 9 (8), 1698-705.
  23.  Rampal, R.; Ahn, J.; Abdel-Wahab, O.; Nahas, M.; Wang, K.; Lipson, D.; Otto, G. A.; Yelensky, R.; Hricik, T.; McKenney, A. S.; Chiosis, G.; Chung, Y. R.; Pandey, S.; van den Brink, M. R.; Armstrong, S. A.; Dogan, A.; Intlekofer, A.; Manshouri, T.; Park, C. Y.; Verstovsek, S.; Rapaport, F.; Stephens, P. J.; Miller, V. A.; Levine, R. L., Genomic and functional analysis of leukemic transformation of myeloproliferative neoplasms. Proc Natl Acad Sci U S A 2014, 111 (50), E5401-10.
  24.  Rachidi S, Sun S, Wu BX, Jones E, Drake RR, Ogretmen B, Cowart A, Clarke CJ, Hannun YA, Chiosis G, Liu B, Li Z. Endoplasmic reticulum heat shock protein gp96 maintains liver homeostasis and promotes hepatocellular carcinogenesis. J Hepatol. 2014 Nov 22. pii: S0168-8278(14)00854-X. [Epub ahead of print]
  25.  Kang, Y.; Taldone, T.; Patel, H. J.; Patel, P. D.; Rodina, A.; Gozman, A.; Maharaj, R.; Clement, C. C.; Patel, M. R.; Brodsky, J. L.; Young, J. C.; Chiosis, G., Heat shock protein 70 inhibitors. 1. 2,5’-thiodipyrimidine and 5-(phenylthio)pyrimidine acrylamides as irreversible binders to an allosteric site on heat shock protein 70. J Med Chem 2014, 57 (4), 1188-207.
  26.  Kaittanis, C.; Shaffer, T. M.; Ogirala, A.; Santra, S.; Perez, J. M.; Chiosis, G.; Li, Y.; Josephson, L.; Grimm, J., Environment-responsive nanophores for therapy and treatment monitoring via molecular MRI quenching. Nat Commun 2014, 5, 3384.
  27.  Jhaveri, K.; Ochiana, S. O.; Dunphy, M. P.; Gerecitano, J. F.; Corben, A. D.; Peter, R. I.; Janjigian, Y. Y.; Gomes-DaGama, E. M.; Koren, J., 3rd; Modi, S.; Chiosis, G., Heat shock protein 90 inhibitors in the treatment of cancer: current status and future directions. Expert Opin Investig Drugs 2014, 23 (5), 611-28.
  28.  Corben, A. D.; Uddin, M. M.; Crawford, B.; Farooq, M.; Modi, S.; Gerecitano, J.; Chiosis, G.; Alpaugh, M. L., Ex vivo treatment response of primary tumors and/or associated metastases for preclinical and clinical development of therapeutics. J Vis Exp 2014,  (92), e52157.
  29.  Chan, C. T.; Qi, J.; Smith, W.; Paranol, R.; Mazitschek, R.; West, N.; Reeves, R.; Chiosis, G.; Schreiber, S. L.; Bradner, J. E.; Paulmurugan, R.; Gambhir, S. S., Syntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects. Cancer Res 2014, 74 (24), 7475-86.
  30.  Carman, A.; Kishinevsky, S.; Koren, J., 3rd; Luo, W.; Chiosis, G., Regulatory chaperone complexes in neurodegenerative diseases: a perspective on therapeutic intervention. Curr Alzheimer Res 2014, 11 (1), 59-68.
  31.  Bhagwat, N.; Koppikar, P.; Keller, M.; Marubayashi, S.; Shank, K.; Rampal, R.; Qi, J.; Kleppe, M.; Patel, H. J.; Shah, S. K.; Taldone, T.; Bradner, J. E.; Chiosis, G.; Levine, R. L., Improved targeting of JAK2 leads to increased therapeutic efficacy in myeloproliferative neoplasms. Blood 2014, 123 (13), 2075-83.
  32.  Azoitei, N.; Diepold, K.; Brunner, C.; Rouhi, A.; Genze, F.; Becher, A.; Kestler, H.; van Lint, J.; Chiosis, G.; Koren, J., 3rd; Frohling, S.; Scholl, C.; Seufferlein, T., HSP90 supports tumor growth and angiogenesis through PRKD2 protein stabilization. Cancer Res 2014, 74 (23), 7125-36.
  33.  Ambati, S. R.; Lopes, E. C.; Kosugi, K.; Mony, U.; Zehir, A.; Shah, S. K.; Taldone, T.; Moreira, A. L.; Meyers, P. A.; Chiosis, G.; Moore, M. A., Pre-clinical efficacy of PU-H71, a novel HSP90 inhibitor, alone and in combination with bortezomib in Ewing sarcoma. Mol Oncol 2014, 8 (2), 323-36.
  34.  Taldone, T.; Rodina, A.; Dagama Gomes, E. M.; Riolo, M.; Patel, H. J.; Alonso-Sabadell, R.; Zatorska, D.; Patel, M. R.; Kishinevsky, S.; Chiosis, G., Synthesis and evaluation of cell-permeable biotinylated PU-H71 derivatives as tumor Hsp90 probes. Beilstein J Org Chem 2013, 9, 544-56.
  35.  Taldone, T.; Patel, P. D.; Patel, M.; Patel, H. J.; Evans, C. E.; Rodina, A.; Ochiana, S.; Shah, S. K.; Uddin, M.; Gewirth, D.; Chiosis, G., Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. J Med Chem 2013, 56 (17), 6803-18.
  36.  Shahinas, D.; Folefoc, A.; Taldone, T.; Chiosis, G.; Crandall, I.; Pillai, D. R., A purine analog synergizes with chloroquine (CQ) by targeting Plasmodium falciparum Hsp90 (PfHsp90). PLoS One 2013, 8 (9), e75446.
  37.  Rodina, A.; Patel, P. D.; Kang, Y.; Patel, Y.; Baaklini, I.; Wong, M. J.; Taldone, T.; Yan, P.; Yang, C.; Maharaj, R.; Gozman, A.; Patel, M. R.; Patel, H. J.; Chirico, W.; Erdjument-Bromage, H.; Talele, T. T.; Young, J. C.; Chiosis, G., Identification of an allosteric pocket on human hsp70 reveals a mode of inhibition of this therapeutically important protein. Chem Biol 2013, 20 (12), 1469-80.
  38.  Patel, P. D.; Yan, P.; Seidler, P. M.; Patel, H. J.; Sun, W.; Yang, C.; Que, N. S.; Taldone, T.; Finotti, P.; Stephani, R. A.; Gewirth, D. T.; Chiosis, G., Paralog-selective Hsp90 inhibitors define tumor-specific regulation of HER2. Nat Chem Biol 2013, 9 (11), 677-84.
  39.  Nayar, U.; Lu, P.; Goldstein, R. L.; Vider, J.; Ballon, G.; Rodina, A.; Taldone, T.; Erdjument-Bromage, H.; Chomet, M.; Blasberg, R.; Melnick, A.; Cerchietti, L.; Chiosis, G.; Wang, Y. L.; Cesarman, E., Targeting the Hsp90-associated viral oncoproteome in gammaherpesvirus-associated malignancies. Blood 2013, 122 (16), 2837-47.
  40.  Lisi, L.; McGuire, S.; Sharp, A.; Chiosis, G.; Navarra, P.; Feinstein, D. L.; Dello Russo, C., The novel HSP90 inhibitor, PU-H71, suppresses glial cell activation but weakly affects clinical signs of EAE. J Neuroimmunol 2013, 255 (1-2), 1-7.
  41.  Janjigian, Y. Y.; Viola-Villegas, N.; Holland, J. P.; Divilov, V.; Carlin, S. D.; Gomes-DaGama, E. M.; Chiosis, G.; Carbonetti, G.; de Stanchina, E.; Lewis, J. S., Monitoring afatinib treatment in HER2-positive gastric cancer with 18F-FDG and 89Zr-trastuzumab PET. J Nucl Med 2013, 54 (6), 936-43.
  42.  Hua, Y.; White-Gilbertson, S.; Kellner, J.; Rachidi, S.; Usmani, S. Z.; Chiosis, G.; Depinho, R.; Li, Z.; Liu, B., Molecular chaperone gp96 is a novel therapeutic target of multiple myeloma. Clin Cancer Res 2013, 19 (22), 6242-51.
  43.  Hong, F.; Liu, B.; Chiosis, G.; Gewirth, D. T.; Li, Z., alpha7 helix region of alphaI domain is crucial for integrin binding to endoplasmic reticulum chaperone gp96: a potential therapeutic target for cancer metastasis. J Biol Chem 2013, 288 (25), 18243-8.
  44.  Chiosis, G.; Dickey, C. A.; Johnson, J. L., A global view of Hsp90 functions. Nat Struct Mol Biol 2013, 20 (1), 1-4.
  45. Carman, A.; Kishinevsky, S.; Koren, J., 3rd; Lou, W.; Chiosis, G., Chaperone-dependent Neurodegeneration: A Molecular Perspective on Therapeutic Intervention. J Alzheimers Dis Parkinsonism 2013, (Suppl 10).
  46.  Beebe, K.; Mollapour, M.; Scroggins, B.; Prodromou, C.; Xu, W.; Tokita, M.; Taldone, T.; Pullen, L.; Zierer, B. K.; Lee, M. J.; Trepel, J.; Buchner, J.; Bolon, D.; Chiosis, G.; Neckers, L., Posttranslational modification and conformational state of heat shock protein 90 differentially affect binding of chemically diverse small molecule inhibitors. Oncotarget 2013, 4 (7), 1065-74.
  47.  Koppikar, P.; Bhagwat, N.; Kilpivaara, O.; Manshouri, T.; Adli, M.; Hricik, T.; Liu, F.; Saunders, L. M.; Mullally, A.; Abdel-Wahab, O.; Leung, L.; Weinstein, A.; Marubayashi, S.; Goel, A.; Gonen, M.; Estrov, Z.; Ebert, B. L.; Chiosis, G.; Nimer, S. D.; Bernstein, B. E.; Verstovsek, S.; Levine, R. L., Heterodimeric JAK-STAT activation as a mechanism of persistence to JAK2 inhibitor therapy. Nature 2012, 489 (7414), 155-9.
  48.  Jhaveri, K.; Taldone, T.; Modi, S.; Chiosis, G., Advances in the clinical development of heat shock protein 90 (Hsp90) inhibitors in cancers. Biochim Biophys Acta 2012, 1823 (3), 742-55.
  49.  Chan, C. T.; Reeves, R. E.; Geller, R.; Yaghoubi, S. S.; Hoehne, A.; Solow-Cordero, D. E.; Chiosis, G.; Massoud, T. F.; Paulmurugan, R.; Gambhir, S. S., Discovery and validation of small-molecule heat-shock protein 90 inhibitors through multimodality molecular imaging in living subjects. Proc Natl Acad Sci U S A 2012, 109 (37), E2476-85.
  50.  Taldone T, Zatorska D, Patel HJ, Sun W, Patel MR, Chiosis G. Preparation of a diverse purine-scaffold library via one-step palladium catalyzed cross-coupling. Heterocycles, 87, 2013, 91 – 113
  51.  Brooks, J. C.; Sun, W.; Chiosis, G.; Leifer, C. A., Heat shock protein gp96 regulates Toll-like receptor 9 proteolytic processing and conformational stability. Biochem Biophys Res Commun 2012, 421 (4), 780-4.
  52.  Azoitei, N.; Hoffmann, C. M.; Ellegast, J. M.; Ball, C. R.; Obermayer, K.; Gossele, U.; Koch, B.; Faber, K.; Genze, F.; Schrader, M.; Kestler, H. A.; Dohner, H.; Chiosis, G.; Glimm, H.; Frohling, S.; Scholl, C., Targeting of KRAS mutant tumors by HSP90 inhibitors involves degradation of STK33. J Exp Med 2012, 209 (4), 697-711.
  53.  Sun W, Patel P, Chiosis G. An efficient copper catalyzed microwave-assisted S-arylation towards the synthesis of 8-aryl-sulfanyl adenines. SynLett 2011; 20: 3008-3012.
  54.  Usmani, S. Z.; Chiosis, G., HSP90 inhibitors as therapy for multiple myeloma. Clin Lymphoma Myeloma Leuk 2011, 11 Suppl 1, S77-81.
  55.  Taldone T, Zatorska D, Chiosis G. Reaction of 2-naphthylamine with sodium iodate/sodium sulfite: Synthesis of 2-amino-1-iodonaphthalene Synthetic Communications 2012;42(5):635-638.
  56. Taldone, T.; Zatorska, D.; Patel, P. D.; Zong, H.; Rodina, A.; Ahn, J. H.; Moulick, K.; Guzman, M. L.; Chiosis, G., Design, synthesis, and evaluation of small molecule Hsp90 probes. Bioorg Med Chem 2011, 19 (8), 2603-14.
  57.  Taldone, T.; Gomes-DaGama, E. M.; Zong, H.; Sen, S.; Alpaugh, M. L.; Zatorska, D.; Alonso-Sabadell, R.; Guzman, M. L.; Chiosis, G., Synthesis of purine-scaffold fluorescent probes for heat shock protein 90 with use in flow cytometry and fluorescence microscopy. Bioorg Med Chem Lett 2011, 21 (18), 5347-52.
  58.  Patel, H. J.; Modi, S.; Chiosis, G.; Taldone, T., Advances in the discovery and development of heat-shock protein 90 inhibitors for cancer treatment. Expert Opin Drug Discov 2011, 6 (5), 559-587.
  59.  Moulick, K.; Ahn, J. H.; Zong, H.; Rodina, A.; Cerchietti, L.; Gomes DaGama, E. M.; Caldas-Lopes, E.; Beebe, K.; Perna, F.; Hatzi, K.; Vu, L. P.; Zhao, X.; Zatorska, D.; Taldone, T.; Smith-Jones, P.; Alpaugh, M.; Gross, S. S.; Pillarsetty, N.; Ku, T.; Lewis, J. S.; Larson, S. M.; Levine, R.; Erdjument-Bromage, H.; Guzman, M. L.; Nimer, S. D.; Melnick, A.; Neckers, L.; Chiosis, G., Affinity-based proteomics reveal cancer-specific networks coordinated by Hsp90. Nat Chem Biol 2011, 7 (11), 818-26.
  60.  Breinig, M.; Mayer, P.; Harjung, A.; Goeppert, B.; Malz, M.; Penzel, R.; Neumann, O.; Hartmann, A.; Dienemann, H.; Giaccone, G.; Schirmacher, P.; Kern, M. A.; Chiosis, G.; Rieker, R. J., Heat shock protein 90-sheltered overexpression of insulin-like growth factor 1 receptor contributes to malignancy of thymic epithelial tumors. Clin Cancer Res 2011, 17 (8), 2237-49.
  61.  Ahn, J. H.; Luo, W.; Kim, J.; Rodina, A.; Clement, C. C.; Aguirre, J.; Sun, W.; Kang, Y.; Maharaj, R.; Moulick, K.; Zatorska, D.; Kokoszka, M.; Brodsky, J. L.; Chiosis, G., Design of a flexible cell-based assay for the evaluation of heat shock protein 70 expression modulators. Assay Drug Dev Technol 2011, 9 (3), 236-46.
  62.  Wrona, I. E.; Gozman, A.; Taldone, T.; Chiosis, G.; Panek, J. S., Synthesis of reblastatin, autolytimycin, and non-benzoquinone analogues: potent inhibitors of heat shock protein 90. J Org Chem 2010, 75 (9), 2820-35.
  63.  Usmani, S. Z.; Bona, R. D.; Chiosis, G.; Li, Z., The anti-myeloma activity of a novel purine scaffold HSP90 inhibitor PU-H71 is via inhibition of both HSP90A and HSP90B1. J Hematol Oncol 2010, 3, 40.
  64.  Taldone, T.; Gillan, V.; Sun, W.; Rodina, A.; Patel, P.; Maitland, K.; O’Neill, K.; Chiosis, G.; Devaney, E., Assay strategies for the discovery and validation of therapeutics targeting Brugia pahangi Hsp90. PLoS Negl Trop Dis 2010, 4 (6), e714.
  65.  Taldone, T., Zatorska, D., Kang, Y. and Chiosis, G. A facile and efficient synthesis of d6-labelled PU-H71, a purine scaffold Hsp90 inhibitor. Journal of Labelled Compounds and Radiopharmaceuticals. 53(1), 47-49 (2010).
  66. Marubayashi, S.; Koppikar, P.; Taldone, T.; Abdel-Wahab, O.; West, N.; Bhagwat, N.; Caldas-Lopes, E.; Ross, K. N.; Gonen, M.; Gozman, A.; Ahn, J. H.; Rodina, A.; Ouerfelli, O.; Yang, G.; Hedvat, C.; Bradner, J. E.; Chiosis, G.; Levine, R. L., HSP90 is a therapeutic target in JAK2-dependent myeloproliferative neoplasms in mice and humans. J Clin Invest 2010, 120 (10), 3578-93. Highlighted in Nature/ SciBx issue September 30
  67.  Luo, W.; Sun, W.; Taldone, T.; Rodina, A.; Chiosis, G., Heat shock protein 90 in neurodegenerative diseases. Mol Neurodegener 2010, 5, 24.
  68.  Holland, J. P.; Caldas-Lopes, E.; Divilov, V.; Longo, V. A.; Taldone, T.; Zatorska, D.; Chiosis, G.; Lewis, J. S., Measuring the pharmacodynamic effects of a novel Hsp90 inhibitor on HER2/neu expression in mice using Zr-DFO-trastuzumab. PLoS One 2010, 5 (1), e8859.
  69.  Cerchietti, L. C.; Hatzi, K.; Caldas-Lopes, E.; Yang, S. N.; Figueroa, M. E.; Morin, R. D.; Hirst, M.; Mendez, L.; Shaknovich, R.; Cole, P. A.; Bhalla, K.; Gascoyne, R. D.; Marra, M.; Chiosis, G.; Melnick, A., BCL6 repression of EP300 in human diffuse large B cell lymphoma cells provides a basis for rational combinatorial therapy. J Clin Invest 2010, 120 (12), 4569-82.
  70.  Tao, H.; Kang, Y.; Taldone, T.; Chiosis, G., Microwave-assisted one step synthesis of 8-arylmethyl-9H-purin-6-amines. Bioorg Med Chem Lett 2009, 19 (2), 415-7.
  71.  Taldone, T.; Sun, W.; Chiosis, G., Discovery and development of heat shock protein 90 inhibitors. Bioorg Med Chem 2009, 17 (6), 2225-35.
  72.  Taldone, T.; Chiosis, G., Purine-scaffold Hsp90 inhibitors. Curr Top Med Chem 2009, 9 (15), 1436-46.
  73.  Chiosis, G.; Keeton, A. B., Assay for isolation of inhibitors of her2-kinase expression. Methods Mol Biol 2009, 486, 139-49.
  74. Cerchietti, L. C.; Lopes, E. C.; Yang, S. N.; Hatzi, K.; Bunting, K. L.; Tsikitas, L. A.; Mallik, A.; Robles, A. I.; Walling, J.; Varticovski, L.; Shaknovich, R.; Bhalla, K. N.; Chiosis, G.; Melnick, A., A purine scaffold Hsp90 inhibitor destabilizes BCL-6 and has specific antitumor activity in BCL-6-dependent B cell lymphomas. Nat Med 2009, 15 (12), 1369-76.
  75.  Caldas-Lopes, E.; Cerchietti, L.; Ahn, J. H.; Clement, C. C.; Robles, A. I.; Rodina, A.; Moulick, K.; Taldone, T.; Gozman, A.; Guo, Y.; Wu, N.; de Stanchina, E.; White, J.; Gross, S. S.; Ma, Y.; Varticovski, L.; Melnick, A.; Chiosis, G., Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models. Proc Natl Acad Sci U S A 2009, 106 (20), 8368-73.
  76.  Breinig, M.; Caldas-Lopes, E.; Goeppert, B.; Malz, M.; Rieker, R.; Bergmann, F.; Schirmacher, P.; Mayer, M.; Chiosis, G.; Kern, M. A., Targeting heat shock protein 90 with non-quinone inhibitors: a novel chemotherapeutic approach in human hepatocellular carcinoma. Hepatology 2009, 50 (1), 102-12.
  77.  Taldone T; Chiosis G. Discovery and Development of Heat Shock Protein 90 Inhibitors. Bioorg Med Chem. 2008 Nov 6.
  78.  Wang, L.; Xie, C.; Greggio, E.; Parisiadou, L.; Shim, H.; Sun, L.; Chandran, J.; Lin, X.; Lai, C.; Yang, W. J.; Moore, D. J.; Dawson, T. M.; Dawson, V. L.; Chiosis, G.; Cookson, M. R.; Cai, H., The chaperone activity of heat shock protein 90 is critical for maintaining the stability of leucine-rich repeat kinase 2. J Neurosci 2008, 28 (13), 3384-91.
  79.  Taldone, T.; Gozman, A.; Maharaj, R.; Chiosis, G., Targeting Hsp90: small-molecule inhibitors and their clinical development. Curr Opin Pharmacol 2008, 8 (4), 370-4.
  80.  Solit, D. B.; Chiosis, G., Development and application of Hsp90 inhibitors. Drug Discov Today 2008, 13 (1-2), 38-43.
  81.  Luo, W.; Rodina, A.; Chiosis, G., Heat shock protein 90: translation from cancer to Alzheimer’s disease treatment? BMC Neurosci 2008, 9 Suppl 2, S7.
  82.  Lopes, E. C.; Valls, E.; Figueroa, M. E.; Mazur, A.; Meng, F. G.; Chiosis, G.; Laird, P. W.; Schreiber-Agus, N.; Greally, J. M.; Prokhortchouk, E.; Melnick, A., Kaiso contributes to DNA methylation-dependent silencing of tumor suppressor genes in colon cancer cell lines. Cancer Res 2008, 68 (18), 7258-63.
  83.  Kang, Y.; Taldone, T.; Clement, C. C.; Fewell, S. W.; Aguirre, J.; Brodsky, J. L.; Chiosis, G., Design of a fluorescence polarization assay platform for the study of human Hsp70. Bioorg Med Chem Lett 2008, 18 (13), 3749-51.
  84. Goeckeler, J. L.; Petruso, A. P.; Aguirre, J.; Clement, C. C.; Chiosis, G.; Brodsky, J. L., The yeast Hsp110, Sse1p, exhibits high-affinity peptide binding. FEBS Lett 2008, 582 (16), 2393-6.
  85.  Ganesh, T.; Min, J.; Thepchatri, P.; Du, Y.; Li, L.; Lewis, I.; Wilson, L.; Fu, H.; Chiosis, G.; Dingledine, R.; Liotta, D.; Snyder, J. P.; Sun, A., Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling. Bioorg Med Chem 2008, 16 (14), 6903-10.
  86.  Didelot, C.; Lanneau, D.; Brunet, M.; Bouchot, A.; Cartier, J.; Jacquel, A.; Ducoroy, P.; Cathelin, S.; Decologne, N.; Chiosis, G.; Dubrez-Daloz, L.; Solary, E.; Garrido, C., Interaction of heat-shock protein 90beta isoform (HSP90beta) with cellular inhibitor of apoptosis 1 (c-IAP1) is required for cell differentiation. Cell Death Differ 2008.
  87.  Chan, C. T.; Paulmurugan, R.; Gheysens, O. S.; Kim, J.; Chiosis, G.; Gambhir, S. S., Molecular imaging of the efficacy of heat shock protein 90 inhibitors in living subjects. Cancer Res 2008, 68 (1), 216-26.
  88.  Rodina, A.; Vilenchik, M.; Moulick, K.; Aguirre, J.; Kim, J.; Chiang, A.; Litz, J.; Clement, C. C.; Kang, Y.; She, Y.; Wu, N.; Felts, S.; Wipf, P.; Massague, J.; Jiang, X.; Brodsky, J. L.; Krystal, G. W.; Chiosis, G., Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. Nat Chem Biol 2007, 3 (8), 498-507. Recommended Faculty of 1000 Biology
  89.  Luo, W.; Dou, F.; Rodina, A.; Chip, S.; Kim, J.; Zhao, Q.; Moulick, K.; Aguirre, J.; Wu, N.; Greengard, P.; Chiosis, G., Roles of heat-shock protein 90 in maintaining and facilitating the neurodegenerative phenotype in tauopathies. Proc Natl Acad Sci U S A 2007, 104 (22), 9511-6.
  90.  Du, Y.; Moulick, K.; Rodina, A.; Aguirre, J.; Felts, S.; Dingledine, R.; Fu, H.; Chiosis, G., High-throughput screening fluorescence polarization assay for tumor-specific Hsp90. J Biomol Screen 2007, 12 (7), 915-24.
  91.  Didelot, C.; Lanneau, D.; Brunet, M.; Joly, A. L.; De Thonel, A.; Chiosis, G.; Garrido, C., Anti-cancer therapeutic approaches based on intracellular and extracellular heat shock proteins. Curr Med Chem 2007, 14 (27), 2839-47.
  92.  Moulick, K.; Clement, C. C.; Aguirre, J.; Kim, J.; Kang, Y.; Felts, S.; Chiosis, G., Synthesis of a red-shifted fluorescence polarization probe for Hsp90. Bioorg Med Chem Lett 2006, 16 (17), 4515-8.
  93.  Immormino, R. M.; Kang, Y.; Chiosis, G.; Gewirth, D. T., Structural and quantum chemical studies of 8-aryl-sulfanyl adenine class Hsp90 inhibitors. J Med Chem 2006, 49 (16), 4953-60.
  94. Hieronymus, H.; Lamb, J.; Ross, K. N.; Peng, X. P.; Clement, C.; Rodina, A.; Nieto, M.; Du, J.; Stegmaier, K.; Raj, S. M.; Maloney, K. N.; Clardy, J.; Hahn, W. C.; Chiosis, G.; Golub, T. R., Gene expression signature-based chemical genomic prediction identifies a novel class of HSP90 pathway modulators. Cancer Cell 2006, 10 (4), 321-30.
  95.  He, H.; Zatorska, D.; Kim, J.; Aguirre, J.; Llauger, L.; She, Y.; Wu, N.; Immormino, R. M.; Gewirth, D. T.; Chiosis, G., Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90. J Med Chem 2006, 49 (1), 381-90. Featured as “Hot Paper” and “Number 1 most cited” on the American Chemical Society site.
  96.  De Martino, G.; Edler, M. C.; La Regina, G.; Coluccia, A.; Barbera, M. C.; Barrow, D.; Nicholson, R. I.; Chiosis, G.; Brancale, A.; Hamel, E.; Artico, M.; Silvestri, R., New arylthioindoles: potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies. J Med Chem 2006, 49 (3), 947-54.
  97.  Chu, F.; Maynard, J. C.; Chiosis, G.; Nicchitta, C. V.; Burlingame, A. L., Identification of novel quaternary domain interactions in the Hsp90 chaperone, GRP94. Protein Sci 2006, 15 (6), 1260-9.
  98.  Chiosis, G.; Tao, H., Purine-scaffold Hsp90 inhibitors. IDrugs 2006, 9 (11), 778-82.
  99.  Chiosis, G.; Rodina, A.; Moulick, K., Emerging Hsp90 inhibitors: from discovery to clinic. Anticancer Agents Med Chem 2006, 6 (1), 1-8.
  100.  Chiosis, G.; Neckers, L., Tumor selectivity of Hsp90 inhibitors: the explanation remains elusive. ACS Chem Biol 2006, 1 (5), 279-84.
  101.  Chiosis, G.; Caldas Lopes, E.; Solit, D., Heat shock protein-90 inhibitors: a chronicle from geldanamycin to today’s agents. Curr Opin Investig Drugs 2006, 7 (6), 534-41.
  102.  Chiosis, G.; Aguirre, J.; Nicchitta, C. V., Synthesis of Hsp90 dimerization modulators. Bioorg Med Chem Lett 2006, 16 (13), 3529-32.
  103.  Chiosis, G., Targeting chaperones in transformed systems—a focus on Hsp90 and cancer. Expert Opin Ther Targets 2006, 10 (1), 37-50.
  104.  Chiosis, G., Discovery and development of purine-scaffold Hsp90 inhibitors. Curr Top Med Chem 2006, 6 (11), 1183-91.
  105.  Brodsky, J. L.; Chiosis, G., Hsp70 molecular chaperones: emerging roles in human disease and identification of small molecule modulators. Curr Top Med Chem 2006, 6 (11), 1215-25.
  106.  Chiosis G. Molecular chaperones as targets in medicinal chemistry and drug discovery. Curr Top Med Chem 2006, 6(11):1161
  107.  Llauger, L.; He, H.; Kim, J.; Aguirre, J.; Rosen, N.; Peters, U.; Davies, P.; Chiosis, G., Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90. J Med Chem 2005, 48 (8), 2892-905.
  108.  Chiosis, G.; Brodsky, J. L., Small molecule microarrays: from proteins to mammalian cells - are we there yet? Trends Biotechnol 2005, 23 (6), 271-4.
  109. Vilenchik, M.; Solit, D.; Basso, A.; Huezo, H.; Lucas, B.; He, H.; Rosen, N.; Spampinato, C.; Modrich, P.; Chiosis, G., Targeting wide-range oncogenic transformation via PU24FCl, a specific inhibitor of tumor Hsp90. Chem Biol 2004, 11 (6), 787-97.
  110.  Kim, J.; Felts, S.; Llauger, L.; He, H.; Huezo, H.; Rosen, N.; Chiosis, G., Development of a fluorescence polarization assay for the molecular chaperone Hsp90. J Biomol Screen 2004, 9 (5), 375-81.
  111.  He, H.; Llauger, L.; Rosen, N.; Chiosis, G., General method for the synthesis of 8-arylsulfanyl adenine derivatives. J Org Chem 2004, 69 (9), 3230-2.
  112.  Chiosis, G.; Vilenchik, M.; Kim, J.; Solit, D., Hsp90: the vulnerable chaperone. Drug Discov Today 2004, 9 (20), 881-8.
  113.  Yamamoto, K.; Garbaccio, R. M.; Stachel, S. J.; Solit, D. B.; Chiosis, G.; Rosen, N.; Danishefsky, S. J., Total synthesis as a resource in the discovery of potentially valuable antitumor agents: cycloproparadicicol. Angew Chem Int Ed Engl 2003, 42 (11), 1280-4.
  114.  Llauger-Bufi, L.; Felts, S. J.; Huezo, H.; Rosen, N.; Chiosis, G., Synthesis of novel fluorescent probes for the molecular chaperone Hsp90. Bioorg Med Chem Lett 2003, 13 (22), 3975-8.
  115.  Huezo, H.; Vilenchik, M.; Rosen, N.; Chiosis, G., Microtiter cell-based assay for detection of agents that alter cellular levels of Her2 and EGFR. Chem Biol 2003, 10 (7), 629-34.
  116.  Chiosis, G.; Lucas, B.; Huezo, H.; Solit, D.; Basso, A.; Rosen, N., Development of purine-scaffold small molecule inhibitors of Hsp90. Curr Cancer Drug Targets 2003, 3 (5), 371-6.
  117. Chiosis, G.; Huezo, H.; Rosen, N.; Mimnaugh, E.; Whitesell, L.; Neckers, L., 17AAG: low target binding affinity and potent cell activity—finding an explanation. Mol Cancer Ther 2003, 2 (2), 123-9.
  118.  Boneca, I. G.; Chiosis, G., Vancomycin resistance: occurrence, mechanisms and strategies to combat it. Expert Opin Ther Targets 2003, 7 (3), 311-28.
  119.  Gorre, M. E.; Ellwood-Yen, K.; Chiosis, G.; Rosen, N.; Sawyers, C. L., 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. Blood 2002, 100 (8), 3041-4.
  120.  Chiosis, G.; Lucas, B.; Shtil, A.; Huezo, H.; Rosen, N., 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. Bioorg Med Chem 2002, 10 (11), 3555-64.
  121.  Basso, A. D.; Solit, D. B.; Chiosis, G.; Giri, B.; Tsichlis, P.; Rosen, N., Akt forms an intracellular complex with heat shock protein 90 (Hsp90) and Cdc37 and is destabilized by inhibitors of Hsp90 function. J Biol Chem 2002, 277 (42), 39858-66.
  122. Boneca IG, Chiosis G. A new strategy for fighting vancomycin resistant-enterococci. APUA Newsletter 2002; 20: 1-3.
  123. Lucas, B.; Rosen, N.; Chiosis, G., Facile synthesis of a library of 9-alkyl-8-benzyl-9H-purin-6-ylamine derivatives. J Comb Chem 2001, 3 (6), 518-20.
  124. Chiosis, G.; Timaul, M. N.; Lucas, B.; Munster, P. N.; Zheng, F. F.; Sepp-Lorenzino, L.; Rosen, N., 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. Chem Biol 2001, 8 (3), 289-99. 
  125. Chiosis, G.; Rosen, N.; Sepp-Lorenzino, L., LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family. Bioorg Med Chem Lett 2001, 11 (7), 909-13.
  126. Chiosis, G.; Boneca, I. G., Selective cleavage of D-Ala-D-Lac by small molecules: re-sensitizing resistant bacteria to vancomycin. Science 2001, 293 (5534), 1484-7.
  127. Chiosis G, Shtil A, Lucas B, Huezo H, Rosen N. Development of 9-alkyl-8-benzyl-9H-purin-6-ylamines as inhibitors of the hsp90 family. Clinic. Cancer Res. 2001, 7: 474 Suppl. S.
  128. Zheng, F. F.; Kuduk, S. D.; Chiosis, G.; Munster, P. N.; Sepp-Lorenzino, L.; Danishefsky, S. J.; Rosen, N., Identification of a geldanamycin dimer that induces the selective degradation of HER-family tyrosine kinases. Cancer Res 2000, 60 (8), 2090-4.
  129. Chiosis G. Studs. Tetrahedy Into the Cyclization of an Epoxy-Alcohol to the Energetically Disfavored Product by Peptides from Non-biased Combinatorial Librarieron Lett. 2000; 41:801-806.