LY294002-Geldanamycin Heterodimers as Selective Inhibitors of the PI3K and PI3K-related Family. Chiosis G, Rosen N, Sepp-Lorenzino L. Bioorg. Med. Chem. Lett. 2001; 11: 909-915.
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. Chiosis G, Timaul MN, Lucas B, Munster PN, Zheng FF, Sepp-Lorenzino L, Rosen N. Chem. Biol. 2001; 8:289-299.
Selective cleavage of D-Ala-D-Lac by small molecules: re-sensitizing resistant bacteria to vancomycin. Chiosis G, Boneca IG. Science. 2001 Aug 24;293(5534):1484-7.
Facile synthesis of 9-Alkyl-8-benzyl-9H-purin-6-ylamine Derivatives. Lucas B, Rosen N, Chiosis G. J. Comb. Chem. 2001; 3: 518-520.
Development of a Purine-based Novel Class of Hsp90 Binders That Inhibit the Proliferation of Cancer Cells and Induce the Degradation of Her2 Tyrosine Kinase. Chiosis G, Huezo H, Lucas B, Rosen N. Bioorg. Med. Chem. 2002; 10: 3555-3564.
17AAG - Low target binding affinity and potent cell activity: Finding an explanation. Chiosis G, Huezo H, Rosen N, Mimnaugh E, Whitesell L, Neckers L. Molec. Cancer Ther. 2003; 2: 123-129.
Vancomycin resistance: Occurrence, mechanism and therapeutic approaches.Boneca IG, Chiosis G. Expert Opinion on Therapeutic Targets, 2003; 7(3), 311-328.
Development of purine-scaffold small molecule inhibitors of Hsp90. Chiosis G, Lucas B, Huezo H, Solit D, Basso A, Rosen N. Curr. Cancer Drug Targets 2003, 3, 363-368.
Microtiter cell-based assay for the detection of agents that alter cellular levels of Her2 and EGFR. Huezo H, Vilenchik M, Rosen N, Chiosis G. Chem Biol. 2003, 10(7), 629-634.
Synthesis of novel fluorescent probes for the molecular chaperone Hsp90. Llauger L, Felts S, Huezo H, Rosen N, Chiosis G. Bioorg. Med. Chem. Lett. 2003, 13, 3975-3978.
General Method for the Synthesis of 8-Arylsulfanyl Adenine Derivatives, He H, Llauger L, Rosen N, Chiosis G. J. Org. Chem. 2004, 69, 3230-3232.
Targeting wide-range oncogenic transformation via PU24FCl, a specific inhibitor of tumor Hsp90. Vilenchik M, Solit D, Basso M, Huezo H, Lucas B, Huazhong H, Rosen N, Spampinato C, Modrich P, Chiosis G. Chem. Biol. 2004, 11, 787-797.
Development of a fluorescence polarization assay for the molecular chaperone Hsp90. Kim J, Felts S, He H, Llauger L, Huezo H, Rosen N, Chiosis G. J. Biomolecular Screening 2004, 9(5):375-81.
Hsp90 - the vulnerable chaperone. Chiosis G, Vilenchik M, Kim J, Solit D. Drug Discovery Today, 2004, 9(20):881-8.
Synthesis of 8-arylsulfoxyl/sulfonyl adenines. Llauger L, He H, Chiosis G. Tet. Lett. 2004, 45, 9549-9552.
8-Arylsulfanyl and 8-Arylsulfoxyl Adenine Derivatives as Inhibitors of the Heat Shock Protein 90. Llauger L, He H, Kim J, Aguirre J, Rosen N, Peters U, Davies P, Chiosis G. J. Med. Chem. 2005, 48, 2892-2905.
The journey of small molecule microarrays: From proteins to mammalian cells - are we there yet? Chiosis G, Brodsky J. Trends Biotech. 2005, (6):271-4.
Identification of Potent Water-Soluble Purine-Scaffold Inhibitors of the Heat Shock Protein 90. He H, Zatorska D, Kim J, Aguirre J, Llauger L, She Y, Wu N, Immormino RM, Gewirth DT, Chiosis G. J. Med. Chem. 2006, 49(1):381-90.
Targeting chaperones in transformed systems - a focus on Hsp90 and cancer. Chiosis G. Expert Opinion on Therapeutic Targets. 2006, 10(1):37-50.
Synthesis of Hsp90 dimerization modulators. Chiosis G, Aguirre J, Nicchitta CV. Bioorg. Med. Chem. Lett. 2006,16:3529-3532.
Hsp90 inhibitors - a chronicle from geldanamycin to today's agents. Chiosis G, Caldas Lopes E, Solit D. Current Opinion in Investigational Drugs 2006 (6):534-41.
Synthesis of a red-shifted fluorescence polarization probe for Hsp90. Moulick K, Clement CC, Aguirre J, Kim J, Kang Y, Felts S, Chiosis G. Bioorg. Med. Chem. Lett. 2006 Sep 1;16(17):4515-8.
Tumor Selectivity of Hsp90 Inhibitors - The Explanation Remains Elusive. Chiosis G, Neckers L. ACS Chemical Biology 2006, (1):279-284.
Structural and quantum chemical studies of 8-aryl-sulfanyl adenine class Hsp90 inhibitors. Immormino RM, Kang Y, Chiosis G, Gewirth DT. J Med Chem. 2006 Aug 10;49(16):4953-60.
Discovery and development of purine-scaffold Hsp90 inhibitors. Chiosis G. Curr Top Med Chem. 2006;6(11):1183-91. Review.
Gene expression signature-based chemical genomic prediction identifies a novel class of HSP90 pathway modulators. Hieronymus H, Lamb J, Ross KN, Peng XP, Clement C, Rodina A, Nieto M, Du J, Stegmaier K, Raj SM, Maloney KN, Clardy J, Hahn WC, Chiosis G, Golub TR. Cancer Cell. 2006 Oct;10(4):321-30.
Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. Rodina A, Vilenchik M, Moulick K, Aguirre J, Kim J, Chiang A, Litz J, Clement CC, Kang Y, She Y, Wu N, Felts S, Wipf P, Massague J, Jiang X, Brodsky JL, Krystal GW, Chiosis G. Nat Chem Biol. 2007 Aug;3(8):498-507.
Roles of heat-shock protein 90 in maintaining and facilitating the neurodegenerative phenotype in tauopathies.vLuo W, Dou F, Rodina A, Chip S, Kim J, Zhao Q, Moulick K, Aguirre J, Wu N, Greengard P, Chiosis G. Proc Natl Acad Sci U S A. 2007 May 29;104(22):9511-6.
High-throughput screening fluorescence polarization assay for tumor-specific Hsp90. Du Y, Moulick K, Rodina A, Aguirre J, Felts S, Dingledine R, Fu H, Chiosis G. J Biomol Screen. 2007 Oct;12(7):915-24.
Anti-cancer therapeutic approaches based on intracellular and extracellular heat shock proteins.Didelot C, Lanneau D, Brunet M, Joly AL, De Thonel A, Chiosis G, Garrido C.Curr Med Chem. 2007;14(27):2839-47.
Molecular imaging of the efficacy of heat shock protein 90 inhibitors in living subjects.Chan CT, Paulmurugan R, Gheysens OS, Kim J, Chiosis G, Gambhir SS.Cancer Res. 2008 Jan 1;68(1):216-26.
Development and application of Hsp90 inhibitors.Solit DB, Chiosis G.Drug Discov Today. 2008 Jan;13(1-2):38-43.
Interaction of heat-shock protein 90 beta isoform (HSP90 beta) with cellular inhibitor of apoptosis 1 (c-IAP1) is required for cell differentiation.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.Cell Death Differ. 2008 May;15(5):859-66.
The chaperone activity of heat shock protein 90 is critical for maintaining the stability of leucine-rich repeat kinase 2.Wang L, Xie C, Greggio E, Parisiadou L, Shim H, Sun L, Chandran J, Lin X, Lai C, Yang WJ, Moore DJ, Dawson TM, Dawson VL, Chiosis G, Cookson MR, Cai H.J Neurosci. 2008 Mar 26;28(13):3384-91.
Design of a fluorescence polarization assay platform for the study of human Hsp70.Kang Y, Taldone T, Clement CC, Fewell SW, Aguirre J, Brodsky JL, Chiosis G.Bioorg Med Chem Lett. 2008 Jul 1;18(13):3749-51.
The yeast Hsp110, Sse1p, exhibits high-affinity peptide binding.Goeckeler JL, Petruso AP, Aguirre J, Clement CC, Chiosis G, Brodsky JL.FEBS Lett. 2008 Jul 9;582(16):2393-6.
Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling.Ganesh T, Min J, Thepchatri P, Du Y, Li L, Lewis I, Wilson L, Fu H, Chiosis G, Dingledine R, Liotta D, Snyder JP, Sun A.Bioorg Med Chem. 2008 Jul 15;16(14):6903-10.
Targeting Hsp90: small-molecule inhibitors and their clinical development.Taldone T, Gozman A, Maharaj R, Chiosis G.Curr Opin Pharmacol. 2008 Aug;8(4):370-4.
Kaiso contributes to DNA methylation-dependent silencing of tumor suppressor genes in colon cancer cell lines.Lopes EC, Valls E, Figueroa ME, Mazur A, Meng FG, Chiosis G, Laird PW, Schreiber-Agus N, Greally JM, Prokhortchouk E, Melnick A.Cancer Res. 2008 Sep 15;68(18):7258-63.
Discovery and development of heat shock protein 90 inhibitors.Taldone T, Sun W, Chiosis G.Bioorg Med Chem. 2009 Mar 15;17(6):2225-35.
Microwave-assisted one step synthesis of 8-arylmethyl-9H-purin-6-amines.Tao H, Kang Y, Taldone T, Chiosis G.Bioorg Med Chem Lett. 2009 Jan 15;19(2):415-7.
Heat shock protein 90: translation from cancer to Alzheimer's disease treatment?Luo W, Rodina A, Chiosis G.BMC Neurosci. 2008 Dec 3;9 Suppl 2:S7.
Assay for isolation of inhibitors of her2-kinase expression.Chiosis G, Keeton AB.Methods Mol Biol. 2009;486:139-49.
Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models.Caldas-Lopes E, Cerchietti L, Ahn JH, Clement CC, Robles AI, Rodina A, Moulick K, Taldone T, Gozman A, Guo Y, Wu N, de Stanchina E, White J, Gross SS, Ma Y, Varticovski L, Melnick A, Chiosis G.Proc Natl Acad Sci U S A. 2009 May 19;106(20):8368-73.
Targeting heat shock protein 90 with non-quinone inhibitors: a novel chemotherapeutic approach in human hepatocellular carcinoma.Breinig M, Caldas-Lopes E, Goeppert B, Malz M, Rieker R, Bergmann F, Schirmacher P, Mayer M, Chiosis G, Kern MA.Hepatology. 2009 Jul;50(1):102-12.
Purine-scaffold Hsp90 inhibitors.Taldone T, Chiosis G.Curr Top Med Chem. 2009;9(15):1436-46.
A purine scaffold Hsp90 inhibitor destabilizes BCL-6 and has specific antitumor activity in BCL-6-dependent B cell lymphomas.Cerchietti LC, Lopes EC, Yang SN, Hatzi K, Bunting KL, Tsikitas LA, Mallik A, Robles AI, Walling J, Varticovski L, Shaknovich R, Bhalla KN, Chiosis G, Melnick A.Nat Med. 2009 Dec;15(12):1369-76.
Measuring the pharmacodynamic effects of a novel Hsp90 inhibitor on HER2/neu expression in mice using Zr-DFO-trastuzumab.Holland JP, Caldas-Lopes E, Divilov V, Longo VA, Taldone T, Zatorska D, Chiosis G, Lewis JS.PLoS One. 2010 Jan 25;5(1):e8859.
Heat shock protein 90 in neurodegenerative diseases. Luo W, Sun W, Taldone T, Rodina A, Chiosis G. Mol Neurodegener. 2010 Jun 3;5:24.
Assay strategies for the discovery and validation of therapeutics targeting Brugia pahangi Hsp90.Taldone T, Gillan V, Sun W, Rodina A, Patel P, Maitland K, O'Neill K, Chiosis G, Devaney E.PLoS Negl Trop Dis. 2010 Jun 15;4(6):e714.
HSP90 is a therapeutic target in JAK2-dependent myeloproliferative neoplasms in mice and humans.Marubayashi S, Koppikar P, Taldone T, Abdel-Wahab O, West N, Bhagwat N, Caldas-Lopes E, Ross KN, Gönen M, Gozman A, Ahn JH, Rodina A, Ouerfelli O, Yang G, Hedvat C, Bradner JE, Chiosis G, Levine RL.J Clin Invest. 2010 Oct 1;120(10):3578-93. doi: 10.1172/JCI42442.
The anti-myeloma activity of a novel purine scaffold HSP90 inhibitor PU-H71 is via inhibition of both HSP90A and HSP90B1. Usmani SZ, Bona RD, Chiosis G, Li Z. J Hematol Oncol. 2010 Oct 26;3:40.
BCL6 repression of EP300 in human diffuse large B cell lymphoma cells provides a basis for rational combinatorial therapy. Cerchietti LC, Hatzi K, Caldas-Lopes E, Yang SN, Figueroa ME, Morin RD, Hirst M, Mendez L, Shaknovich R, Cole PA, Bhalla K, Gascoyne RD, Marra M, Chiosis G, Melnick A. J Clin Invest. 2010 Nov 1. pii: 42869. doi: 10.1172/JCI42869
Design of a Flexible Cell-Based Assay for the Evaluation of Heat Shock Protein 70 Expression Modulators. Ahn JH, Luo W, Kim J, Rodina A, Clement CC, Aguirre J, Sun W, Kang Y, Maharaj R, Moulick K, Zatorska D, Kokoszka M, Brodsky JL, Chiosis G. Assay Drug Dev Technol. 2010 Dec 6.
Heat shock protein 90-sheltered overexpression of insulin-like growth factor 1 receptor contributes to malignancy of thymic epithelial tumors. Breinig M, Mayer P, Harjung A, Goeppert B, Malz M, Penzel R, Neumann O, Hartmann A, Dienemann H, Giaccone G, Schirmacher P, Kern MA, Chiosis G, Rieker RJ. Clin Cancer Res. 2011 Apr 15;17(8):2237-49.
Design, synthesis, and evaluation of small molecule Hsp90 probes. Taldone T, Zatorska D, Patel PD, Zong H, Rodina A, Ahn JH, Moulick K, Guzman ML, Chiosis G. Bioorg Med Chem. 2011 Apr 15;19(8):2603-14. Epub 2011 Mar 12.
Advances in the clinical development of heat shock protein 90 (Hsp90) inhibitors in cancers. Jhaveri K, Taldone T, Modi S, Chiosis G. Biochim Biophys Acta. 2011 Oct 29. Epub ahead of print.
HSP90 inhibitors as therapy for multiple myeloma. Usmani SZ, Chiosis G. Clin Lymphoma Myeloma Leuk. 2011 Jun;11 Suppl 1:S77-81. Epub 2011 Apr 28.
Affinity-based proteomics reveal cancer-specific networks coordinated by Hsp90. Moulick K, Ahn JH, Zong H, Rodina A, Cerchietti L, Gomes DaGama EM, Caldas-Lopes E,Beebe K, Perna F, Hatzi K, Vu LP, Zhao X, Zatorska D, Taldone T, Smith-Jones P, Alpaugh M, Gross SS, Pillarsetty N, Ku T, Lewis JS, Larson SM, Levine R, Erdjument-Bromage H, Guzman ML, Nimer SD, Melnick A, Neckers L, Chiosis G. Nat Chem Biol. 2011 Sep 25;7(11):818-26. doi: 10.1038/nchembio.670.
Synthesis of purine-scaffold fluorescent probes for heat shock protein 90 with use inflow cytometry and fluorescence microscopy.Taldone T, Gomes-DaGama EM, Zong H, Sen S, Alpaugh ML, Zatorska D, Alonso-Sabadell R, Guzman ML, Chiosis G. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5347-52. Epub2011 Jul 14.
