Major Research Areas

Publications

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: 909-915.

Chiosis G, Timaul MN, Lucas B, Munster PN, Zheng FF, 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; 8:289-299.

Chiosis G, Boneca IG. Selective cleavage of D-Ala-D-Lac by small molecules: re-sensitizing resistant bacteria to vancomycin. Science. 2001 Aug 24;293(5534):1484-7.

Lucas B, Rosen N, Chiosis G. Facile synthesis of 9-Alkyl-8-benzyl-9H-purin-6-ylamine Derivatives. J. Comb. Chem. 2001; 3: 518-520.

Chiosis G, Huezo H, Lucas B, Rosen N. 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. Bioorg. Med. Chem. 2002; 10: 3555-3564.

Chiosis G, Huezo H, Rosen N, Mimnaugh E, Whitesell L, Neckers L. 17AAG - Low target binding affinity and potent cell activity: Finding an explanation. Molec. Cancer Ther. 2003; 2: 123-129.

Boneca IG, Chiosis G. Vancomycin resistance: Occurrence, mechanism and therapeutic approaches. Expert Opinion on Therapeutic Targets, 2003; 7(3), 311-328.

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, 363-368.

Huezo H, Vilenchik M, Rosen N, Chiosis G. Microtiter cell-based assay for the detection of agents that alter cellular levels of Her2 and EGFR. Chem Biol. 2003, 10(7), 629-634.

Llauger L, Felts S, Huezo H, Rosen N, Chiosis G. Synthesis of novel fluorescent probes for the molecular chaperone Hsp90. Bioorg. Med. Chem. Lett. 2003, 13, 3975-3978.

He H, Llauger L, Rosen N, Chiosis G. General Method for the Synthesis of 8-Arylsulfanyl Adenine Derivatives, J. Org. Chem. 2004, 69, 3230-3232.

Vilenchik M, Solit D, Basso M, Huezo H, Lucas B, Huazhong 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, 787-797.

Kim J, Felts S, He H, Llauger L, Huezo H, Rosen N, Chiosis G. Development of a fluorescence polarization assay for the molecular chaperone Hsp90. J. Biomolecular Screening 2004, 9(5):375-81.

Chiosis G, Vilenchik M, Kim J, Solit D. Hsp90 - the vulnerable chaperone. Drug Discovery Today, 2004, 9(20):881-8.

Llauger L, He H, Chiosis G. Synthesis of 8-arylsulfoxyl/sulfonyl adenines. Tet. Lett. 2004, 45, 9549-9552.

Boneca IG, Chiosis G. A new strategy for fighting vancomycin resistant-enterococci. APUA Newsletter 2002; 20: 1-3.

Llauger L, He H, Kim J, Aguirre J, Rosen N, Peters U, Davies P, Chiosis G. 8-Arylsulfanyl and 8-Arylsulfoxyl Adenine Derivatives as Inhibitors of the Heat Shock Protein 90. J. Med. Chem. 2005, 48, 2892-2905.

Chiosis G, Brodsky J. The journey of small molecule microarrays: From proteins to mammalian cells - are we there yet? Trends Biotech. 2005, (6):271-4.

He H, Zatorska D, Kim J, Aguirre J, Llauger L, She Y, Wu N, Immormino RM, Gewirth DT, Chiosis G. Identification of Potent Water-Soluble Purine-Scaffold Inhibitors of the Heat Shock Protein 90. J. Med. Chem. 2006, 49(1):381-90.

Chiosis G. Targeting chaperones in transformed systems - a focus on Hsp90 and cancer. Expert Opinion on Therapeutic Targets. 2006, 10(1):37-50.

Chiosis G, Aguirre J, Nicchitta CV. Synthesis of Hsp90 dimerization modulators. Bioorg. Med. Chem. Lett. 2006,16:3529-3532.

Chiosis G., Rodina A, Moulick K. Emerging Hsp90 inhibitors: from discovery to clinic. Current medicinal chemistry-Anti-cancer agents. 2006, 6, 1-8.

Chiosis G, Caldas Lopes E, Solit D. Hsp90 inhibitors - a chronicle from geldanamycin to today's agents. Current Opinion in Investigational Drugs 2006 (6):534-41.

Moulick K, Clement CC, 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 Sep 1;16(17):4515-8.

Chiosis G, Neckers L. Tumor Selectivity of Hsp90 Inhibitors - The Explanation Remains Elusive. ACS Chemical Biology 2006, (1):279-284.

Immormino RM, Kang Y, Chiosis G, Gewirth DT. Structural and quantum chemical studies of 8-aryl-sulfanyl adenine class Hsp90 inhibitors. J Med Chem. 2006 Aug 10;49(16):4953-60.

Chiosis G. Discovery and development of purine-scaffold Hsp90 inhibitors. Curr Top Med Chem. 2006;6(11):1183-91. Review.

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. Gene expression signature-based chemical genomic prediction identifies a novel class of HSP90 pathway modulators. Cancer Cell. 2006 Oct;10(4):321-30.

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. Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. Nat Chem Biol. 2007 Aug;3(8):498-507.

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 May 29;104(22):9511-6.

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