Major Research Areas

Selected Publications

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.

Purine-scaffold Hsp90 inhibitors.Taldone T, Chiosis G.Curr Top Med Chem. 2009;9(15):1436-46.

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.

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.

Solit DB, Chiosis G.Development and application of Hsp90 inhibitors.
Drug Discov Today. 2008 Jan;13(1-2):38-43. Epub 2007 Nov 26. Review.

Didelot C, Lanneau D, Brunet M, Joly AL, 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. Review.

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.

Brodsky JL, 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. Review.

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 Jan 12;49(1):381-90.

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 Apr 21;48(8):2892-905.

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 Jun;11(6):787-97.

Gorre ME, Ellwood-Yen K, Chiosis G, Rosen N, Sawyers CL.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 Oct 15;100(8):3041-4.

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 Nov;10(11):3555-64.

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