ATPase inhibitors of heat-shock protein 90, second season.

In the past four years, the ATP-dependent heat-shock protein 90 has remained the focus of much interest. Phase I and phase II anticancer clinical trials with first-generation inhibitors, although sometimes disappointing, have yet to report a forbidding side-effect inherent to the inhibition of this chaperone, which has a very complex and widespread role in cell biochemistry. Research in the field has started to unravel an elaborate regulation picture leading to the proper folding of many proteins. On the medicinal chemistry side, a second wave of inhibitors has been reported. This review attempts to describe all the ATPase inhibitors of HSP90 reported since our last survey.

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[53]  Mark Whittaker,et al.  Fragment‐based Identification of Hsp90 Inhibitors , 2009, ChemMedChem.

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[56]  B. Blagg,et al.  Design, synthesis, and structure--activity relationships for chimeric inhibitors of Hsp90. , 2006, The Journal of organic chemistry.

[57]  J. Veal,et al.  Discovery of benzamide tetrahydro-4H-carbazol-4-ones as novel small molecule inhibitors of Hsp90. , 2008, Bioorganic & medicinal chemistry letters.

[58]  L. Neckers,et al.  Inhibition of HSP90 with Pochoximes: SAR and Structure‐Based Insights , 2009, Chembiochem : a European journal of chemical biology.

[59]  M. Gerstein,et al.  Diverse Cellular Functions of the Hsp90 Molecular Chaperone Uncovered Using Systems Approaches , 2007, Cell.

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[63]  Jean M. Severin,et al.  Discovery and Design of Novel HSP90 Inhibitors Using Multiple Fragment‐based Design Strategies , 2007, Chemical biology & drug design.

[64]  P. Forterre,et al.  The HSP90 and DNA topoisomerase VI inhibitor radicicol also inhibits human type II DNA topoisomerase. , 2006, Biochemical pharmacology.

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[66]  F. Corelli,et al.  Preparation of a set of 4,5-dihydro-3H-pyrrolo[3,2-d]pyrimidin-4-ones as potential Hsp90 ligands , 2008 .

[67]  J. Peyrat,et al.  Recent advances in Hsp90 inhibitors as antitumor agents. , 2008, Anti-cancer agents in medicinal chemistry.

[68]  Weilin Sun,et al.  Discovery and development of purine-scaffold Hsp90 inhibitors , 2008, Expert opinion on drug discovery.

[69]  Suzanne F. Jones,et al.  A Phase 1 dose-escalation study of the safety and pharmacokinetics (PK) of the oral Hsp90 inhibitor SNX-5422 , 2008 .

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[78]  B. Blagg,et al.  High-throughput assay for the identification of Hsp90 inhibitors based on Hsp90-dependent refolding of firefly luciferase. , 2007, Bioorganic & medicinal chemistry.

[79]  Mike Wood,et al.  4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. , 2007, Journal of medicinal chemistry.

[80]  Yves L Janin,et al.  Heat shock protein 90 inhibitors. A text book example of medicinal chemistry? , 2005, Journal of medicinal chemistry.

[81]  T. Ishii,et al.  A Novel Heat Shock Protein (HSP) 90 Inhibitor KW-2478 shows Activity in B-Cell Malignancies in Vitro and in Vivo. , 2008 .

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[83]  Laura G. Dubois,et al.  Small molecule inhibitors of Hsp90 potently affect inflammatory disease pathways and exhibit activity in models of rheumatoid arthritis. , 2008, Arthritis and rheumatism.

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[85]  M. Adler,et al.  Potent Triazolothione Inhibitor of Heat‐Shock Protein‐90 , 2009, Chemical biology & drug design.

[86]  Mohammad Nur-E-Alam,et al.  Optimizing natural products by biosynthetic engineering: discovery of nonquinone Hsp90 inhibitors. , 2008, Journal of medicinal chemistry.

[87]  J. Buchner,et al.  The Hsp90 Chaperone Machinery* , 2008, Journal of Biological Chemistry.

[88]  B. Blagg,et al.  Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors. , 2009, Bioorganic & medicinal chemistry letters.

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[90]  M. Karplus,et al.  The HSP90 binding mode of a radicicol-like E-oxime determined by docking, binding free energy estimations, and NMR 15N chemical shifts. , 2009, Biophysical chemistry.

[91]  D. Ross,et al.  The Bioreduction of a Series of Benzoquinone Ansamycins by NAD(P)H:Quinone Oxidoreductase 1 to More Potent Heat Shock Protein 90 Inhibitors, the Hydroquinone Ansamycins , 2006, Molecular Pharmacology.

[92]  C. Richard Hutchinson,et al.  Insights into the Biosynthesis of the Benzoquinone Ansamycins Geldanamycin and Herbimycin, Obtained by Gene Sequencing and Disruption , 2005, Applied and Environmental Microbiology.

[93]  D. Solit,et al.  Development and application of Hsp90 inhibitors. , 2008, Drug discovery today.

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[97]  A. Rubenstein,et al.  Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. , 2009, Bioorganic & medicinal chemistry letters.

[98]  J. Snyder,et al.  Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling. , 2008, Bioorganic & medicinal chemistry.

[99]  S. Pennington,et al.  The topoisomerase II–Hsp90 complex: A new chemotherapeutic target? , 2006, International journal of cancer.

[100]  A. Slawin,et al.  Synthetic ansamycins prepared by a ring-expanding Claisen rearrangement. Synthesis and biological evaluation of ring and conformational analogues of the Hsp90 molecular chaperone inhibitor geldanamycin. , 2007, Organic & biomolecular chemistry.

[101]  S. Kasibhatla,et al.  7'-substituted benzothiazolothio- and pyridinothiazolothio-purines as potent heat shock protein 90 inhibitors. , 2006, Journal of medicinal chemistry.

[102]  L. Pearl,et al.  The Hsp90 molecular chaperone: an open and shut case for treatment. , 2008, The Biochemical journal.

[103]  S. Knapp,et al.  Propionate Analogues of Zearalenone Bind to Hsp90 , 2009, Chembiochem : a European journal of chemical biology.

[104]  L. Pearl,et al.  Structure and mechanism of the Hsp90 molecular chaperone machinery. , 2006, Annual review of biochemistry.

[105]  Yaoquan Liu,et al.  Potent cytotoxic C-11 modified geldanamycin analogues. , 2009, Journal of medicinal chemistry.

[106]  Hiroshi Yasui,et al.  SNX-2112, a selective Hsp90 inhibitor, potently inhibits tumor cell growth, angiogenesis, and osteoclastogenesis in multiple myeloma and other hematologic tumors by abrogating signaling via Akt and ERK. , 2009, Blood.

[107]  Jie Ge,et al.  Development of 17-allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride (IPI-504), an anti-cancer agent directed against Hsp90 , 2006, Proceedings of the National Academy of Sciences.

[108]  B. Blagg,et al.  High-throughput screening for Hsp90 ATPase inhibitors. , 2006, Bioorganic & medicinal chemistry letters.

[109]  Andrew J. S. Knox,et al.  Integration of ligand and structure-based virtual screening for the identification of the first dual targeting agent for heat shock protein 90 (Hsp90) and tubulin. , 2009, Journal of medicinal chemistry.

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[115]  J. Snyder,et al.  Synthesis and SAR study of N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)-arylsulfonamides: heat shock protein 90 (Hsp90) inhibitors with submicromolar activity in an in vitro assay. , 2008, Bioorganic & medicinal chemistry letters.

[116]  S. Faeth,et al.  Search for Hsp90 inhibitors with potential anticancer activity: isolation and SAR studies of radicicol and monocillin I from two plant-associated fungi of the Sonoran desert. , 2006, Journal of natural products.

[117]  K. Foley,et al.  The novel HSP90 inhibitor STA‐1474 exhibits biologic activity against osteosarcoma cell lines , 2009, International journal of cancer.

[118]  G. Leo,et al.  Biotransformation of Geldanamycin and 17-Allylamino-17-Demethoxygeldanamycin by Human Liver Microsomes: Reductive versus Oxidative Metabolism and Implications , 2007, Drug Metabolism and Disposition.

[119]  Xiaoguang Lei,et al.  Efficient Synthesis of a Novel Resorcyclide as Anticancer Agent Based on Hsp90 Inhibition. , 2008, Advanced synthesis & catalysis.

[120]  Y. Zhen,et al.  A novel derivative of geldanamycin and its antitumor activity , 2009 .

[121]  J. Ritter.  Intestinal UGTs as potential modifiers of pharmacokinetics and biological responses to drugs and xenobiotics , 2007, Expert opinion on drug metabolism & toxicology.

[122]  Gabriela Chiosis,et al.  Discovery and development of heat shock protein 90 inhibitors. , 2009, Bioorganic & medicinal chemistry.

[123]  Young-Soo Hong,et al.  Mutasynthesis of Geldanamycin by the Disruption of a Gene Producing Starter Unit: Generation of Structural Diversity at the Benzoquinone Ring , 2007, Chembiochem : a European journal of chemical biology.

[124]  D. Ross,et al.  Enzymatic Reduction and Glutathione Conjugation of Benzoquinone Ansamycin Heat Shock Protein 90 Inhibitors: Relevance for Toxicity and Mechanism of Action , 2008, Drug Metabolism and Disposition.

[125]  J. Marugan,et al.  Dihydroquinone ansamycins: toward resolving the conflict between low in vitro affinity and high cellular potency of geldanamycin derivatives. , 2006, Biochemistry.

[126]  X. Barril,et al.  Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone. , 2009, Journal of medicinal chemistry.

[127]  C. Erlichman.  Tanespimycin: the opportunities and challenges of targeting heat shock protein 90 , 2009, Expert opinion on investigational drugs.

[128]  C. Hudis,et al.  The heat shock protein 90 chaperone complex: an evolving therapeutic target. , 2008, Current cancer drug targets.

[129]  Gabriela Chiosis,et al.  Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90. , 2006, Journal of medicinal chemistry.

[130]  J. Renoir,et al.  Antiproliferative and apoptotic activities of tosylcyclonovobiocic acids as potent heat shock protein 90 inhibitors in human cancer cells. , 2009, Cancer letters.

[131]  J. Galazzo,et al.  Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. , 2009, Journal of medicinal chemistry.

[132]  Zihai Li,et al.  17 AAG for HSP90 inhibition in cancer--from bench to bedside. , 2009, Current molecular medicine.

[133]  Christine J. Martin,et al.  Molecular characterization of macbecin as an Hsp90 inhibitor. , 2008, Journal of medicinal chemistry.

[134]  M. Drysdale,et al.  Preclinical pharmacokinetics and metabolism of a novel diaryl pyrazole resorcinol series of heat shock protein 90 inhibitors , 2006, Molecular Cancer Therapeutics.