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Contents |
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* Residue conservation analysis
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Gene Ontology (GO) functional annotation
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Biological process
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response to stress
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2 terms
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Biochemical function
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unfolded protein binding
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2 terms
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DOI no:
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J Med Chem
42:260-266
(1999)
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PubMed id:
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Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin.
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S.M.Roe,
C.Prodromou,
R.O'Brien,
J.E.Ladbury,
P.W.Piper,
L.H.Pearl.
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ABSTRACT
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The cellular activity of several regulatory and signal transduction proteins,
which depend on the Hsp90 molecular chaperone for folding, is markedly decreased
by geldanamycin and by radicicol (monorden). We now show that these unrelated
compounds both bind to the N-terminal ATP/ADP-binding domain of Hsp90, with
radicicol displaying nanomolar affinity, and both inhibit the inherent ATPase
activity of Hsp90 which is essential for its function in vivo. Crystal structure
determinations of Hsp90 N-terminal domain complexes with geldanamycin and
radicicol identify key aspects of their nucleotide mimicry and suggest a
rational basis for the design of novel antichaperone drugs.
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Literature references that cite this PDB file's key reference
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PubMed id
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Reference
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K.Matsumoto,
M.Minami,
F.Shinozaki,
Y.Suzuki,
K.Abe,
S.Zenno,
S.Matsumoto,
and
Y.Minami
(2011).
Hsp90 is involved in the formation of P-bodies and stress granules.
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Biochem Biophys Res Commun, 407,
720-724.
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M.T.Guarnieri,
B.S.Blagg,
and
R.Zhao
(2011).
A high-throughput TNP-ATP displacement assay for screening inhibitors of ATP-binding in bacterial histidine kinases.
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| |
Assay Drug Dev Technol, 9,
174-183.
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P.G.Richardson,
C.S.Mitsiades,
J.P.Laubach,
S.Lonial,
A.A.Chanan-Khan,
and
K.C.Anderson
(2011).
Inhibition of heat shock protein 90 (HSP90) as a therapeutic strategy for the treatment of myeloma and other cancers.
|
| |
Br J Haematol, 152,
367-379.
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Q.Xie,
R.Wondergem,
Y.Shen,
G.Cavey,
J.Ke,
R.Thompson,
R.Bradley,
J.Daughtery-Holtrop,
Y.Xu,
E.Chen,
H.Omar,
N.Rosen,
D.Wenkert,
H.E.Xu,
and
G.F.Vande Woude
(2011).
Benzoquinone ansamycin 17AAG binds to mitochondrial voltage-dependent anion channel and inhibits cell invasion.
|
| |
Proc Natl Acad Sci U S A, 108,
4105-4110.
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T.Taldone,
D.Zatorska,
P.D.Patel,
H.Zong,
A.Rodina,
J.H.Ahn,
K.Moulick,
M.L.Guzman,
and
G.Chiosis
(2011).
Design, synthesis, and evaluation of small molecule Hsp90 probes.
|
| |
Bioorg Med Chem, 19,
2603-2614.
|
|
|
|
|
|
|
A.Giménez Ortiz,
and
J.Montalar Salcedo
(2010).
Heat shock proteins as targets in oncology.
|
| |
Clin Transl Oncol, 12,
166-173.
|
|
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|
|
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|
C.Giommarelli,
V.Zuco,
E.Favini,
C.Pisano,
F.Dal Piaz,
N.De Tommasi,
and
F.Zunino
(2010).
The enhancement of antiproliferative and proapoptotic activity of HDAC inhibitors by curcumin is mediated by Hsp90 inhibition.
|
| |
Cell Mol Life Sci, 67,
995.
|
|
|
|
|
|
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C.Rink,
F.Sasse,
A.Zubrienė,
D.Matulis,
and
M.E.Maier
(2010).
Probing the influence of an allylic methyl group in zearalenone analogues on binding to Hsp90.
|
| |
Chemistry, 16,
14469-14478.
|
|
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|
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J.E.Bohonowych,
U.Gopal,
and
J.S.Isaacs
(2010).
Hsp90 as a gatekeeper of tumor angiogenesis: clinical promise and potential pitfalls.
|
| |
J Oncol, 2010,
412985.
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J.E.Day,
S.Y.Sharp,
M.G.Rowlands,
W.Aherne,
P.Workman,
and
C.J.Moody
(2010).
Targeting the Hsp90 chaperone: synthesis of novel resorcylic acid macrolactone inhibitors of Hsp90.
|
| |
Chemistry, 16,
2758-2763.
|
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J.E.Day,
S.Y.Sharp,
M.G.Rowlands,
W.Aherne,
W.Lewis,
S.M.Roe,
C.Prodromou,
L.H.Pearl,
P.Workman,
and
C.J.Moody
(2010).
Inhibition of Hsp90 with resorcylic acid macrolactones: synthesis and binding studies.
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Chemistry, 16,
10366-10372.
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PDB code:
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J.J.Gano,
and
J.A.Simon
(2010).
A proteomic investigation of ligand-dependent HSP90 complexes reveals CHORDC1 as a novel ADP-dependent HSP90-interacting protein.
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| |
Mol Cell Proteomics, 9,
255-270.
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J.R.Porter,
C.C.Fritz,
and
K.M.Depew
(2010).
Discovery and development of Hsp90 inhibitors: a promising pathway for cancer therapy.
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| |
Curr Opin Chem Biol, 14,
412-420.
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J.Trepel,
M.Mollapour,
G.Giaccone,
and
L.Neckers
(2010).
Targeting the dynamic HSP90 complex in cancer.
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Nat Rev Cancer, 10,
537-549.
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K.D.Corbett,
and
J.M.Berger
(2010).
Structure of the ATP-binding domain of Plasmodium falciparum Hsp90.
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Proteins, 78,
2738-2744.
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PDB code:
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L.Vozzolo,
B.Loh,
P.J.Gane,
M.Tribak,
L.Zhou,
I.Anderson,
E.Nyakatura,
R.G.Jenner,
D.Selwood,
and
A.Fassati
(2010).
Gyrase B inhibitor impairs HIV-1 replication by targeting Hsp90 and the capsid protein.
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| |
J Biol Chem, 285,
39314-39328.
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P.Fadden,
K.H.Huang,
J.M.Veal,
P.M.Steed,
A.F.Barabasz,
B.Foley,
M.Hu,
J.M.Partridge,
J.Rice,
A.Scott,
L.G.Dubois,
T.A.Freed,
M.A.Silinski,
T.E.Barta,
P.F.Hughes,
A.Ommen,
W.Ma,
E.D.Smith,
A.W.Spangenberg,
J.Eaves,
G.J.Hanson,
L.Hinkley,
M.Jenks,
M.Lewis,
J.Otto,
G.J.Pronk,
K.Verleysen,
T.A.Haystead,
and
S.E.Hall
(2010).
Application of chemoproteomics to drug discovery: identification of a clinical candidate targeting hsp90.
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Chem Biol, 17,
686-694.
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PDB code:
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P.Workman,
and
I.Collins
(2010).
Probing the probes: fitness factors for small molecule tools.
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| |
Chem Biol, 17,
561-577.
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T.Miyoshi,
A.Takeuchi,
H.Siomi,
and
M.C.Siomi
(2010).
A direct role for Hsp90 in pre-RISC formation in Drosophila.
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| |
Nat Struct Mol Biol, 17,
1024-1026.
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A.S.Duerfeldt,
G.E.Brandt,
and
B.S.Blagg
(2009).
Design, synthesis, and biological evaluation of conformationally constrained cis-amide Hsp90 inhibitors.
|
| |
Org Lett, 11,
2353-2356.
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A.Seaton,
P.J.Maxwell,
A.Hill,
R.Gallagher,
J.Pettigrew,
R.H.Wilson,
and
D.J.Waugh
(2009).
Inhibition of constitutive and cxc-chemokine-induced NF-kappaB activity potentiates ansamycin-based HSP90-inhibitor cytotoxicity in castrate-resistant prostate cancer cells.
|
| |
Br J Cancer, 101,
1620-1629.
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A.Zubrienė,
J.Matulienė,
L.Baranauskienė,
J.Jachno,
J.Torresan,
V.Michailovienė,
P.Cimmperman,
and
D.Matulis
(2009).
Measurement of Nanomolar Dissociation Constants by Titration Calorimetry and Thermal Shift Assay - Radicicol Binding to Hsp90 and Ethoxzolamide Binding to CAII.
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Int J Mol Sci, 10,
2662-2680.
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G.Morra,
G.Verkhivker,
and
G.Colombo
(2009).
Modeling signal propagation mechanisms and ligand-based conformational dynamics of the Hsp90 molecular chaperone full-length dimer.
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| |
PLoS Comput Biol, 5,
e1000323.
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J.L.Houlihan,
J.J.Metzler,
and
J.S.Blum
(2009).
HSP90alpha and HSP90beta isoforms selectively modulate MHC class II antigen presentation in B cells.
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| |
J Immunol, 182,
7451-7458.
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J.R.Smith,
P.A.Clarke,
E.de Billy,
and
P.Workman
(2009).
Silencing the cochaperone CDC37 destabilizes kinase clients and sensitizes cancer cells to HSP90 inhibitors.
|
| |
Oncogene, 28,
157-169.
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L.B.Peterson,
and
B.S.Blagg
(2009).
To fold or not to fold: modulation and consequences of Hsp90 inhibition.
|
| |
Future Med Chem, 1,
267-283.
|
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|
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M.K.Hadden,
and
B.S.Blagg
(2009).
Synthesis and evaluation of radamide analogues, a chimera of radicicol and geldanamycin.
|
| |
J Org Chem, 74,
4697-4704.
|
|
|
|
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|
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M.P.Xiong,
J.A.Yáñez,
G.S.Kwon,
N.M.Davies,
and
M.L.Forrest
(2009).
A cremophor-free formulation for tanespimycin (17-AAG) using PEO-b-PDLLA micelles: characterization and pharmacokinetics in rats.
|
| |
J Pharm Sci, 98,
1577-1586.
|
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|
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M.Sgobba,
and
G.Rastelli
(2009).
Structure-based and in silico design of Hsp90 inhibitors.
|
| |
ChemMedChem, 4,
1399-1409.
|
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|
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|
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M.Spichty,
A.Taly,
F.Hagn,
H.Kessler,
S.Barluenga,
N.Winssinger,
and
M.Karplus
(2009).
The HSP90 binding mode of a radicicol-like E-oxime determined by docking, binding free energy estimations, and NMR 15N chemical shifts.
|
| |
Biophys Chem, 143,
111-123.
|
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|
|
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M.Ugele,
F.Sasse,
S.Knapp,
O.Fedorov,
A.Zubriene,
D.Matulis,
and
M.E.Maier
(2009).
Propionate analogues of zearalenone bind to Hsp90.
|
| |
Chembiochem, 10,
2203-2212.
|
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|
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M.W.Amolins,
and
B.S.Blagg
(2009).
Natural product inhibitors of Hsp90: potential leads for drug discovery.
|
| |
Mini Rev Med Chem, 9,
140-152.
|
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|
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O.Ayrault,
M.D.Godeny,
C.Dillon,
F.Zindy,
P.Fitzgerald,
M.F.Roussel,
and
H.M.Beere
(2009).
Inhibition of Hsp90 via 17-DMAG induces apoptosis in a p53-dependent manner to prevent medulloblastoma.
|
| |
Proc Natl Acad Sci U S A, 106,
17037-17042.
|
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|
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O.Doppelt-Azeroual,
F.Moriaud,
F.Delfaud,
and
A.G.de Brevern
(2009).
Analysis of HSP90-related folds with MED-SuMo classification approach.
|
| |
Drug Des Devel Ther, 3,
59-72.
|
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|
|
|
|
R.Conde,
Z.R.Belak,
M.Nair,
R.F.O'Carroll,
and
N.Ovsenek
(2009).
Modulation of Hsf1 activity by novobiocin and geldanamycin.
|
| |
Biochem Cell Biol, 87,
845-851.
|
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|
|
|
|
R.I.Feldman,
B.Mintzer,
D.Zhu,
J.M.Wu,
S.L.Biroc,
S.Yuan,
K.Emayan,
Z.Chang,
D.Chen,
D.O.Arnaiz,
J.Bryant,
X.S.Ge,
M.Whitlow,
M.Adler,
M.A.Polokoff,
W.W.Li,
M.Ferrer,
T.Sato,
J.M.Gu,
J.Shen,
J.L.Tseng,
H.Dinter,
and
B.Buckman
(2009).
Potent triazolothione inhibitor of heat-shock protein-90.
|
| |
Chem Biol Drug Des, 74,
43-50.
|
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PDB code:
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|
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R.L.van Montfort,
and
P.Workman
(2009).
Structure-based design of molecular cancer therapeutics.
|
| |
Trends Biotechnol, 27,
315-328.
|
|
|
|
|
|
|
R.M.Immormino,
L.E.Metzger,
P.N.Reardon,
D.E.Dollins,
B.S.Blagg,
and
D.T.Gewirth
(2009).
Different poses for ligand and chaperone in inhibitor-bound Hsp90 and GRP94: implications for paralog-specific drug design.
|
| |
J Mol Biol, 388,
1033-1042.
|
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PDB codes:
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S.Barluenga,
J.G.Fontaine,
C.Wang,
K.Aouadi,
R.Chen,
K.Beebe,
L.Neckers,
and
N.Winssinger
(2009).
Inhibition of HSP90 with pochoximes: SAR and structure-based insights.
|
| |
Chembiochem, 10,
2753-2759.
|
|
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PDB codes:
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S.D.Singh,
N.Robbins,
A.K.Zaas,
W.A.Schell,
J.R.Perfect,
and
L.E.Cowen
(2009).
Hsp90 governs echinocandin resistance in the pathogenic yeast Candida albicans via calcineurin.
|
| |
PLoS Pathog, 5,
e1000532.
|
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|
|
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S.N.Shelton,
M.E.Shawgo,
S.B.Matthews,
Y.Lu,
A.C.Donnelly,
K.Szabla,
M.Tanol,
G.A.Vielhauer,
R.A.Rajewski,
R.L.Matts,
B.S.Blagg,
and
J.D.Robertson
(2009).
KU135, a novel novobiocin-derived C-terminal inhibitor of the 90-kDa heat shock protein, exerts potent antiproliferative effects in human leukemic cells.
|
| |
Mol Pharmacol, 76,
1314-1322.
|
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|
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|
|
T.Taldone,
W.Sun,
and
G.Chiosis
(2009).
Discovery and development of heat shock protein 90 inhibitors.
|
| |
Bioorg Med Chem, 17,
2225-2235.
|
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|
|
V.D.Jadhav,
A.S.Duerfeldt,
and
B.S.Blagg
(2009).
Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors.
|
| |
Bioorg Med Chem Lett, 19,
6845-6850.
|
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|
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|
|
Y.Li,
T.Zhang,
S.J.Schwartz,
and
D.Sun
(2009).
New developments in Hsp90 inhibitors as anti-cancer therapeutics: mechanisms, clinical perspective and more potential.
|
| |
Drug Resist Updat, 12,
17-27.
|
|
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|
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|
|
Y.Li,
T.Zhang,
Y.Jiang,
H.F.Lee,
S.J.Schwartz,
and
D.Sun
(2009).
(-)-Epigallocatechin-3-gallate inhibits Hsp90 function by impairing Hsp90 association with cochaperones in pancreatic cancer cell line Mia Paca-2.
|
| |
Mol Pharm, 6,
1152-1159.
|
|
|
|
|
|
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A.C.Donnelly,
J.R.Mays,
J.A.Burlison,
J.T.Nelson,
G.Vielhauer,
J.Holzbeierlein,
and
B.S.Blagg
(2008).
The design, synthesis, and evaluation of coumarin ring derivatives of the novobiocin scaffold that exhibit antiproliferative activity.
|
| |
J Org Chem, 73,
8901-8920.
|
|
|
|
|
|
|
A.Chakraborty,
M.A.Koldobskiy,
K.M.Sixt,
K.R.Juluri,
A.K.Mustafa,
A.M.Snowman,
D.B.van Rossum,
R.L.Patterson,
and
S.H.Snyder
(2008).
HSP90 regulates cell survival via inositol hexakisphosphate kinase-2.
|
| |
Proc Natl Acad Sci U S A, 105,
1134-1139.
|
|
|
|
|
|
|
A.Donnelly,
and
B.S.Blagg
(2008).
Novobiocin and additional inhibitors of the Hsp90 C-terminal nucleotide-binding pocket.
|
| |
Curr Med Chem, 15,
2702-2717.
|
|
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|
|
|
|
A.Leskovar,
H.Wegele,
N.D.Werbeck,
J.Buchner,
and
J.Reinstein
(2008).
The ATPase cycle of the mitochondrial Hsp90 analog Trap1.
|
| |
J Biol Chem, 283,
11677-11688.
|
|
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|
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|
|
A.Yan,
G.H.Grant,
and
W.G.Richards
(2008).
Dynamics of conserved waters in human Hsp90: implications for drug design.
|
| |
J R Soc Interface, 5,
S199-S205.
|
|
|
|
|
|
|
C.Garcia-Echeverria,
and
W.R.Sellers
(2008).
Drug discovery approaches targeting the PI3K/Akt pathway in cancer.
|
| |
Oncogene, 27,
5511-5526.
|
|
|
|
|
|
|
D.E.Tucker,
M.A.Gijón,
D.M.Spencer,
Z.H.Qiu,
M.H.Gelb,
and
C.C.Leslie
(2008).
Regulation of cytosolic phospholipase A2alpha by hsp90 and a p54 kinase in okadaic acid-stimulated macrophages.
|
| |
J Leukoc Biol, 84,
798-806.
|
|
|
|
|
|
|
D.Hughes,
J.B.Guttenplan,
C.B.Marcus,
K.Subbaramaiah,
and
A.J.Dannenberg
(2008).
Heat shock protein 90 inhibitors suppress aryl hydrocarbon receptor-mediated activation of CYP1A1 and CYP1B1 transcription and DNA adduct formation.
|
| |
Cancer Prev Res (Phila Pa), 1,
485-493.
|
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|
|
D.R.Southworth,
and
D.A.Agard
(2008).
Species-dependent ensembles of conserved conformational states define the Hsp90 chaperone ATPase cycle.
|
| |
Mol Cell, 32,
631-640.
|
|
|
|
|
|
|
E.Jin,
and
M.Sano
(2008).
Neurite outgrowth of NG108-15 cells induced by heat shock protein 90 inhibitors.
|
| |
Cell Biochem Funct, 26,
825-832.
|
|
|
|
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|
|
G.Rancati,
N.Pavelka,
B.Fleharty,
A.Noll,
R.Trimble,
K.Walton,
A.Perera,
K.Staehling-Hampton,
C.W.Seidel,
and
R.Li
(2008).
Aneuploidy underlies rapid adaptive evolution of yeast cells deprived of a conserved cytokinesis motor.
|
| |
Cell, 135,
879-893.
|
|
|
|
|
|
|
J.Y.Cho,
and
J.Park
(2008).
Contribution of Natural Inhibitors to the Understanding of the PI3K/PDK1/PKB Pathway in the Insulin-mediated Intracellular Signaling Cascade.
|
| |
Int J Mol Sci, 9,
2217-2230.
|
|
|
|
|
|
|
L.E.Cowen
(2008).
The evolution of fungal drug resistance: modulating the trajectory from genotype to phenotype.
|
| |
Nat Rev Microbiol, 6,
187-198.
|
|
|
|
|
|
|
L.E.Cowen,
and
W.J.Steinbach
(2008).
Stress, drugs, and evolution: the role of cellular signaling in fungal drug resistance.
|
| |
Eukaryot Cell, 7,
747-764.
|
|
|
|
|
|
|
L.R.Gorbacheva,
T.P.Storozhevykh,
V.G.Pinelis,
O.N.Davydova,
S.Ishiwata,
and
S.M.Strukova
(2008).
Activated protein C via PAR1 receptor regulates survival of neurons under conditions of glutamate excitotoxicity.
|
| |
Biochemistry (Mosc), 73,
717-724.
|
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Structures of the N-terminal and middle domains of E. coli Hsp90 and conformation changes upon ADP binding.
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PDB codes:
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Q.Xie,
C.F.Gao,
N.Shinomiya,
E.Sausville,
R.Hay,
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Geldanamycins exquisitely inhibit HGF/SF-mediated tumor cell invasion.
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Oncogene, 24,
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Hsp90 inhibitors deplete key anti-apoptotic proteins in pediatric solid tumor cells and demonstrate synergistic anticancer activity with cisplatin.
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Int J Cancer, 113,
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Solution- and solid-phase synthesis of radicicol (monorden) and pochonin C.
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Chemistry, 11,
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Regulation of the Src family kinase Lck by Hsp90 and ubiquitination.
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Mol Cell Biol, 24,
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Therapeutic and diagnostic implications of Hsp90 activation.
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Rapid glucocorticoid receptor exchange at a promoter is coupled to transcription and regulated by chaperones and proteasomes.
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Mol Cell Biol, 24,
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S.J.Santos,
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Hsp90/p50cdc37 is required for mixed-lineage kinase (MLK) 3 signaling.
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J Biol Chem, 279,
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Kaposi's sarcoma as a model for cancer immunotherapy.
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Trends Mol Med, 10,
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Hsp90 regulates the activity of wild type p53 under physiological and elevated temperatures.
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J Biol Chem, 279,
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Evidence that hsp90 is involved in the altered interactions of Acanthamoeba castellanii variants with bacteria.
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Eukaryot Cell, 3,
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M.D.Galigniana,
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Hsp90-binding immunophilins link p53 to dynein during p53 transport to the nucleus.
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J Biol Chem, 279,
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Trends Mol Med, 10,
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Ligand-induced conformational shift in the N-terminal domain of GRP94, an Hsp90 chaperone.
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J Biol Chem, 279,
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PDB codes:
|
|
|
|
|
|
|
|
T.Gidalevitz,
C.Biswas,
H.Ding,
D.Schneidman-Duhovny,
H.J.Wolfson,
F.Stevens,
S.Radford,
and
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Identification of the N-terminal peptide binding site of glucose-regulated protein 94.
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J Biol Chem, 279,
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Geldanamycin, a ligand of heat shock protein 90, inhibits the replication of herpes simplex virus type 1 in vitro.
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Antimicrob Agents Chemother, 48,
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A.Dehner,
J.Furrer,
K.Richter,
I.Schuster,
J.Buchner,
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NMR chemical shift perturbation study of the N-terminal domain of Hsp90 upon binding of ADP, AMP-PNP, geldanamycin, and radicicol.
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Chembiochem, 4,
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C.L.David,
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D.A.Raynes,
E.J.Pulcini,
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Expression of a unique drug-resistant Hsp90 ortholog by the nematode Caenorhabditis elegans.
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Cell Stress Chaperones, 8,
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J.M.Jez,
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R.M.Stroud,
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(2003).
Crystal structure and molecular modeling of 17-DMAG in complex with human Hsp90.
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| |
Chem Biol, 10,
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PDB code:
|
|
|
|
|
|
|
|
J.Ou,
Z.Ou,
A.W.Ackerman,
K.T.Oldham,
and
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(2003).
Inhibition of heat shock protein 90 (hsp90) in proliferating endothelial cells uncouples endothelial nitric oxide synthase activity.
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Free Radic Biol Med, 34,
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K.L.Soldano,
A.Jivan,
C.V.Nicchitta,
and
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(2003).
Structure of the N-terminal domain of GRP94. Basis for ligand specificity and regulation.
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| |
J Biol Chem, 278,
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PDB codes:
|
|
|
|
|
|
|
|
L.Wang,
W.Sullivan,
D.Toft,
and
R.Weinshilboum
(2003).
Thiopurine S-methyltransferase pharmacogenetics: chaperone protein association and allozyme degradation.
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| |
Pharmacogenetics, 13,
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P.Chène
(2003).
The ATPases: a new family for a family-based drug design approach.
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Expert Opin Ther Targets, 7,
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P.Meyer,
C.Prodromou,
B.Hu,
C.Vaughan,
S.M.Roe,
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P.W.Piper,
and
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(2003).
Structural and functional analysis of the middle segment of hsp90: implications for ATP hydrolysis and client protein and cochaperone interactions.
|
| |
Mol Cell, 11,
647-658.
|
|
|
PDB code:
|
|
|
|
|
|
|
|
P.W.Piper,
S.H.Millson,
M.Mollapour,
B.Panaretou,
G.Siligardi,
L.H.Pearl,
and
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(2003).
Sensitivity to Hsp90-targeting drugs can arise with mutation to the Hsp90 chaperone, cochaperones and plasma membrane ATP binding cassette transporters of yeast.
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| |
Eur J Biochem, 270,
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The heat shock protein 90 of Plasmodium falciparum and antimalarial activity of its inhibitor, geldanamycin.
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Malar J, 2,
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Hsp90 inhibition depletes Chk1 and sensitizes tumor cells to replication stress.
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J Biol Chem, 278,
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S.Kim,
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W.Hu,
B.M.Evers,
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Geldanamycin decreases Raf-1 and Akt levels and induces apoptosis in neuroblastomas.
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Int J Cancer, 103,
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S.Wax,
M.Piecyk,
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and
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Geldanamycin inhibits the production of inflammatory cytokines in activated macrophages by reducing the stability and translation of cytokine transcripts.
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| |
Arthritis Rheum, 48,
541-550.
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and
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HSP90 as a new therapeutic target for cancer therapy: the story unfolds.
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Expert Opin Biol Ther, 2,
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T.A.Sangster,
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Hsp90 as a capacitor of phenotypic variation.
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Nature, 417,
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A Nucleotide-dependent molecular switch controls ATP binding at the C-terminal domain of Hsp90. N-terminal nucleotide binding unmasks a C-terminal binding pocket.
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J Biol Chem, 277,
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H.C.Lee,
T.Hon,
and
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(2002).
The molecular chaperone Hsp90 mediates heme activation of the yeast transcriptional activator Hap1.
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J Biol Chem, 277,
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I.Luque,
and
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Structural parameterization of the binding enthalpy of small ligands.
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Hsp90 inhibitors as novel cancer chemotherapeutic agents.
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ATPases as drug targets: learning from their structure.
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Nat Rev Drug Discov, 1,
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S.A.Harvey,
K.O.Jensen,
L.W.Elmore,
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S.E.Holt
(2002).
Pharmacological approaches to defining the role of chaperones in aging and prostate cancer progression.
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| |
Cell Stress Chaperones, 7,
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S.E.Graefe,
M.Wiesgigl,
I.Gaworski,
A.Macdonald,
and
J.Clos
(2002).
Inhibition of HSP90 in Trypanosoma cruzi induces a stress response but no stage differentiation.
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| |
Eukaryot Cell, 1,
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S.S.Billecke,
A.T.Bender,
K.C.Kanelakis,
P.J.Murphy,
E.R.Lowe,
Y.Kamada,
W.B.Pratt,
and
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hsp90 is required for heme binding and activation of apo-neuronal nitric-oxide synthase: geldanamycin-mediated oxidant generation is unrelated to any action of hsp90.
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J Biol Chem, 277,
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T.Gidalevitz,
C.Biswas,
B.B.Simen,
E.Stein,
F.Gulmen,
and
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Radicicol-sensitive peptide binding to the N-terminal portion of GRP94.
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J Biol Chem, 277,
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T.Sakisaka,
T.Meerlo,
J.Matteson,
H.Plutner,
and
W.E.Balch
(2002).
Rab-alphaGDI activity is regulated by a Hsp90 chaperone complex.
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| |
EMBO J, 21,
6125-6135.
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A.Tuganova,
M.D.Yoder,
and
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An essential role of Glu-243 and His-239 in the phosphotransfer reaction catalyzed by pyruvate dehydrogenase kinase.
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J Biol Chem, 276,
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F.G.Zhu,
and
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(2001).
Role of the heat shock protein 90 in immune response stimulation by bacterial DNA and synthetic oligonucleotides.
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Infect Immun, 69,
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G.Chiosis,
M.N.Timaul,
B.Lucas,
P.N.Munster,
F.F.Zheng,
L.Sepp-Lorenzino,
and
N.Rosen
(2001).
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.
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| |
Chem Biol, 8,
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H.J.Ochel,
K.Eichhorn,
and
G.Gademann
(2001).
Geldanamycin: the prototype of a class of antitumor drugs targeting the heat shock protein 90 family of molecular chaperones.
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K.Richter,
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Hsp90: chaperoning signal transduction.
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J Cell Physiol, 188,
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L.Waxman,
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B.A.Pollok,
L.C.Kuo,
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P.L.Darke
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Host cell factor requirement for hepatitis C virus enzyme maturation.
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Proc Natl Acad Sci U S A, 98,
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M.C.Rosenhagen,
J.C.Young,
G.M.Wochnik,
A.S.Herr,
U.Schmidt,
F.U.Hartl,
F.Holsboer,
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Synergistic inhibition of the glucocorticoid receptor by radicicol and benzoquinone ansamycins.
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Biol Chem, 382,
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O.Donzé,
T.Abbas-Terki,
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The Hsp90 chaperone complex is both a facilitator and a repressor of the dsRNA-dependent kinase PKR.
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EMBO J, 20,
3771-3780.
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Radicicol binding to Swo1/Hsp90 and inhibition of growth of specific temperature-sensitive cell cycle mutants of fission yeast.
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Biosci Biotechnol Biochem, 65,
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C.Prodromou,
B.Panaretou,
S.Chohan,
G.Siligardi,
R.O'Brien,
J.E.Ladbury,
S.M.Roe,
P.W.Piper,
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The ATPase cycle of Hsp90 drives a molecular 'clamp' via transient dimerization of the N-terminal domains.
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| |
EMBO J, 19,
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L.H.Pearl,
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Hsp90 is essential for the synthesis and subsequent membrane association, but not the maintenance, of the Src-kinase p56(lck).
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| |
Mol Biol Cell, 11,
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S.J.Felts,
B.A.Owen,
P.Nguyen,
J.Trepel,
D.B.Donner,
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The hsp90-related protein TRAP1 is a mitochondrial protein with distinct functional properties.
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J Biol Chem, 275,
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T.Schnaider,
J.Somogyi,
P.Csermely,
and
M.Szamel
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The Hsp90-specific inhibitor geldanamycin selectively disrupts kinase-mediated signaling events of T-lymphocyte activation.
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| |
Cell Stress Chaperones, 5,
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L.Neckers,
E.Mimnaugh,
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T.W.Schulte
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Hsp90 as an anti-cancer target.
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| |
Drug Resist Updat, 2,
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S.Y.Sharp,
P.M.Rogers,
T.G.Myers,
and
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DT-Diaphorase expression and tumor cell sensitivity to 17-allylamino, 17-demethoxygeldanamycin, an inhibitor of heat shock protein 90.
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J Natl Cancer Inst, 91,
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|
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|
|
|
The most recent references are shown first.
Citation data come partly from CiteXplore and partly
from an automated harvesting procedure. Note that this is likely to be
only a partial list as not all journals are covered by
either method. However, we are continually building up the citation data
so more and more references will be included with time.
Where a reference describes a PDB structure, the PDB
code is
shown on the right.
|
|
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