The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28199108 |
106 |
Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
Vernalis (R&D) |
10340605 |
5 |
Synthesis and evaluation of geldanamycin-estradiol hybrids. |
Sloan-Kettering Institute For Cancer Research |
27783977 |
12 |
Targeting the entry region of Hsp90's ATP binding pocket with a novel 6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl amide. |
Keimyung University |
27914802 |
12 |
Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors. |
Korea University |
27913182 |
5 |
Virtual screening and biophysical studies lead to HSP90 inhibitors. |
University of Auckland |
27003516 |
78 |
Development of Glucose Regulated Protein 94-Selective Inhibitors Based on the BnIm and Radamide Scaffold. |
The University of Kansas |
26112442 |
74 |
Synthesis and biological evaluation of 3,5-disubstituted-4-alkynylisoxozales as a novel class of HSP90 inhibitors. |
Chengdu University of Tcm |
25799158 |
6 |
Volume of Distribution in Drug Design. |
Pharmacokinetics |
25901531 |
211 |
Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94. |
Sloan-Kettering Institute For Cancer Research |
25677667 |
17 |
Discovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors. |
Vertex Pharmaceuticals |
25105924 |
5 |
Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
Shandong University |
25368984 |
14 |
Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990. |
Novartis Institutes For Biomedical Research |
25313505 |
35 |
Discovery of potent N-(isoxazol-5-yl)amides as HSP90 inhibitors. |
Chinese Academy of Sciences |
25277067 |
7 |
Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
Shandong University |
24751441 |
18 |
Identification of a new series of potent diphenol HSP90 inhibitors by fragment merging and structure-based optimization. |
Chinese Academy of Sciences |
24588105 |
56 |
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold. |
Universit£ |
24580531 |
6 |
Differences in conformational dynamics between Plasmodium falciparum and human Hsp90 orthologues enable the structure-based discovery of pathogen-selective inhibitors. |
University of Geneva |
24565573 |
35 |
4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
Universit£ |
24673104 |
185 |
Identification of novel HSP90a/ß isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as Huntington's disease. |
Vertex Pharmaceuticals |
23362862 |
13 |
A chemical-biological study reveals C9-type iridoids as novel heat shock protein 90 (Hsp90) inhibitors. |
Universit£ |
22938030 |
22 |
EC144 is a potent inhibitor of the heat shock protein 90. |
Biogen Idec |
21438541 |
45 |
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyr |
Pfizer |
20055425 |
29 |
Heat shock protein 90: inhibitors in clinical trials. |
Biogen Idec |
19231864 |
6 |
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
Kosan Biosciences |
16854066 |
44 |
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
Infinity Pharmaceuticals |
16165354 |
19 |
Structure-based design of 7-carbamate analogs of geldanamycin. |
Kosan Biosciences |
9925731 |
4 |
Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin. |
University College London |
22192591 |
17 |
Design and synthesis of novel macrocyclic 2-amino-6-arylpyrimidine Hsp90 inhibitors. |
Chugai Pharmaceutical |
21875802 |
33 |
Lead generation of heat shock protein 90 inhibitors by a combination of fragment-based approach, virtual screening, and structure-based drug design. |
Chugai Pharmaceutical |
21920765 |
12 |
Lead identification ofß-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90. |
Trinity College |
21715165 |
31 |
Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model. |
Pfizer |
21106457 |
41 |
N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors. |
Abbott Laboratories |
21605975 |
31 |
Discovery of a macrocyclic o-aminobenzamide Hsp90 inhibitor with heterocyclic tether that shows extended biomarker activity and in vivo efficacy in a mouse xenograft model. |
Pfizer |
21420297 |
19 |
Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity. |
Pfizer |
20609590 |
10 |
Efficient synthesis of Hsp90 inhibitor dimers as potential antitumor agents. |
Hokkaido University |
19168355 |
7 |
5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone. |
Fermentas |
16797988 |
4 |
Synthesis of a red-shifted fluorescence polarization probe for Hsp90. |
Memorial Sloan-Kettering Cancer Center |
16621545 |
6 |
Synthesis of Hsp90 dimerization modulators. |
Memorial Sloan-Kettering Cancer Center |
16530412 |
13 |
High-throughput screening for Hsp90 ATPase inhibitors. |
The University of Kansas |
16480864 |
38 |
4-Amino derivatives of the Hsp90 inhibitor CCT018159. |
Vernalis |
15828828 |
136 |
Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90. |
Memorial Sloan-Kettering Cancer Center |
15713410 |
2 |
Crystal structures of human HSP90alpha-complexed with dihydroxyphenylpyrazoles. |
Genomics Institute of The Novartis Research Foundation |
15239664 |
92 |
Synthesis and biological evaluation of a new class of geldanamycin derivatives as potent inhibitors of Hsp90. |
Conforma Therapeutics |
14698151 |
14 |
Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures. |
Ribotargets |
14592488 |
2 |
Synthesis of novel fluorescent probes for the molecular chaperone Hsp90. |
Memorial Sloan-Kettering Cancer Center |
32305165 |
72 |
Discovery of novel heat shock protein (Hsp90) inhibitors based on luminespib with potent antitumor activity. |
Seoul National University |
32222339 |
5 |
Synthesis of novel dual target inhibitors of PARP and HSP90 and their antitumor activities. |
Fujian Medical University (Fmu) |
32832020 |
1 |
From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition. |
The University of Notre Dame |
32527461 |
1 |
Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents. |
Bengbu Medical College |
32324396 |
17 |
p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators. |
China Pharmaceutical University |
32273216 |
6 |
Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities. |
South China Sea Institute of Oceanology |
11294389 |
27 |
LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family. |
Department of Molecular Oncogenesis |
31839539 |
60 |
Discovery of 2-((4-resorcinolyl)-5-aryl-1,2,3-triazol-1-yl)acetates as potent Hsp90 inhibitors with selectivity over TRAP1. |
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif) |
27485604 |
5 |
Blinded predictions of binding modes and energies of HSP90-? ligands for the 2015 D3R grand challenge. |
University of Edinburgh |
27527413 |
25 |
Structure-activity relationship of Garcinia xanthones analogues: Potent Hsp90 inhibitors with cytotoxicity and antiangiogenesis activity. |
China Pharmaceutical University |
27476419 |
70 |
C15-methoxyphenylated 18-deoxy-herbimycin A analogues, their in vitro anticancer activity and heat shock protein 90 binding affinity. |
Peking Union Medical College & Chinese Academy of Medical Sciences |
26844689 |
22 |
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
Chinese Academy of Sciences |
30839211 |
12 |
Fusicoccane Diterpenes from Hypoestes forsskaolii as Heat Shock Protein 90 (Hsp90) Modulators. |
Universit£ |
30597326 |
50 |
High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity. |
Jiangsu Normal University |
31663736 |
15 |
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions. |
China Pharmaceutical University |
31469962 |
122 |
Identification of Novel Resorcinol Amide Derivatives as Potent and Specific Pyruvate Dehydrogenase Kinase (PDHK) Inhibitors. |
Korea University |
31935086 |
19 |
Discovery and Optimization of Small Molecules Targeting the Protein-Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer. |
China Pharmaceutical University |
31655430 |
56 |
N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-? induced PD-L1 expression. |
Taipei Medical University |
30525599 |
33 |
Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor. |
Taiho Pharmaceutical |
32352777 |
8 |
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
East China Normal University |
30769242 |
14 |
Clinical candidates modulating protein-protein interactions: The fragment-based experience. |
Taros Chemicals |
30784881 |
8 |
Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors. |
China Pharmaceutical University |
31188592 |
39 |
Why Some Targets Benefit from beyond Rule of Five Drugs. |
Boston University |
30048133 |
1 |
Allosteric Modulators of HSP90 and HSP70: Dynamics Meets Function through Structure-Based Drug Design. |
Istituto Di Chimica Del Riconoscimento Molecolare |
31519378 |
1 |
C-terminal modulators of heat shock protein of 90?kDa (HSP90): State of development and modes of action. |
Heinrich Heine University D£Sseldorf |
27818030 |
5 |
Optimization and bioevaluation of Cdc37-derived peptides: An insight into Hsp90-Cdc37 protein-protein interaction modulators. |
China Pharmaceutical University |
25141341 |
1 |
Progress in the discovery and development of heat shock protein 90 (Hsp90) inhibitors. |
Montclair State University |
24499352 |
3 |
Bioactive limonoids from the leaves of Azaridachta indica (Neem). |
Universidad De Los Andes |
24369839 |
18 |
Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors. |
Chugai Pharmaceutical |
24125885 |
2 |
Targeting the hydrophobic region of Hsp90's ATP binding pocket with novel 1,3,5-triazines. |
Kyungpook National University |
23859777 |
5 |
Synthesis and biological evaluation of novobiocin analogues as potential heat shock protein 90 inhibitors. |
University of Arizona |
23520985 |
12 |
Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening. |
Universit£ |
23606927 |
11 |
3D-QSAR Assisted Design, Synthesis and Evaluation of Novobiocin Analogues. |
The University of Kansas |
22877636 |
60 |
Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90. |
Exelixis |
22913511 |
91 |
Discovery of (2S)-1-[4-(2-{6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9H-purin-9-yl}ethyl)piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a purine-based Hsp90 inhibitor. |
Myrexis |
21486005 |
3 |
Gambogic acid, a natural product inhibitor of Hsp90. |
Oklahoma State University |
21612924 |
10 |
Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone. |
Pfizer |
20718493 |
29 |
Fragment-based drug discovery applied to Hsp90. Discovery of two lead series with high ligand efficiency. |
Astex Therapeutics |
20655237 |
8 |
Natural and semisynthetic azaphilones as a new scaffold for Hsp90 inhibitors. |
Universit£ |
20570149 |
4 |
Click chemistry to probe Hsp90: Synthesis and evaluation of a series of triazole-containing novobiocin analogues. |
The University of Kansas |
19908836 |
11 |
Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone. |
Pfizer |
19395259 |
28 |
Discovery of 5-substituted 2-amino-4-chloro-8-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7,8-dihydropteridin-6(5H)-ones as potent and selective Hsp90 inhibitors. |
Poniard Pharmaceuticals |
19552433 |
49 |
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
Serenex |
18929486 |
41 |
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone. |
Pfizer |
19101151 |
34 |
Synthesis and evaluation of Hsp90 inhibitors that contain the 1,4-naphthoquinone scaffold. |
The University of Kansas |
18762423 |
20 |
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. |
Emory University |
18571929 |
45 |
Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling. |
Emory University |
18020309 |
1 |
Derrubone, an inhibitor of the Hsp90 protein folding machinery. |
The University of Kansas |
29202402 |
24 |
Design, synthesis, and biological evaluation of a series of resorcinol-based N-benzyl benzamide derivatives as potent Hsp90 inhibitors. |
Keimyung University |
29567459 |
49 |
1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
Taipei Medical University |
29545103 |
27 |
Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90). |
National University of Singapore |
29701469 |
52 |
Ligand Desolvation Steers On-Rate and Impacts Drug Residence Time of Heat Shock Protein 90 (Hsp90) Inhibitors. |
University of Vienna |
30351001 |
16 |
Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis. |
China Pharmaceutical University |
29698859 |
30 |
Design, synthesis and pharmacological evaluation of ALK and Hsp90 dual inhibitors bearing resorcinol and 2,4-diaminopyrimidine motifs. |
Chinese Academy of Sciences |
28482218 |
3 |
Structure-based virtual screening and optimization of modulators targeting Hsp90-Cdc37 interaction. |
China Pharmaceutical University |
29057043 |
40 |
Resorcinol-Based Grp94-Selective Inhibitors. |
The University of Kansas |
29807796 |
12 |
New TRAP1 and Hsp90 chaperone inhibitors with cationic components: Preliminary studies on mitochondrial targeting. |
University of Ferrara |
29528635 |
14 |
Structure Based Design of a Grp94-Selective Inhibitor: Exploiting a Key Residue in Grp94 To Optimize Paralog-Selective Binding. |
Hauptman-Woodward Medical Research Institute |
27688186 |
31 |
Design, synthesis and pharmacological evaluation of 4,5-diarylisoxazols bearing amino acid residues within the 3-amido motif as potent heat shock protein 90 (Hsp90) inhibitors. |
China Pharmaceutical University |
28426997 |
4 |
Design and synthesis of neolamellarin a derivatives targeting heat shock protein 90. |
Ocean University of China |
28933546 |
1 |
Rational Design of Selective Adenine-Based Scaffolds for Inactivation of Bacterial Histidine Kinases. |
University of Minnesota |
28816449 |
14 |
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors. |
Ulsan National Institutes of Science and Technology (Unist) |
28500957 |
30 |
Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors. |
Cairo University |
10498829 |
62 |
Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells. |
Cerebrus |
19374444 |
45 |
Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
Csic |
18921992 |
9 |
Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications. |
Pfizer |
17125252 |
60 |
Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization. |
Human Biomolecular Research Institute |
12694187 |
9 |
Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors. |
Uppsala University |
16420031 |
46 |
Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties. |
Instituto De Quimica Medica (Csic) |