106 articles for thisTarget
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Article Title
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Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase.
Vernalis (R&D)
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
Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors.
Korea University
Virtual screening and biophysical studies lead to HSP90 inhibitors.
University of Auckland
Development of Glucose Regulated Protein 94-Selective Inhibitors Based on the BnIm and Radamide Scaffold.
The University of Kansas
Synthesis and biological evaluation of 3,5-disubstituted-4-alkynylisoxozales as a novel class of HSP90 inhibitors.
Chengdu University of Tcm
Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94.
Sloan-Kettering Institute For Cancer Research
Discovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors.
Vertex Pharmaceuticals
Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors.
Shandong University
Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990.
Novartis Institutes For Biomedical Research
Discovery of potent N-(isoxazol-5-yl)amides as HSP90 inhibitors.
Chinese Academy of Sciences
Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors.
Shandong University
Identification of a new series of potent diphenol HSP90 inhibitors by fragment merging and structure-based optimization.
Chinese Academy of Sciences
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
Universit£
Differences in conformational dynamics between Plasmodium falciparum and human Hsp90 orthologues enable the structure-based discovery of pathogen-selective inhibitors.
University of Geneva
4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.
Universit£
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
A chemical-biological study reveals C9-type iridoids as novel heat shock protein 90 (Hsp90) inhibitors.
Universit£
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
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
Kosan Biosciences
Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin.
University College London
Design and synthesis of novel macrocyclic 2-amino-6-arylpyrimidine Hsp90 inhibitors.
Chugai Pharmaceutical
Lead generation of heat shock protein 90 inhibitors by a combination of fragment-based approach, virtual screening, and structure-based drug design.
Chugai Pharmaceutical
Lead identification ofß-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90.
Trinity College
Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model.
Pfizer
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
Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity.
Pfizer
Efficient synthesis of Hsp90 inhibitor dimers as potential antitumor agents.
Hokkaido University
5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone.
Fermentas
Synthesis of a red-shifted fluorescence polarization probe for Hsp90.
Memorial Sloan-Kettering Cancer Center
Pan- and isoform-specific inhibition of Hsp90: Design strategy and recent advances.
Shandong University
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
Design, synthesis, and biological evalution of bifunctional inhibitors against Hsp90-HDAC6 interplay.
Keimyung University
Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90.
Memorial Sloan-Kettering Cancer Center
Novel N-(4-thiocyanatophenyl)-1H-1,2,3-triazole-4-carboxamides exhibit selective cytotoxic activity at nanomolar doses towards human leukemic T-cells.
Ivan Franko National University of Lviv
Crystal structures of human HSP90alpha-complexed with dihydroxyphenylpyrazoles.
Genomics Institute of The Novartis Research Foundation
Design and synthesis of Grp94 selective inhibitors based on Phe199 induced fit mechanism and their anti-inflammatory effects.
China Pharmaceutical University
Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors.
Taiho Pharmaceutical
Design and Synthesis of TRAP1 Selective Inhibitors: H-Bonding with Asn171 Residue in TRAP1 Increases Paralog Selectivity.
Ewha Womans University
2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents.
China Medical University
Fluoropyrimidin-2,4-dihydroxy-5-isopropylbenzamides as antitumor agents against CRC and NSCLC cancer cells.
Taipei Medical University
Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach.
Sun Yat-Sen University
The Development of Hsp90?-Selective Inhibitors to Overcome Detriments Associated with
The University of Notre Dame
Novel Tetrahydropyrido[4,3-d]pyrimidines as Potent Inhibitors of Chaperone Heat Shock Protein 90.
China Pharmaceutical University
Biological Evaluation of 5'-(
National Institute of Diabetes and Digestive and Kidney Diseases
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
Taipei Medical University
Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
South China Sea Institute of Oceanology
LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family.
Department of Molecular Oncogenesis
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)
Blinded predictions of binding modes and energies of HSP90-? ligands for the 2015 D3R grand challenge.
University of Edinburgh
Structure-activity relationship of Garcinia xanthones analogues: Potent Hsp90 inhibitors with cytotoxicity and antiangiogenesis activity.
China Pharmaceutical University
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
Fusicoccane Diterpenes from Hypoestes forsskaolii as Heat Shock Protein 90 (Hsp90) Modulators.
Universit£
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions.
China Pharmaceutical University
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
N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-? induced PD-L1 expression.
Taipei Medical University
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
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
East China Normal University
Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.
China Pharmaceutical University
Bioactive limonoids from the leaves of Azaridachta indica (Neem).
Universidad De Los Andes
Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors.
Chugai Pharmaceutical
Targeting the hydrophobic region of Hsp90's ATP binding pocket with novel 1,3,5-triazines.
Kyungpook National University
Design, synthesis, and biological evaluation of a series of resorcinol-based N-benzyl benzamide derivatives as potent Hsp90 inhibitors.
Keimyung University
1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
Taipei Medical University
Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90).
National University of Singapore
Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis.
China Pharmaceutical University
Design, synthesis and pharmacological evaluation of ALK and Hsp90 dual inhibitors bearing resorcinol and 2,4-diaminopyrimidine motifs.
Chinese Academy of Sciences
New TRAP1 and Hsp90 chaperone inhibitors with cationic components: Preliminary studies on mitochondrial targeting.
University of Ferrara
Structure Based Design of a Grp94-Selective Inhibitor: Exploiting a Key Residue in Grp94 To Optimize Paralog-Selective Binding.
Hauptman-Woodward Medical Research Institute
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
Design and synthesis of neolamellarin a derivatives targeting heat shock protein 90.
Ocean University of China
Rational Design of Selective Adenine-Based Scaffolds for Inactivation of Bacterial Histidine Kinases.
University of Minnesota
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.
Ulsan National Institutes of Science and Technology (Unist)
Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors.
Cairo University
Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells.
Cerebrus
Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.
Csic
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
Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization.
Human Biomolecular Research Institute
Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors.
Uppsala University