Activation of the ATPase activity of hsp90 by the stress-regulated cochaperone aha1Mechanistic evaluation of the novel HSP90 inhibitor NVP-AUY922 in adult and pediatric glioblastomaA selective PIKfyve inhibitor blocks PtdIns(3,5)P(2) production and disrupts endomembrane transport and retroviral budding.Finding the needle in the haystack: why high-throughput screening is good for your health.Maximizing the Therapeutic Potential of HSP90 InhibitorsA structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancerIdentification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaborationThe identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancerStructural basis of the radicicol resistance displayed by a fungal hsp90Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperoneImidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidateInhibition of Hsp90 with resorcylic acid macrolactones: synthesis and binding studiesCo-Crystalization and In Vitro Biological Characterization of 5-Aryl-4-(5-Substituted-2-4-Dihydroxyphenyl)-1,2,3-Thiadiazole Hsp90 InhibitorsTargeting the Hsp90 molecular chaperone with novel macrolactams. Synthesis, structural, binding, and cellular studiesOptimization of Imidazo[4,5- b ]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid LeukemiaAurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells.AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activityNaturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug ResistanceDiscovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70.BRAF and NRAS mutations in melanoma: potential relationships to clinical response to HSP90 inhibitors.Critical parameters in targeted drug development: the pharmacological audit trailNiacin induces PPARgamma expression and transcriptional activation in macrophages via HM74 and HM74a-mediated induction of prostaglandin synthesis pathwaysPharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft modelsNVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasisPharmacodynamic biomarkers for molecular cancer therapeuticsA phase I study of the heat shock protein 90 inhibitor alvespimycin (17-DMAG) given intravenously to patients with advanced solid tumorsMolecular and phenotypic characterisation of paediatric glioma cell lines as models for preclinical drug developmentMechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signallingDistinctive Behaviors of Druggable Proteins in Cellular NetworksThe HSP90 inhibitor NVP-AUY922 radiosensitizes by abrogation of homologous recombination resulting in mitotic entry with unresolved DNA damageAssessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinasesExpression of kinase-defective mutants of c-Src in human metastatic colon cancer cells decreases Bcl-xL and increases oxaliplatin- and Fas-induced apoptosis.Imaging biomarker roadmap for cancer studiesA fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms.Polypharmacology in Precision Oncology: Current Applications and Future ProspectsAssays for the identification and evaluation of histone acetyltransferase inhibitors.Minimizing bias in target selection by exploiting multidisciplinary Big Data and the protein interactome.Cassette dosing pharmacokinetics of a library of 2,6,9-trisubstituted purine cyclin-dependent kinase 2 inhibitors prepared by parallel synthesis.
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