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BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90
Inhibition of heat shock protein 90 (Hsp90) results in the degradation of oncoproteins that drive malignant progression, inducing cell death, making Hsp90 a target of substantial interest for cancerExpand
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Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.
Heat shock protein 90 (Hsp90) is a molecular chaperone protein implicated in stabilizing the conformation and maintaining the function of many cell-signaling proteins. Many oncogenic proteins areExpand
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Intrinsically disordered proteins drive membrane curvature
Assembly of highly curved membrane structures is essential to cellular physiology. The prevailing view has been that proteins with curvature-promoting structural motifs, such as wedge-likeExpand
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Synuclein accumulation is associated with cell‐specific neuronal death after spinal cord injury
Spinal cord injury axotomizes neurons and induces many of them to die, whereas others survive. Therefore, it is important to identify factors that lead to neuronal death after injury as a first stepExpand
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7'-substituted benzothiazolothio- and pyridinothiazolothio-purines as potent heat shock protein 90 inhibitors.
We report on the discovery of benzo- and pyridino- thiazolothiopurines as potent heat shock protein 90 inhibitors. The benzothiazole moiety is exceptionally sensitive to substitutions on the aromaticExpand
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Acute increase of α-synuclein inhibits synaptic vesicle recycling evoked during intense stimulation
This is the first study to show the direct effects of α-synuclein on synaptic vesicle trafficking and to elucidate the underlying structural mechanisms. Acutely increasing α-synuclein severelyExpand
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Orally active purine-based inhibitors of the heat shock protein 90.
Orally active Hsp90 inhibitors are of interest as potential chemotherapeutic agents. Recently, fully synthetic 8-benzyladenines and 8-sulfanyladenines such as 4 were disclosed as Hsp90 inhibitors,Expand
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BIIB 021 , an orally available , fully synthetic small-molecule inhibitor of the heat shock protein Hsp 90
Inhibition of heat shock protein 90 (Hsp90) results in the degradation of oncoproteins that drive malignant progression, inducing cell death, making Hsp90 a target of substantial interest for cancerExpand
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Multifunctional Transmembrane Protein Ligands for Cell-Specific Targeting of Plasma Membrane-Derived Vesicles.
Liposomes and nanoparticles that bind selectively to cell-surface receptors can target specific populations of cells. However, chemical conjugation of ligands to these particles is difficult toExpand
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Reducing synuclein accumulation improves neuronal survival after spinal cord injury
Spinal cord injury causes neuronal death, limiting subsequent regeneration and recovery. Thus, there is a need to develop strategies for improving neuronal survival after injury. Relative to ourExpand
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