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Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A.
TLDR
Tubastatin A, a hydroxamate-containing HDAC6-selective compound, displayed no neuronal toxicity, thus, forecasting the potential application of this agent and its analogues to neurodegenerative conditions.
HDAC6 inhibitors reverse axonal loss in a mouse model of mutant HSPB1–induced Charcot-Marie-Tooth disease
TLDR
An increase of α-tubulin acetylation induced by pharmacological inhibition of histone deacetylase 6 (HDAC6) corrected the axonal transport defects caused by HSPB1 mutations and rescued the CMT phenotype of symptomatic mutant H SPB1 mice.
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth.
TLDR
This work represents the first attempt to examine the effects of 3-modified PI analogues on these two crucial cell signaling proteins, PI3-K and Akt, in an effort to better understand their cell growth inhibitory properties.
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
TLDR
A series of hydroxamate based HDAC inhibitors containing a phenylisoxazole as the CAP group has been synthesized using nitrile oxide cycloaddition chemistry, providing valuable, new molecular probes for use in exploring HDAC biology.
HDAC6 is a target for protection and regeneration following injury in the nervous system
TLDR
It is shown that pan-HDAC inhibition not only promotes neuronal protection against oxidative stress, a common mediator of injury in many neurological conditions, but also promotes neurite growth on myelin-associated glycoprotein and chondroitin sulfate proteoglycan substrates.
The amino terminus of tau inhibits kinesin‐dependent axonal transport: Implications for filament toxicity
TLDR
It is suggested that pathological tau aggregation contributes to neurodegeneration by altering a regulatory pathway for FAT in response to Alzheimer's disease and other tauopathies.
RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells
TLDR
RI-1 is described, a small molecule that inhibits the central recombination protein RAD51 and specifically reduces gene conversion in human cells while stimulating single strand annealing and potentiates the lethal effects of a DNA cross-linking drug inhuman cells.
Novel PI analogues selectively block activation of the pro-survival serine/threonine kinase Akt.
TLDR
Specific inhibition of Akt by these compounds validates ligand design targeted to the PH domains of crucial signaling proteins, thus providing a unique class of possible cancer therapeutics.
Histone Deacetylase 6 and Heat Shock Protein 90 Control the Functions of Foxp3+ T-Regulatory Cells
TLDR
It is shown that HDAC6 inhibition promotes Treg suppressive activity in models of inflammation and autoimmunity, including multiple forms of experimental colitis and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection.
NAAG peptidase inhibitors and their potential for diagnosis and therapy
TLDR
This new class of compounds, of which at least one has entered clinical trials and proven to be well tolerated, has demonstrated efficacy in experimental models of pain, schizophrenia, amyotrophic lateral sclerosis, traumatic brain injury and, when appropriately functionalized, can image prostate cancer.
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