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Histone Deacetylase (HDAC) Inhibitors - emerging roles in neuronal memory, learning, synaptic plasticity and neural regeneration.
Abstract Epigenetic regulation of neuronal signalling through histone acetylation dictates transcription programs that govern neuronal memory, plasticity and learning paradigms. Histone Acetyl Transferases (HATs) and Histone Deacetylases (HDACs) are antagonistic enzymes that regulate gene expression through acetylation and deacetylation of histone proteins around which DNA is wrapped inside a eukaryotic cell nucleus. The epigenetic control of HDACs and the cellular imbalance between HATs and HDACs dictate disease states and have been implicated in muscular dystrophy, loss of memory, neurodegeneration and autistic ...
Source: Current Neuropharmacology - October 21, 2015 Category: Drugs & Pharmacology Authors: Ganai SA, Ramadoss M, Mahadevan V Tags: Curr Neuropharmacol Source Type: research

LL-00066471, a novel positive allosteric modulator of α7 nicotinic acetylcholine receptor ameliorates cognitive and sensorimotor gating deficits in animal models: Discovery and preclinical characterization.
Abstract α7 nicotinic acetylcholine receptor (α7 nAChR) is an extensively validated target for several neurological and psychiatric conditions namely, dementia and schizophrenia, owing to its vital roles in cognition and sensorimotor gating. Positive allosteric modulation (PAM) of α7 nAChR represents an innovative approach to amplify endogenous cholinergic signaling in a temporally restricted manner in learning and memory centers of brain. α7 nAChR PAMs are anticipated to side-step burgeoning issues observed with several clinical-stage orthosteric α7 nAChR agonists, related to selectivity, tolerance/tachyphyl...
Source: European Journal of Pharmacology - October 27, 2020 Category: Drugs & Pharmacology Authors: Verma MK, Goel RN, Bokare AM, Dandekar MP, Koul S, Desai S, Tota S, Singh N, Nigade PB, Patil VB, Modi D, Mehta M, Gundu J, Walunj SS, Karche NP, Sinha N, Kamboj RK, Palle VP Tags: Eur J Pharmacol Source Type: research