In silico docking and electrophysiological characterization of lacosamide binding sites on collapsin response mediator protein-2 identifies a pocket important in modulating sodium channel slow inactivation
about
Development of lacosamide for the treatment of partial-onset seizuresSpecific binding of lacosamide to collapsin response mediator protein 2 (CRMP2) and direct impairment of its canonical function: implications for the therapeutic potential of lacosamideCollapsin response mediator protein 2: high-resolution crystal structure sheds light on small-molecule binding, post-translational modifications, and conformational flexibility.Differential regulation of collapsin response mediator protein 2 (CRMP2) phosphorylation by GSK3ß and CDK5 following traumatic brain injury.The functionalized amino acid (S)-Lacosamide subverts CRMP2-mediated tubulin polymerization to prevent constitutive and activity-dependent increase in neurite outgrowthSubstituted N-(biphenyl-4'-yl)methyl (R)-2-acetamido-3-methoxypropionamides: potent anticonvulsants that affect frequency (use) dependence and slow inactivation of sodium channels.Prevention of posttraumatic axon sprouting by blocking collapsin response mediator protein 2-mediated neurite outgrowth and tubulin polymerization.Development and characterization of novel derivatives of the antiepileptic drug lacosamide that exhibit far greater enhancement in slow inactivation of voltage-gated sodium channels.Merging Structural Motifs of Functionalized Amino Acids and α-Aminoamides Results in Novel Anticonvulsant Compounds with Significant Effects on Slow and Fast Inactivation of Voltage-gated Sodium Channels and in the Treatment of Neuropathic Pain.Chimeric agents derived from the functionalized amino acid, lacosamide, and the α-aminoamide, safinamide: evaluation of their inhibitory actions on voltage-gated sodium channels, and antiseizure and antinociception activities and comparison with lacVOLTAGE-GATED CALCIUM CHANNELS ARE NOT AFFECTED BY THE NOVEL ANTI-EPILEPTIC DRUG LACOSAMIDE.Suppression of inflammatory and neuropathic pain by uncoupling CRMP-2 from the presynaptic Ca²⁺ channel complexChimeric derivatives of functionalized amino acids and α-aminoamides: compounds with anticonvulsant activity in seizure models and inhibitory actions on central, peripheral, and cardiac isoforms of voltage-gated sodium channels.Safety of lacosamide in children with refractory partial epilepsy.Post-translational modifications of voltage-gated sodium channels in chronic pain syndromesInhibition of transmitter release and attenuation of anti-retroviral-associated and tibial nerve injury-related painful peripheral neuropathy by novel synthetic Ca2+ channel peptides.Identification of the benzyloxyphenyl pharmacophore: a structural unit that promotes sodium channel slow inactivationOpening Pandora's jar: a primer on the putative roles of CRMP2 in a panoply of neurodegenerative, sensory and motor neuron, and central disorders.Discovery of lacosamide affinity bait agents that exhibit potent voltage-gated sodium channel blocking properties.SUMOylation alters CRMP2 regulation of calcium influx in sensory neurons.CRMP2 protein SUMOylation modulates NaV1.7 channel trafficking.mTORC1-dependent translation of collapsin response mediator protein-2 drives neuroadaptations underlying excessive alcohol-drinking behaviors.Novel medications for epilepsy.Ion channel drug discovery: challenges and future directions.Lacosamide for the treatment of partial-onset seizures.Neurological perspectives on voltage-gated sodium channels.Advances in epilepsy treatment: lacosamide pharmacokinetic profile.CRMPs: critical molecules for neurite morphogenesis and neuropsychiatric diseases.Role of Sodium Channels in Epilepsy.Sustained relief of ongoing experimental neuropathic pain by a CRMP2 peptide aptamer with low abuse potential.Drug binding assays do not reveal specific binding of lacosamide to collapsin response mediator protein 2 (CRMP-2).Analgesic ineffectiveness of lacosamide after spinal nerve ligation and its sodium channel activity in injured neurons.Distribution of lacosamide in the rat brain assessed by in vitro slice technique.(S)-Lacosamide Binding to Collapsin Response Mediator Protein 2 (CRMP2) Regulates CaV2.2 Activity by Subverting Its Phosphorylation by Cdk5.Mapping protein interactions of sodium channel NaV1.7 using epitope-tagged gene-targeted mice.Cdk5-mediated phosphorylation of CRMP-2 enhances its interaction with CaV2.2.Lanthionine ketimine ethyl ester partially rescues neurodevelopmental defects in unc-33 (DPYSL2/CRMP2) mutants.
P2860
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P2860
In silico docking and electrophysiological characterization of lacosamide binding sites on collapsin response mediator protein-2 identifies a pocket important in modulating sodium channel slow inactivation
description
2010 nî lūn-bûn
@nan
2010 թուականի Յունիսին հրատարակուած գիտական յօդուած
@hyw
2010 թվականի հունիսին հրատարակված գիտական հոդված
@hy
2010年の論文
@ja
2010年論文
@yue
2010年論文
@zh-hant
2010年論文
@zh-hk
2010年論文
@zh-mo
2010年論文
@zh-tw
2010年论文
@wuu
name
In silico docking and electrop ...... dium channel slow inactivation
@ast
In silico docking and electrop ...... dium channel slow inactivation
@en
In silico docking and electrop ...... dium channel slow inactivation
@nl
type
label
In silico docking and electrop ...... dium channel slow inactivation
@ast
In silico docking and electrop ...... dium channel slow inactivation
@en
In silico docking and electrop ...... dium channel slow inactivation
@nl
prefLabel
In silico docking and electrop ...... dium channel slow inactivation
@ast
In silico docking and electrop ...... dium channel slow inactivation
@en
In silico docking and electrop ...... dium channel slow inactivation
@nl
P2093
P2860
P356
P1476
In silico docking and electrop ...... dium channel slow inactivation
@en
P2093
Brian W Jarecki
Joel M Brittain
Ki Duk Park
Rachel Hale
Samy O Meroueh
Sarah M Wilson
Theodore R Cummins
Yuying Wang
P2860
P304
25296-25307
P356
10.1074/JBC.M110.128801
P407
P577
2010-06-09T00:00:00Z