An Intracellular Allosteric Modulator Binding Pocket in SK2 Ion Channels Is Shared by Multiple Chemotypes.

No abstract is available for this paper.

• Publication year

  2018

• Venue

  Structure

• Publication date

  2018-04-03

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/j.str.2018.02.017PMID 29576321
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Structural Determinants for the Selectivity of the Positive KCa3.1 Gating Modulator 5-Methylnaphtho[2,1-d]oxazol-2-amine (SKA-121)

  2017cited by this paper
• Riluzole in patients with hereditary cerebellar ataxia: a randomised, double-blind, placebo-controlled trial.

  2015cited by this paper
• Using chemical shift perturbation to characterise ligand binding.

  2013cited by this paper
• The therapeutic potential of small-conductance KCa2 channels in neurodegenerative and psychiatric diseases

  2013cited by this paper
• Unstructured to structured transition of an intrinsically disordered protein peptide in coupling Ca2+-sensing and SK channel activation

  2013cited by this paper
• Selective positive modulator of calcium-activated potassium channels exerts beneficial effects in a mouse model of spinocerebellar ataxia type 2.

  2012cited by this paper
• Identification of the functional binding pocket for compounds targeting small-conductance Ca2+-activated potassium channels

  2012cited by this paper
• Development of a Rule-Based Method for the Assessment of Protein Druggability

  2012cited by this paper
• Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes

  2011cited by this paper
• Negative Gating Modulation by (R)-N-(Benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphthylamine (NS8593) Depends on Residues in the Inner Pore Vestibule: Pharmacological Evidence of Deep-Pore Gating of KCa2 Channels

  2011cited by this paper
• KCa Channels as Therapeutic Targets in Episodic Ataxia Type-2

  2010cited by this paper
• Viral calciomics: Interplays between Ca2+ and virus

  2009cited by this paper
• Naphtho[1,2-d]thiazol-2-ylamine (SKA-31), a New Activator of KCa2 and KCa3.1 Potassium Channels, Potentiates the Endothelium-Derived Hyperpolarizing Factor Response and Lowers Blood Pressure

  2009cited by this paper
• Identifying and Characterizing Binding Sites and Assessing Druggability

  2009cited by this paper
• Synthesis and Structure−Activity Relationship Studies of 2-(N-Substituted)-aminobenzimidazoles as Potent Negative Gating Modulators of Small Conductance Ca2+-Activated K+ Channels

  2008cited by this paper
• Structure-based maximal affinity model predicts small-molecule druggability

  2007cited by this paper
• In vivo characterisation of the small-conductance KCa (SK) channel activator 1-ethyl-2-benzimidazolinone (1-EBIO) as a potential anticonvulsant.

  2006cited by this paper
• Small-conductance, Ca2+-activated K+ channel SK3 generates age-related memory and LTP deficits

  2003cited by this paper
• Modulation of recombinant and native neuronal SK channels by the neuroprotective drug riluzole.

  2002cited by this paper
• Small Conductance Ca2+-Activated K+Channels Modulate Synaptic Plasticity and Memory Encoding

  2002cited by this paper
• Calmodulin in action: diversity in target recognition and activation mechanisms.

  2002cited by this paper
• Structure of the gating domain of a Ca2+-activated K+ channel complexed with Ca2+/calmodulin

  2001cited by this paper
• Small conductance potassium channels cause an activity-dependent spike frequency adaptation and make the transfer function of neurons logarithmic.

  1999cited by this paper
• Involvement of apamin-sensitive SK channels in spike frequency adaptation of neurons in nucleus tractus solitarii of the rat.

  1999cited by this paper
• Mechanism of calcium gating in small-conductance calcium-activated potassium channels

  1998cited by this paper
• Sequence motifs for calmodulin recognition

  1997cited by this paper
• Secondary structure and side-chain 1H and 13C resonance assignments of calmodulin in solution by heteronuclear multidimensional NMR spectroscopy.

  1991cited by this paper

• Structural basis for the subtype-selectivity of KCa2.2 channel activators

  2026cites this paper
• Structural mechanisms for inhibition and activation of human small-conductance Ca2+-activated potassium channel SK2

  2026cites this paper
• Small-conductance Ca2⁺-activated K⁺ channels in cardiac excitation-contraction coupling: Bridging mitochondria, sarcolemma and antiarrhythmic therapy.

  2025cites this paper
• The structure, function, and pharmacology of SK channel family.

  2025cites this paper
• Machine Learning Approach for Predicting Drug-Like Molecules Targeting Calmodulin Pathway Proteins

  2025cites this paper
• Fragment-Based Screening Identifies Novel Non-Amino Acid Inhibitors of the Sodium-Coupled Neutral Amino Acid Transporter SNAT2

  2025cites this paper
• 6,7-Dichloro-1H-indole-2,3-dione-3-oxime functions as a superagonist for the intermediate-conductance Ca2+-activated K+ channel KCa3.1.

  2025cites this paper
• Structural basis for the subtype-selectivity of KCa2.2 channel activators

  2025cites this paper
• Transcriptomic decoding of regional cortical vulnerability to drug-resistant epilepsy using 7T MRI

  2025cites this paper
• Know your molecule: pharmacological characterization of drug candidates to enhance efficacy and reduce late-stage attrition

  2024cites this paper
• Identification of Riluzole derivatives as novel calmodulin inhibitors with neuroprotective activity by a joint synthesis, biosensor, and computational guided strategy.

  2024cites this paper
• Novel SK channel positive modulators prevent ferroptosis and excitotoxicity in neuronal cells.

  2024cites this paper
• Effects of the novel acaricide acynonapyr on the calcium-activated potassium channel.

  2024cites this paper
• TRPC1: The housekeeper of the hippocampus.

  2024cites this paper
• Unsupervised evolution of protein and antibody complexes with a structure-informed language model

  2024cites this paper
• Inverse folding of protein complexes with a structure-informed language model enables unsupervised antibody evolution

  2023cites this paper
• Design, synthesis and biological evaluation of pyrrolopyrimidine derivatives as novel and selective positive modulator of the small conductance Ca2+-activated K+ channels.

  2023cites this paper
• Current and emerging treatment modalities for spinocerebellar ataxias

  2022cites this paper
• Structural identification of riluzole-binding site on human TRPC5

  2022cites this paper
• Halogen Bonding: Types and Role in Biological Activities of Halogenated Molecules

  2021cites this paper
• Effects of calcium-activated potassium channel modulators on afterhyperpolarizing potentials in identified motor and mechanosensory neurons of the medicinal leech

  2021cites this paper
• Physiology and Therapeutic Potential of SK, H, and M Medium AfterHyperPolarization Ion Channels

  2021cites this paper
• Subtype‐selective positive modulation of KCa2 channels depends on the HA/HB helices

  2021cites this paper
• Structure-Activity Relationship Study of Subtype-Selective Positive Modulators of KCa2 Channels.

  2021cites this paper
• Pharmacology of Small- and Intermediate-Conductance Calcium-Activated Potassium Channels.

  2020cites this paper
• Ataxic Symptoms in Huntington’s Disease Transgenic Mouse Model Are Alleviated by Chlorzoxazone

  2020cites this paper
• Atomistic Insights of Calmodulin Gating of Complete Ion Channels

  2020cites this paper
• A Pilot Study of All-Computational Drug Design Protocol–From Structure Prediction to Interaction Analysis

  2020influential citation
• New Approaches in Studies of the Molecular Pathogenesis of Type 2 Spinocerebellar Ataxia

  2020cites this paper
• In vivo analysis of the spontaneous firing of cerebellar Purkinje cells in awake transgenic mice that model spinocerebellar ataxia type 2.

  2020cites this paper
• Ion channel discovery – partnering to access specialized expertise

  2020cites this paper
• New Approaches in Studies of the Molecular Pathogenesis of Type 2 Spinocerebellar Ataxia

  2020cites this paper
• Polyglutamine spinocerebellar ataxias: emerging therapeutic targets

  2020cites this paper
• NMR spectroscopy: the swiss army knife of drug discovery

  2020cites this paper
• The Trials and Tribulations of Structure Assisted Design of KCa Channel Activators

  2019cites this paper
• Molecular Mechanisms and Therapeutics for Spinocerebellar Ataxia Type 2

  2019cites this paper
• Lipidic synthetic alkaloids as SK3 channel modulators. Synthesis and biological evaluation of 2-substituted tetrahydropyridine derivatives with potential anti-metastatic activity.

  2019cites this paper
• Concomitant SK current activation and sodium current inhibition cause J wave syndrome.

  2018cites this paper