Novel Drug Design and Activity Targeting Ion Channels
A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: closed (31 August 2023) | Viewed by 2021
Special Issue Editors
2. Barrow Neurological Institute, Phoenix, AZ, USA
Interests: nicotinic acetylcholine receptor; drug discovery; epilepsy; chaperone proteins
Special Issue Information
Dear Colleagues,
Ion channels (ICs) are transmembrane ionotropic receptors that pass mono- and/or divalant ions when a chemical messenger, such as a neurotransmitter, activates the receptor. This family of channels is involved in neuronal excitation and/or inhibition, the mediation of neurotransmitter release, and the initiation of secondary signalling. ICs are involved in a wide range of neurological disorders of high clinical significance, including nicotine addiction, depression and Alzimer’s disease. An endogenous agonist (ligand) binds at the conserved ‘orthosteric’ binding pocket located in the extracellular domain (ECD) to activate the receptor, which opens the channel pore that is distinctly located in the transmembrane domain (TMD). Drugs targeting ICs can bind competitively or noncompetitively to activate or inhibit an agonist response. Ligands that bind at a distinct (allosteric) binding site modulate the response of an agonist. Molecules binding in distinct modalities can reveal how a specific IC functions, which can facilitate the development of novel therapies.
In recent decades, ICs have been prime targets for drug discovery efforts, resulting in some clinical translation success, including anaesthetics, analgesics, antidepressants and addiction thearapies. ICs remain one of the most important proteins used to study structure–activity relationships (SARs) and targets for novel drug design efforts. This Special Issue invites papers on drug action and/or drug design for drugs targeting ICs.
Topics of particular interest include, but are not limited to the following:
- Structural analysis of ligand-bound ion channels.
- Novel approaches for drug design targeting ion channel receptors.
- Design and action of small peptides on ICs.
- Understanding drug action on ICs.
- Drug action on disease-causing mutant receptors.
Dr. Maegan Weltzin
Dr. Dinesh Indurthi
Guest Editors
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Keywords
- ion channel
- structure–activity relationship (SAR)
- neuropharmacology
- orthosteric binding site
- allosteric binding site
- allosteric receptor function
- drug design
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