Design of Therapeutic Small-Molecular Blockers Against Channel Proteins

Dear Colleagues,

Transport of ions and molecules across biological membranes is a key step in all life-sustaining processes, and this process is conducted and regulated by a class of biological macromolecules called channel proteins. Starting with earlier theoretical models of membrane potential and culminating in the later elucidation of K⁺ channel structure at the molecular level, membrane channel proteins have been recognized as key determinants of physiological processes, such as neuronal signal transfer, signal transduction, ion homeostasis, establishing resting membrane potential, cardiac pacemaking, epithelial fluid/electrolyte transport, regulation of hormonal secretion, and many others. Consequently, several diseases have also been found linked to the malfunction of these channels, making them excellent targets for treating a range of diseases. Membrane channel proteins exhibit diverse structural features; therefore, strategies to block their activity can be diverse. Some blockers, for example, block channel transport by actively blocking the conduction pathway; others can passively block the channel through allosteric effects. In both cases, the design and optimization of drugs are very important. This Special Issue aims to address key concepts used in the design of channel-blocking drugs with potential therapeutic outcomes. With comprehensive knowledge of the structural, mechanistic, and physiological impacts of channel blockade, future development of blocking agents would be more efficient.

This Special Issue invites original research papers and literature review articles, encompassing the following scopes and aims:

[a] Designing strategies for channel blockers.
[b] Mechanism of channel blocking.
[c] Therapeutic impacts and advantages of small molecular channel blockers.

Dr. Kingshuk Basu
Guest Editor

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