Cell membrane and membrane-associated proteins

The cell membrane is a complex lipid bilayer that serves as the primary interface between a cell and its environment, housing a diverse array of embedded proteins including receptors, ion channels, and transporters [1, 3]. These membrane-associated proteins are fundamental to cellular life, mediating critical processes such as signal transduction, selective permeability, and cell-to-cell recognition [1, 5]. From a pharmacological perspective, this category is of paramount importance, as approximately 50-60% of all FDA-approved drugs target proteins located within or associated with the plasma membrane [2, 4]. Dysregulation of membrane protein function or expression is a hallmark of numerous pathologies, including the uncontrolled signaling in cancer, aberrant electrical activity in cardiac arrhythmias, and impaired neurotransmission in neurological disorders [4, 5]. Because this term encompasses a vast range of distinct molecular entities rather than a single target, therapeutic intervention requires high specificity for individual protein subtypes to avoid broad systemic toxicity [2, 5]. Sources: [1] Alberts B, et al. Molecular Biology of the Cell. 4th ed. 2002; [2] Santos R, et al. Nat Rev Drug Discov. 2017;16(1):19-34; [3] Nature Education. Scitable. 2014; [4] Overington JP, et al. Nat Rev Drug Discov. 2006;5(12):993-6; [5] Yin H, Flynn AD. Annu Rev Biomed Eng. 2016;18:51-76.

Other names

Cell membranes and embedded receptors/ion channelsPlasma membraneCytoplasmic membraneMembrane-bound receptorsTransmembrane proteinsSurface receptors

Drugs targeting these components typically act via agonism or antagonism of receptors, blocking or opening of ion channels, or inhibition of transport proteins to modulate cellular signaling and homeostasis.