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Cell surface components refer to the diverse set of molecules—including proteins, lipids, and carbohydrates—that reside on or are embedded within the plasma membrane of a cell [Alberts et al., 2002]. These components are vital for maintaining cellular integrity and facilitating communication between the cell and its external environment through processes like signal transduction, cell adhesion, and molecular transport [Lodish et al., 2000]. In pharmacology, cell surface proteins represent the most significant class of therapeutic targets, accounting for more than half of all FDA-approved drug targets, including G protein-coupled receptors (GPCRs), ion channels, and transporters [Santos et al., 2017]. While specific components like HER2 or the LDL receptor are discrete targets, the term "Cell surface components" is a broad descriptive category rather than a single target [NCBI MeSH]. Dysregulation of these surface molecules is a hallmark of various pathologies, particularly in oncology where they serve as antigens for monoclonal antibodies and CAR-T cell therapies [Scott et al., 2012]. Consequently, while the category is essential to drug discovery, therapeutic intervention requires the identification of specific molecular entities within this group to ensure efficacy and minimize off-target effects.
Drugs targeting cell surface components act through diverse mechanisms including competitive inhibition of receptors, modulation of ion channel conductance, stabilization of transporters, or induction of antibody-dependent cellular cytotoxicity (ADCC) [Santos et al., 2017; Scott et al., 2012].
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