Receptors are specialised membrane‐bound proteins that play a fundamental role in translating extracellular signals into precise intracellular responses. Integral to cellular communication, these receptors encompass a diverse family—including G protein‐coupled receptors (GPCRs), ligand‐gated ion channels, enzyme‐linked receptors and nuclear hormone receptors—each characterised by unique architectures and signalling mechanisms. The dynamic conformational changes that occur upon ligand binding allow receptors to bridge the gap between the external environment and the cell’s interior, often through interactions with specific subsets of lipids and other membrane components. These interactions not only facilitate the transmission of signals across the plasma membrane but also help organise receptors into microdomains, thereby influencing signal strength and specificity.
Contributions from recent Nature Portfolio studies have further refined our insight into receptor biology. For example, investigations into the astrocytic α7 nicotinic acetylcholine receptors in Alzheimer’s disease have revealed how altered receptor expression may not only act as a biomarker of early pathology but also contribute actively to disease progression through disrupted synaptic modulation. Alongside this, detailed analyses of allosteric sites in receptors have uncovered new binding pockets that promise to inform the rational design of next‐generation ligands. These studies underscore the importance of integrating structural biology with functional assays to better delineate the nuances of receptor–ligand interactions and their impact on cell function.
Recent advances have been driven by state‐of‐the‐art structural techniques such as cryo‐electron microscopy and X‐ray crystallography, which have revealed high‐resolution details of receptor conformations and their adaptive changes upon ligand binding. Studies have now shown that even minute alterations in receptor structure may bias downstream pathways, leading to a phenomenon known as biased agonism. This has significant implications for drug design, as selective modulation of receptor activity could reduce adverse effects while enhancing therapeutic benefits. Furthermore, research has elucidated the role of receptor oligomerisation and the formation of dynamic clusters within the membrane, processes that modulate both the amplitude and duration of signalling. These findings collectively enhance our understanding of receptor activation dynamics and the interplay between receptor structure, membrane composition and cellular context.
G protein‐coupled receptor (GPCR): A large family of seven‐transmembrane-spanning receptors that activate heterotrimeric G proteins to propagate intracellular signals.
Ligand: Any molecule that binds to a receptor to provoke a biological response.
Agonist: A compound that binds to a receptor and stabilises its active conformation, thereby initiating a response.
Antagonist: A molecule that binds to a receptor without activating it, blocking the action of an agonist.
Allosteric modulation: Regulation of receptor activity via binding at a site distinct from the primary (orthosteric) ligand‐binding domain.
Oligomerisation: The assembly of multiple receptor subunits into a larger complex, which can affect signalling specificity and strength.
The graph below shows the total number of publications each year in Receptors and Membrane Biology.
Ammonium Transport Proteins and Their Mechanisms
Bitter Taste Receptors and Their Physiological Implications
Bombesin Receptor Subtype-3 and Its Biological Implications
Calcium-Activated Chloride Channels in Health and Disease
Cancer Research and Dopamine Receptor Interactions
CD93 and Endothelial Cell Interactions in Inflammation and Disease
Chloride Channels and Antiport Mechanisms in Membrane Proteins
Chloride Channels and Lysosomal Transport Mechanisms
Choline Transport Mechanisms and Their Role in Cancer and Neurodegeneration
Coxsackievirus and Adenovirus Receptor in Health and Disease
Cysteinyl Leukotriene Receptors in Neurological Disorders
Decoy Receptor 3 in Cancer and Inflammatory Diseases
Discoidin Domain Receptors in Cancer and Tissue Regulation
GABA Receptors in Immune Function and Central Nervous System Disorders
GABA Transporters and Their Inhibitors in Central Nervous System Disorders
Gonadotropin Hormone Receptors and Signal Transduction
G-Protein-Coupled Receptor 84 and Medium-Chain Fatty Acids
G Protein-Coupled Receptors in Ovarian Cancer and Inflammation
Guanine Nucleotide Exchange Factors in Membrane Traffic and Cancer
Inhibitory Synaptic Transmission and GABAergic Mechanisms
Insulin Receptor Signaling and Tyrosine Kinase Mechanisms
Large-Conductance Calcium-Activated Potassium Channels in Smooth Muscle Physiology
Mechanosensitive Ion Channels and Sensory Mechanotransduction
Metabotropic Glutamate Receptors in Neuropsychiatric Disorders
Microbial Rhodopsins And Their Functional Mechanisms
Mitochondrial Carrier Proteins and Transport Mechanisms
Na+/Ca2+ Exchanger Proteins and Their Functional Dynamics
Neurotrophin Signaling and Axonal Transport in Sympathetic Neurons
Olfaction and Vibrational Theory in Chemical Sensing
P2Y14 Receptor Signaling and Antagonism in Inflammation and Gout
P2Y Receptors and Their Role in Cellular Signaling
Peptide Transport Mechanisms and Membrane Proteins
Plasma Membrane Calcium Pumps and Their Role in Cellular Function
Pore-Forming Toxins and Cell Membrane Interactions
Prokineticins and Vascular Endothelial Growth Factors in Health and Disease
Protease-Activated Receptors and Platelet Activation
Protease-Activated Receptors In Cardiovascular Disease
