Drug Targets & Biological Macromolecules

receptor

A receptor is a protein that acts like a lock waiting for a specific key. When the right signaling molecule, such as a hormone or neurotransmitter, slots into it, the receptor changes shape and passes a message into or across the cell. The cell does not respond to the molecule floating around outside; it responds because the receptor was triggered.

Receptors recognize their natural messengers with great precision through a binding pocket whose shape and chemistry match the messenger. Activation typically alters the receptor's three-dimensional conformation, which then turns on a downstream chain of events: opening an ion channel, switching on an internal protein, or changing which genes a cell reads. Because so many physiological signals run through receptors, they are among the most important targets in drug discovery.

Drugs that bind receptors fall into broad behavioral classes. An agonist mimics the natural messenger and switches the receptor on, while an antagonist blocks the pocket and prevents activation without triggering it itself. It is worth remembering that a single protein labeled a receptor may have several subtypes spread across different tissues, so a drug's effect depends on which subtype it engages and where.

Beta-blockers such as propranolol bind to beta-adrenergic receptors in the heart and block adrenaline from activating them, slowing heart rate and lowering blood pressure.

A receptor as a drug target: the antagonist occupies the pocket meant for the natural messenger.

Not every drug target is a receptor, and not every protein that binds a small molecule is one. The term is usually reserved for proteins whose physiological job is to detect a signal and relay it onward.

Also called
receptor protein受体蛋白受體蛋白