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Targets for Drug Action: Overview

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...

Transducer Mechanism: Enzyme-Linked Receptors

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:

G Protein-coupled Receptors

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...

G Protein-coupled Receptors

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...

Drug-Receptor Interactions

Drug-Receptor Interactions

Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.

Principles of Drug Action

Principles of Drug Action

Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...

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Related Experiment Video

Updated: May 25, 2026

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

Published on: December 11, 2016

Receptors as drug targets.

Michael Williams¹, Rita Raddatz

¹Worldwide Discovery Research Cephalon, Inc., West Chester, Pennsylvania, USA.

Current Protocols in Pharmacology

|February 2, 2012

Summary

Drug targets called receptors, crucial for treating diseases, have evolved from simple concepts to complex molecular interactions. Understanding these receptor dynamics is key to developing effective therapies.

Area of Science:

Pharmacology
Molecular Biology
Biochemistry

Background:

Receptors are key molecular targets for drug action, located on cell surfaces or internally.
Early receptor concepts by Ehrlich and Langley laid the foundation for modern pharmacology.
Receptor theory has evolved significantly since its inception.

Purpose of the Study:

To review the historical development and current understanding of receptor concepts.
To highlight the molecular characterization and functional complexity of receptors.
To discuss the evolving understanding of ligand-receptor interactions.

Main Methods:

Literature review of historical and contemporary research on receptors.
Analysis of the molecular structure and function of various receptor types.

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A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction

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Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

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Examination of refined concepts in ligand-receptor interactions.

Main Results:

Receptor concepts have advanced from basic models to include complex molecular interactions.
Ancillary proteins (G proteins, arrestins, RAMPs) and functional states (constitutive activity, internalization, dimerization) add complexity.
Ligand interactions are now understood beyond simple agonism/antagonism, including partial agonism, allosteric modulation, and inverse agonism.

Conclusions:

Receptors are dynamic molecular entities whose complex interactions are central to drug efficacy.
A deeper understanding of receptor behavior is essential for precise characterization in disease and homeostasis.
Continued research into receptor mechanisms will drive the development of novel therapeutics.