Related Experiment Video
Updated: Jul 4, 2026
10:08
Microtransplantation of Synaptic Membranes to Reactivate Human Synaptic Receptors for Functional Studies
Published on: July 20, 2022
New ways to target old receptors.
Adrian Whitty1, Thomas V Riera
1Department of Chemistry, Boston University, Metcalf Center for Science and Engineering, 590 Commonwealth Avenue, Boston, MA 02215-2521, USA. whitty@bu.edu
Current Opinion in Chemical Biology
|June 24, 2008
Summary
Advances in understanding receptor activation and signaling mechanisms are crucial for developing targeted therapies. New methods offer insights into drug discovery for cytokines and growth factors.
Area of Science:
- Molecular biology
- Pharmacology
- Cell signaling
Background:
- Many drugs target cytokines, growth factors, and their receptors.
- Understanding receptor activation and signaling mechanisms is vital for drug discovery.
- Current drug discovery strategies are limited by incomplete knowledge of these pathways.
Purpose of the Study:
- To highlight recent progress in understanding receptor activation and signaling.
- To identify new opportunities for developing improved drugs targeting these pathways.
Main Methods:
- Development of improved methods to determine receptor activation mechanisms.
- Biochemical analysis of differential signaling by common receptor ligands.
- In vivo measurement of receptor activation step affinities.
- Advancement towards systems-level understanding of receptor signaling.
Main Results:
- Substantial progress has been made in key areas of receptor signaling research.
- New methods provide deeper insights into receptor activation and ligand-specific signaling.
- Systems-level approaches are enhancing our comprehension of receptor function.
Conclusions:
- Recent advances offer a new understanding of receptor function.
- These insights create opportunities for developing more effective drugs.
- Improved drug discovery strategies can be developed based on this enhanced knowledge.
Related Concept Videos
01:30Spare Receptors
Some receptors remain unoccupied even when an agonist produces a maximal response. Such empty ones are called spare receptors. In presence of spare receptors the maximum effect of an agonist drug is achieved with fewer than 100% of the receptors being occupied. To determine the presence of spare receptors, scientists often compare the concentration of the drug needed to produce 50% of the maximum effect (EC50) with the concentration of the drug needed to occupy 50% of the receptors (Kd). If the...
01:15G 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...
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...
01:25Drug-Receptor Interaction: Agonist
Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
01:26Targets 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...
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...
01:30Ligand-Gated Ion Channel Receptor: Gating Mechanism
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
01:24Modified-Release Drug Delivery Systems: Site-Targeted
Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.