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Drug Discovery: Overview

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...

GPCRs Regulate Adenylyl Cylase Activity

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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
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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.
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G Protein-coupled Receptors

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Preclinical Development: Overview

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Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...

Transducer Mechanism: G Protein–Coupled Receptors

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
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Related Experiment Video

Updated: Jul 2, 2026

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

An online GPCR drug discovery resource.

Jimmy Caroli¹, Søren N Andreassen¹, Javier Sánchez Lorente¹

¹Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen, Denmark.

Npj Drug Discovery

|July 1, 2026

Summary

This study introduces GPCRdb, an online resource detailing G protein-coupled receptor (GPCR) drugs and clinical trial agents. It aids in identifying trends and prioritizing GPCR targets for future drug discovery efforts.

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A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors

A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors

Published on: December 2, 2022

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Last Updated: Jul 2, 2026

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors

A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors

Published on: December 2, 2022

Area of Science:

Pharmacology
Biotechnology
Drug Discovery

Background:

G protein-coupled receptors (GPCRs) are crucial drug targets, involved in 516 approved drugs and 337 agents in clinical trials.
Currently, 121 GPCRs are targeted by approved drugs, with 30 more in clinical trials, indicating a growing 'drugged GPCRome'.

Purpose of the Study:

To present a comprehensive online resource for GPCR drugs, clinical trial agents, targets, and associated disease indications.
To provide tools for analyzing GPCR drug discovery trends and prioritizing potential therapeutic targets.

Main Methods:

Integration of a new 'Drugs and Agents in trial' section into the existing GPCR database, GPCRdb.
Development of a target selection tool for prioritizing GPCRs in drug discovery.

Main Results:

GPCRdb now offers curated data on GPCR-targeted drugs and clinical trial agents.
The resource includes analysis, visualization, and a tool for receptor prioritization.

Conclusions:

The updated GPCRdb serves as a valuable knowledge base for understanding GPCR drug discovery.
It offers insights into current strategies, trends, and the therapeutic potential of both drugged and untapped GPCR targets for specific diseases.