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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...

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Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
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Drug-receptor bonds are formed through various chemical forces when drugs interact with target cells. Covalent bonds, strong and irreversible, are exemplified by DNA-alkylating anticancer agents that inhibit cell division. However, such irreversible drug binding lacks selectivity and can modify the DNA of the surrounding healthy cells. Covalent binding often contributes to tissue toxicity, as seen with chloroform and paracetamol metabolites binding to the liver, causing hepatotoxicity.
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Quantitative Aspects of Drug-Receptor Interaction

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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.
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Pharmacogenomics: Identification of New Drug Targets

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Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...

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

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Published on: December 11, 2016

DREADDs: novel tools for drug discovery and development.

Hyeong-Min Lee¹, Patrick M Giguere¹, Bryan L Roth¹

¹Department of Pharmacology, Program in Neuroscience, Division of Chemical Biology and Medicinal Chemistry, and NIMH Psychoactive Drug Screening Program, University of North Carolina, Chapel Hill Medical School, 4072 Genetic Medicine Building, Chapel Hill, NC 27514, USA.

Drug Discovery Today

|November 5, 2013

Summary

Designer receptors exclusively activated by designer drugs (DREADDs) are powerful tools for studying biological processes and behaviors. This technology offers significant potential for identifying drug targets and advancing drug discovery and development.

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Area of Science:

Pharmacology
Neuroscience
Molecular Biology

Background:

Engineered G protein-coupled receptors (GPCRs), known as DREADDs, are widely used in biological research.
DREADD technology provides a method to selectively activate or inhibit specific cellular pathways.

Purpose of the Study:

To discuss the application of DREADDs in drug discovery and development.
To highlight the potential of DREADDs for identifying novel therapeutic targets.

Main Methods:

Utilizing DREADDs to modulate GPCR activity in biological systems.
Investigating the effects of designer drugs on cellular functions and behaviors.

Main Results:

DREADDs enable precise control over GPCR signaling pathways.
The technology facilitates the exploration of drug effects on known and orphan GPCRs.

Conclusions:

DREADD technology is a valuable tool for advancing drug discovery and development.
DREADDs can accelerate the identification of druggable targets for therapeutic interventions.