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Related Concept Videos

Drug Discovery: Overview01:26

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...
Targets for Drug Action: Overview01:26

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...
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

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.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Therapeutic Drug Monitoring: Drug Analysis Methods01:26

Therapeutic Drug Monitoring: Drug Analysis Methods

Therapeutic Drug Monitoring (TDM) is a clinical practice that measures specific drug levels in a patient's blood or body tissues to tailor drug therapy effectively. This monitoring is critical for managing drugs with narrow therapeutic indices like digoxin and phenytoin, ensuring they are both safe and effective. For instance, monitoring theophylline levels in asthma patients involves precision and sensitivity to adjust doses according to individual responses to therapy, ensuring efficacy and...
Modified-Release Drug Delivery Systems: Site-Targeted01:24

Modified-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.
Dose-Response Relationship: Selectivity and Specificity01:25

Dose-Response Relationship: Selectivity and Specificity

Drugs exert their therapeutic effects by interacting with receptors, enzymes, or ion channels that are present throughout the human body. The strength and duration of the interaction between a drug and its target receptor are characterized by the selectivity and specificity of the drug. Selectivity refers to a drug's strong preference for its intended target over other targets. For instance, isoprenaline, a non-selective β-adrenergic agonist, interacts with both β1- and β2-adrenergic receptors...

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Related Experiment Video

Updated: Jun 17, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
05:28

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

Published on: August 27, 2019

Target identification using drug affinity responsive target stability (DARTS).

Brett Lomenick1, Rui Hao, Nao Jonai

  • 1Department of Molecular and Medical Pharmacology and the Molecular Biology Institute, David Geffen School of Medicine, University of California, Los Angeles, CA 90095, USA.

Proceedings of the National Academy of Sciences of the United States of America
|December 10, 2009
PubMed
Summary
This summary is machine-generated.

We developed drug affinity responsive target stability (DARTS) to identify drug targets. This method revealed resveratrol

More Related Videos

Protein Target Prediction and Validation of Small Molecule Compound
10:21

Protein Target Prediction and Validation of Small Molecule Compound

Published on: February 23, 2024

Related Experiment Videos

Last Updated: Jun 17, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
05:28

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

Published on: August 27, 2019

Protein Target Prediction and Validation of Small Molecule Compound
10:21

Protein Target Prediction and Validation of Small Molecule Compound

Published on: February 23, 2024

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Drug Discovery

Background:

  • Identifying molecular targets of small-molecule drugs is a significant challenge in pharmacology.
  • Existing methods may require drug modification or are mechanism-dependent.

Purpose of the Study:

  • To present a novel, universally applicable method for identifying drug targets.
  • To demonstrate the utility of this method in identifying known interactions and novel targets.

Main Methods:

  • Drug Affinity Responsive Target Stability (DARTS) assay.
  • Utilizes reduced protease susceptibility of target proteins upon drug binding.
  • Requires no drug modification and is independent of drug action mechanism.

Main Results:

  • Successfully identified known small-molecule-protein interactions.
  • Revealed the eukaryotic translation initiation machinery as a molecular target of resveratrol.
  • Demonstrated the potential for label-free screening and mapping of protein-metabolite interactions.

Conclusions:

  • DARTS is a versatile and broadly applicable method for drug target identification.
  • This technique facilitates the discovery of molecular targets for natural products like resveratrol.
  • DARTS holds promise for advancing chemical biology and drug development.