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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...
Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

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...
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.
Principles of Drug Action01:24

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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.
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Related Experiment Video

Updated: May 31, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
08:31

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Published on: December 1, 2020

Structure-based druggability assessment--identifying suitable targets for small molecule therapeutics.

Eric B Fauman1, Brajesh K Rai, Enoch S Huang

  • 1Computational Sciences Center of Emphasis, Pfizer Worldwide Research and Development, Cambridge, MA, United States.

Current Opinion in Chemical Biology
|June 28, 2011
PubMed
Summary
This summary is machine-generated.

Identifying druggable protein targets involves assessing their potential to bind drug-like molecules. Structure-based methods analyze protein pockets for complementary size, shape, and hydrophobicity, crucial for drug discovery.

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A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
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Published on: August 27, 2019

Related Experiment Videos

Last Updated: May 31, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
08:31

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Published on: December 1, 2020

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

Area of Science:

  • Biochemistry
  • Pharmacology
  • Computational Biology

Background:

  • Drug discovery requires identifying targets that can be modulated by small molecules.
  • The 'rule of 5' provides general guidelines for oral drug properties like size and lipophilicity.
  • Structure-based drug design necessitates predicting ligand-binding sites on protein targets.

Purpose of the Study:

  • To outline methods for assessing target druggability using structure-based approaches.
  • To highlight key features of protein pockets that indicate druggability.
  • To discuss the role of validation sets in advancing druggability prediction methods.

Main Methods:

  • Structure-based analysis of protein targets to identify potential ligand-binding sites.
  • Utilizing geometrical and physicochemical properties of protein surfaces for pocket identification.
  • Employing features such as pocket size, shape, and hydrophobicity for assessment.

Main Results:

  • Automated methods can identify suitable drug-binding pockets based on specific criteria.
  • Pocket size, shape, and hydrophobicity are critical indicators of druggability.
  • The development of more sophisticated druggability assessment methods is ongoing.

Conclusions:

  • Structure-based druggability assessment is a key step in the drug discovery pipeline.
  • Computational methods analyzing protein pocket characteristics aid in identifying viable drug targets.
  • Advancements in validation datasets are crucial for refining and improving druggability prediction models.