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Related Concept Videos

Drug Discovery: Overview01:26

Drug Discovery: Overview

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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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Targets for Drug Action: Overview01:26

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

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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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Targeted Cancer Therapies02:57

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Principles of Drug Action01:24

Principles of Drug Action

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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.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
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Transducer Mechanism: Enzyme-Linked Receptors01:27

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Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
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Related Experiment Video

Updated: Jun 26, 2025

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
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Bridging the gap between target-based and phenotypic-based drug discovery.

Cecília R C Calado1,2

  • 1ISEL-Instituto Superior de Engenharia de Lisboa, Instituto Politécnico de Lisboa, Lisboa, Portugal.

Expert Opinion on Drug Discovery
|May 15, 2024
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Summary

Drug discovery faces challenges despite molecular understanding. Bridging target-based and phenotypic approaches enhances efficiency and reduces adverse effects for novel therapeutics.

Keywords:
Drug discoverycellular-based assayphenotypic assaysystems biologytarget-based

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Area of Science:

  • Biomedical Sciences
  • Pharmacology
  • Drug Discovery

Background:

  • Recent scientific progress has improved understanding of molecular disease mechanisms, driving target-based drug discovery.
  • Despite advancements, there's a concerning decline in the development of first-in-class drugs.

Approach:

  • This review examines challenges, advances, and opportunities in rational target-based and empirical phenotypic drug discovery strategies.
  • It evaluates methods to integrate these approaches for a more efficient drug discovery process.

Key Points:

  • Lack of knowledge in complex biological networks leads to irrelevant targets and adverse drug effects.
  • Phenotypic systems, informed by molecular mechanisms, can address these knowledge gaps.
  • Integrating expanded chemical space and advanced technologies with early target and mechanism identification streamlines drug discovery.

Conclusions:

  • A combined approach, leveraging both molecular and phenotypic insights, is crucial for efficient drug discovery.
  • Technological and scientific advancements are key to identifying drug targets and mechanisms of action earlier in the pipeline.
  • Addressing knowledge gaps in biological networks will improve drug relevance and safety profiles.