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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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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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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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Drug-Receptor Interaction: Agonist01:25

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Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
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Drug-Receptor Interactions01:29

Drug-Receptor Interactions

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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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Agonism and Antagonism: Quantification01:14

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When drugs are administered, they can elicit either an agonist or antagonist effect on the body. Agonism occurs when a drug activates a specific receptor, triggering a biological response. On the other hand, antagonism happens when a drug binds to the same receptors but blocks their activation, thereby preventing a biological response.
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Utilizing an Orally Dissolving Strip for Pharmacological and Toxicological Studies: A Simple and Humane Alternative to Oral Gavage for Animals
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Allostery in Drug Development.

Xi Cheng1, Hualiang Jiang2

  • 1State Key Laboratory of Drug Research, Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.

Advances in Experimental Medicine and Biology
|November 11, 2019
PubMed
Summary
This summary is machine-generated.

Allosteric modulators offer a promising avenue for drug development by precisely controlling protein-substrate interactions. Advances in understanding allosteric regulation and drug development techniques signal a future with numerous novel allosteric drugs.

Keywords:
Allosteric perturbationBiased agonistsConformational changesProtein dynamicsRational drug design

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Allosteric regulation is a fundamental biological mechanism controlling cellular processes by modulating biomolecule affinities.
  • Allosteric modulators offer predictable tuning of protein/substrate affinity, indicating potential as safe therapeutic agents.

Purpose of the Study:

  • To introduce representative allosteric modulators targeting key drug targets, including G protein-coupled receptors.
  • To review current experimental and computational methodologies in allosteric drug discovery.

Main Methods:

  • Review of existing literature on allosteric modulators and their targets.
  • Discussion of experimental techniques for characterizing allosteric interactions.
  • Overview of computational approaches applied in allosteric drug development.

Main Results:

  • Identification of G protein-coupled receptors as significant therapeutic targets for allosteric modulators.
  • Highlighting the progress in both experimental and computational strategies for allosteric drug development.

Conclusions:

  • The growing knowledge of allosteric regulation and advancements in drug development are poised to yield a significant number of new allosteric drugs.
  • Allosteric modulators represent a promising class of therapeutics with potential for enhanced safety and efficacy.