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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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Preclinical Development: Overview01:28

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Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...
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Prodrugs01:30

Prodrugs

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Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
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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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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.
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Related Experiment Video

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Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
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Lead/Drug Discovery from Natural Resources.

Zhihong Xu1,2,3, Barrett Eichler1, Eytan A Klausner3

  • 1Department of Chemistry and Biochemistry, Augustana University, 2001 S Summit Ave., Sioux Falls, SD 57197, USA.

Molecules (Basel, Switzerland)
|December 11, 2022
PubMed
Summary

Nature provides a rich source of therapeutic agents. This review highlights potent natural products discovered between 2016-2022 for anticancer, anti-HIV, antibacterial, and antimalarial applications, including marine compounds and computational drug design strategies.

Keywords:
antibacterialanticancerantimalarialantiviralcomputer-assisteddrug discoverylead discoverynatural product

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Area of Science:

  • Natural Product Chemistry
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Natural products have historically served as a vital source for drug discovery, yielding significant anti-infective and anticancer agents.
  • Nature's vast biodiversity offers a continuous supply of novel therapeutic compounds with unique chemical structures.

Purpose of the Study:

  • To review potent natural product-derived drugs and lead compounds discovered from 2016 to 2022.
  • To cover anticancer, anti-HIV, antibacterial, and antimalarial agents, including marine bioactive products.
  • To briefly review the role of computational techniques in natural product drug discovery.

Main Methods:

  • Literature review of natural product-derived therapeutics and lead compounds.
  • Inclusion of marine bioactive products with distinct structures.
  • Consideration of computer-assisted techniques like molecular modeling and machine learning.

Main Results:

  • Identification of numerous natural product-related compounds with significant therapeutic potential.
  • Focus on agents discovered or developed between 2016 and 2022.
  • Inclusion of marine-derived compounds and their structural characteristics.

Conclusions:

  • Natural products remain a crucial resource for developing novel drugs against major diseases.
  • Computational methods are increasingly important for identifying and optimizing natural product-based drug candidates.
  • Continued exploration of natural sources, especially marine environments, is essential for future drug discovery.