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Related Concept Videos

Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

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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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Drug interactions occur when the pharmacological effect of one drug is altered by another substance, either enhancing or diminishing its activity. The drug whose activity is altered is known as the object drug, and the substance causing the alteration is called the agent drug or the precipitant. The net effects of these interactions are mostly undesirable, leading to decreased effectiveness or increased adverse effects. In rare cases, interactions can be beneficial, such as the enhanced...
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The concept of therapeutic equivalence (TE) in drugs with multiple indications is complex. A generic drug may be therapeutically equivalent to a brand-name product for one specific indication, but this doesn't necessarily mean it's equivalent for all other indications. Evidence of TE in one patient group and bioequivalence shown in healthy volunteers can support—but not confirm—TE for other indications. However, definitive proof requires individual clinical studies for each...
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FDA Approved Drugs: Changes to Approved Drugs01:26

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Post-approval, manufacturers may modify an approved new or generic drug product. Such modifications can encompass alterations in the Active Pharmaceutical Ingredient (API), manufacturing process, formulation, batch size, manufacturing site, and container closure system (FDA Guidance for Industry, April 2004). Often, a drug product may undergo multiple changes.These modifications require careful evaluation to determine their potential impact on the drug product's identity, strength, quality,...
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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Factors Affecting Protein-Drug Binding: Drug-Related Factors01:18

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Drug binding to proteins is a complex phenomenon influenced by various drug-related factors, each playing a significant role in the interaction between drugs and proteins within the body.
One crucial factor in drug-protein binding is the drug's lipophilicity or its affinity for fat. More lipophilic drugs tend to have higher binding extents. For example, highly lipophilic drugs like cloxacillin exhibit substantial protein binding, with as much as 95% of the drug binding to proteins. In...
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Related Experiment Video

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Assessing drug target suitability using TargetMine.

Yi-An Chen1, Erika Yogo2, Naoko Kurihara2

  • 1National Institutes of Biomedical Innovation, Health and Nutrition, Ibaraki, Osaka, 5670085, Japan.

F1000Research
|April 16, 2019
PubMed
Summary
This summary is machine-generated.

TargetMine was updated to help select drug targets by integrating gene-disease links and target tractability data. This data mining tool aids pharmaceutical research by improving drug efficacy assessments.

Keywords:
diseasedrug assessmentgenetic variationtractability

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Area of Science:

  • Biomedical Informatics
  • Pharmacology
  • Genetics

Background:

  • Selecting effective drug targets requires assessing both gene-disease links and target tractability.
  • Existing resources often lack comprehensive data for evaluating target tractability.
  • Efficiently identifying promising drug candidates necessitates integrated information on genetic associations and target properties.

Purpose of the Study:

  • To enhance the TargetMine data warehouse for improved drug target prioritization.
  • To integrate new data sources for gene-disease associations and target tractability.
  • To provide a flexible platform for assessing candidate genes' relevance and druggability.

Main Methods:

  • Updated TargetMine by incorporating diverse data sources for gene-disease associations.
  • Integrated new functionalities for assessing drug target tractability.
  • Developed a data mining platform with query capabilities for genetic evidence and target features.
  • Utilized protein structures and chemical compound data within the platform.

Main Results:

  • TargetMine now offers comprehensive data for evaluating gene-disease associations.
  • Enhanced functionalities allow for robust assessment of drug target tractability.
  • The platform provides a powerful interface for querying genetic evidence and target characteristics.
  • Demonstrated utility through specific examples of candidate gene assessment.

Conclusions:

  • The updated TargetMine facilitates more informed decisions in drug target selection.
  • Improved data integration and assessment functionalities enhance pharmaceutical research efficiency.
  • TargetMine serves as a valuable resource for prioritizing drug candidates based on disease linkage and tractability.