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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...
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...
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...
Therapeutic Drug Monitoring: Drug Analysis Methods01:26

Therapeutic Drug Monitoring: Drug Analysis Methods

Therapeutic Drug Monitoring (TDM) is a clinical practice that measures specific drug levels in a patient's blood or body tissues to tailor drug therapy effectively. This monitoring is critical for managing drugs with narrow therapeutic indices like digoxin and phenytoin, ensuring they are both safe and effective. For instance, monitoring theophylline levels in asthma patients involves precision and sensitivity to adjust doses according to individual responses to therapy, ensuring efficacy and...
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...

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NMR-Based Fragment Screening in a Minimum Sample but Maximum Automation Mode
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Drug profiling: knowing where it hits.

Alejandro Merino1, Agnieszka K Bronowska, David B Jackson

  • 1Conway Institute of Biomolecular & Biomedical Research, School of Medicine and Medical Science, University College Dublin, Belfield, Dublin 4, Ireland.

Drug Discovery Today
|July 6, 2010
PubMed
Summary
This summary is machine-generated.

Understanding drug promiscuity is key in drug discovery. This review covers cost-effective profiling methods to predict drug effects and improve therapeutic utility, addressing industry-wide challenges.

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Area of Science:

  • Pharmacology and Drug Discovery
  • Medicinal Chemistry
  • Biotechnology

Background:

  • Off-target drug interactions can cause adverse effects or reveal new therapeutic uses.
  • Drug selectivity profiling is crucial for minimizing attrition and maximizing therapeutic potential in drug discovery.
  • Polypharmacology, where drugs interact with multiple targets, extends beyond known target families, posing a challenge.

Purpose of the Study:

  • To review current and emerging drug profiling alternatives.
  • To discuss commercial solutions for expanding target coverage in drug discovery.
  • To address the industry-wide challenge of lowering profiling costs and improving prediction accuracy for drug promiscuity.

Main Methods:

  • Review of existing literature on drug profiling techniques.
  • Analysis of current commercial solutions for selectivity profiling.
  • Exploration of emerging technologies in drug target interaction analysis.

Main Results:

  • Identification of various drug profiling alternatives and commercial solutions.
  • Highlighting the trend of polypharmacology beyond traditional target families.
  • Emphasis on the need for cost-effective and broad-coverage profiling methods.

Conclusions:

  • Cost-effective and expanded drug profiling is essential for modern drug discovery.
  • Advances in profiling technologies are crucial for managing polypharmacology.
  • Improved prediction of drug interactions will enhance therapeutic utility and safety.