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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...
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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...
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Genetic variations significantly influence drug response through pharmacokinetics, receptor interactions, and biologic milieu modifications. Pharmacokinetic alterations impact drug metabolism and clearance, affecting efficacy and toxicity. Variants in drug-metabolizing enzymes, such as CYP2C9 and CYP2C19, alter drug activation and elimination. For example, CYP2C9 loss-of-function variants require lower warfarin doses to prevent excessive bleeding, while CYP2C19 variants reduce clopidogrel...

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Updated: May 18, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

System-based drug discovery within the human kinome.

Paul Bamborough1

  • 1Computational and Structural Chemistry, Molecular Discovery Research, GlaxoSmithKline Medicines Research Centre, Stevenage, UK. Paul.A.Bamborough@gsk.com

Expert Opinion on Drug Discovery
|September 14, 2012
PubMed
Summary

Kinase inhibitor drug discovery shows promise, with approved drugs mainly in oncology. Further research is needed to identify therapeutically relevant kinases and maximize drug efficacy across diverse diseases.

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Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
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Published on: December 1, 2020

Area of Science:

  • Drug Discovery
  • Biochemistry
  • Pharmacology

Background:

  • Significant efforts have focused on human protein kinase inhibitors for over a decade.
  • Five kinase inhibitor drugs have been approved since 2011, primarily in oncology.
  • Success in other therapeutic areas remains limited despite initial promise.

Purpose of the Study:

  • To review prospects for kinase inhibitor drug discovery in oncology and other therapeutic areas.
  • To discuss the application of kinome profiling and system-based research in kinase target validation.
  • To outline properties of effective small molecule kinase probes.

Main Methods:

  • Review of current literature on kinase inhibitor drug discovery.
  • Analysis of kinome profiling and system-based research methodologies.
  • Discussion of target validation and classification of kinases as liabilities.

Main Results:

  • Protein kinases are highly tractable to small molecule discovery with achievable selectivity.
  • Advanced screening enables compound profiling across the kinome.
  • Decisions on desirable inhibition profiles are crucial but challenging due to incomplete disease biology understanding.

Conclusions:

  • Drug discovery must balance tractability with the risk of clinical trial failure due to incomplete disease understanding.
  • Determining therapeutically relevant kinases is critical for specific diseases.
  • Early screening via phenotypic assays can maximize opportunities for repurposing drug candidates.