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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...
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...
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...
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...
Measurement of Bioavailability: Pharmacodynamic Methods01:20

Measurement of Bioavailability: Pharmacodynamic Methods

Pharmacodynamic methods provide insights into a drug's effects on physiological processes over time and play a crucial role in understanding bioavailability and therapeutic efficacy. These methods can be broadly classified into acute pharmacological and therapeutic response approaches, each with distinct mechanisms and applications.The acute pharmacological response method directly correlates a drug's physiological effects, such as ECG or pupil diameter changes, to its time course in the body.
Protein-Drug Binding: Determination Methods01:22

Protein-Drug Binding: Determination Methods

Determining protein-drug binding can be achieved through indirect and direct methods, each providing valuable insights into the interaction between proteins and drugs.
Indirect methods involve isolating the bound drug from its free form in biological samples such as blood, serum, or plasma. These techniques aim to measure the percentage of drugs bound to proteins. Equilibrium dialysis is a commonly used method where the free drug concentration at equilibrium is measured by separating the bound...

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Related Experiment Video

Updated: Jun 2, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
08:31

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Published on: December 1, 2020

Activity-based profiling for drug discovery.

Remigiusz Serwa1, Edward W Tate

  • 1Institute of Chemical Biology, Department of Chemistry, Imperial College London, South Kensington Campus, London SW72AZ, UK.

Chemistry & Biology
|April 26, 2011
PubMed
Summary
This summary is machine-generated.

Activity-based protein profiling (ABPP) enabled the discovery of JW480, a potent inhibitor of KIAA1363. This breakthrough significantly hinders the in vivo growth of human prostate cancer cell lines, offering new therapeutic avenues.

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Cost-Efficient Transcriptomic-Based Drug Screening
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Cost-Efficient Transcriptomic-Based Drug Screening

Published on: February 23, 2024

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Last Updated: Jun 2, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
08:31

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Published on: December 1, 2020

Cost-Efficient Transcriptomic-Based Drug Screening
06:40

Cost-Efficient Transcriptomic-Based Drug Screening

Published on: February 23, 2024

Area of Science:

  • Biochemistry
  • Chemical Biology
  • Drug Discovery

Background:

  • Activity-based protein profiling (ABPP) is a powerful chemical proteomics strategy.
  • ABPP enables the discovery of novel enzyme inhibitors and biological probes.
  • Target validation and drug discovery are key applications of ABPP.

Discussion:

  • Chang et al. utilized ABPP to identify JW480, a selective inhibitor of monoalkylglycerol ether hydrolase KIAA1363.
  • JW480 demonstrates high potency and oral bioavailability.
  • The inhibitor was shown to significantly impair the in vivo growth of human prostate cancer cell lines.

Key Insights:

  • Discovery of JW480, a novel KIAA1363 inhibitor.
  • Demonstration of JW480's efficacy in reducing prostate cancer cell growth in vivo.
  • Validation of ABPP as a method for identifying potent anti-cancer drug candidates.

Outlook:

  • JW480 represents a promising therapeutic candidate for prostate cancer.
  • Further investigation into KIAA1363's role in cancer progression is warranted.
  • ABPP continues to be a valuable platform for advancing drug discovery and target validation.