Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

A high-throughput method for enzyme kinetic studies.

Lakshmi D Saraswat1, Kimberley A Caserta, Kathy Laws

  • 1Department of Biology and Bioanalytical Chemistry, ArQule, Inc., Woburn, MA 01801, USA. lsaraswat@arqule.com

Journal of Biomolecular Screening
|October 22, 2003
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Antiretroviral Activity, Pharmacokinetics, and Safety of MK-8527, an Oral Nucleoside Reverse Transcriptase Translocation Inhibitor, in Adults With HIV-1 Who Had Not Previously Taken Antiretroviral Agents: Results From 2 Open-Label, Phase 1 Studies.

Clinical infectious diseases : an official publication of the Infectious Diseases Society of America·2026
Same author

Exploring the Past, Present, and Future of Anti-Angiogenic Therapy in Glioblastoma.

Cancers·2023
Same author

Drug-Drug Interaction of Letermovir and Atorvastatin in Healthy Participants.

Clinical pharmacology in drug development·2022
Same author

HDAC6 Inhibition Alleviates CLL-Induced T-Cell Dysfunction and Enhances Immune Checkpoint Blockade Efficacy in the Eμ-TCL1 Model.

Frontiers in immunology·2020
Same author

Assessment of Pharmacokinetic Interaction Between Letermovir and Fluconazole in Healthy Participants.

Clinical pharmacology in drug development·2020
Same author

Lung penetration, bronchopulmonary pharmacokinetic/pharmacodynamic profile and safety of 3 g of ceftolozane/tazobactam administered to ventilated, critically ill patients with pneumonia.

The Journal of antimicrobial chemotherapy·2020

A new, high-throughput drug metabolism screening system was developed using a modified liquid handler. This validated setup accelerates drug discovery by enabling rapid, reproducible analysis of metabolic stability and enzyme inhibition for numerous compounds.

Area of Science:

  • Pharmacology
  • Biochemistry
  • Drug Discovery

Background:

  • Drug metabolism studies are crucial for identifying potential drug candidates.
  • High-throughput screening methods are needed to accelerate drug discovery.
  • Existing methods can be time-consuming and require significant sample volumes.

Purpose of the Study:

  • To develop and validate a simple, flexible, and high-throughput setup for drug metabolism studies.
  • To enable rapid assessment of metabolic stability and enzyme inhibition.
  • To facilitate drug screening in early-stage drug discovery.

Main Methods:

  • Designed a heating block for the Multimek liquid handler platform for 37°C incubation in a 96-well format.
  • Validated the system by assessing the in vitro half-life of midazolam across the plate.

Related Experiment Videos

  • Determined metabolic and inhibition parameters for various reference compounds and proprietary molecules.

    • Main Results:

    • Demonstrated reproducible and consistent determination of midazolam in vitro half-life.
    • Obtained metabolic and inhibition parameter values comparable to literature data for multiple compounds.
    • Successfully applied the setup to assess metabolic stability and cytochrome P450 (CYP) enzyme inhibition, including simultaneous measurements.

    Conclusions:

    • The developed system offers a simple, high-throughput, and validated solution for drug metabolism screening.
    • This tool can significantly accelerate the early stages of drug discovery.
    • The setup is versatile for assessing metabolic stability, CYP inhibition, and combination effects.