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 Concept Videos

tRNA Activation02:26

tRNA Activation

Aminoacyl-tRNA synthetases are present in both eukaryotes and bacteria. Though eukaryotes have 20 different aminoacyl-tRNA synthetases to couple to 20 amino acids, many bacteria do not have genes for all of these aminoacyl-tRNA synthetases. Despite this, they still use all 20 amino acids to synthesize their proteins. For instance, some bacteria do not have the gene encoding the enzyme that couples glutamine with its partner tRNA. In these organisms, one enzyme adds glutamic acid to all of the...
tRNA Activation02:26

tRNA Activation

Aminoacyl-tRNA synthetases are present in both eukaryotes and bacteria. Though eukaryotes have 20 different aminoacyl-tRNA synthetases to couple to 20 amino acids, many bacteria do not have genes for all of these aminoacyl-tRNA synthetases. Despite this, they still use all 20 amino acids to synthesize their proteins. For instance, some bacteria do not have the gene encoding the enzyme that couples glutamine with its partner tRNA. In these organisms, one enzyme adds glutamic acid to all of the...
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a rapamycin-insensitive companion...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:

You might also read

Related Articles

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

Sort by
Same author

Synthesis of BODIPY@MOFs as Hybrid Materials for Emerging Applications: A Review.

Molecules (Basel, Switzerland)·2025
Same author

The IMS Library: from IN-Stock to Virtual.

ChemMedChem·2024
Same author

Hetero-Diels-Alder and CuAAC Click Reactions for Fluorine-18 Labeling of Peptides: Automation and Comparative Study of the Two Methods.

Molecules (Basel, Switzerland)·2024
Same author

A New Derivative of Retro-2 Displays Antiviral Activity against Respiratory Syncytial Virus.

International journal of molecular sciences·2024
Same author

Pasteurized <i>akkermansia muciniphila</i> improves irritable bowel syndrome-like symptoms and related behavioral disorders in mice.

Gut microbes·2024
Same author

Exploring Serum Biomarkers for Neuropathic Pain in Rat Models of Chemotherapy-Induced Peripheral Neuropathy: A Comparative Pilot Study with Oxaliplatin, Paclitaxel, Bortezomib, and Vincristine.

Toxics·2023

Related Experiment Video

Updated: Jun 19, 2026

MISSION LentiPlex Pooled shRNA Library Screening in Mammalian Cells
09:12

MISSION LentiPlex Pooled shRNA Library Screening in Mammalian Cells

Published on: December 21, 2011

19.1K

LPS2336, a New TREK-1 Channel Activator Identified by High Throughput Screening.

Romane Boyer1, Romane Bony1, Maxence Maugis1

  • 1Université Clermont Auvergne, Inserm, CHU Clermont-Ferrand, Neuro-Dol, 63000 Clermont-Ferrand, France.

Biomolecules
|May 28, 2025
PubMed
Summary
This summary is machine-generated.

Researchers optimized a thallium flux assay to find TREK-1 channel activators for pain relief. They identified LPS2336, a potent activator, but its analogs were inactive, highlighting the need for early adverse effect investigation.

Keywords:
TREK-1analgesiahigh throughput screeningpainstructure–activity relationship

More Related Videos

A Multiplexed Luciferase-based Screening Platform for Interrogating Cancer-associated Signal Transduction in Cultured Cells
10:13

A Multiplexed Luciferase-based Screening Platform for Interrogating Cancer-associated Signal Transduction in Cultured Cells

Published on: July 3, 2013

11.8K
High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes
09:44

High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes

Published on: March 3, 2015

10.1K

Related Experiment Videos

Last Updated: Jun 19, 2026

MISSION LentiPlex Pooled shRNA Library Screening in Mammalian Cells
09:12

MISSION LentiPlex Pooled shRNA Library Screening in Mammalian Cells

Published on: December 21, 2011

19.1K
A Multiplexed Luciferase-based Screening Platform for Interrogating Cancer-associated Signal Transduction in Cultured Cells
10:13

A Multiplexed Luciferase-based Screening Platform for Interrogating Cancer-associated Signal Transduction in Cultured Cells

Published on: July 3, 2013

11.8K
High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes
09:44

High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes

Published on: March 3, 2015

10.1K

Area of Science:

  • Neuroscience
  • Pharmacology
  • Ion Channel Biology

Background:

  • TWIK-related K+ (TREK-1) channels play a role in pain perception.
  • Pharmacological activation of TREK-1 channels offers potential for pain relief.
  • Developing novel pharmacological tools is crucial for studying TREK-1 channels and structure-activity relationships.

Purpose of the Study:

  • To optimize a high-throughput screening (HTS) method for identifying TREK-1 activators.
  • To discover new chemical tools for TREK-1 channel research.
  • To investigate the in vivo effects and potential adverse effects of identified TREK-1 activators.

Main Methods:

  • Optimized a thallium flux monitoring assay for HTS.
  • Screened 1040 compounds from the French National Essential Chemical Library.
  • Tested LPS2336 analogs and evaluated LPS2336 in vivo (systemic, intracerebroventricular, intrathecal administration).

Main Results:

  • Identified LPS2336 as a potent TREK-1 activator (EC50 = 11.76 µM).
  • None of the 33 LPS2336 analogs retained TREK-1 activity.
  • LPS2336 demonstrated systemic and intracerebroventricular antinociceptive activity, but not intrathecal.
  • Observed sedation and hypothermia in vivo, likely mediated by off-target effects.

Conclusions:

  • Optimized thallium-based assays provide a valuable tool for TREK-1 channel research.
  • Peripheral TREK-1 channel targeting may be key for pain relief with reduced central side effects.
  • Early in vivo investigation of adverse effects is critical in drug discovery.