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

The Two-State Receptor Model01:29

The Two-State Receptor Model

2.7K
The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
2.7K
Types of RNA01:23

Types of RNA

69.9K
Overview
Three main types of RNA are involved in protein synthesis: messenger RNA (mRNA), transfer RNA (tRNA), and ribosomal RNA (rRNA). These RNAs perform diverse functions and can be broadly classified as protein-coding or non-coding RNA. Non-coding RNAs play important roles in the regulation of gene expression in response to developmental and environmental changes. Non-coding RNAs in prokaryotes can be manipulated to develop more effective antibacterial drugs for human or animal use.
RNA...
69.9K
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

8.4K
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...
8.4K
Positive Regulator Molecules01:45

Positive Regulator Molecules

116.2K
To consistently produce healthy cells, the cell cycle—the process that generates daughter cells—must be precisely regulated.
116.2K
Cooperative Allosteric Transitions01:58

Cooperative Allosteric Transitions

8.3K
Cooperative allosteric transitions can occur in multimeric proteins, where each subunit of the protein has its own ligand-binding site. When a ligand binds to any of these subunits, it triggers a conformational change that affects the binding sites in the other subunits; this can change the affinity of the other sites for their respective ligands. The ability of the protein to change the shape of its binding site is attributed to the presence of a mix of flexible and stable segments in the...
8.3K
Antiasthma Drugs: Leukotriene Modifiers01:19

Antiasthma Drugs: Leukotriene Modifiers

1.4K
Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
1.4K

You might also read

Related Articles

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

Sort by
Same author

A Method for Extracting Sedimentary Outcrops from UAV Oblique Photogrammetry Point Clouds.

Sensors (Basel, Switzerland)·2026
Same author

Chemical ecology and convergent evolution of natural hallucinogens: From ecological defense to conserved neural targets.

Proceedings of the National Academy of Sciences of the United States of America·2026
Same author

Overcoming Pharmacokinetic and Peripheral Safety Challenges in Psychedelic Therapies: The Promise of Advanced Drug Delivery Systems.

ACS pharmacology & translational science·2026
Same author

Breaking the Transparency-Piezoelectricity Trade-Off in Lead-Free Ceramics via Tailoring Local Polarization Configuration.

ACS nano·2026
Same author

AGREE-YOLO: A Framework for Seafood Recognition and Cross-Cultural Gastronomic Recommendation.

Foods (Basel, Switzerland)·2026
Same author

Icariin promotes lysosomal degradation of amyloid-β precursor protein via enhanced endosome-lysosome trafficking to reduce amyloid-β accumulation and improve cognitive function in Alzheimer's disease models.

Brain research bulletin·2026
Same journal

Harnessing multispecific antibodies for next-generation cancer treatments.

Pharmacology & therapeutics·2026
Same journal

Protein acetylation modification in tissue fibrosis: Opportunities and challenges.

Pharmacology & therapeutics·2026
Same journal

Nipocalimab and other FcRn blockers in neuromuscular disorders.

Pharmacology & therapeutics·2026
Same journal

C26:0-lysophosphatidylcholine in X-linked adrenoleukodystrophy.

Pharmacology & therapeutics·2026
Same journal

The CircRNA/miRNA axis in breast cancer: From molecular mechanisms to clinical translation.

Pharmacology & therapeutics·2026
Same journal

Glymphatic-meningeal lymphatic dysfunction in epilepsy: novel mechanistic insights and therapeutic avenues.

Pharmacology & therapeutics·2026
See all related articles

Related Experiment Video

Updated: Nov 1, 2025

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
10:07

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels

Published on: January 27, 2013

15.4K

TLR4 biased small molecule modulators.

Cong Lin1, Hongshuang Wang2, Miyuan Zhang3

  • 1Laboratory of Chemical Biology, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, Jilin 130022, China; State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, Jiangsu 210023, China.

Pharmacology & Therapeutics
|June 25, 2021
PubMed
Summary
This summary is machine-generated.

Biased modulators offer targeted therapies by enhancing specificity and reducing side effects. This review explores biased modulators for Toll-like receptor 4 (TLR4), a non-G protein-coupled receptor, highlighting their therapeutic potential.

Keywords:
Biased ligandBiased signalingDrug discoveryMyD88TRIFToll-like receptor 4

More Related Videos

Screening Bioactive Nanoparticles in Phagocytic Immune Cells for Inhibitors of Toll-like Receptor Signaling
09:51

Screening Bioactive Nanoparticles in Phagocytic Immune Cells for Inhibitors of Toll-like Receptor Signaling

Published on: July 26, 2017

12.6K
Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
10:20

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b

Published on: November 11, 2016

8.7K

Related Experiment Videos

Last Updated: Nov 1, 2025

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
10:07

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels

Published on: January 27, 2013

15.4K
Screening Bioactive Nanoparticles in Phagocytic Immune Cells for Inhibitors of Toll-like Receptor Signaling
09:51

Screening Bioactive Nanoparticles in Phagocytic Immune Cells for Inhibitors of Toll-like Receptor Signaling

Published on: July 26, 2017

12.6K
Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
10:20

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b

Published on: November 11, 2016

8.7K

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Drug Discovery

Background:

  • Biased pharmacological modulators offer improved specificity, efficiency, and safety profiles.
  • Current research primarily focuses on biased modulators for G protein-coupled receptors (GPCRs).
  • Non-GPCR receptors, such as Toll-like receptor 4 (TLR4), remain largely unexplored for biased modulation.

Purpose of the Study:

  • To review recent advancements in the discovery of biased modulators targeting Toll-like receptor 4 (TLR4).
  • To outline challenges and methodologies associated with identifying TLR4 biased modulators.
  • To emphasize the therapeutic potential of biased TLR4 modulators for various diseases.

Main Methods:

  • Literature review of recent studies on biased modulators.
  • Analysis of signaling pathways involving Toll-like receptor 4 (TLR4).
  • Discussion of small molecule discovery strategies for biased modulators.

Main Results:

  • Toll-like receptor 4 (TLR4) possesses distinct MyD88-dependent and TRIF-dependent signaling pathways.
  • Dysregulation of TLR4 is implicated in numerous diseases, underscoring the need for targeted therapies.
  • Small molecules can selectively modulate TLR4 signaling, offering therapeutic opportunities.

Conclusions:

  • Biased modulators of TLR4 represent a promising avenue for developing novel therapeutics.
  • The development of TLR4 biased modulators can serve as a model for other non-GPCR targets.
  • Targeting TLR4 with biased modulators can provide valuable research tools and drug candidates.