Related Experiment Video
Updated: May 20, 2025

Using In Vitro and In-cell SHAPE to Investigate Small Molecule Induced Pre-mRNA Structural Changes
Published on: January 30, 2019
Small molecule compounds targeting G9a/GLP: Recent advances and perspectives
Qiangsheng Zhang1, Lu Li2, Siyan Li3
1School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031, China.
Small molecule inhibitors targeting G9a/GLP, crucial in diseases like cancer, have advanced significantly. This review details their discovery, design, and development, offering insights for pharmaceutical research.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Pharmacology
Background:
- G9a/GLP, a histone methyltransferase, is implicated in diseases including tumors, fibrosis, and malaria.
- Over 40 G9a modulators have been developed since 2007, targeting this enzyme family.
Purpose of the Study:
- To systematically review small molecule inhibitors targeting G9a/GLP.
- To analyze discovery methods, design strategies, and development challenges for G9a/GLP modulators.
Main Methods:
- Literature review of G9a/GLP inhibitors.
- Classification of inhibitors based on binding site (SAM-competitive, substrate-competitive) and mechanism (reversible, irreversible, dual, degraders).
- Analysis of structural optimization, binding modes, biological activity, and pharmacokinetics.
Main Results:
- Categorization of G9a/GLP inhibitors by binding site and mechanism of action.
- Detailed overview of small molecule discovery, design, and optimization strategies.
- Compilation of biological activity and pharmacokinetic data for various G9a/GLP modulators.
Conclusions:
- Significant progress has been made in developing small molecule inhibitors for G9a/GLP.
- The review provides valuable insights into challenges and opportunities for future drug development targeting G9a/GLP.
More Related Videos
04:48A High-throughput Calcium-flux Assay to Study NMDA-receptors with Sensitivity to Glycine/D-serine and Glutamate
Published on: July 10, 2018
07:16Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Related Concept Videos
GTPases and their Regulation
Large G-proteins,...
Glucagon-like Receptor Agonists
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
Targets for Drug Action: Overview
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...
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include: