Related Experiment Video
Updated: Aug 30, 2025
08:48
Specificity Analysis of Protein Lysine Methyltransferases Using SPOT Peptide Arrays
Published on: November 29, 2014
14.0K
Protein Lysine Methyltransferases Inhibitors
Ying Li1, Lei Ding1, Shuang Ren1
1College of Pharmaceutical Science, Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Hangzhou 310014, P.R. China.
Current Medicinal Chemistry
|August 31, 2022
Summary
Protein lysine methylation, a key epigenetic regulator, involves protein lysine methyltransferases (PKMTs). Aberrant PKMT activity links to cancers, driving research into selective PKMT inhibitors for therapeutic development.
Area of Science:
- Biochemistry
- Epigenetics
- Molecular Biology
Background:
- Protein lysine methylation is a crucial post-translational modification (PTM) impacting epigenetic regulation.
- Protein lysine methyltransferases (PKMTs) catalyze this modification on histones and non-histone proteins.
- Dysregulated PKMT activity is implicated in various cancers and diseases.
Approach:
- This review synthesizes current knowledge on PKMTs' biochemical and biological functions.
- It examines the association between PKMTs and cancer development.
- The paper details selective small-molecule inhibitors, including their chemical structures and structure-activity relationships.
Key Points:
- PKMTs play a vital role in cellular processes and disease pathogenesis.
- Several PKMT inhibitors have advanced to clinical trials, indicating therapeutic potential.
- Understanding structure-activity relationships is key for developing potent and selective inhibitors.
Conclusions:
- The field of PKMTs and their inhibitors is rapidly evolving.
- This review provides insights for designing novel, highly effective PKMT inhibitors.
- Targeting PKMTs represents a promising strategy for cancer therapy.
Related Concept Videos
01:52Eukaryotic Transcription Inhibitors
10.0K
Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
10.0K
01:19Antiasthma Drugs: Leukotriene Modifiers
428
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:
Leukotriene modifiers work through two distinct mechanisms:
428