Related Experiment Video

Updated: Nov 4, 2025

Specificity Analysis of Protein Lysine Methyltransferases Using SPOT Peptide Arrays
08:48

Specificity Analysis of Protein Lysine Methyltransferases Using SPOT Peptide Arrays

Published on: November 29, 2014

14.2K

Histone lysine methyltransferase SET8 is a novel therapeutic target for cancer treatment

Chao Yang1, Kai Wang2, YingTang Zhou1

  • 1National Engineering Research Center for Marine Aquaculture, Institute of Innovation & Application, Zhejiang Ocean University, Zhoushan, Zhejiang Province 316022, China.

Drug Discovery Today
|May 22, 2021
PubMed

Insights

SET8, a key enzyme in cell regulation, is implicated in cancer progression. Inhibiting SET8 presents a promising therapeutic strategy for various cancers.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • SET8 is the sole enzyme catalyzing H4K20 monomethylation.
  • SET8 regulates critical cellular processes including cell cycle, DNA repair, and apoptosis.

Purpose of the Study:

  • To elucidate the molecular structure and biological roles of SET8.
  • To highlight SET8's involvement in tumorigenesis.
  • To review the development of SET8 inhibitors for cancer therapy.

Main Methods:

  • Literature review of SET8's molecular structure and functions.
  • Analysis of SET8's role in various cancer types.
  • Summary of current research on SET8 inhibitors.

Main Results:

  • SET8's unique role in histone modification.
  • Aberrant SET8 expression correlates with cancer proliferation, invasion, metastasis, and prognosis.
  • SET8 inhibitors show therapeutic potential.

Conclusions:

  • SET8 is a crucial regulator of cellular processes and a significant factor in cancer development.
  • Targeting SET8 with inhibitors offers a viable therapeutic avenue for cancer treatment.
Keywords:
Cancer therapyEpigenetic modificationHistone methylationSET8 inhibitor

More Related Videos

Author Spotlight: Epigenetic Modifications and Metabolic Rewiring as Targets for Cancer Therapy07:20

Author Spotlight: Epigenetic Modifications and Metabolic Rewiring as Targets for Cancer Therapy

Published on: October 18, 2024

743
Assays for Validating Histone Acetyltransferase Inhibitors09:11

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

6.7K

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
8.0K
Epigenetic Regulation01:37

Epigenetic Regulation

Epigenetic changes alter the physical structure of the DNA without changing the genetic sequence and often regulate whether genes are turned on or off. This regulation ensures that each cell produces only proteins necessary for its function. For example, proteins that promote bone growth are not produced in muscle cells. Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
X-chromosome...
3.3K
Cancer Therapies02:49

Cancer Therapies

Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
8.9K
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
5.1K
Abnormal Proliferation02:23

Abnormal Proliferation

Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the...
4.8K
Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
2.3K