Related Experiment Video
Updated: Jul 18, 2025

Genome-wide Mapping of Drug-DNA Interactions in Cells with COSMIC Crosslinking of Small Molecules to Isolate Chromatin
Published on: January 20, 2016
Natural and Synthetic Anticancer Epidrugs Targeting the Epigenetic Integrator UHRF1
Waseem Ashraf1, Tanveer Ahmad2, Nicolas Reynoird2
1Department of Pharmacology, Faculty of Pharmacy, Bahauddin Zakariya University, Multan 60800, Pakistan.
Abstract:
Cancer is one of the leading causes of death worldwide, and its incidence and mortality are increasing each year. Improved therapeutic strategies against cancer have progressed, but remain insufficient to invert this trend. Along with several other risk factors, abnormal genetic and epigenetic regulations play a critical role in the initiation of cellular transformation, as well as tumorigenesis. The epigenetic regulator UHRF1 (ubiquitin-like, containing PHD and RING finger domains 1) is a multidomain protein with oncogenic abilities overexpressed in most cancers. Through the coordination of its multiple domains and other epigenetic key players, UHRF1 regulates DNA methylation and histone modifications. This well-coordinated dialogue leads to the silencing of tumor-suppressor genes (TSGs) and facilitates tumor cells' resistance toward anticancer drugs, ultimately promoting apoptosis escape and uncontrolled proliferation. Several studies have shown that the downregulation of UHRF1 with natural compounds in tumor cells induces the reactivation of various TSGs, inhibits cell growth, and promotes apoptosis. In this review, we discuss the underlying mechanisms and the potential of various natural and synthetic compounds that can inhibit/minimize UHRF1's oncogenic activities and/or its expression.
Insights
The epigenetic regulator UHRF1 drives cancer by silencing tumor-suppressor genes. Natural compounds can inhibit UHRF1, reactivating these genes to fight cancer growth and promote apoptosis.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Cancer remains a leading global cause of death, with increasing incidence and mortality.
- Abnormal genetic and epigenetic regulations are critical in cancer initiation and progression.
- The UHRF1 protein is an overexpressed epigenetic regulator with oncogenic properties in most cancers.
Purpose of the Study:
- To review the mechanisms by which UHRF1 promotes cancer.
- To explore the potential of natural and synthetic compounds in targeting UHRF1.
- To discuss strategies for inhibiting UHRF1's oncogenic activities and expression.
Main Methods:
- Review of existing scientific literature on UHRF1 function and regulation.
- Analysis of studies investigating the effects of natural compounds on UHRF1.
- Examination of UHRF1's role in DNA methylation and histone modification.
Main Results:
- UHRF1 coordinates epigenetic modifications, leading to tumor-suppressor gene silencing.
- Overexpression of UHRF1 facilitates drug resistance, apoptosis evasion, and uncontrolled proliferation.
- Downregulation of UHRF1 by natural compounds can reactivate tumor-suppressor genes, inhibit growth, and induce apoptosis.
Conclusions:
- UHRF1 is a key oncogenic driver in cancer through epigenetic dysregulation.
- Targeting UHRF1 with natural or synthetic compounds presents a promising therapeutic strategy.
- Further research into UHRF1 inhibition could lead to novel anticancer treatments.
More Related Videos
07:48Utilizing Functional Genomics Screening to Identify Potentially Novel Drug Targets in Cancer Cell Spheroid Cultures
Published on: December 26, 2016
06:00Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics
Published on: May 14, 2016
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against...
Mitogens and the Cell Cycle
Epigenetic Regulation
X-chromosome...
Treatment Resistant Cancers
Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Drugs that Destabilize Microtubules