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Eukaryotic Transcription Inhibitors

Eukaryotic Transcription Inhibitors

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...

Inhibition of Cdk Activity

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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...

Covalently Linked Protein Regulators

Covalently Linked Protein Regulators

Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
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Covalently Linked Protein Regulators

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Heterochromatin

Heterochromatin

The extent of chromatin compaction can be studied by staining chromatin using specific DNA binding dyes. Under the microscope, the dense-compacted regions that take up more dye are called heterochromatin. Heterochromatin is further classified into two forms – constitutive heterochromatin and facultative heterochromatin.
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Cooperative Binding of Transcription Regulators

Cooperative Binding of Transcription Regulators

Transcriptional regulators bind to specific cis-regulatory sequences in the DNA to regulate gene transcription. These cis-regulatory sequences are very short, usually less than ten nucleotide pairs in length. The short length means that there is a high probability of the exact same sequence randomly occurring throughout the genome. Since regulators can also bind to groups of similar sequences, this further increases the chances of random binding. Transcriptional regulators form...

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Related Experiment Video

Updated: Nov 1, 2025

Toxicological Assays for Testing Effects of an Epigenetic Drug on Development, Fecundity and Survivorship of Malaria Mosquitoes

Toxicological Assays for Testing Effects of an Epigenetic Drug on Development, Fecundity and Survivorship of Malaria Mosquitoes

Published on: January 16, 2015

Small-molecule inhibitors targeting Polycomb repressive complex 1 RING domain.

Shirish Shukla¹, Weijiang Ying¹, Felicia Gray¹

¹Department of Pathology, University of Michigan, Ann Arbor, MI, USA.

Nature Chemical Biology

|June 22, 2021

Summary

Researchers developed small-molecule inhibitors targeting Polycomb Repressive Complex 1 (PRC1) by binding to the RING1B-BMI1 complex. These inhibitors block H2A ubiquitination and show potential in treating acute myeloid leukemia (AML).

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A Method to Study de novo Formation of Chromatin Domains

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Genome-wide Mapping of Drug-DNA Interactions in Cells with COSMIC Crosslinking of Small Molecules to Isolate Chromatin

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Published on: January 20, 2016

A Method to Study de novo Formation of Chromatin Domains

A Method to Study de novo Formation of Chromatin Domains

Published on: August 23, 2019

Area of Science:

Chromatin biology
Epigenetics
Cancer research

Background:

Polycomb Repressive Complex 1 (PRC1) is crucial for maintaining repressed chromatin states via histone H2A monoubiquitination.
PRC1's role in cancer necessitates targeted small-molecule inhibitors with clear mechanisms of action.

Purpose of the Study:

To develop and characterize small molecules that directly inhibit the E3 ligase activity of the PRC1 RING1B-BMI1 complex.
To investigate the therapeutic potential of PRC1 inhibitors in leukemia models.

Main Methods:

Development of small-molecule inhibitors targeting the RING1B-BMI1 heterodimer.
Structural studies to elucidate inhibitor binding mechanisms.
Assessment of inhibitor efficacy in cellular assays and primary acute myeloid leukemia (AML) samples.

Main Results:

Compounds were identified that bind to RING1B, inducing a hydrophobic pocket and blocking PRC1 chromatin association.
The inhibitor RB-3 effectively decreased global H2A ubiquitination levels.
RB-3 induced cellular differentiation in leukemia cell lines and primary AML samples.

Conclusions:

Targeting the PRC1 RING domain with small molecules is a viable therapeutic strategy.
RB-3 is a potent chemical tool for studying PRC1 function and exploring its therapeutic applications in cancer, particularly AML.