Proteomics contributions to epigenetic drug discovery

Area of Science:

• Biochemistry
• Molecular Biology
• Pharmacology

Background:

• Epigenetic features like histone modifications and DNA methylation regulate gene expression and cell phenotypes without altering DNA sequence.
• Dysregulation of epigenetic processes is implicated in various diseases, notably cancer, driving the need for targeted therapies.
• Epigenetic drug discovery focuses on targeting proteins involved in modifying or reading epigenetic marks.

Purpose of the Study:

• To provide an overview of mass spectrometry (MS)-based proteomics applications in epigenetic drug discovery.
• To describe MS-based proteomics approaches supporting drug discovery pipelines.
• To highlight the role of MS-based proteomics in developing and characterizing epigenetic drugs.

Main Methods:

• Mass spectrometry (MS)-based proteomics.
• Analysis of histone post-translational modifications.
• DNA methylation profiling.
• Nucleosome positioning studies.

Main Results:

• MS-based proteomics is a versatile tool for epigenetic drug discovery.
• It aids in target validation, target deconvolution, and monitoring drug efficacy.
• Specific MS approaches support various stages of the drug discovery pipeline.

Conclusions:

• MS-based proteomics is crucial for advancing epigenetic drug discovery.
• It facilitates the identification and characterization of novel epigenetic drug targets and therapies.
• This technology plays a significant role in developing treatments for epigenetic-related diseases.