AI Article Synopsis
- Scientists are looking at special proteins that help understand tiny changes in DNA called histone modifications, which could help treat various diseases.
- They have been using special chemicals, called probes, to study these proteins more effectively, especially in areas like cancer and inflammation.
- The text talks about some recent advances and challenges in using these probes to better target proteins, including new strategies like using modified proteins and different types of drug molecules.
Article Abstract
Responsible for interpreting histone post-translational modifications, epigenetic reader proteins have emerged as novel therapeutic targets for a wide range of diseases. Chemical probes have been critical in enabling target validation studies and have led to translational advances in cancer and inflammation-related pathologies. Here, we present the most recently reported probes of reader proteins that recognize acylated and methylated lysine. We will discuss challenges associated with achieving potent antagonism of reader domains and review ongoing efforts to overcome these hurdles, focusing on targeting strategies including the use of peptidomimetic ligands, allosteric modulators, and protein degraders.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8384657 | PMC |
| http://dx.doi.org/10.1016/j.cbpa.2021.03.002 | DOI Listing |
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