Our DNA contains the instructions for producing all the molecules necessary for life. To read these instructions, the DNA must be “turned on” or “turned off” at the right time. Recent studies have identified an enzyme called GCN5 which plays an important role in this “gene regulation”. When this enzyme malfunctions, diseases such as cancer and diabetes can develop.
What is GCN5 and how does it work
The GCN5 acetyltransferase it is a crucial enzyme for turning genes on and off. It transfers chemical groups, called acetyls, onto other molecules, changing their shape and function.
This enzyme acts mainly on histone, fundamental components of the DNA structure in cells. By altering histones with the addition of acetyls, the enzyme regulates gene expression, increasing or decreasing the production of certain proteins.
Why it is important in diseases
By modifying the activity of genes, GCN5 controls many cellular processes crucial for health, such as proliferation, metabolism, differentiation.
When the enzyme is altered, it can lead to a uncontrolled growth as in cancer, or to a metabolic malfunction as in diabetes.
In cancer
In several tumors GCN5 is present in excessive quantities. This causes it to overactivate genes that promote the multiplication of cancer cells.
Inhibiting the enzyme would reduce the growth of tumors. For example, in lung, breast and cervical cancer, the action of GCN5 has been correlated with the progression of the disease.
In diabetes
In type II diabetes, GCN5 is hyperactive and alters sugar metabolism. The enzyme aberrantly modifies a key protein, PGC-1α, which regulates blood glucose levels.
Curbing the activity of GCN5 could therefore also help control blood sugar in diabetic patients.
GCN5, a "miracle" molecule for future drugs against cancer, diabetes and more?
A recent study (I link it here) Published in Biomedicine & Pharmacotherapy da Hai-Tao Xiao and colleagues from South China Pharmaceutical University took stock of knowledge about GCN5.
It is the second study in just over a year: in 2022 the University of Ottawa had noted a really important role for this enzyme in rebuilding muscles in older people.
To exploit these discoveries, researchers are now looking for molecules capable of selectively inhibiting the enzyme.
Various natural compounds with promising effects have been identified, such as curcumin and garcinol. But more effective and specific drugs against GCN5 are still needed to treat cancer, diabetes and other diseases.
Understanding the mechanisms by which this enzyme controls gene expression has opened interesting perspectives for the development of new drugs against widespread and disabling pathologies such as tumors and diabetes. Further research on this promising molecule will be crucial to turning these hopes into reality.
