Hope for new oral drugs comes from an Australian study.
Perhaps soon it will be possible to replace the annoying ones insulin injections with some pills. A group of researchers from the Walter and Eliza Hall Institute di Melbourne in fact, he discovered a molecule that mimics insulin and can be taken orally. The research, which appeared in Nature Communications, paves the way for the development of new oral drugs for diabetic patients.
“For 100 years now, the development of an insulin pill has been a dream of researchers but, after decades of trying, there has been little success,” they explain Nicholas Kirk e Mike Lawrence, principal investigators of the study. Indeed, insulin is very unstable and degrades immediately during digestion.
The team tried to work around this problem using the cryo-electron microscopy (cryo-EM), a new technology that can display complicated molecules in atomic detail. This allowed for rapid generation of 3D images of the insulin receptor. In the experimental stages, one was identified peptide molecule which mimics insulin and can bind to and activate the hormone receptor—the first step in getting cells to absorb glucose when blood sugar levels are too high.
“The human insulin receptor signaling system plays a critical role in glucose homeostasis,” Kirk and Lawrence say. Insulin binding results in a large conformational change in the extracellular region of the receptor which in turn affects the trans-activation of intracellular tyrosine kinase domains and downstream signaling. The 33-mer polypeptide engages the receptor via two helical binding patterns, each of which is potentially imitable by small molecules.”
The researchers conclude: “The resulting conformation of the receptor is different from, but related to, those of existing three-dimensional structures of the insulin-complexed receptor. Our findings therefore illuminate unexplored pathways for the control of insulin receptor signaling and opportunities for the development of insulin mimetics. It’s still a long way to go, requiring more research, but it’s exciting to know that our discovery opens the door to oral treatments for type 1 diabetes.”
Nurse Times editorial team
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