Researchers at Dartmouth College have developed a novel strategy for drug discovery and development such development can be used to target new therapies against cancer and possibly neurodegenerative diseases.
Learn more about the traditional process involved in drug discovery and development:
The new technique utilizes a novel synthesis approach by uniting molecular building blocks for a class of organic compounds known as tetracyclic terpenoids—which are responsible for the generation of many FDA-approved drugs and are considered the most successful class of natural product-inspired pharmaceuticals.
"Until now, there was nothing like this available for drug discovery and development," said Glenn Micalizio, the New Hampshire Professor of Chemistry at Dartmouth. "While additional development is expected to enhance the power of this new technology, I believe that we are at the beginning of establishing a truly enabling and potentially transformative technology for the pharmaceutical industry."
Ultimately, the process combines two new chemical reactions that establish bonds between carbon atoms with a unique metal-centered ring-forming reaction. The chemical combination allows for the investigation of pharmaceutically-privileged regions.
"This is an important first step toward establishing a new technology platform to greatly facilitate drug discovery across a diverse landscape of therapeutic indications," said Micalizio.
A new chemical pathway from simple commercially-available materials to medicinally-relevant molecules. Image courtesy of Glenn Micalizio via Dartmouth.edu
Findings of the study, published in Nature Communications, can provide the basis for a future in large-scale production of new pharmaceuticals.
To test the efficacy of their technique, researchers describe the discovery of a selective toxic molecule to an aggressive and deadly form of a brain tumor known as glioblastoma.
"Glioblastomas are incurable, and existing therapies have horrific side effects," said Arti Gaur, an assistant professor of neurology at Dartmouth's Geisel School of Medicine. "It is extremely exciting and encouraging to see that these novel compounds can selectively kill patient-derived brain tumor cells without harming cells from normal, healthy brain tissue."
The research advances organic chemistry to enable the discovery of new therapeutics for a wide range of malignancies as well as neurodegeneration and neuro-inflammation.
Source: Dartmouth Press Release
