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Scientists manipulate single atoms within molecules with magic-like technique

Scientists manipulate single atoms within molecules with magic-like technique

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Skeletal Editing: A Revolutionary Technique for Efficient Drug Discovery

Half a decade ago, chemist Mark Levin was a postdoc looking for a visionary project that could change his field. He found inspiration in a set of published wish lists from pharmaceutical-industry scientists who were looking for ways to transform medicinal chemistry. Among their dreams, one concept stood out: the ability to precisely edit a molecule by deleting, adding or swapping single atoms in its core.

This sort of molecular surgery could dramatically speed up drug discovery and revolutionize how organic chemists design molecules. Levin is now the head of a team at the University of Chicago pioneering these techniques, aiming to more efficiently forge new drugs, polymers and biological molecules such as peptides.

The Potential of Skeletal Editing

Compared to conventional approaches that involve synthesizing modified skeletons from scratch, skeletal editing could potentially massively speed up the process of drug discovery. However, at this stage, many of these methods only work on specific molecules, or edit them inefficiently. Researchers are excited but also wary of overhyping a young field.

Understanding Skeletal Editing and its Challenges

Understanding skeletal editing requires knowledge of organic chemistry, including chemical compounds’ structural representations and reactions. Each vertex in a shape represents a carbon atom, accompanied by hydrogen atoms that are not shown, while the lines between them are chemical bonds. Adding a set of reliable skeletal editing reactions to the chemists’ toolkit could provide a new set of disconnections, enabling more efficient syntheses and ways to make previously inaccessible compounds. However, it is challenging to add skeletal editing to chemists’ existing techniques because it requires special skills.

Applications of Skeletal Editing in Medicinal Chemistry

Skeletal editing also holds promising applications in medicinal chemistry. The skeletal editing reactions chemists have developed are generally tailored to the needs of medicinal chemists. Many are designed to edit molecular rings that contain non-carbon atoms such as O, N or S, called heterocycles. These heterocycles are ubiquitous in medicinal chemistry. For instance, a chemist may want to modify a molecule to improve solubility or optimize the potency of nitrogen atoms in drug candidates. However, constructing these variants is time-consuming, and having the capability of skeletal editing can save valuable time.

The Excitement Around Skeletal Editing

Despite the challenges of the skeletal editing approach, chemists at drug makers and universities are already testing various skeletal editing reactions. They recognize it could be transformative, and they believe it won’t be long before some of these methods become widely used.

FAQs

1. What is skeletal editing?
Skeletal editing is the ability to precisely edit a molecule by deleting, adding, or swapping single atoms in its core.

2. How can skeletal editing revolutionize drug discovery?
Skeletal editing can dramatically speed up drug discovery by providing a new set of disconnections, enabling more efficient syntheses and ways to make previously inaccessible compounds.

3. What are the challenges of skeletal editing?
Skeletal editing is challenging because it requires special skills and many methods only work on specific molecules or edit them inefficiently.

4. What are the applications of skeletal editing in medicinal chemistry?
Skeletal editing can optimize the potency of nitrogen atoms in drug candidates and improve the solubility of molecules. Chemists also tailor skeletal editing reactions to the needs of medicinal chemists.

5. Is skeletal editing widely used in drug discovery?
At this stage, many of these methods only work on specific molecules or edit them inefficiently. However, researchers in drug makers and universities are already testing various skeletal editing reactions. They believe it could be transformative and recognize it won’t be long before some of these methods become widely used.

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