Infographic: Drugging the Undruggable: Leveraging the Right Screening Methods for Challenging Targets

01/03/2022 - 2 minutes

Challenging targets, such as membrane proteins or protein-protein interactions were considered undruggable in the past. However, today a variety of screening methods can be used to help develop drugs against these formerly undruggable targets. Discover more in this infographic!

There are thousands of challenging targets against which it is incredibly difficult to develop a drug. Examples include protein-protein interactions, membrane proteins, and proteins that interact with RNA or DNA.

Most of these challenging targets have very characteristic traits, such as a lack of catalytic active sites, unknown or featureless binding sites, or the presence of metal ions.

Fortunately, researchers have come up with a number of screening methods to address undruggable targets. This can help to develop essential drugs.

Each screening method has distinctive traits and can therefore screen different challenging targets. Some, like the affinity selection mass spectrometry screen and the high throughput screen, can screen around 300,000 molecules at once. Others, including DNA encoded libraries (DEL) and DEL-enhanced virtual screening, can screen billions of molecules at the same time.

One example in which finding the right screening method for challenging targets can help is the enzyme Aurora A kinase. While it plays an important role in healthy cell proliferation, this enzyme has been found to be highly expressed in a number of tumor types. This means that it could be a promising target for cancer therapy.

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Recently, the researchers at WuXi AppTec used their expertise to find promising hits for Aurora A kinase with the help of DELs and virtual screening. As a result, the researchers validated promising hits and found new chemical structures that could be useful for future drug development.

In this infographic, created in collaboration with WuXi AppTec, we have listed a number of different screening methods developed to help find suitable molecules to drug formerly challenging targets. Each screening method is described and its advantages and limitations are revealed.

You can download a free version of the infographic here!

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Are you working with challenging targets and struggling to find the right lead-finding option? Learn more at wuxiapptec.com or get in touch with the expert:

Nuska Tschammer, Head of DEL Lab Operations Europe at WuXi AppTec HitS/CRELUX at nuska_tschammer@wuxiapptec.com

Design: Elena Resko and Anastasiia Slynko

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This infographic was originally published in September 2019 and has since been updated.

 

 

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