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In-solution aptamer selection for small molecule targets

Small molecules, like drugs, hormones, vitamins, and pesticides, are ubiquitous in our environment and form key analytes that are routinely monitored in healthcare and drug development.

Our Optimer platform has a discovery process tuned specifically for increased success in identifying small molecule binders. We perform Optimer discovery with the small molecule target freely available in solution to increase the availability of functional groups for binding.

When you are analysing small molecules, you typically do this with the analyte free in solution, so working with ligands that were generated in this way offers you the best performance possible.

Why do we need small molecule ligands?

Simple assays for small molecule analysis have been hindered by problems in generating antibodies to these targets. This has left the industry largely reliant on slow and expensive analytical solutions, such as HPLC coupled with mass spectrometry.

Sticky struggles with small molecule ligands

When selecting aptamers, antibodies, or any other small molecule ligand the standard approach is to immobilise the target.

  • For in vivo discovery this allows the larger size of the immobilised small molecule and carrier molecule to be detected by the immune system to generate antibodies as part of an immune response.
  • For in vitro discovery this allows the aptamers that stick to the small molecule to be easily retained while non-binding aptamers can be washed away.

Immobilisation of small molecules for Optimer selection can reduce availability of functional groups or sterically hinder
potential binding sites.

In summary, immobilising the small molecule target can be essential for antibody generation and makes for simpler aptamer selection. But the simplest method doesn’t always offer the best results. Immobilising small molecules can change chemical characteristics and sterically hinder aptamer interactions.

In-solution small molecule ligand discovery

We have solved this problem for small molecule ligands with our Optimer platform. Optimer discovery for small molecule targets is performed with the small molecule in solution. This increases:

  • The availability of functional groups for interaction
  • The potential for success in discovery

Solution-based selection, used as part of the Optimer development platform, increases the available functional groups for improved success in discovery.

If you require binders for small molecules and want to increase your success in discovery from the outset, get in touch to find out how we can work together.


drug discoveryhormonespesticidessmall moleculevitamins

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