News

Drug discovery company Cresset has announced the extension of its global collaboration with chemical and biological contract research organisation (CRO) Enamine. Both companies will work together in the area of targeted protein degradation (TPD).

TPD is a research strategy with expanding applications in chemical probe and therapeutic agent development. A major class of small molecules commonly used for TPD are known as proteolysis-targeting chimeras (PROTACs), which consist of a POI-binding ligand and an E3-ligase ligand joined by a linker. Designing the linkers can be challenging due to the optimisation of both degradation and physiochemical, and ADME, properties.

Dr Vladimir Ivanov, Enamine’s executive vice president, said: “We are happy to continue our productive collaboration with Cresset. Furthermore, providing streamlined access to Enamine’s TPD-related Linker Library in Spark gives our joined customers a great solution for bioisosteric replacement and scaffold hopping.”

The Entamine TPD-related Linker Library has been integrated into Spark, a linker library, enabling the ability to search for known degrader linkers. Promising results have been shown from early experiments corroborating that the process of designing heterobifunctional molecule linkers could be significantly aided by linker libraries such as Spark. Typical fragments found in existing libraries are usually smaller and less flexible.

Cresset’s chief scientific officer, Dr Mark Mackey, commented, “We are excited to continue working with Enamine to help our customers advance their projects by designing the best molecules they can.”