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Novel E3L platform

Why does novel E3L platform matters?

  • Out of ~600 E3 ligases, only two of them (CRBN and VHL) are practical options for the TPD drug development at the moment.
  • However, CRBN or VHL can not cover every target protein or cell type effectively.
  • Demands for novel E3Ls that could be the alternative or superior options to CRBN, VHL have been increasing.
  • We believe that a company securing a competitive novel E3L platform will hold future hegemony in the TPD field.

What is potential benefits of the novel E3L platform?

Make therapeutic breakthrough
Tackle certain targets or cell types where CRBN, VHL can't effectively or essentially work+Overcome drawbacks of typical degrader or therapy in certain indications or diseases
Expedite pipeline development
Expand degrader pipelines by applying diverse warheads to the well-established novel E3L ligand (& validated linker)
Enhance patentability
Novel chemical structure of the novel E3L binder lends strong patentability & exclusivity to the degrader in which the binder is integrated.
Enable platform business
Generate constant revenue via licensing or sub-licensing of patents claiming novel E3L binder to third-parties.

Why novel E3L platform development is challenging?

  • Novel E3Ls has not been sufficiently explored before the rise of TPD science : Lack of biological or structural studies for the novel E3Ls hinders novel E3L platform development.
  • Most novel E3Ls have no previously developed ligands or inhibitors and therefore it needs to put massive efforts to discover novel ligand for a certain novel E3L to be employed in degrader compounds.

"We have established th full value chain of capabilities required of in-house development of novel E3L platform."

  • UPPGRADER™ and UPPBEAT™, our key catalyst platforms, have been integrated into the path of development.

"We develop novel E3L platforms with distinct features and a robustscientific rationale, each of which has a potential to be superior to CRBN, VHL in a specific aspect"

"We have established th full value chaing of capabilities required ofr in-house development of novel E3L platform."

  • UPPGRADER™ and UPPBEAT™, our key catalyst platforms, have been integrated into the path of development.

"We develop novel E3L platforms with distinct features and a robustscientific rationale, each of which has a potential to be superior to CRBN, VHL in a specific aspect"

Novel E3L platform

  • Project
  • Novel E3L overview
  • Target ID
  • Novel binder
    Screening
  • Novel binder
    Hit
  • Hit opt. &
    PROTAC PoC
  • Initial platform
UP1011Cancer expressing +
blood cell low expressing novel Novel E3L
UP1013Next generation universal Novel E3L
UP1014Immune cell overexpressing Novel E3L