Induced proximity approaches are emerging as powerful modalities in drug discovery. While the field has largely been driven by targeted protein degradation - particularly proteolysis targeting chimeras (PROTACs) and molecular glue degraders - new strategies are expanding this concept. Among them, transcriptional and epigenetic chemical inducers of proximity (TCIPs) aim to reprogram gene expression rather than eliminate proteins, offering complementary gain-of-function approaches to traditional degraders.
In this presentation, I will highlight recent work from my laboratory on induced proximity strategies targeting epigenetic regulators of transcription. First, I will discuss natural product–inspired PROTACs that recruit the underexplored E3 ligase KEAP1 to degrade transcriptional regulators such as BRD4 and CDK9. Second, I will present the development of bifunctional molecules that reprogram the transcriptional repressor BCL6 to reactivate apoptotic gene expression in diffuse large B-cell lymphoma.
Contact
Institut für Biochemie
Felix-Hausdorff-Straße 4, 17489 Greifswald
Telefon +49 3834 420 4356
michael.lammersuni-greifswaldde