Lead Optimization

c-Myc antagonist

A lead optimization program developing an antagonist of the intrinsically disordered transcription factor c-Myc, advanced with UCL Cancer Institute disease biology.

Target
c-Myc
Modality
Small molecule
Indication
MYC-driven solid tumors
Stage
Lead Optimization

Target

c-Myc is a transcription factor that is disordered outside of its complex with MAX and is deregulated across a broad range of cancers. Direct pharmacological control of c-Myc has been considered undruggable because it presents no classical binding pocket.

Approach

Peptone applies its Product Engine to characterise the conformational ensemble of c-Myc and to search for binders that disrupt its productive interactions. This extends the same disorder-first discovery work beyond aggregation targets into transcriptional biology.

Preclinical

Lead optimization work focuses on improving the emerging chemical series against defined disordered regions. Mechanism-of-action studies are advanced with Prof. Marc Mansour at UCL Cancer Institute in MYC-driven leukaemia and transcriptional models.

Development Plan

The program is in lead optimization, where chemical series are pressure-tested in disease models to support later candidate selection.

Collaborations

Peptone’s c-Myc antagonist program is advanced with UCL Cancer Institute and Prof. Marc Mansour. See Partnering and Collaborations on the pipeline page for detail.