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Undruggable cancer proteins such as beta-catenin, MYC and KRAS act through broad flat protein-protein interfaces that small pills cannot cover. Ring-shaped macrocyclic peptides can, some series are cell-permeable, and mRNA display can screen trillions of candidates; the proposal is a focused campaign with open publication of permeability rules.
Protein-protein interfaces are the defining feature of undruggable targets. Macrocycles occupy a chemical space between small molecules and biologics, with demonstrated cell permeability in some series, and mRNA display can screen trillions of candidates in a single tube. A focused campaign against a defined list of oncology interfaces (for example beta-catenin/TCF, MYC/MAX, KRAS/SOS) with open publication of permeability rules would advance both the targets and the modality.
Shares Generate:Biomedicines, Drugging the 'undruggable' cancer targets, The undruggable drivers.
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers.
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers.
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers.
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers.
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers.
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers.
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers, RAS / RAF / MEK / ERK (MAPK).
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