Polyketides as leads
Polyketides represent a huge and underexploited drug discovery resource
Polyketides have numerous benefits as drug leads:
- validated yet neglected compound class
- human biology-rich with high affinity for biologically relevant targets
- ability to address traditionally difficult targets such as protein-protein interactions
- naturally drug-like
- commercial exclusivity through know-how and IP
Validated yet neglected class
There are nearly 50 approved polyketide therapeutics, but thousands of known polyketides that have never been fully characterised. All were identified by their biological activity but have not been considered as drug leads because they are difficult for others to optimise.
Human-biology rich
Polyketides evolved to bind biologically relevant targets, and are high-content chemistry rich with activity relevant to human disease. Their large size and complex structure may make them especially suitable for targets such as protein-protein interactions, and they bind to protein targets with little loss of entropy.
Naturally drug-like
Polyketides can be of high molecular weight and complex structure, with multiple chiral centres, but they tend to have well balanced conformational pre-organisation and flexibility. They are often bioavailable because of their ability to adopt different conformations in aqueous and lipophilic environments.
Commercial exclusivity
The novoPT™ technology provides unique access to novel chemistries not seen in natural polyketides and unachievable through semi-synthesis. Biotica’s IP and know-how adds a layer of exclusivity on top of composition-of-matter patents.
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Links to papers describing novoPT™ and its applications
