Structure-guided peptide optimization: From micromolar hits to nanomolar leads

Peptide optimization is rarely a matter of improving affinity alone. Every modification can change the peptide’s binding mode, conformational ensemble, selectivity and developability, while the most valuable design opportunities often lie in non-canonical amino acids, constrained topologies and chemical space that conventional sequence-based approaches explore only partially.

In this webinar, we will discuss how peptide optimization changes when the target structure becomes part of the design problem.

Tomi Sawyer, peptide discovery advisor to Receptor.AI and PDHC Founder, will discuss where conventional peptide optimization approaches reach their practical limits and why expanding beyond canonical sequence space matters. Semen Yesylevskyy, CSO of Receptor.AI, will present our structure-guided optimization framework, benchmark results, and a real discovery programme in which target-aware design advanced a micromolar-affinity starting point into nanomolar peptides.

Alan Nafiiev, CEO of Receptor.AI, will conclude with how discovery teams can apply and prospectively evaluate this approach in their own active peptide programmes.