Peptide drug discovery has surpassed its first 100-year milestone and is now gaining traction as highly promising therapeutic modality for challenging targets and diseases. Historically, peptide and peptidomimetic drugs modulating receptor and protease targets have had significant clinical impact in metabolic disorders and infectious diseases. Over the past two decades a renaissance of peptide drug discovery has emerged with a focus on overcoming the hurdles of cellular permeability and delivery. Noteworthy, such R&D efforts have leveraged innovative strategies to advance novel macrocyclic peptide therapeutics exemplifying different structural chemotypes and biophysical properties. This presentation will address three core elements relevant of a third wave of peptide drug discovery: (i) engineering mindset; (ii) design rules; and (iii) screening tools. Representative case studies capturing the spirit of both the aforementioned core elements and focus on the hurdles of cellular permeability and delivery will be shared.<br/>

Peptide drug discovery <i>raison d'etre</i>: Engineering mindset, design rules and screening tools

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

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Peptide drug discovery raison d'etre: Engineering mindset, design rules and screening tools