Methods for the Peptide Synthesis and Analysis

• Published in: Peptide Chemistry and Drug Design pp. 11 - 73
• Main Authors: Tulla‐Puche, Judit, El‐Faham, Ayman, Galanis, Athanassios S, de Oliveira, Eliandre, Zompra, Aikaterini A, Albericio, Fernando
• Format: Book Chapter
• Language: English
• Published: United States John Wiley & Sons, Incorporated 2015; Wiley; John Wiley & Sons, Inc
• Subjects: knottins; membrane permeability; peptide therapeutics
• ISBN: 0470317612; 9780470317617
• DOI: 10.1002/9781118995303.ch2

The advent of molecular biology and the understanding of the physiological and pathological function of peptides, coupled with advances in synthetic methodologies and peptidomimetics marked the beginning of anew era in peptide and protein therapeutics, with the vision that there should be no limit to what can be produced as therapeutics. A number of factors have thus far limited the explosion that needs to happen in the peptide field. With the exception of a few peptides, the approved drugs so far target the extracellular compartment, and thus have to compete with biologics. The recent focus on another class of macrocycles, containing multiple disulfides has generated a lot of excitement in maintaining the stability and membrane permeability of the cyclotide Kalata B1, or the knottins in order to create potent peptide drugs. One of the greatest challenges in Drug Discovery is the safety of therapeutics.