Microwave-Assisted Synthesis of Antimicrobial Peptides.

Antimicrobial peptides (AMPs) are emerging as one of the unsurpassed therapeutic tools to treat various devastating diseases that are affecting millions of lives. Conventional synthesis of peptides requires longer times, and hence automated microwave technology could be regarded as an alternative implement which offers advantages like less reaction times and higher yields. In this sense, we herein describe a methodology to prepare AMPs through solid-phase peptide synthesis under microwave conditions. We have used LL37 as an example to discuss the synthetic protocol including the difficulties involved in the preparation of so-called long and difficult peptides and also remedial procedures to overcome these obstacles.

[1]  Carlos M. Marques,et al.  Fluorescent and Photosensitizing Conjugates of Cell-Penetrating Peptide TAT(47-57): Design, Microwave-Assisted Synthesis at 60 °C, and Properties , 2017, ACS omega.

[2]  K. Wehrstedt,et al.  Explosive properties of 1-hydroxybenzotriazoles. , 2005, Journal of hazardous materials.

[3]  Fernando Albericio,et al.  Optimized Microwave Assisted Synthesis of LL37, a Cathelicidin Human Antimicrobial Peptide , 2014, International Journal of Peptide Research and Therapeutics.

[4]  Leila Malik,et al.  Microwave Heating in Solid-Phase Peptide Synthesis , 2012 .

[5]  Fernando Albericio,et al.  Oxyma: an efficient additive for peptide synthesis to replace the benzotriazole-based HOBt and HOAt with a lower risk of explosion. , 2009, Chemistry.

[6]  David A. Phoenix,et al.  Antimicrobial Peptides: PHOENIX:ANTIMICROBIAL PE O-BK , 2013 .

[7]  Michal Lebl,et al.  Search for optimal coupling reagent in multiple peptide synthesizer. , 2006, Biopolymers.

[8]  G. Pirri,et al.  Antimicrobial peptides: an overview of a promising class of therapeutics , 2007, Central European Journal of Biology.

[9]  M. Mutter,et al.  Liquid Phase Synthesis of Peptides , 1972, Nature.

[10]  Ann Thayer,et al.  ISRAEL’S TEVA WILL ACQUIRE CEPHALON , 2011 .

[11]  A. Méndez-Vilas,et al.  Antimicrobial resistance in biofilms , 2012 .

[12]  Lynda F. Bonewald,et al.  Correlation of cleavage techniques with side-reactions following solid-phase peptide synthesis , 1995 .

[13]  Jonathan M. Collins,et al.  High-efficiency solid phase peptide synthesis (HE-SPPS). , 2014, Organic letters.

[14]  K. Sahayaraj,et al.  Science against microbial pathogens : communicating current research and technological advances , 2012 .

[15]  Fernando Albericio,et al.  Peptide synthesis beyond DMF: THF and ACN as excellent and friendlier alternatives. , 2015, Organic & biomolecular chemistry.

[16]  H. Won,et al.  Antimicrobial Peptides for Therapeutic Applications: A Review , 2012, Molecules.