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Mar. Drugs 2014, 12(1), 317-351; doi:10.3390/md12010317

Thiopeptide Antibiotics: Retrospective and Recent Advances

1 Institute for Research in Biomedicine, Barcelona Science Park-University of Barcelona, Baldiri Reixac 10, Barcelona 08028, Spain 2 CIBER-BBN, Networking Centre on Bioengineering Biomaterials and Nanomedicine, Barcelona 08028, Spain 3 Department of Organic Chemistry, University of Barcelona, Barcelona 08028, Spain 4 School of Chemistry and Physics, University of KwaZulu-Natal, 4000-Durban, South Africa 5 Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, Barcelona 08028, Spain
* Author to whom correspondence should be addressed.
Received: 27 November 2013 / Revised: 13 December 2013 / Accepted: 16 December 2013 / Published: 17 January 2014


Thiopeptides, or thiazolyl peptides, are a relatively new family of antibiotics that already counts with more than one hundred different entities. Although they are mainly isolated from soil bacteria, during the last decade, new members have been isolated from marine samples. Far from being limited to their innate antibacterial activity, thiopeptides have been found to possess a wide range of biological properties, including anticancer, antiplasmodial, immunosuppressive, etc. In spite of their ribosomal origin, these highly posttranslationally processed peptides have posed a fascinating synthetic challenge, prompting the development of various methodologies and strategies. Regardless of their limited solubility, intensive investigations are bringing thiopeptide derivatives closer to the clinic, where they are likely to show their veritable therapeutic potential.
Keywords: thiopeptides; antibiotics; natural products; peptides; heterocycles; thiazole; oxazole; dehydroamino acids; pyridine thiopeptides; antibiotics; natural products; peptides; heterocycles; thiazole; oxazole; dehydroamino acids; pyridine
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Just-Baringo, X.; Albericio, F.; Álvarez, M. Thiopeptide Antibiotics: Retrospective and Recent Advances. Mar. Drugs 2014, 12, 317-351.

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