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Antimicrobial Agents and Chemotherapy, July 2002, p. 2279-2283, Vol. 46, No. 7
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.7.2279-2283.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

Structure-Function Relationship Studies on the Frog Skin Antimicrobial Peptide Tigerinin 1: Design of Analogs with Improved Activity and Their Action on Clinical Bacterial Isolates

Narasimhaiah Sitaram,^1* Korrapati Purna Sai,¹ Shashi Singh,¹ Krishnan Sankaran,² and Ramakrishnan Nagaraj^1*

Center for Cellular and Molecular Biology, Hyderabad 500 007,¹ Center for Biotechnology, Anna University, Chennai 600 025, India²

Received 9 October 2001/ Returned for modification 26 February 2002/ Accepted 2 April 2002

Structure-function relationships in antimicrobial peptides have been extensively investigated in order to obtain improved analogs. Most of these studies have targeted either -helical peptides or ß-sheet peptides with multiple disulfide bridges. Tigerinins are short, nonhelical antimicrobial peptides with a single disulfide bridge. In this study, we have synthesized several analogs of tigerinin 1 with an aim to understand the structural basis of activity as well as improve its activity. The studies demonstrate that the loop structure of tigerinin 1 is essential for its optimal activity. However, linearization with increased cationic charges can compensate for loss of loop structure to some extent. Morphology of the cells after treatment with the active analogs shows extensive leakage of cytoplasmic contents. Tigerinin 1 and two of its analogs exhibit impressive activity against a variety of clinical bacterial isolates.

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* Corresponding author. Mailing address: Centre for Cellular and Molecular Biology, Uppal Road, Hyderabad 500 007, India. Phone: 91-40-7160222. Fax: 91-40-7160591. E-mail: sitaram{at}gene.ccmbindia.org.

* Corresponding author. Mailing address: Centre for Cellular and Molecular Biology, Uppal Road, Hyderabad 500 007, India. Phone: 91-40-7160222. Fax: 91-40-7160591. E-mail: nraj{at}gene.ccmbindia.org.

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Antimicrobial Agents and Chemotherapy, July 2002, p. 2279-2283, Vol. 46, No. 7
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.7.2279-2283.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

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