NDLI: Poly-lysine peptidomimetics having potent antimicrobial activity without hemolytic activity

Content Provider	Springer Nature Link
Author	Ahn, Mija Jacob, Binu Gunasekaran, Pethaiah Murugan, Ravichandran N. Ryu, Eun Kyoung Lee, Ga hyang Hyun, Jae Kyung Cheong, Chaejoon Kim, Nam Hyung Shin, Song Yub Bang, Jeong Kyu
Copyright Year	2014
Abstract	Diversity of sequence and structure in naturally occurring antimicrobial peptides (AMPs) limits their intensive structure–activity relationship (SAR) study. In contrast, peptidomimetics have several advantages compared to naturally occurring peptide in terms of simple structure, convenient to analog synthesis, rapid elucidation of optimal physiochemical properties and low-cost synthesis. In search of short antimicrobial peptides using peptidomimetics, which provide facile access to identify the key factors involving in the destruction of pathogens through SAR study, a series of simple and short peptidomimetics consisting of multi-Lys residues and lipophilic moiety have been prepared and found to be active against several Gram-negative and Gram-positive bacteria containing methicillin-resistant Staphylococcus aureus (MRSA) without hemolytic activity. Based on the SAR studies, we found that hydrophobicity, +5 charges of multiple Lys residues, hydrocarbon tail lengths and cyclohexyl group were crucial for antimicrobial activity. Furthermore, membrane depolarization, dye leakage, inner membrane permeability and time-killing kinetics revealed that bacterial-killing mechanism of our peptidomimetics is different from the membrane-targeting AMPs (e. g. melittin and SMAP-29) and implied our peptidomimetics might kill bacteria via the intracellular-targeting mechanism as done by buforin-2.
Starting Page	2259
Ending Page	2269
Page Count	11
File Format	PDF
ISSN	09394451
Journal	Amino Acids
Volume Number	46
Issue Number	9
e-ISSN	14382199
Language	English
Publisher	Springer Vienna
Publisher Date	2014-06-25
Publisher Place	Vienna
Access Restriction	Subscribed
Subject Keyword	Short peptidomimetics Antimicrobial activity Hemolytic activity Structure–activity relationship (SAR) study Poly-Lys peptidomimetics Biochemistry Analytical Chemistry Biochemical Engineering Life Sciences Proteomics Neurobiology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Biochemistry Clinical Biochemistry

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1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
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