Antibiotic activity of Leu-Lys rich model peptides
To develop novel antibiotic peptides useful as therapeutic drugs, short model peptides rich in Leu and Lys were designed by changing not only the net positive charge by Lys-deletion but also in the hydrophobic helix region by Leu-deletion from a peptide analogue of cecropin A (1-8)-magainin 2 (1-12)...
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Veröffentlicht in: | Biotechnology letters 2003-08, Vol.25 (16), p.1305-1310 |
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creator | Park, Yoonkyung Lee, Dong Gun Hahm, Kyung-Soo |
description | To develop novel antibiotic peptides useful as therapeutic drugs, short model peptides rich in Leu and Lys were designed by changing not only the net positive charge by Lys-deletion but also in the hydrophobic helix region by Leu-deletion from a peptide analogue of cecropin A (1-8)-magainin 2 (1-12) (CA-MA) known as P5. In particular, one peptide (P6), which was obtained by deleting Lys residues (positions 1, 3, 5, 9, 10, 13, 14) and Leu residues (positions 4, 7, 8, 11, 12, 15) and keeping Pro (position 6) and Trp (position 2), showed a strong antimicrobial and antitumor activity at 0.2-3.1 microM without hemolytic activity against human erythrocyte cells. Furthermore, P6 causes significant morphological alterations of the bacterial surfaces at 3.1 microM as shown by scanning electron microscopy. |
doi_str_mv | 10.1023/A:1024995105208 |
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In particular, one peptide (P6), which was obtained by deleting Lys residues (positions 1, 3, 5, 9, 10, 13, 14) and Leu residues (positions 4, 7, 8, 11, 12, 15) and keeping Pro (position 6) and Trp (position 2), showed a strong antimicrobial and antitumor activity at 0.2-3.1 microM without hemolytic activity against human erythrocyte cells. Furthermore, P6 causes significant morphological alterations of the bacterial surfaces at 3.1 microM as shown by scanning electron microscopy.</description><identifier>ISSN: 0141-5492</identifier><identifier>EISSN: 1573-6776</identifier><identifier>DOI: 10.1023/A:1024995105208</identifier><identifier>PMID: 14514057</identifier><language>eng</language><publisher>Netherlands: Springer Nature B.V</publisher><subject>Anti-Bacterial Agents - chemical synthesis ; Anti-Bacterial Agents - pharmacology ; Anti-Infective Agents - chemical synthesis ; Anti-Infective Agents - pharmacology ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - pharmacology ; Bacteria - drug effects ; Bacteria - ultrastructure ; Cell Line, Tumor - drug effects ; Cell Survival - drug effects ; Dose-Response Relationship, Drug ; Drug Design ; Drug Screening Assays, Antitumor ; Erythrocytes ; Erythrocytes - drug effects ; Fungi - drug effects ; Hemolysis - drug effects ; Humans ; Leucine - chemistry ; Leucine - pharmacology ; Lysine - chemistry ; Lysine - pharmacology ; Microbial Sensitivity Tests ; Neoplasms - drug therapy ; Peptide Fragments ; Peptides ; Proteins ; Scanning electron microscopy</subject><ispartof>Biotechnology letters, 2003-08, Vol.25 (16), p.1305-1310</ispartof><rights>Kluwer Academic Publishers 2003</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c348t-15b75878c69a6314714136c41b63d78f5487fcd49174aa368901daf761ca91733</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27903,27904</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/14514057$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Park, Yoonkyung</creatorcontrib><creatorcontrib>Lee, Dong Gun</creatorcontrib><creatorcontrib>Hahm, Kyung-Soo</creatorcontrib><title>Antibiotic activity of Leu-Lys rich model peptides</title><title>Biotechnology letters</title><addtitle>Biotechnol Lett</addtitle><description>To develop novel antibiotic peptides useful as therapeutic drugs, short model peptides rich in Leu and Lys were designed by changing not only the net positive charge by Lys-deletion but also in the hydrophobic helix region by Leu-deletion from a peptide analogue of cecropin A (1-8)-magainin 2 (1-12) (CA-MA) known as P5. 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Furthermore, P6 causes significant morphological alterations of the bacterial surfaces at 3.1 microM as shown by scanning electron microscopy.</description><subject>Anti-Bacterial Agents - chemical synthesis</subject><subject>Anti-Bacterial Agents - pharmacology</subject><subject>Anti-Infective Agents - chemical synthesis</subject><subject>Anti-Infective Agents - pharmacology</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Bacteria - drug effects</subject><subject>Bacteria - ultrastructure</subject><subject>Cell Line, Tumor - drug effects</subject><subject>Cell Survival - drug effects</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Design</subject><subject>Drug Screening Assays, Antitumor</subject><subject>Erythrocytes</subject><subject>Erythrocytes - drug effects</subject><subject>Fungi - drug effects</subject><subject>Hemolysis - drug effects</subject><subject>Humans</subject><subject>Leucine - chemistry</subject><subject>Leucine - pharmacology</subject><subject>Lysine - chemistry</subject><subject>Lysine - pharmacology</subject><subject>Microbial Sensitivity Tests</subject><subject>Neoplasms - drug therapy</subject><subject>Peptide Fragments</subject><subject>Peptides</subject><subject>Proteins</subject><subject>Scanning electron microscopy</subject><issn>0141-5492</issn><issn>1573-6776</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNqF0E1LxDAQBuAgiruunr1J8eCtmsnXJN6WxS8oeNFzSdMUs7Tb2qTC_nsLrhcvnl4YHoZ3hpBLoLdAGb9b388hjJFAJaP6iCxBIs8VojomSwoCcikMW5CzGLeUUoMUT8kChARBJS4JW-9SqEKfgsusS-ErpH3WN1nhp7zYx2wM7iPr-tq32eCHFGofz8lJY9voLw65Iu-PD2-b57x4fXrZrIvccaFTDrJCqVE7ZaziIHAuw5UTUCleo26k0Ni4WhhAYS1X2lCobYMKnJ1nnK_Izc_eYew_Jx9T2YXofNvane-nWKJEYELSfyFoIwXVMMPrP3DbT-NuPqLEuTNjWugZXR3QVHW-LocxdHbcl78_49_VCGot</recordid><startdate>20030801</startdate><enddate>20030801</enddate><creator>Park, Yoonkyung</creator><creator>Lee, Dong Gun</creator><creator>Hahm, Kyung-Soo</creator><general>Springer Nature B.V</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>3V.</scope><scope>7QL</scope><scope>7QR</scope><scope>7T7</scope><scope>7TB</scope><scope>7U5</scope><scope>7X7</scope><scope>7XB</scope><scope>88A</scope><scope>88E</scope><scope>88I</scope><scope>8AO</scope><scope>8FD</scope><scope>8FE</scope><scope>8FG</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABJCF</scope><scope>ABUWG</scope><scope>AEUYN</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>BHPHI</scope><scope>C1K</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FR3</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>L6V</scope><scope>L7M</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M2P</scope><scope>M7N</scope><scope>M7P</scope><scope>M7S</scope><scope>P64</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PTHSS</scope><scope>Q9U</scope><scope>7QO</scope><scope>7X8</scope></search><sort><creationdate>20030801</creationdate><title>Antibiotic activity of Leu-Lys rich model peptides</title><author>Park, Yoonkyung ; Lee, Dong Gun ; Hahm, Kyung-Soo</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c348t-15b75878c69a6314714136c41b63d78f5487fcd49174aa368901daf761ca91733</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>Anti-Bacterial Agents - 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Academic</collection><jtitle>Biotechnology letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Park, Yoonkyung</au><au>Lee, Dong Gun</au><au>Hahm, Kyung-Soo</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antibiotic activity of Leu-Lys rich model peptides</atitle><jtitle>Biotechnology letters</jtitle><addtitle>Biotechnol Lett</addtitle><date>2003-08-01</date><risdate>2003</risdate><volume>25</volume><issue>16</issue><spage>1305</spage><epage>1310</epage><pages>1305-1310</pages><issn>0141-5492</issn><eissn>1573-6776</eissn><abstract>To develop novel antibiotic peptides useful as therapeutic drugs, short model peptides rich in Leu and Lys were designed by changing not only the net positive charge by Lys-deletion but also in the hydrophobic helix region by Leu-deletion from a peptide analogue of cecropin A (1-8)-magainin 2 (1-12) (CA-MA) known as P5. In particular, one peptide (P6), which was obtained by deleting Lys residues (positions 1, 3, 5, 9, 10, 13, 14) and Leu residues (positions 4, 7, 8, 11, 12, 15) and keeping Pro (position 6) and Trp (position 2), showed a strong antimicrobial and antitumor activity at 0.2-3.1 microM without hemolytic activity against human erythrocyte cells. Furthermore, P6 causes significant morphological alterations of the bacterial surfaces at 3.1 microM as shown by scanning electron microscopy.</abstract><cop>Netherlands</cop><pub>Springer Nature B.V</pub><pmid>14514057</pmid><doi>10.1023/A:1024995105208</doi><tpages>6</tpages></addata></record> |
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subjects | Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - pharmacology Anti-Infective Agents - chemical synthesis Anti-Infective Agents - pharmacology Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Bacteria - drug effects Bacteria - ultrastructure Cell Line, Tumor - drug effects Cell Survival - drug effects Dose-Response Relationship, Drug Drug Design Drug Screening Assays, Antitumor Erythrocytes Erythrocytes - drug effects Fungi - drug effects Hemolysis - drug effects Humans Leucine - chemistry Leucine - pharmacology Lysine - chemistry Lysine - pharmacology Microbial Sensitivity Tests Neoplasms - drug therapy Peptide Fragments Peptides Proteins Scanning electron microscopy |
title | Antibiotic activity of Leu-Lys rich model peptides |
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