Academic Journal
Properties and structure-activity studies of cyclic beta-hairpin peptidomimetics based on the cationic antimicrobial peptide protegrin I
| العنوان: | Properties and structure-activity studies of cyclic beta-hairpin peptidomimetics based on the cationic antimicrobial peptide protegrin I |
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| المؤلفون: | Robinson, J A, Shankaramma, S C, Jetter, P, Kienzl, U, Schwendener, R, Vrijbloed, J W, Obrecht, D |
| المصدر: | Robinson, J A; Shankaramma, S C; Jetter, P; Kienzl, U; Schwendener, R; Vrijbloed, J W; Obrecht, D (2005). Properties and structure-activity studies of cyclic beta-hairpin peptidomimetics based on the cationic antimicrobial peptide protegrin I. Bioorganic & Medicinal Chemistry, 13(6):2055-2064. |
| بيانات النشر: | Elsevier |
| سنة النشر: | 2005 |
| المجموعة: | University of Zurich (UZH): ZORA (Zurich Open Repository and Archive |
| مصطلحات موضوعية: | Institute of Molecular Cancer Research, 570 Life sciences, biology |
| الوصف: | The properties and structure-activity relationships (SAR) of a macrocyclic analogue of porcine protegrin I (PG-I) have been investigated. The lead compound, having the sequence cyclo-(-Leu-Arg-Leu-Lys-Lys-Arg-Arg-Trp-Lys-Tyr-Arg-Val-d-Pro-Pro-), shows antimicrobial activity against Gram-positive and -negative bacteria, but a much lower haemolytic activity and a much reduced ability to induce dye release from phosphatidylcholine/phosphatidylglycerol liposomes, when compared to PG-I. The enantiomeric form of the lead peptide shows comparable antimicrobial activity, a property shared with other cationic antimicrobial peptides acting on cell membranes. SAR studies involving the synthesis and biological profiling of over 100 single site substituted analogues, showed that the antimicrobial activity was tolerant to a large number of the substitutions tested. Some analogues showed slightly improved antimicrobial activities (2-4-fold lowering of MICs), whereas other substitutions caused large increases in haemolytic activity on human red blood cells. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 0968-0896 |
| Relation: | https://www.zora.uzh.ch/id/eprint/2968/10/Robinson_BioMedChem_2005V.pdf; info:pmid/15727859; urn:issn:0968-0896 |
| DOI: | 10.1016/j.bmc.2005.01.009 |
| الاتاحة: | https://www.zora.uzh.ch/id/eprint/2968/ https://www.zora.uzh.ch/id/eprint/2968/10/Robinson_BioMedChem_2005V.pdf https://doi.org/10.1016/j.bmc.2005.01.009 |
| Rights: | info:eu-repo/semantics/restrictedAccess |
| رقم الانضمام: | edsbas.7FD21F2A |
| قاعدة البيانات: | BASE |
| تدمد: | 09680896 |
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| DOI: | 10.1016/j.bmc.2005.01.009 |