Solid-phase synthesis of cell-penetrating γ-peptide/antimicrobial peptide conjugates and of cyclic lipodepsipeptides derived from fengycins
This thesis is focused on the development of synthetic approaches to obtain new bioactive peptides. The first part deals with the design of new antimicrobial peptide/cell-penetrating peptide conjugates as anticancer agents. Their conjugation enhanced the activity of the antimicrobial peptides agains...
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| Tipo de recurso: | tesis doctoral |
| Estado: | Versión publicada |
| Fecha de publicación: | 2016 |
| País: | España |
| Institución: | CBUC, CESCA |
| Repositorio: | TDR. Tesis Doctorales en Red |
| OAI Identifier: | oai:www.tdx.cat:10803/393895 |
| Acceso en línea: | http://hdl.handle.net/10803/393895 |
| Access Level: | acceso abierto |
| Palabra clave: | Cell-penetrating peptide CPP Anticancer peptide Pèptids anticancerígens Péptidos anticancerígenos Antimicrobial peptide Pèptids antimicrobians Péptidos antimicrobianos Fengycin Fengicina Depsipeptide Depsipèptid Depsipéptido Solid-phase synthesis Síntesi de fase sòlida Síntesis en fase sólida Bioactive peptides Pèptids bioactius Péptidos bioactivos 547 |
| Sumario: | This thesis is focused on the development of synthetic approaches to obtain new bioactive peptides. The first part deals with the design of new antimicrobial peptide/cell-penetrating peptide conjugates as anticancer agents. Their conjugation enhanced the activity of the antimicrobial peptides against cancer cells while maintained their low toxicity. These compounds are interesting for the design of new anticancer agents. On the second part, a new versatile methodology for the synthesis of natural fengycin derivatives is described. Our strategy represents the first synthetic approach for the total solid-phase synthesis of these cyclic lipodepsipeptides and can be easily adapted to obtain a wide range of analogues. |
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