Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Gherbovet, O; Sánchez-Murcia, PA; García Alvarez, MC; Bignon, J; Thoret, S; Gago, F; Roussi, F.
Synthesis and evaluation of hybrid molecules targeting the vinca domain of tubulin.
Org Biomol Chem. 2015; 13(10):3144-3154
Doi: 10.1039/c4ob02114b
Web of Science
PubMed
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- Co-Autor*innen der Med Uni Graz
- Sánchez Murcia Pedro Alejandro
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- Abstract:
- Some hybrids of vinca alkaloids and phomopsin A, linked by a glycine pattern, have been synthesized in one or two steps, by an insertion reaction and shown to inhibit microtubule assembly. These compounds have been elaborated in order to interact with both the "vinca site" and the "peptide site" of the vinca domain in tubulin. Two out of three hybrids are potent inhibitors of microtubules assembly and they present good cytotoxicity against different cell lines. Molecular modelling studies show that they could bind, within the vinca domain, in similar spatial regions as those of vinca and phomopsin thanks to the flexibility provided by the glycine linker used to elaborate these hybrids.
- Find related publications in this database (using NLM MeSH Indexing)
- Alkaloids - chemistry
- Apoptosis -
- Binding Sites -
- Cell Line -
- Glycine - chemistry
- Guanosine Triphosphate - chemistry
- Humans -
- K562 Cells -
- Microtubules - metabolism
- Models, Molecular -
- Mycotoxins - chemical synthesis
- Mycotoxins - chemistry
- Peptides - chemistry
- Protein Structure, Tertiary -
- Signal Transduction -
- Tubulin - chemistry
- Vinblastine - analogs & derivatives
- Vinblastine - chemistry
- Vinca Alkaloids - chemical synthesis
- Vinca Alkaloids - chemistry
- Vinorelbine -