On the Mechanism of Action of Dragmacidins I and J, Two New Representatives of a New Class of Protein Phosphatase 1 and 2A Inhibitors
| Autor: | Patricia G. Cruz, Carmen Cuevas, Marta Pérez, Juan Fernando Martinez Leal, Antonio Hernández Daranas |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Stereochemistry General Chemical Engineering 030106 microbiology Phosphatase Mitotic arrest Article lcsh:Chemistry 03 medical and health sciences medicine Structure–activity relationship Theory Metaphase Indole test Pharmacology Natural products Chemistry Protein phosphatase 1 General Chemistry Protein phosphatase 2 Structure-activity relationship 030104 developmental biology Mechanism of action lcsh:QD1-999 Molecular docking medicine.symptom Molecular structure |
| Zdroj: | ACS Omega, Vol 3, Iss 4, Pp 3760-3767 (2018) ACS Omega Digital.CSIC. Repositorio Institucional del CSIC instname |
| ISSN: | 2470-1343 |
| Popis: | Two new brominated bis(indole) alkaloids, dragmacidins I (1) and J (2), showing low micromolar cytostatic activity, along with three known congeners were isolated from the Tanzanian sponge Dragmacidon sp. and their structures determined by the analysis of their NMR and MS data. From the study of their mechanism of action, it can be concluded that the mitotic arrest at metaphase in treated tumor cells, mediated by inhibition of PP1 and/or PP2A phosphatases is involved in the observed antiproliferative activity. Differences in their bioactivities were rationalized, and a plausible binding mode is proposed on the basis of computational simulations. The Pemba Channel Fishing Club, Shimoni (Kenya), and the Ministry of Livestock and Fisheries, Department of Fisheries and Marine Resources Pemba (Tanzania). |
| Databáze: | OpenAIRE |
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