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Self-Association of Okadaic Acid: Structural and Pharmacological Significance

Okadaic acid (OA) has been an invaluable pharmacological tool in the study of cellular signaling. The great affinity of this polyether for its targets together with its high specificity to inhibit certain protein phosphatases enables the differential study of these proteins. Crystallographic structu...

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Autores principales: Cruz, Patricia G., Norte, Manuel, Hernández Creus, Alberto, Fernández, José J., Hernández Daranas, Antonio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3721210/
https://www.ncbi.nlm.nih.gov/pubmed/23760016
http://dx.doi.org/10.3390/md11061866
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author Cruz, Patricia G.
Norte, Manuel
Hernández Creus, Alberto
Fernández, José J.
Hernández Daranas, Antonio
author_facet Cruz, Patricia G.
Norte, Manuel
Hernández Creus, Alberto
Fernández, José J.
Hernández Daranas, Antonio
author_sort Cruz, Patricia G.
collection PubMed
description Okadaic acid (OA) has been an invaluable pharmacological tool in the study of cellular signaling. The great affinity of this polyether for its targets together with its high specificity to inhibit certain protein phosphatases enables the differential study of these proteins. Crystallographic structures of protein phosphatases in complex with OA show a 1:1 protein to toxin ratio. Nevertheless, it has been found that OA is able to self-associate under certain conditions although very little is known about the importance of this phenomenon. Here we review the available knowledge on the latter topic and we report on the existence of an unusual self-associated tetrameric form. The structure of these oligomers is proposed based on spectroscopic data and molecular modeling calculations.
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spelling pubmed-37212102013-07-24 Self-Association of Okadaic Acid: Structural and Pharmacological Significance Cruz, Patricia G. Norte, Manuel Hernández Creus, Alberto Fernández, José J. Hernández Daranas, Antonio Mar Drugs Article Okadaic acid (OA) has been an invaluable pharmacological tool in the study of cellular signaling. The great affinity of this polyether for its targets together with its high specificity to inhibit certain protein phosphatases enables the differential study of these proteins. Crystallographic structures of protein phosphatases in complex with OA show a 1:1 protein to toxin ratio. Nevertheless, it has been found that OA is able to self-associate under certain conditions although very little is known about the importance of this phenomenon. Here we review the available knowledge on the latter topic and we report on the existence of an unusual self-associated tetrameric form. The structure of these oligomers is proposed based on spectroscopic data and molecular modeling calculations. MDPI 2013-05-29 /pmc/articles/PMC3721210/ /pubmed/23760016 http://dx.doi.org/10.3390/md11061866 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Cruz, Patricia G.
Norte, Manuel
Hernández Creus, Alberto
Fernández, José J.
Hernández Daranas, Antonio
Self-Association of Okadaic Acid: Structural and Pharmacological Significance
title Self-Association of Okadaic Acid: Structural and Pharmacological Significance
title_full Self-Association of Okadaic Acid: Structural and Pharmacological Significance
title_fullStr Self-Association of Okadaic Acid: Structural and Pharmacological Significance
title_full_unstemmed Self-Association of Okadaic Acid: Structural and Pharmacological Significance
title_short Self-Association of Okadaic Acid: Structural and Pharmacological Significance
title_sort self-association of okadaic acid: structural and pharmacological significance
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3721210/
https://www.ncbi.nlm.nih.gov/pubmed/23760016
http://dx.doi.org/10.3390/md11061866
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