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Natural Product Polyamines That Inhibit Human Carbonic Anhydrases
Joint Authors
Vullo, Daniela
Poulsen, Sally-Ann
Davis, Rohan A.
Supuran, Claudiu T.
Source
Issue
Vol. 2014, Issue 2014 (31 Dec. 2014), pp.1-6, 6 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2014-08-05
Country of Publication
Egypt
No. of Pages
6
Main Subjects
Abstract EN
Natural product compound collections have proven an effective way to access chemical diversity and recent findings have identified phenolic, coumarin, and polyamine natural products as atypical chemotypes that inhibit carbonic anhydrases (CAs).
CA enzymes are implicated as targets of variable drug therapeutic classes and the discovery of selective, drug-like CA inhibitors is essential.
Just two natural product polyamines, spermine and spermidine, have until now been investigated as CA inhibitors.
In this study, five more complex natural product polyamines 1–5, derived from either marine sponge or fungi, were considered for inhibition of six different human CA isozymes of interest in therapeutic drug development.
All compounds share a simple polyamine core fragment, either spermine or spermidine, yet display substantially different structure activity relationships for CA inhibition.
Notably, polyamines 1–5 were submicromolar inhibitors of the cancer drug target CA IX, this is more potent than either spermine or spermidine.
American Psychological Association (APA)
Davis, Rohan A.& Vullo, Daniela& Supuran, Claudiu T.& Poulsen, Sally-Ann. 2014. Natural Product Polyamines That Inhibit Human Carbonic Anhydrases. BioMed Research International،Vol. 2014, no. 2014, pp.1-6.
https://search.emarefa.net/detail/BIM-466994
Modern Language Association (MLA)
Davis, Rohan A.…[et al.]. Natural Product Polyamines That Inhibit Human Carbonic Anhydrases. BioMed Research International No. 2014 (2014), pp.1-6.
https://search.emarefa.net/detail/BIM-466994
American Medical Association (AMA)
Davis, Rohan A.& Vullo, Daniela& Supuran, Claudiu T.& Poulsen, Sally-Ann. Natural Product Polyamines That Inhibit Human Carbonic Anhydrases. BioMed Research International. 2014. Vol. 2014, no. 2014, pp.1-6.
https://search.emarefa.net/detail/BIM-466994
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-466994