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Design, Synthesis, and Evaluation of New Tripeptides as COX-2 Inhibitors
Joint Authors
Bertamino, Alessia
Alcaro, Stefano
Vernieri, Ermelinda
Grieco, Paolo
Gomez-Monterrey, Isabel
Novellino, Ettore
Sala, Marina
Musella, Simona
Milite, Ciro
Campiglia, Pietro
Artese, Anna
Scognamiglio, Ilaria
Ortuso, Francesco
Source
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-7, 7 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-02-26
Country of Publication
Egypt
No. of Pages
7
Main Subjects
Abstract EN
Cyclooxygenase (COX) is a key enzyme in the biosynthetic pathway leading to the formation of prostaglandins, which are mediators of inflammation.
It exists mainly in two isoforms COX-1 and COX-2.
The conventional nonsteroidal anti-inflammatory drugs (NSAIDs) have gastrointestinal side effects because they inhibit both isoforms.
Recent data demonstrate that the overexpression of these enzymes, and in particular of cyclooxygenases-2, promotes multiple events involved in tumorigenesis; in addition, numerous studies show that the inhibition of cyclooxygenases-2 can delay or prevent certain forms of cancer.
Agents that inhibit COX-2 while sparing COX-1 represent a new attractive therapeutic development and offer a new perspective for a further use of COX-2 inhibitors.
The present study extends the evaluation of the COX activity to all 203 possible natural tripeptide sequences following a rational approach consisting in molecular modeling, synthesis, and biological tests.
Based on data obtained from virtual screening, only those peptides with better profile of affinity have been selected and classified into two groups called S and E.
Our results suggest that these novel compounds may have potential as structural templates for the design and subsequent development of the new selective COX-2 inhibitors drugs.
American Psychological Association (APA)
Vernieri, Ermelinda& Gomez-Monterrey, Isabel& Milite, Ciro& Grieco, Paolo& Musella, Simona& Bertamino, Alessia…[et al.]. 2013. Design, Synthesis, and Evaluation of New Tripeptides as COX-2 Inhibitors. Journal of Amino Acids،Vol. 2013, no. 2013, pp.1-7.
https://search.emarefa.net/detail/BIM-484554
Modern Language Association (MLA)
Vernieri, Ermelinda…[et al.]. Design, Synthesis, and Evaluation of New Tripeptides as COX-2 Inhibitors. Journal of Amino Acids No. 2013 (2013), pp.1-7.
https://search.emarefa.net/detail/BIM-484554
American Medical Association (AMA)
Vernieri, Ermelinda& Gomez-Monterrey, Isabel& Milite, Ciro& Grieco, Paolo& Musella, Simona& Bertamino, Alessia…[et al.]. Design, Synthesis, and Evaluation of New Tripeptides as COX-2 Inhibitors. Journal of Amino Acids. 2013. Vol. 2013, no. 2013, pp.1-7.
https://search.emarefa.net/detail/BIM-484554
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-484554