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Probing the Surface of Human Carbonic Anhydrase for Clues towards the Design of Isoform Specific Inhibitors
Joint Authors
Pinard, Melissa A.
Mahon, Brian
McKenna, Robert
Source
Issue
Vol. 2015, Issue 2015 (31 Dec. 2015), pp.1-15, 15 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2015-02-24
Country of Publication
Egypt
No. of Pages
15
Main Subjects
Abstract EN
The alpha carbonic anhydrases (α-CAs) are a group of structurally related zinc metalloenzymes that catalyze the reversible hydration of CO2 to HCO 3 - .
Humans have 15 different α-CAs with numerous physiological roles and expression patterns.
Of these, 12 are catalytically active, and abnormal expression and activities are linked with various diseases, including glaucoma and cancer.
Hence there is a need for CA isoform specific inhibitors to avoid off-target CA inhibition, but due to the high amino acid conservation of the active site and surrounding regions between each enzyme, this has proven difficult.
However, residues towards the exit of the active site are variable and can be exploited to design isoform selective inhibitors.
Here we discuss and characterize this region of “selective drug targetability” and how these observations can be utilized to develop isoform selective CA inhibitors.
American Psychological Association (APA)
Pinard, Melissa A.& Mahon, Brian& McKenna, Robert. 2015. Probing the Surface of Human Carbonic Anhydrase for Clues towards the Design of Isoform Specific Inhibitors. BioMed Research International،Vol. 2015, no. 2015, pp.1-15.
https://search.emarefa.net/detail/BIM-1055519
Modern Language Association (MLA)
Pinard, Melissa A.…[et al.]. Probing the Surface of Human Carbonic Anhydrase for Clues towards the Design of Isoform Specific Inhibitors. BioMed Research International No. 2015 (2015), pp.1-15.
https://search.emarefa.net/detail/BIM-1055519
American Medical Association (AMA)
Pinard, Melissa A.& Mahon, Brian& McKenna, Robert. Probing the Surface of Human Carbonic Anhydrase for Clues towards the Design of Isoform Specific Inhibitors. BioMed Research International. 2015. Vol. 2015, no. 2015, pp.1-15.
https://search.emarefa.net/detail/BIM-1055519
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1055519