1
40
2
-
Text
A resource consisting primarily of words for reading. Examples include books, letters, dissertations, poems, newspapers, articles, archives of mailing lists. Note that facsimiles or images of texts are still of the genre Text.
URL Address
<a href="http://doi.org/10.1021/ml200196p" target="_blank" rel="noreferrer noopener">http://doi.org/10.1021/ml200196p</a>
Rights
Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
Pages
39-42
Issue
1
Volume
3
Search for Full-text
Locate full-text within NEOMED Library's e-journal collections
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Dublin Core
The Dublin Core metadata element set is common to all Omeka records, including items, files, and collections. For more information see, http://dublincore.org/documents/dces/.
Title
A name given to the resource
Molecular Insights Into Human Monoamine Oxidase B Inhibition By The Glitazone Antidiabetes Drugs
Publisher
An entity responsible for making the resource available
Acs Medicinal Chemistry Letters
Date
A point or period of time associated with an event in the lifecycle of the resource
2012
2012-01
Subject
The topic of the resource
Antidiabetes drug; Chemistry; drug design; gamma agonist pioglitazone; high-level expression; lsd1; monoamine oxidase; mouse model; neurodegeneration; neuroprotection; parkinsons-disease; parkinsons-disease; Pharmacology & Pharmacy; pichia-pastoris; pioglitazone; rosiglitazone
Creator
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Binda C; Aldeco M; Geldenhuys W J; Tortorici M; Mattevi A; Edmondson D E
Description
An account of the resource
The widely employed antidiabetic drug pioglitazone (Actos) is shown to be a specific and reversible inhibitor of human monoamine oxidase B (MAO B). The crystal structure of the enzyme-inhibitor complex shows that the R-enantiomer is bound with the thiazolidinedione ring near the flavin. The molecule occupies both substrate and entrance cavities of the active site, establishing noncovalent interactions with the surrounding amino acids. These binding properties differentiate pioglitazone from the clinically used MAO inhibitors, which act through covalent inhibition mechanisms and do not exhibit a high degree of MAO A versus B selectivity. Rosiglitazone (Avandia) and troglitazone, other members of the glitazone class, are less selective in that they are weaker inhibitors of both MAO A and MAO B. These results suggest that pioglitazone may have utility as a "repurposed" neuroprotectant drug in retarding the progression of disease in Parkinson's patients. They also provide new insights for the development of reversible isoenzyme-specific MAO inhibitors.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1021/ml200196p" target="_blank" rel="noreferrer noopener">10.1021/ml200196p</a>
Format
The file format, physical medium, or dimensions of the resource
Journal Article or Conference Abstract Publication
2012
Acs Medicinal Chemistry Letters
Aldeco M
Antidiabetes drug
Binda C
Chemistry
Drug Design
Edmondson D E
gamma agonist pioglitazone
Geldenhuys W J
high-level expression
Journal Article or Conference Abstract Publication
lsd1
Mattevi A
monoamine oxidase
Mouse model
Neurodegeneration
Neuroprotection
parkinsons-disease
Pharmacology & Pharmacy
pichia-pastoris
pioglitazone
Rosiglitazone
Tortorici M
-
Text
A resource consisting primarily of words for reading. Examples include books, letters, dissertations, poems, newspapers, articles, archives of mailing lists. Note that facsimiles or images of texts are still of the genre Text.
URL Address
<a href="http://doi.org/10.1021/ml200196p" target="_blank" rel="noreferrer noopener">http://doi.org/10.1021/ml200196p</a>
Rights
Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
Pages
39-42
Issue
1
Volume
3
Search for Full-text
Locate full-text within NEOMED Library's e-journal collections
<p>Users with a NEOMED Library login can search for full-text journal articles at the following url: <a href="https://libraryguides.neomed.edu/home">https://libraryguides.neomed.edu/home</a></p>
Dublin Core
The Dublin Core metadata element set is common to all Omeka records, including items, files, and collections. For more information see, http://dublincore.org/documents/dces/.
Title
A name given to the resource
Molecular Insights Into Human Monoamine Oxidase B Inhibition By The Glitazone Antidiabetes Drugs
Publisher
An entity responsible for making the resource available
Acs Medicinal Chemistry Letters
Date
A point or period of time associated with an event in the lifecycle of the resource
2012
2012-01
Subject
The topic of the resource
Antidiabetes drug; Chemistry; drug design; gamma agonist pioglitazone; high-level expression; lsd1; monoamine oxidase; mouse model; neurodegeneration; neuroprotection; parkinsons-disease; parkinsons-disease; Pharmacology & Pharmacy; pichia-pastoris; pioglitazone; rosiglitazone
Creator
An entity primarily responsible for making the resource
Binda C; Aldeco M; Geldenhuys W J; Tortorici M; Mattevi A; Edmondson D E
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1021/ml200196p" target="_blank" rel="noreferrer noopener">10.1021/ml200196p</a>
Format
The file format, physical medium, or dimensions of the resource
Journal Article or Conference Abstract Publication
2012
Acs Medicinal Chemistry Letters
Aldeco M
Antidiabetes drug
Binda C
Chemistry
Drug Design
Edmondson D E
gamma agonist pioglitazone
Geldenhuys W J
high-level expression
lsd1
Mattevi A
monoamine oxidase
Mouse model
Neurodegeneration
Neuroprotection
parkinsons-disease
Pharmacology & Pharmacy
pichia-pastoris
pioglitazone
Rosiglitazone
Tortorici M