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40
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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/10.1016/j.bmcl.2011.06.111" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2011.06.111</a>
Pages
5498–5501
Issue
18
Volume
21
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
A novel binding assay identifies high affinity ligands to the rosiglitazone binding site of mitoNEET.
Publisher
An entity responsible for making the resource available
Bioorganic & medicinal chemistry letters
Date
A point or period of time associated with an event in the lifecycle of the resource
2011
2011-09
Subject
The topic of the resource
Binding Sites/drug effects; Dose-Response Relationship; Drug; Ligands; Mitochondrial Proteins/*antagonists & inhibitors/metabolism; Molecular Structure; Recombinant Proteins/antagonists & inhibitors/metabolism; Rosiglitazone; Stereoisomerism; Structure-Activity Relationship; Thiazolidinediones/chemical synthesis/chemistry/*pharmacology
Creator
An entity primarily responsible for making the resource
Geldenhuys Werner J; Funk Max O; Awale Prabha S; Lin Li; Carroll Richard T
Description
An account of the resource
A novel outer mitochondrial membrane protein containing [2Fe-2S] clusters, mitoNEET was first identified through its binding to the anti-diabetic drug pioglitazone. Pioglitazone belongs to a family of drugs that are peroxisome proliferator-activated receptor (PPAR) gamma agonists, collectively known as glitazones. With the lack of pharmacological tools available to fully elucidate mitoNEET's function, we developed a binding assay to probe the glitazone binding site with the aim of developing selective and high affinity compounds. We used multiple thiazolidine-2,4-dione (TZD), 2-thioxothiazolidin-4-one (TTD), and
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.bmcl.2011.06.111" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2011.06.111</a>
Rights
Information about rights held in and over the resource
Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
2011
Awale Prabha S
Binding Sites/drug effects
Bioorganic & medicinal chemistry letters
Carroll Richard T
Dose-Response Relationship
Drug
Funk Max O
Geldenhuys Werner J
Ligands
Lin Li
Mitochondrial Proteins/*antagonists & inhibitors/metabolism
Molecular Structure
Recombinant Proteins/antagonists & inhibitors/metabolism
Rosiglitazone
Stereoisomerism
Structure-Activity Relationship
Thiazolidinediones/chemical synthesis/chemistry/*pharmacology
-
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/10.1016/j.bmcl.2011.06.060" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2011.06.060</a>
Pages
4798–4803
Issue
16
Volume
21
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
Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.
Publisher
An entity responsible for making the resource available
Bioorganic & medicinal chemistry letters
Date
A point or period of time associated with an event in the lifecycle of the resource
2011
2011-08
Subject
The topic of the resource
Animals; Humans; Inbred C57BL; Male; Mice; Models; Molecular; Molecular Structure; Monoamine Oxidase Inhibitors/chemical synthesis/chemistry/*pharmacology; Monoamine Oxidase/*metabolism; Stereoisomerism; Structure-Activity Relationship; Thiazolidinediones/chemical synthesis/chemistry/*pharmacology
Creator
An entity primarily responsible for making the resource
Carroll Richard T; Dluzen Dean E; Stinnett Hilary; Awale Prabha S; Funk Max O; Geldenhuys Werner J
Description
An account of the resource
The neuroprotective activity of pioglitazone and rosiglitazone in the MPTP parkinsonian mouse prompted us to evaluate a set of thiazolidinedione (TZD) type compounds for monoamine oxidase A and B inhibition activity. These compounds were able to inhibit MAO-B over several log units of magnitude (82 nM to 600 muM). Initial structure-activity relationship studies identified key areas to modify the aromatic substituted TZD compounds. Primarily, substitutions on the aromatic group and the TZD nitrogen were key areas where activity was enhanced within this group of compounds.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.bmcl.2011.06.060" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2011.06.060</a>
Rights
Information about rights held in and over the resource
Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
2011
Animals
Awale Prabha S
Bioorganic & medicinal chemistry letters
Carroll Richard T
Dluzen Dean E
Funk Max O
Geldenhuys Werner J
Humans
Inbred C57BL
Male
Mice
Models
Molecular
Molecular Structure
Monoamine Oxidase Inhibitors/chemical synthesis/chemistry/*pharmacology
Monoamine Oxidase/*metabolism
Stereoisomerism
Stinnett Hilary
Structure-Activity Relationship
Thiazolidinediones/chemical synthesis/chemistry/*pharmacology