1
40
3
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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.nurt.2008.10.037" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.nurt.2008.10.037</a>
Pages
175–186
Issue
1
Volume
6
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
Polycyclic compounds: ideal drug scaffolds for the design of multiple mechanism drugs?
Publisher
An entity responsible for making the resource available
Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics
Date
A point or period of time associated with an event in the lifecycle of the resource
2009
2009-01
Subject
The topic of the resource
*Drug Design; Adamantane/chemistry/pharmacology; Animals; Central Nervous System Diseases/*drug therapy; Humans; Molecular Structure; Neuroprotective Agents/chemistry/*pharmacology/therapeutic use; Polycyclic Compounds/*chemistry/pharmacology/therapeutic use; Psychotropic Drugs/chemistry/*pharmacology/therapeutic use; Quantitative Structure-Activity Relationship
Creator
An entity primarily responsible for making the resource
Van der Schyf Cornelis J; Geldenhuys Werner J
Description
An account of the resource
Recently there has been a resurging interest in developing multi-functional drugs to treat diseases with complex pathological mechanisms. Such drug molecules simultaneously target multiple etiologies that have been found to be important modulators in specific diseases. This approach has significant promise and may be more effective than using one compound specific for one drug target or, by a polypharmaceutical approach, using a cocktail of two or more drugs. Polycyclic ring structures are useful as starting scaffolds in medicinal chemistry programs to develop multi-functional drugs, and may also be useful moieties added to existing structures to improve the pharmacokinetic properties of drugs currently used in the clinic or under development. This review attempts to provide a synopsis of current published research to exemplify the use of polycyclic compounds as starting molecules to develop multi-functional drugs.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.nurt.2008.10.037" target="_blank" rel="noreferrer noopener">10.1016/j.nurt.2008.10.037</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).
*Drug Design
2009
Adamantane/chemistry/pharmacology
Animals
Central Nervous System Diseases/*drug therapy
Geldenhuys Werner J
Humans
Molecular Structure
Neuroprotective Agents/chemistry/*pharmacology/therapeutic use
Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics
Polycyclic Compounds/*chemistry/pharmacology/therapeutic use
Psychotropic Drugs/chemistry/*pharmacology/therapeutic use
Quantitative Structure-Activity Relationship
Van der Schyf Cornelis J
-
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.2010.06.090" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2010.06.090</a>
Pages
4870–4877
Issue
16
Volume
20
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
3-D-QSAR and docking studies on the neuronal choline transporter.
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
2010
2010-08
Subject
The topic of the resource
Binding Sites; Blood-Brain Barrier/metabolism; Computer Simulation; Membrane Transport Proteins/*chemistry/metabolism; Models; Molecular; Neurons/*metabolism; Quantitative Structure-Activity Relationship; Quaternary Ammonium Compounds/chemistry
Creator
An entity primarily responsible for making the resource
Geldenhuys Werner J; Allen David D; Lockman Paul R
Description
An account of the resource
The high affinity neuronal choline transporter (CHT1) is responsible for the uptake of choline into the pre-synaptic terminal of cholinergic neurons. Considering our past experience with modeling the blood-brain barrier choline transporter (BBBCHT) as drug delivery vector to the CNS, we investigated the
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.bmcl.2010.06.090" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2010.06.090</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).
2010
Allen David D
Binding Sites
Bioorganic & medicinal chemistry letters
Blood-Brain Barrier/metabolism
Computer Simulation
Geldenhuys Werner J
Lockman Paul R
Membrane Transport Proteins/*chemistry/metabolism
Models
Molecular
Neurons/*metabolism
Quantitative Structure-Activity Relationship
Quaternary Ammonium Compounds/chemistry
-
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.2010.01.140" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2010.01.140</a>
Pages
1918–1923
Issue
6
Volume
20
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
3D-QSAR and docking studies on transforming growth factor (TGF)-beta receptor 1 antagonists.
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
2010
2010-03
Subject
The topic of the resource
Models; Molecular; Quantitative Structure-Activity Relationship; Receptors; Transforming Growth Factor beta/*antagonists & inhibitors
Creator
An entity primarily responsible for making the resource
Geldenhuys Werner J; Nakamura Hiroshi
Description
An account of the resource
The transforming growth factor-beta (TGF-beta) is part of a family of cytokines which regulate various signaling pathways such as cell development, growth, and tissue injury. Although several studies have been published describing the synthesis of small compounds which inhibit the receptor of TGF-beta, especially the subtype 1 receptor (TGBR1) kinase, no 3D-quantitiative structure-activity relationship study has been published. Here we describe the development of a comparative molecular field analysis (CoMFA) model which yielded a partial least squares statistical cross validated r(2) of \textgreater0.3. CoMFA maps agree with docking studies and pharmacophore analysis that hydrogen bonding is important for binding to ALK-5. These studies could enable the medicinal chemist to develop novel inhibitors which can be used in glaucoma filtration surgery.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.bmcl.2010.01.140" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2010.01.140</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).
2010
Bioorganic & medicinal chemistry letters
Geldenhuys Werner J
Models
Molecular
Nakamura Hiroshi
Quantitative Structure-Activity Relationship
Receptors
Transforming Growth Factor beta/*antagonists & inhibitors