1
40
8
-
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/10.1002/cmdc.201100559" target="_blank" rel="noreferrer noopener">http://doi.org/10.1002/cmdc.201100559</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
375-384
Issue
3
Volume
7
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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
Polycyclic Cage Structures As Lipophilic Scaffolds For Neuroactive Drugs
Publisher
An entity responsible for making the resource available
Chemmedchem
Date
A point or period of time associated with an event in the lifecycle of the resource
2012
2012-03
Subject
The topic of the resource
Alzheimer's disease; apoptosis; benzodiazepine-receptors; biological activity; cage compounds; calcium-antagonists; carbonic-anhydrase inhibitors; d-aspartate receptor; drug design; fluorescent ligands; monoamine-oxidase-b; neuroprotection; nitric-oxide; parkinsons-disease; Pharmacology & Pharmacy; sigma-receptors
Creator
An entity primarily responsible for making the resource
Joubert J; Geldenhuys W J; Van der Schyf C J; Oliver D W; Kruger H G; Govender T; Malan S F
Description
An account of the resource
Polycyclic cage scaffolds have been successfully used in the development of numerous lead compounds demonstrating activity in the central nervous system (CNS). Several neurodegenerative diseases, such as Alzheimers disease, Parkinsons disease, Huntingtons disease, schizophrenia, and stroke, as well as drug abuse, can be modulated with polycyclic cage derivatives. These cage moieties, including adamantane and pentacycloundecane derivatives, improve the pharmacokinetic and pharmacodynamic properties of conjugated parent drugs and serve as an important scaffold in the design of therapeutically active agents for the treatment of neurological disorders. In this Minireview, we focus on the recent developments in the field of polycyclic cage compounds, as well as the relationship between the lipophilic character of these cage-derived drugs and the ability of such compounds to target and reach the CNS and improve the pharmacodynamic properties of compounds conjugated to it.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1002/cmdc.201100559" target="_blank" rel="noreferrer noopener">10.1002/cmdc.201100559</a>
Format
The file format, physical medium, or dimensions of the resource
Journal Article or Conference Abstract Publication
2012
Alzheimer's disease
Apoptosis
benzodiazepine-receptors
biological activity
cage compounds
calcium-antagonists
carbonic-anhydrase inhibitors
Chemmedchem
d-aspartate receptor
Drug Design
fluorescent ligands
Geldenhuys W J
Govender T
Joubert J
Journal Article or Conference Abstract Publication
Kruger H G
Malan S F
monoamine-oxidase-b
Neuroprotection
nitric-oxide
Oliver D W
parkinsons-disease
Pharmacology & Pharmacy
sigma-receptors
Van der Schyf C 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/10.1021/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
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<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
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
-
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/10.2741/1543" target="_blank" rel="noreferrer noopener">http://doi.org/10.2741/1543</a>
Pages
478–482
Volume
10
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
Immune peptide enhancement of peptide based vaccines.
Publisher
An entity responsible for making the resource available
Frontiers in bioscience : a journal and virtual library
Date
A point or period of time associated with an event in the lifecycle of the resource
2005
2005-01
Subject
The topic of the resource
Humans; Animals; Drug Design; B-Lymphocytes/immunology; T-Lymphocytes/immunology; Cancer Vaccines/chemistry; Epitopes/chemistry; Immune System/pathology; Peptides/*chemistry; Vaccines; Subunit/*chemistry
Creator
An entity primarily responsible for making the resource
Rosenthal Ken S
Description
An account of the resource
Vaccines optimize the presentation of an immunogen to the immune system, oftentimes enhancing or replacing the natural activators of antigen presenting cells in order to promote the delivery and the response of T and B lymphocytes to the immunogen. The purpose of this series is to describe new technologies which allow vaccine design, based on our understanding of the immune response, using different approaches to immune peptide enhancement of peptide based vaccines. In this introduction to the series entitled, "Immune Peptide Enhancement of Peptide Based Vaccines", some of the immunological concepts relevant to vaccine design are presented.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.2741/1543" target="_blank" rel="noreferrer noopener">10.2741/1543</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).
2005
Animals
B-Lymphocytes/immunology
Cancer Vaccines/chemistry
Drug Design
Epitopes/chemistry
Frontiers in bioscience : a journal and virtual library
Humans
Immune System/pathology
Peptides/*chemistry
Rosenthal Ken S
Subunit/*chemistry
T-Lymphocytes/immunology
Vaccines
-
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/10.2174/156720507783018226" target="_blank" rel="noreferrer noopener">http://doi.org/10.2174/156720507783018226</a>
Pages
522–536
Issue
5
Volume
4
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
Novel multifunctional anti-Alzheimer drugs with various CNS neurotransmitter targets and neuroprotective moieties.
Publisher
An entity responsible for making the resource available
Current Alzheimer research
Date
A point or period of time associated with an event in the lifecycle of the resource
2007
2007-12
Subject
The topic of the resource
Humans; Animals; Drug Design; Alzheimer Disease/pathology/*prevention & control; Central Nervous System/chemistry/*drug effects/metabolism; Neuroprotective Agents/*chemistry/pharmacology/*therapeutic use; Neurotransmitter Agents/chemistry/*metabolism; Biological; Models
Creator
An entity primarily responsible for making the resource
Van der Schyf Cornelis J; Mandel Silvia; Geldenhuys Werner J; Amit Tamar; Avramovich Yael; Zheng Hailin; Fridkin Mati; Gal Shunit; Weinreb Orly; Bar Am Orit; Sagi Yotam; Youdim Moussa B H
Description
An account of the resource
Traditionally, drug design programs are focused on optimizing the specificity of lead compounds against a carefully selected drug target. Disappointingly, this approach to discover a "magic bullet" drug has not met with the expected success for CNS disorders. Transcriptomics and proteomic profiling of neurodegenerative diseases have indicated that they are poly-etiological in origin and that the processes leading to neuronal death are multifactorial. An emerging concept is the design of drug ligands that modulate multiple drug targets identified for a particular disease. In this review we explore some examples of multifunctional drugs which may be useful in the treatment of neurodegenerative diseases, such as Alzheimer's and Parkinson's disease.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.2174/156720507783018226" target="_blank" rel="noreferrer noopener">10.2174/156720507783018226</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).
2007
Alzheimer Disease/pathology/*prevention & control
Amit Tamar
Animals
Avramovich Yael
Bar Am Orit
Biological
Central Nervous System/chemistry/*drug effects/metabolism
Current Alzheimer research
Drug Design
Fridkin Mati
Gal Shunit
Geldenhuys Werner J
Humans
Mandel Silvia
Models
Neuroprotective Agents/*chemistry/pharmacology/*therapeutic use
Neurotransmitter Agents/chemistry/*metabolism
Sagi Yotam
Van der Schyf Cornelis J
Weinreb Orly
Youdim Moussa B H
Zheng Hailin
-
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/10.1586/ern.09.51" target="_blank" rel="noreferrer noopener">http://doi.org/10.1586/ern.09.51</a>
Pages
1073–1085
Issue
7
Volume
9
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
The serotonin 5-HT6 receptor: a viable drug target for treating cognitive deficits in Alzheimer's disease.
Publisher
An entity responsible for making the resource available
Expert review of neurotherapeutics
Date
A point or period of time associated with an event in the lifecycle of the resource
2009
2009-07
Subject
The topic of the resource
Humans; Animals; Structure-Activity Relationship; Serotonin/*metabolism; Drug Design; Alzheimer Disease/*complications; Cognition Disorders/*drug therapy/*etiology; Serotonin Antagonists/chemistry/*therapeutic use; Receptors; Biological; Models
Creator
An entity primarily responsible for making the resource
Geldenhuys Werner J; Van der Schyf Cornelis J
Description
An account of the resource
The serotonin 6 receptor is attracting attention as an etiological contributor in cognition deficits in diseases such as Alzheimer's disease, anxiety/depression and schizophrenia. In this review, we discuss the role of this recently discovered G protein-coupled receptor in cognition and memory, particularly in Alzheimer's disease. A surge in publications that describe the development of ligands for this receptor have recently come to light, underscoring the emerging interest in this receptor as a drug target. We also explore the current status of structure-activity relationship studies that have focused on the design of novel antagonists for the serotonin 6 receptor.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1586/ern.09.51" target="_blank" rel="noreferrer noopener">10.1586/ern.09.51</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).
2009
Alzheimer Disease/*complications
Animals
Biological
Cognition Disorders/*drug therapy/*etiology
Drug Design
Expert review of neurotherapeutics
Geldenhuys Werner J
Humans
Models
Receptors
Serotonin Antagonists/chemistry/*therapeutic use
Serotonin/*metabolism
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/10.1155/2014/316153" target="_blank" rel="noreferrer noopener">http://doi.org/10.1155/2014/316153</a>
Pages
316153–316153
Volume
2014
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
Advances in statistical medicine.
Publisher
An entity responsible for making the resource available
Computational and mathematical methods in medicine
Date
A point or period of time associated with an event in the lifecycle of the resource
2014
1905-07
Subject
The topic of the resource
*Statistics as Topic; Biotechnology/trends; Computers; Decision Trees; Drug Design; Humans; Medical Informatics/*methods; Models; Neoplasms/therapy; Statistical
Creator
An entity primarily responsible for making the resource
Datta Sujay; Xia Xiao-Qin; Bhattacharjee Samsiddhi; Jia Zhenyu
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1155/2014/316153" target="_blank" rel="noreferrer noopener">10.1155/2014/316153</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).
*Statistics as Topic
2014
Bhattacharjee Samsiddhi
Biotechnology/trends
Computational and mathematical methods in medicine
Computers
Datta Sujay
Decision Trees
Drug Design
Humans
Jia Zhenyu
Medical Informatics/*methods
Models
Neoplasms/therapy
Statistical
Xia Xiao-Qin
-
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.2011.10.014" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2011.10.014</a>
Pages
7405–7411
Issue
24
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
3D-Quantitative structure-activity relationship and docking studies of the tachykinin NK3 receptor.
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
2011-12
Subject
The topic of the resource
*Quantitative Structure-Activity Relationship; Binding Sites; Computer Simulation; Drug Design; Humans; Ligands; Models; Molecular; Neurokinin-3/*chemistry/metabolism; Protein Structure; Quinolines/chemistry; Receptors; Tertiary
Creator
An entity primarily responsible for making the resource
Geldenhuys Werner J; Simmons Mark A
Description
An account of the resource
The tachykinin NK(3) receptor (NK(3)R) is a novel drug target for schizophrenia and drug abuse. Since few non-peptide antagonists of this G protein-coupled receptor are available, we have initiated this study to gain a better understanding of the structure-activity relationships of NK(3) antagonist compounds. We developed a 3D comparative molecular similarity index analysis (CoMSIA) model that gave cross-validated PLS values with q(2) \textgreater0.5 which were validated using a test set. We also describe the development of a homology model of the NK(3)R. The model was then used to develop a pharmacophore for docked ligands. This pharmacophore showed two aromatic, two hydrogen donor and one acceptor/aromatic points. These data will be useful for future structure-based drug discovery of ligands for the NK(3)R.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.bmcl.2011.10.014" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2011.10.014</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).
*Quantitative Structure-Activity Relationship
2011
Binding Sites
Bioorganic & medicinal chemistry letters
Computer Simulation
Drug Design
Geldenhuys Werner J
Humans
Ligands
Models
Molecular
Neurokinin-3/*chemistry/metabolism
Protein Structure
Quinolines/chemistry
Receptors
Simmons Mark A
Tertiary