1
40
14
-
Text
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URL Address
<a href="http://doi.org/10.1021/acs.analchem.9b02757" target="_blank" rel="noreferrer noopener">http://doi.org/10.1021/acs.analchem.9b02757</a>
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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
14340-14351
Issue
22
Volume
91
ISSN
1520-6882
Search for Full-text
Locate full-text within NEOMED Library's e-journal collections
<a href="http://ezproxy.neomed.idm.oclc.org/login?url=http://doi.org/10.1021/acs.analchem.9b02757" target="_blank" rel="noreferrer noopener">NEOMED Full-text Holding (if available) - Proxy DOI: 10.1021/acs.analchem.9b02757</a>
<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
Calculation of the Protein Turnover Rate Using the Number of Incorporated 2H Atoms and Proteomics Analysis of a Single Labeled Sample
Publisher
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Analytical Chemistry
Date
A point or period of time associated with an event in the lifecycle of the resource
2019
2019-11-19
Creator
An entity primarily responsible for making the resource
Ilchenko Serguei; Haddad Andrew; Sadana Prabodh; Recchia Fabio A; Sadygov Rovshan G; Kasumov Takhar
Description
An account of the resource
Rate constant estimation with heavy water requires a long-term experiment with data collection at multiple time points (3-4 weeks for mitochondrial proteome dynamics in mice and much longer in other species). When tissue proteins are analyzed, this approach requires euthanizing animals at each time point or multiple tissue biopsies in humans. Although short-term protocols are available, they require knowledge of the maximum number of isotope labels (N) and accurate quantification of observed 2H-enrichment in the peptide. The high-resolution accurate mass spectrometers used for proteome dynamics studies are characterized by a systematic spectral error that compromises these measurements. To circumvent these issues, we developed a simple algorithm for the rate constant calculation based on a single labeled sample and comparable unlabeled (time 0) sample. The algorithm determines N for all proteogenic amino acids from a long-term experiment to calculate the predicted plateau 2H-labeling of peptides for a short-term protocol and estimates the rate constant based on the measured baseline and the predicted plateau 2H-labeling of peptides. The method was validated based on the rate constant estimation in a long-term experiment in mice and dogs. The improved 2 time-point method enables the rate constant calculation with less than 10% relative error compared to the bench-marked multi-point method in mice and dogs and allows us to detect diet-induced subtle changes in ApoAI turnover in mice. In conclusion, we have developed and validated a new algorithm for protein rate constant calculation based on 2-time point measurements that could also be applied to other biomolecules.
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<a href="http://doi.org/10.1021/acs.analchem.9b02757" target="_blank" rel="noreferrer noopener">10.1021/acs.analchem.9b02757</a>
PMID: 31638786
Format
The file format, physical medium, or dimensions of the resource
Journal Article
2019
Analytical Chemistry
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Haddad Andrew
Ilchenko Serguei
Journal Article
Kasumov Takhar
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
November 2019 Update
Recchia Fabio A
Sadana Prabodh
Sadygov Rovshan G
-
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/10.1111/jphp.13138" target="_blank" rel="noreferrer noopener">http://doi.org/10.1111/jphp.13138</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
1421-1428
Issue
9
Volume
71
Search for Full-text
Locate full-text within NEOMED Library's e-journal collections
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Dublin Core
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Title
A name given to the resource
AMPK‐SIRT1‐independent inhibition of ANGPTL3 gene expression is a potential lipid‐lowering mechanism of metformin.
Publisher
An entity responsible for making the resource available
Journal of Pharmacy & Pharmacology
Date
A point or period of time associated with an event in the lifecycle of the resource
2019
2019-09
Subject
The topic of the resource
angiopoietin‐like 3; diabetes; dyslipidaemia; lipoprotein lipase; metformin
Creator
An entity primarily responsible for making the resource
Lin Li; Burke Jamie; Venkatesh Sahana; Sadana Prabodh
Description
An account of the resource
Objectives: Hypertriglyceridaemia enhances cardiovascular disease risk in patients with diabetes. Lipoprotein lipase (LPL) regulates plasma triglyceride levels by hydrolysing chylomicrons and very‐low‐density lipoprotein (VLDL). Metformin, an antidiabetic drug, improves plasma lipids including triglycerides. We examined metformin's regulation of angiopoietin‐like 3 (ANGPTL3), a liver‐derived secretory protein with LPL inhibitory property. Methods: Using HepG2 cells, a human hepatocyte cell line, the effects of metformin on ANGPTL3 gene and protein expression were determined. The role of AMPK‐SIRT1 pathway in metformin regulation of ANGPTL3 was determined using pharmacological, RNAi and reporter assays. Metformin regulation of ANGPTL3 expression was also examined in sodium palmitate‐induced insulin resistance. Key findings: Metformin and pharmacological activators of AMPK and SIRT1 inhibited the expression of ANGPTL3 in HepG2 cells. Pharmacological or RNAi‐based antagonism of AMPK or SIRT1 failed to affect metformin inhibition of ANGPTL3. AMPK‐SIRT1 activators and metformin exhibited distinct effects on the expression of ANGPTL3 gene luciferase reporter. Sodium palmitate‐induced insulin resistance in cells resulted in increased ANGPTL3 gene expression which was suppressed by pretreatment with metformin. Conclusions: Metformin inhibits ANGPTL3 expression in the liver in an AMPK‐SIRT1‐independent manner as a potential mechanism to regulate LPL and lower plasma lipids. [ABSTRACT FROM AUTHOR]
Identifier
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<a href="http://doi.org/10.1111/jphp.13138" target="_blank" rel="noreferrer noopener">10.1111/jphp.13138</a>
2019
angiopoietin‐like 3
Burke Jamie
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Diabetes
dyslipidaemia
Journal of Pharmacy & Pharmacology
Lin Li
Lipoprotein lipase
metformin
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Sadana Prabodh
September 2019 Update
Venkatesh Sahana
-
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/10.4088/JCP.18m12588" target="_blank" rel="noreferrer noopener">http://doi.org/10.4088/JCP.18m12588</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).
Issue
4
Volume
80
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
Prevalence and Predictors of Benzodiazepine Monotherapy in Patients With Depression: A National Cross-Sectional Study
Publisher
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The Journal of Clinical Psychiatry
Date
A point or period of time associated with an event in the lifecycle of the resource
2019
2019-05
Creator
An entity primarily responsible for making the resource
Soric Mate M; Paxos Chris; Dugan Sara E; Fosnight Susan M; Turosky Jodie Z; Sadana Prabodh; Emshoff Jessica B; Everly Lukas; Snyder Brittany M; Mistry Bhavin K; Bhat Shubha; Unruh Amy E; Safi Ismail M
Description
An account of the resource
OBJECTIVE: Depression guidelines discourage benzodiazepine monotherapy and limit use to short-term adjunctive therapy with antidepressants; however, patients with depression continue to receive benzodiazepine monotherapy. The prevalence and predictors of this prescribing pattern have not been described previously and are warranted to assist clinicians in identifying patients at highest risk of receiving benzodiazepine monotherapy. METHODS: A national, cross-sectional analysis of the National Ambulatory Medical Care Survey from 2012 to 2015 was performed for adults treated for depression. Depression was identified using a survey item specifically assessing the presence of depression. Office visits involving patients with bipolar disorder, schizoaffective disorder, or pregnancy were identified by ICD-9 code or specific survey item and were excluded. The primary endpoint was benzodiazepine monotherapy prescribing rate defined as initiation or continuation of a benzodiazepine in the absence of any antidepressant agent. A multivariate logistic regression model was created to identify variables associated with benzodiazepine monotherapy. RESULTS: In total, 9,426 unweighted visits were eligible for inclusion. Benzodiazepine monotherapy was identified in 9.3% of patients treated for depression (95% CI, 8.2%-10.6%). Predictors of benzodiazepine monotherapy included age of 45-64 years (OR = 1.39; 95% CI, 1.01-1.91), epilepsy-related office visit (OR = 5.34; 95% CI, 1.39-20.44), anxiety-related office visit (OR = 1.67; 95% CI, 1.23-2.27), underlying pulmonary disease (OR = 1.43; 95% CI, 1.09-1.87), and concomitant opiate prescribing (OR = 2.86; 95% CI, 2.01-4.06). Psychiatrists were less likely to prescribe benzodiazepine monotherapy than were other providers (OR = 0.42; 95% CI, 0.29-0.61). CONCLUSIONS: Benzodiazepine monotherapy is utilized in nearly 1 in 10 patients treated for depression. Adults aged 45 to 65 years, patients prescribed opioids, patients seen by primary care providers, and those with underlying anxiety, epilepsy, or pulmonary disorders are at highest risk.
Identifier
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<a href="http://doi.org/10.4088/JCP.18m12588" target="_blank" rel="noreferrer noopener">10.4088/JCP.18m12588</a>
2019
Bhat Shubha
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Dugan Sara E
Emshoff Jessica B
Everly Lukas
Fosnight Susan M
June 2019 Update
Mistry Bhavin K
NEOMED College of Graduate Studies
NEOMED College of Medicine
NEOMED College of Pharmacy
Paxos Chris
Sadana Prabodh
Safi Ismail M
Snyder Brittany M
Soric Mate M
The Journal of clinical psychiatry
Turosky Jodie Z
Unruh Amy E
-
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.jacl.2017.04.100" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.jacl.2017.04.100</a>
Pages
832–834
Issue
3
Volume
11
Dublin Core
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Title
A name given to the resource
Development of Small Molecule Screening Assay for Modulation of Lipoprotein Lipase activity Using Hepatocyte Secretome.
Publisher
An entity responsible for making the resource available
Journal of Clinical Lipidology
Date
A point or period of time associated with an event in the lifecycle of the resource
2017
2017-05
Subject
The topic of the resource
Lipoproteins; Health Screening; Lipase
Creator
An entity primarily responsible for making the resource
Venkatesh Sahana; Sadana Prabodh; Lin Li
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.jacl.2017.04.100" target="_blank" rel="noreferrer noopener">10.1016/j.jacl.2017.04.100</a>
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
2017
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Health Screening
Journal of Clinical Lipidology
Lin Li
Lipase
Lipoproteins
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Sadana Prabodh
Venkatesh Sahana
-
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/10.4155/fmc.12.72" target="_blank" rel="noreferrer noopener">http://doi.org/10.4155/fmc.12.72</a>
Pages
1307–1333
Issue
10
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
Noncanonical mechanisms to regulate nuclear receptor signaling.
Publisher
An entity responsible for making the resource available
Future medicinal chemistry
Date
A point or period of time associated with an event in the lifecycle of the resource
2012
2012-06
Subject
The topic of the resource
Humans; Protein Binding; MicroRNAs/metabolism; Signal Transduction/drug effects; Ligands; DNA/metabolism; Peptides/chemistry/pharmacology; Small Molecule Libraries/chemistry/pharmacology; Receptors; Drug Evaluation; Preclinical; Cytoplasmic and Nuclear/antagonists & inhibitors/*metabolism
Creator
An entity primarily responsible for making the resource
Sadana Prabodh
Description
An account of the resource
Nuclear receptor (NR)-targeted therapies comprise a large class of clinically employed drugs. A number of drugs currently being used against this protein class were designed as structural analogs of the endogenous ligand of these receptors. In recent years, there has been significant interest in developing newer strategies to target NRs, especially those that rely on mechanistic pathways of NR function. Prominent among these are noncanonical means of targeting NRs, which include selective NR modulation, NR coactivator interaction inhibition, inhibition of NR DNA binding, modulation of NR cellular localization, modulation of NR ligand biosynthesis and downregulation of NR levels in target tissues. This article reviews each of these promising emerging strategies for NR drug development and highlights some of most significant successes achieved in using them.
Identifier
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<a href="http://doi.org/10.4155/fmc.12.72" target="_blank" rel="noreferrer noopener">10.4155/fmc.12.72</a>
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
2012
Cytoplasmic and Nuclear/antagonists & inhibitors/*metabolism
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
DNA/metabolism
Drug Evaluation
Future medicinal chemistry
Humans
Ligands
MicroRNAs/metabolism
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Peptides/chemistry/pharmacology
Preclinical
Protein Binding
Receptors
Sadana Prabodh
Signal Transduction/drug effects
Small Molecule Libraries/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/10.3109/10837450.2015.1041043" target="_blank" rel="noreferrer noopener">http://doi.org/10.3109/10837450.2015.1041043</a>
Pages
647–654
Issue
6
Volume
21
Dublin Core
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Title
A name given to the resource
Gelucire-stabilized nanoparticles as a potential DNA delivery system.
Publisher
An entity responsible for making the resource available
Pharmaceutical development and technology
Date
A point or period of time associated with an event in the lifecycle of the resource
2016
2016-09
Subject
The topic of the resource
Humans; Animals; Mice; nanoparticles; Cell Line; Hep G2 Cells; gene therapy; *Gene Transfer Techniques; Cationic lipids; Cell Survival/drug effects/physiology; DNA/*administration & dosage/chemistry; macrophage activation; Macrophages/drug effects/physiology; Nanoparticles/*administration & dosage/chemistry; Polyethylene Glycols/*administration & dosage/chemistry; transfection
Creator
An entity primarily responsible for making the resource
Oyewumi Moses O; Wehrung Daniel; Sadana Prabodh
Description
An account of the resource
Clinical viability of gene delivery systems has been greatly impacted by potential toxicity of the delivery systems. Recently, we reported the nanoparticle (NP) preparation process that employs biocompatible materials such as Gelucire(R) 44/14 and cetyl alcohol as matrix materials. In the current study, the NP preparation was modified for pDNA loading through: (i) inclusion of cationic lipids (DOTAP or DDAB) with NP matrix materials; or (ii) application of cationic surfactants (CTAB) to generate NPs with desired surface charges for pDNA complexation. Colloidal stability and efficiency of loading pGL3-DR4X2-luciferase plasmid DNA in NPs were verified by gel permeation chromatography. Compared to pDNA alone, all the NPs were effective in preserving pDNA from digestion by DNase. While pDNA loading using CTAB-NPs involved fewer steps compared to
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.3109/10837450.2015.1041043" target="_blank" rel="noreferrer noopener">10.3109/10837450.2015.1041043</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).
*Gene Transfer Techniques
2016
Animals
Cationic lipids
Cell Line
Cell Survival/drug effects/physiology
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
DNA/*administration & dosage/chemistry
gene therapy
Hep G2 Cells
Humans
macrophage activation
Macrophages/drug effects/physiology
Mice
Nanoparticles
Nanoparticles/*administration & dosage/chemistry
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Oyewumi Moses O
Pharmaceutical development and technology
Polyethylene Glycols/*administration & dosage/chemistry
Sadana Prabodh
Transfection
Wehrung Daniel
-
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/10.2174/1874467208666150817112109" target="_blank" rel="noreferrer noopener">http://doi.org/10.2174/1874467208666150817112109</a>
Pages
226–236
Issue
3
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
Signal Transduction Mechanisms of Alcoholic Fatty Liver Disease: Emer ging Role of Lipin-1.
Publisher
An entity responsible for making the resource available
Current molecular pharmacology
Date
A point or period of time associated with an event in the lifecycle of the resource
2017
1905-7
Subject
The topic of the resource
Humans; Animals; AMP-Activated Protein Kinases/metabolism; Signal Transduction; Lipid Metabolism; Fatty Liver; Liver/metabolism; lipid metabolism; alcoholic fatty liver disease; inflammation; Lipin-1; signal transduction; transcriptional regulators; Phosphatidate Phosphatase/*metabolism; Inflammation/metabolism; Ethanol/chemistry/*metabolism; Sirtuin 1/metabolism; Alcoholic/*metabolism/pathology
Creator
An entity primarily responsible for making the resource
You Min; Jogasuria Alvin; Lee Kwangwon; Wu Jiashin; Zhang Yanqiao; Lee Yoon-Kwang; Sadana Prabodh
Description
An account of the resource
Lipin-1, a mammalian phosphatidic acid phosphatase (PAP), is a bi-functional molecule involved in various signaling pathways via its function as a PAP enzyme in the triglyceride synthesis pathway and in the nucleus as a transcriptional co-regulator. In the liver, lipin-1 is known to play a vital role in controlling the lipid metabolism and inflammation process at multiple regulatory levels. Alcoholic fatty liver disease (AFLD) is one of the earliest forms of liver injury and approximately 8-20% of patients with simple steatosis can develop into more severe forms of liver injury, including steatohepatitis, fibrosis/ cirrhosis, and eventually hepatocellular carcinoma (HCC). The signal transduction mechanisms for alcohol-induced detrimental effects in liver involves alteration of complex and multiple signaling pathways largely governed by a central and upstream signaling system, namely, sirtuin 1 (SIRT1)-AMP activated kinase (AMPK) axis. Emerging evidence suggests a pivotal role of lipin-1 as a crucial downstream regulator of
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.2174/1874467208666150817112109" target="_blank" rel="noreferrer noopener">10.2174/1874467208666150817112109</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).
2017
alcoholic fatty liver disease
Alcoholic/*metabolism/pathology
AMP-Activated Protein Kinases/metabolism
Animals
Current molecular pharmacology
Department of Integrative Medical Sciences
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Ethanol/chemistry/*metabolism
Fatty Liver
Humans
Inflammation
Inflammation/metabolism
Jogasuria Alvin
Lee Kwangwon
Lee Yoon-Kwang
Lipid Metabolism
Lipin-1
Liver/metabolism
NEOMED College of Graduate Studies
NEOMED College of Medicine
NEOMED College of Pharmacy
Phosphatidate Phosphatase/*metabolism
Sadana Prabodh
Signal Transduction
Sirtuin 1/metabolism
transcriptional regulators
Wu Jiashin
You Min
Zhang Yanqiao
-
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.jns.2015.04.042" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.jns.2015.04.042</a>
Pages
37–45
Issue
1
Volume
354
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
Anti-edema action of thyroid hormone in MCAO model of ischemic brain stroke: Possible association with AQP4 modulation.
Publisher
An entity responsible for making the resource available
Journal of the neurological sciences
Date
A point or period of time associated with an event in the lifecycle of the resource
2015
2015-07
Subject
The topic of the resource
Animals; Aquaporin 4/*physiology; Aquaporin-4; Brain Edema/*drug therapy/pathology; Cerebral edema; Cerebrovascular Circulation/drug effects/physiology; Diiodothyronines/*administration & dosage; Erythropoietin; Infarction; Injections; Intravenous; Ischemic brain stroke; Male; Mice; Middle cerebral artery occlusion (MCAO); Middle Cerebral Artery/*drug therapy/pathology; Stroke/*drug therapy/pathology; Thyroid hormone; Triiodothyronine/*administration & dosage
Creator
An entity primarily responsible for making the resource
Sadana Prabodh; Coughlin Lucy; Burke Jamie; Woods Robert; Mdzinarishvili Alexander
Description
An account of the resource
The use of neuroprotective strategies to mitigate the fatal consequences of ischemic brain stroke is a focus of robust research activity. We have previously demonstrated that thyroid hormone (T3; 3,3',5-triiodo-l-thyronine) possesses neuroprotective and anti-edema activity in pre-stroke treatment regimens when administered as a solution or as a nanoparticle formulation. In this study we have extended our evaluation of thyroid hormone use in animal models of brain stroke. We have used both transient middle cerebral artery occlusion (t-MCAO) and permanent (p-MCAO) models of ischemic brain stroke. A significant reduction of tissue infarction and a concurrent decrease in edema were observed in the t-MCAO model of brain stroke. However, no benefit of T3 was observed in p-MCAO stroke setting. Significant improvement of neurological outcomes was observed upon T3 treatment in t-MCAO mice. Further, we tested T2 (3,5-diiodo-l-thyronine) a natural deiodination metabolite of T3 in MCAO model of brain stroke. T2 potently decreased infarct size as well as edema formation. Additionally, we report here that T3 suppresses the expression of aquaporin-4 (AQP4) water channels which could be a likely mechanism of its anti-edema activity. Our studies provide evidence to stimulate clinical development of thyroid hormones for use in ischemic brain stroke.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.jns.2015.04.042" target="_blank" rel="noreferrer noopener">10.1016/j.jns.2015.04.042</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).
2015
Animals
Aquaporin 4/*physiology
Aquaporin-4
Brain Edema/*drug therapy/pathology
Burke Jamie
Cerebral edema
Cerebrovascular Circulation/drug effects/physiology
Coughlin Lucy
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Diiodothyronines/*administration & dosage
Erythropoietin
Infarction
Injections
Intravenous
Ischemic brain stroke
Journal of the neurological sciences
Male
Mdzinarishvili Alexander
Mice
Middle cerebral artery occlusion (MCAO)
Middle Cerebral Artery/*drug therapy/pathology
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Sadana Prabodh
Stroke/*drug therapy/pathology
Thyroid hormone
Triiodothyronine/*administration & dosage
Woods Robert
-
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.drudis.2016.10.007" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.drudis.2016.10.007</a>
Pages
352–365
Issue
2
Volume
22
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
Emerging strategies of targeting lipoprotein lipase for metabolic and cardiovascular diseases.
Publisher
An entity responsible for making the resource available
Drug Discovery Today
Date
A point or period of time associated with an event in the lifecycle of the resource
2017
2017-02
Subject
The topic of the resource
Animals; Cardiovascular Diseases/drug therapy/*enzymology; Humans; Lipoprotein Lipase/chemistry/*metabolism; Metabolic Diseases/drug therapy/*enzymology
Creator
An entity primarily responsible for making the resource
Geldenhuys Werner J; Lin Li; Darvesh Altaf S; Sadana Prabodh
Description
An account of the resource
Although statins and other pharmacological approaches have improved the management of lipid abnormalities, there exists a need for newer treatment modalities especially for the management of hypertriglyceridemia. Lipoprotein lipase (LPL), by promoting hydrolytic cleavage of the triglyceride core of lipoproteins, is a crucial node in the management of plasma lipid levels. Although LPL expression and activity modulation is observed as a pleiotropic action of some the commonly used lipid lowering drugs, the deliberate development of drugs targeting LPL has not occurred yet. In this review, we present the biology of LPL, highlight the LPL modulation property of currently used drugs and review the novel emerging approaches to target LPL.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.drudis.2016.10.007" target="_blank" rel="noreferrer noopener">10.1016/j.drudis.2016.10.007</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).
2017
Animals
Cardiovascular Diseases/drug therapy/*enzymology
Darvesh Altaf S
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Drug Discovery Today
Geldenhuys Werner J
Humans
Lin Li
Lipoprotein Lipase/chemistry/*metabolism
Metabolic Diseases/drug therapy/*enzymology
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Sadana Prabodh
-
Text
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URL Address
<a href="http://doi.org/10.1016/j.bmcl.2018.03.061" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2018.03.061</a>
Pages
1937–1942
Issue
10
Volume
28
Dublin Core
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Title
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Novel compounds that target lipoprotein lipase and mediate growth arrest in acute lymphoblastic leukemia.
Publisher
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Bioorganic & medicinal chemistry letters
Date
A point or period of time associated with an event in the lifecycle of the resource
2018
2018-06
Subject
The topic of the resource
*Acute lymphoblastic leukemia; *Cancer; *Co-culture model; *Lipids; *Lipoprotein lipase; *Metabolism; Amides/chemistry/metabolism/pharmacology; Antineoplastic Agents/*chemistry/metabolism/pharmacology; Binding Sites; Cell Line; Cell Proliferation/drug effects; Coculture Techniques; Dyslipidemias/complications/metabolism/pathology; Humans; Lipoprotein Lipase/antagonists & inhibitors/*metabolism; Mesenchymal Stem Cells/cytology/metabolism; Molecular Docking Simulation; Precursor Cell Lymphoblastic Leukemia-Lymphoma/complications/metabolism/pathology; Protein Binding; Protein Structure; Serum Albumin/chemistry/metabolism; Tertiary; Tumor
Creator
An entity primarily responsible for making the resource
Nair Rajesh R; Geldenhuys Werner J; Piktel Debbie; Sadana Prabodh; Gibson Laura F
Description
An account of the resource
Over the past decade, the therapeutic strategies employed to treat B-precursor acute lymphoblastic leukemia (ALL) have been progressively successful in treating the disease. Unfortunately, the treatment associated dyslipidemia, either acute or chronic, is very prevalent and a cause for decreased quality of life in the surviving patients. To overcome this hurdle, we tested a series of cylopropanecarboxamides, a family demonstrated to target lipid metabolism, for their anti-leukemic activity in ALL. Several of the compounds tested showed anti-proliferative activity, with one, compound 22, inhibiting both Philadelphia chromosome negative REH and Philadelphia chromosome positive SupB15 ALL cell division. The novel advantage of these compounds is the potential synergy with standard chemotherapeutic agents, while concomitantly blunting the emergence of dyslipidemia. Thus, the cylopropanecarboxamides represent a novel class of compounds that can be potentially used in combination with the present standard-of-care to limit treatment associated dyslipidemia in ALL patients.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.bmcl.2018.03.061" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2018.03.061</a>
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
*Acute lymphoblastic leukemia
*Cancer
*Co-culture model
*Lipids
*Lipoprotein lipase
*Metabolism
2018
Amides/chemistry/metabolism/pharmacology
Antineoplastic Agents/*chemistry/metabolism/pharmacology
Binding Sites
Bioorganic & medicinal chemistry letters
Cell Line
Cell Proliferation/drug effects
Coculture Techniques
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Dyslipidemias/complications/metabolism/pathology
Geldenhuys Werner J
Gibson Laura F
Humans
Lipoprotein Lipase/antagonists & inhibitors/*metabolism
Mesenchymal Stem Cells/cytology/metabolism
Molecular Docking Simulation
Nair Rajesh R
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Piktel Debbie
Precursor Cell Lymphoblastic Leukemia-Lymphoma/complications/metabolism/pathology
Protein Binding
Protein Structure
Sadana Prabodh
Serum Albumin/chemistry/metabolism
Tertiary
Tumor
-
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.2016.11.053" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2016.11.053</a>
Pages
303–308
Issue
2
Volume
27
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
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Structure-activity and in vivo evaluation of a novel lipoprotein lipase (LPL) activator.
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
2017
2017-01
Subject
The topic of the resource
*Diabetes; *High-fat diet; *Homology modeling; *Hyperlipidemia; *Lipoprotein lipase; *Liver cirrhosis; *Obesity; Animals; Benzeneacetamides/chemical synthesis/chemistry/*pharmacology; Dose-Response Relationship; Drug; Imidazoles/chemical synthesis/chemistry/*pharmacology; Lipoprotein Lipase/*metabolism; Mice; Molecular Docking Simulation; Molecular Structure; Structure-Activity Relationship
Creator
An entity primarily responsible for making the resource
Geldenhuys Werner J; Caporoso Joel; Leeper Thomas C; Lee Yoon-Kwang; Lin Li; Darvesh Altaf S; Sadana Prabodh
Description
An account of the resource
Elevated triglycerides (TG) contribute towards increased risk for cardiovascular disease. Lipoprotein lipase (LPL) is an enzyme that is responsible for the metabolism of core triglycerides of very-low density lipoproteins (VLDL) and chylomicrons in the vasculature. In this study, we explored the structure-activity relationships of our lead compound (C10d) that we have previously identified as an LPL agonist. We found that the cyclopropyl moiety of C10d is not absolutely necessary for LPL activity. Several substitutions were found to result in loss of LPL activity. The compound C10d was also tested in vivo for its lipid lowering activity. Mice were fed a high-fat diet (HFD) for four months, and treated for one week at 10mg/kg. At this dose, C10d exhibited in vivo biological activity as indicated by lower TG and cholesterol levels as well as reduced body fat content as determined by ECHO-MRI. Furthermore, C10d also reduced the HFD induced fat accumulation in the liver. Our study has provided insights into the structural and functional characteristics of this novel LPL activator.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.bmcl.2016.11.053" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2016.11.053</a>
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
*Diabetes
*High-fat diet
*Homology modeling
*Hyperlipidemia
*Lipoprotein lipase
*Liver cirrhosis
*Obesity
2017
Animals
Benzeneacetamides/chemical synthesis/chemistry/*pharmacology
Bioorganic & medicinal chemistry letters
Caporoso Joel
Darvesh Altaf S
Department of Integrative Medical Sciences
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Dose-Response Relationship
Drug
Geldenhuys Werner J
Imidazoles/chemical synthesis/chemistry/*pharmacology
Lee Yoon-Kwang
Leeper Thomas C
Lin Li
Lipoprotein Lipase/*metabolism
Mice
Molecular Docking Simulation
Molecular Structure
NEOMED College of Graduate Studies
NEOMED College of Medicine
NEOMED College of Pharmacy
Sadana Prabodh
Structure-Activity Relationship
-
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.2014.03.021" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2014.03.021</a>
Pages
2163–2167
Issue
9
Volume
24
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
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A novel Lipoprotein lipase (LPL) agonist rescues the enzyme from inhibition by angiopoietin-like 4 (ANGPTL4).
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
2014
2014-05
Subject
The topic of the resource
Angiopoietin-like 4 Protein; Angiopoietins/*metabolism; ANGPTL4; Atherosclerosis; Benzamides/pharmacology; Drug Discovery; Enzyme Activation/*drug effects; High-throughput screen; Homology model; Humans; Ibrolipim; Lipoprotein Lipase/*metabolism; LPL; Molecular Docking Simulation; NO-1886; Organophosphorus Compounds/pharmacology
Creator
An entity primarily responsible for making the resource
Geldenhuys Werner J; Aring Danielle; Sadana Prabodh
Description
An account of the resource
Lipoprotein lipase (LPL) is a key physiological regulator of triglycerides and atherosclerosis risk. Random screening identified a compound designated C10, showing greater LPL agonist activity than NO-1886, a known LPL agonist. Structure-activity relationship (SAR) exploration of C10 led to the identification of C10d exhibiting at least two fold greater LPL activation than
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.bmcl.2014.03.021" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2014.03.021</a>
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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).
2014
Angiopoietin-like 4 Protein
Angiopoietins/*metabolism
ANGPTL4
Aring Danielle
Atherosclerosis
Benzamides/pharmacology
Bioorganic & medicinal chemistry letters
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Drug Discovery
Enzyme Activation/*drug effects
Geldenhuys Werner J
High-throughput screen
Homology model
Humans
Ibrolipim
Lipoprotein Lipase/*metabolism
LPL
Molecular Docking Simulation
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
NO-1886
Organophosphorus Compounds/pharmacology
Sadana Prabodh
-
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.2012.06.096" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2012.06.096</a>
Pages
5675–5678
Issue
17
Volume
22
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
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Identification of a novel serum and glucocorticoid regulated kinase-1 (SGK1) ligand from virtual screening.
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
2012
2012-09
Subject
The topic of the resource
Binding Sites; Drug Discovery; Humans; Immediate-Early Proteins/*antagonists & inhibitors/chemistry/metabolism; Ligands; Molecular Docking Simulation; Protein Kinase Inhibitors/*chemistry/*pharmacology; Protein-Serine-Threonine Kinases/*antagonists & inhibitors/chemistry/metabolism
Creator
An entity primarily responsible for making the resource
Geldenhuys Werner J; Talasila Phani K; Sadana Prabodh
Description
An account of the resource
The serum and glucocorticoid regulated kinase-1 (SGK1) is part of the serine/threonine kinase family and has therapeutic potential in several neurodegenerative diseases such as ischemic stroke and Parkinson's disease. Here we use structure-based virtual screening to identify a novel ligand which inhibits SGK1 activity. The data presented here can be used for future scaffold hopping and possible drug development efforts.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.bmcl.2012.06.096" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2012.06.096</a>
Rights
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
2012
Binding Sites
Bioorganic & medicinal chemistry letters
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Drug Discovery
Geldenhuys Werner J
Humans
Immediate-Early Proteins/*antagonists & inhibitors/chemistry/metabolism
Ligands
Molecular Docking Simulation
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Protein Kinase Inhibitors/*chemistry/*pharmacology
Protein-Serine-Threonine Kinases/*antagonists & inhibitors/chemistry/metabolism
Sadana Prabodh
Talasila Phani K
-
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/10.1007/s13346-012-0117-8" target="_blank" rel="noreferrer noopener">http://doi.org/10.1007/s13346-012-0117-8</a>
Pages
309–317
Issue
4
Volume
3
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
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Engineering triiodothyronine (T3) nanoparticle for use in ischemic brain stroke.
Publisher
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Drug delivery and translational research
Date
A point or period of time associated with an event in the lifecycle of the resource
2013
2013-08
Subject
The topic of the resource
Blood-brain barrier; Brain stroke; Nanoparticles; Neuroprotection; Thyroid hormone
Creator
An entity primarily responsible for making the resource
Mdzinarishvili Alexander; Sutariya Vijaykumar; Talasila Phani K; Geldenhuys Werner J; Sadana Prabodh
Description
An account of the resource
A potential means of pharmacological management of ischemic stroke is rapid intervention using potent neuroprotective agents. Thyroid hormone (T3) has been shown to protect against ischemic damage in middle cerebral artery occlusion (MCAO) model of ischemic brain stroke. While thyroid hormone is permeable across the blood-brain barrier, we hypothesized that efficacy of thyroid hormone in ischemic brain stroke can be enhanced by encapsulation in nanoparticulate delivery vehicles. We tested our hypothesis by generating poly-(lactide-co-glycolide)-polyethyleneglycol (PLGA-b-PEG) nanoparticles that are either coated with glutathione or are not coated. We have previously reported that glutathione coating of PLGA-PEG nanoparticles is an efficient means of brain targeted drug delivery. Encapsulation of T3 in PLGA-PEG delivery vehicle resulted in particles that were in the nano range and exhibited a zeta potential of -6.51 mV (uncoated) or -1.70 mV (coated). We observed that both glutathione-coated and uncoated nanoparticles are taken up in cells wherein they stimulated the expression of thyroid hormone response element driven reporter robustly. In MCAO model of ischemic stroke, significant benefit of administering T3 in nanoparticulate form was observed over injection of a T3 solution. A 34 % decrease in tissue infarction and a 59 % decrease in brain edema were seen upon administration of T3 solution in MCAO stroke model. Corresponding measurements for uncoated T3 nanoparticles were 51 % and 68 %, whereas for the glutathione coated were 58 % and 75 %. Our study demonstrates that using nanoparticle formulations can significantly improve the efficacy of neuroprotective drugs in ischemic brain stroke.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1007/s13346-012-0117-8" target="_blank" rel="noreferrer noopener">10.1007/s13346-012-0117-8</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).
2013
Blood-brain barrier
Brain stroke
Department of Pharmaceutical Sciences
Department of Pharmacy Practice
Drug delivery and translational research
Geldenhuys Werner J
Mdzinarishvili Alexander
Nanoparticles
NEOMED College of Graduate Studies
NEOMED College of Pharmacy
Neuroprotection
Sadana Prabodh
Sutariya Vijaykumar
Talasila Phani K
Thyroid hormone