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Article ; Online: Atherogenesis on the chopping block.

Gargalovic, Peter S

2009 Volume 9, Issue 5, Page(s) 399–401

Abstract: Endoplasmic reticulum (ER) stress and the unfolded protein response (UPR) are now established features of the atherosclerotic plaque. In this issue, Thorp et al. (2009) provide initial insights into the causative relationship between UPR and the ... ...

Abstract	Endoplasmic reticulum (ER) stress and the unfolded protein response (UPR) are now established features of the atherosclerotic plaque. In this issue, Thorp et al. (2009) provide initial insights into the causative relationship between UPR and the atherosclerotic disease process, specifically linking the proapoptotic mediator CHOP to plaque growth and necrosis.
MeSH term(s)	Animals ; Apolipoproteins E/deficiency ; Apolipoproteins E/genetics ; Apoptosis ; Atherosclerosis/metabolism ; Atherosclerosis/pathology ; Cell Line ; Endoplasmic Reticulum/metabolism ; Humans ; Mice ; Mice, Knockout ; RNA, Small Interfering/metabolism ; Receptors, LDL/deficiency ; Receptors, LDL/genetics ; Transcription Factor CHOP/deficiency ; Transcription Factor CHOP/genetics ; Transcription Factor CHOP/metabolism
Chemical Substances	Apolipoproteins E ; DDIT3 protein, human ; Ddit3 protein, mouse ; Lrp4 protein, mouse ; RNA, Small Interfering ; Receptors, LDL ; Transcription Factor CHOP (147336-12-7)
Language	English
Publishing date	2009-05
Publishing country	United States
Document type	Comment ; Journal Article
ZDB-ID	2176834-1
ISSN	1932-7420 ; 1550-4131
ISSN (online)	1932-7420
ISSN	1550-4131
DOI	10.1016/j.cmet.2009.04.003
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Zs.A 6169: Show issues

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Article ; Online: Apixaban Use in Obese Patients: A Review of the Pharmacokinetic, Interventional, and Observational Study Data.

Jamieson, Michael J / Byon, Wonkyung / Dettloff, Richard W / Crawford, Matthew / Gargalovic, Peter S / Merali, Samira J / Onorato, Joelle / Quintero, Andres J / Russ, Cristina

American journal of cardiovascular drugs : drugs, devices, and other interventions

2022 Volume 22, Issue 6, Page(s) 615–631

Abstract: Relatively little is known about the influence of extreme body weight on the pharmacokinetics (PK), pharmacodynamics (PD), efficacy, and safety of drugs used in many disease states. While direct oral anticoagulants (DOACs) have an advantage over warfarin ...

Abstract	Relatively little is known about the influence of extreme body weight on the pharmacokinetics (PK), pharmacodynamics (PD), efficacy, and safety of drugs used in many disease states. While direct oral anticoagulants (DOACs) have an advantage over warfarin in that they do not require routine drug monitoring, some may regard this convenience as less compelling in obese patients. Some consensus guidelines discourage using DOACs in patients weighing > 120 kg or with a body mass index > 35-40 kg/m
MeSH term(s)	Humans ; Venous Thromboembolism/drug therapy ; Pyridones/adverse effects ; Warfarin/therapeutic use ; Anticoagulants/therapeutic use ; Atrial Fibrillation/drug therapy ; Obesity/complications ; Obesity/drug therapy ; Stroke/epidemiology ; Administration, Oral ; Observational Studies as Topic
Chemical Substances	apixaban (3Z9Y7UWC1J) ; Pyridones ; Warfarin (5Q7ZVV76EI) ; Anticoagulants
Language	English
Publishing date	2022-05-16
Publishing country	New Zealand
Document type	Journal Article ; Review
ZDB-ID	2052547-3
ISSN	1179-187X ; 1175-3277
ISSN (online)	1179-187X
ISSN	1175-3277
DOI	10.1007/s40256-022-00524-x
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Zs.A 5487: Show issues

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Article ; Online: Design and preparation of N-linked hydroxypyridine-based APJ agonists.

Richter, Jeremy M / Alex Bates, J / Gargalovic, Peter / Onorato, Joelle M / Generaux, Claudia / Wang, Tao / Gordon, David A / Wexler, Ruth R / Finlay, Heather J

Bioorganic & medicinal chemistry letters

2022 Volume 73, Page(s) 128882

Abstract: Agonism of the apelin receptor (APJ) has demonstrated beneficial effects in models of heart failure. We have previously disclosed compounds such as 4, which showed good APJ agonist activity but were metabolized to the mono-demethylated, non- ... ...

Abstract	Agonism of the apelin receptor (APJ) has demonstrated beneficial effects in models of heart failure. We have previously disclosed compounds such as 4, which showed good APJ agonist activity but were metabolized to the mono-demethylated, non-interconverting atropisomer metabolites. Herein, we detail the design and optimization of a novel series of N-linked APJ agonists with good potency, metabolic stability, and rat pharmacokinetic profile, which are unable to undergo the same metabolic mono-demethylation cleavage.
MeSH term(s)	Animals ; Apelin ; Apelin Receptors/agonists ; Pyridines ; Rats ; Receptors, G-Protein-Coupled/agonists
Chemical Substances	Apelin ; Apelin Receptors ; Pyridines ; Receptors, G-Protein-Coupled ; hydroxypyridines
Language	English
Publishing date	2022-07-08
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2022.128882
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Zs.A 3203: Show issues

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Article ; Online: Identification of a Hydroxypyrimidinone Compound (

Meng, Wei / Pi, Zulan / Brigance, Robert / Rossi, Karen A / Schumacher, William A / Bostwick, Jeffrey S / Gargalovic, Peter S / Onorato, Joelle M / Luk, Chiuwa E / Generaux, Claudia N / Wang, Tao / Wexler, Ruth R / Finlay, Heather J

Journal of medicinal chemistry

2021 Volume 64, Issue 24, Page(s) 18102–18113

Abstract: This paper describes our continued efforts in the area of small-molecule apelin receptor agonists. Recently disclosed ... ...

Abstract	This paper describes our continued efforts in the area of small-molecule apelin receptor agonists. Recently disclosed compound
MeSH term(s)	Animals ; Apelin Receptors/agonists ; Dogs ; Drug Discovery ; Heart Failure/drug therapy ; Humans ; Pyrimidinones/chemistry ; Pyrimidinones/pharmacokinetics ; Pyrimidinones/pharmacology ; Pyrimidinones/therapeutic use ; Rats ; Structure-Activity Relationship
Chemical Substances	APLNR protein, human ; Apelin Receptors ; Pyrimidinones
Language	English
Publishing date	2021-12-02
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.1c01504
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Zs.B 151: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular ab Jg. 2022: Lesesaal (EG)
Zs.MB 1: Show issues

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Article ; Online: Identification of 6-hydroxy-5-phenyl sulfonylpyrimidin-4(1H)-one APJ receptor agonists.

Tora, George / Jiang, Ji / Bostwick, Jeffrey S / Gargalovic, Peter S / Onorato, Joelle M / Luk, Chiuwa E / Generaux, Claudia / Xu, Carrie / Galella, Michael A / Wang, Tao / He, Yan / Wexler, Ruth R / Finlay, Heather J

Bioorganic & medicinal chemistry letters

2021 Volume 50, Page(s) 128325

Abstract: Heart failure (HF) treatment remains a critical unmet medical need. Studies in normal healthy volunteers and HF patients have shown that [ ... ...

Abstract	Heart failure (HF) treatment remains a critical unmet medical need. Studies in normal healthy volunteers and HF patients have shown that [Pyr
MeSH term(s)	Animals ; Apelin Receptors/agonists ; Area Under Curve ; Cardiovascular Agents/chemical synthesis ; Cardiovascular Agents/pharmacokinetics ; Cardiovascular Agents/pharmacology ; Drug Design ; Half-Life ; Humans ; Intercellular Signaling Peptides and Proteins/chemistry ; Intercellular Signaling Peptides and Proteins/pharmacology ; Macaca fascicularis ; Molecular Structure ; Pyrimidinones/chemistry ; Pyrimidinones/pharmacology ; Rats ; Structure-Activity Relationship
Chemical Substances	APLNR protein, human ; Apelin Receptors ; Cardiovascular Agents ; Intercellular Signaling Peptides and Proteins ; Pyrimidinones ; apelin 13, Pyr(1)-
Language	English
Publishing date	2021-08-14
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2021.128325
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Zs.A 3203: Show issues

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Article: Identification of 6-Hydroxypyrimidin-4(1

Pi, Zulan / Johnson, James A / Meng, Wei / Phillips, Monique / Schumacher, William A / Bostwick, Jeffrey S / Gargalovic, Peter S / Onorato, Joelle M / Generaux, Claudia N / Wang, Tao / He, Yan / Gordon, David A / Wexler, Ruth R / Finlay, Heather J

ACS medicinal chemistry letters

2021 Volume 12, Issue 11, Page(s) 1766–1772

Abstract: The apelin receptor (APJ) is a significant regulator of cardiovascular function and is involved in heart failure and other cardiovascular diseases. ( ... ...

Abstract	The apelin receptor (APJ) is a significant regulator of cardiovascular function and is involved in heart failure and other cardiovascular diseases. (Pyr
Language	English
Publishing date	2021-10-22
Publishing country	United States
Document type	Journal Article
ISSN	1948-5875
ISSN	1948-5875
DOI	10.1021/acsmedchemlett.1c00385
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Article ; Online: In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure.

Gargalovic, Peter / Wong, Pancras / Onorato, Joelle / Finlay, Heather / Wang, Tao / Yan, Mujing / Crain, Earl / St-Onge, Stéphane / Héroux, Madeleine / Bouvier, Michel / Xu, Carrie / Chen, Xue-Qing / Generaux, Claudia / Lawrence, Michael / Wexler, Ruth / Gordon, David

Circulation. Heart failure

2021 Volume 14, Issue 3, Page(s) e007351

Abstract: Background: New heart failure therapies that safely augment cardiac contractility and output are needed. Previous apelin peptide studies have highlighted the potential for APJ (apelin receptor) agonism to enhance cardiac function in heart failure. ... ...

Abstract	Background: New heart failure therapies that safely augment cardiac contractility and output are needed. Previous apelin peptide studies have highlighted the potential for APJ (apelin receptor) agonism to enhance cardiac function in heart failure. However, apelin's short half-life limits its therapeutic utility. Here, we describe the preclinical characterization of a novel, orally bioavailable APJ agonist, BMS-986224. Methods: BMS-986224 pharmacology was compared with (Pyr Results: BMS-986224 was a potent (Kd=0.3 nmol/L) and selective APJ agonist, exhibiting similar receptor binding and signaling profile to (Pyr Conclusions: We identify a novel, potent, and orally bioavailable nonpeptidic APJ agonist that closely recapitulates the signaling properties of (Pyr
Language	English
Publishing date	2021-03-05
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2429459-7
ISSN	1941-3297 ; 1941-3289
ISSN (online)	1941-3297
ISSN	1941-3289
DOI	10.1161/CIRCHEARTFAILURE.120.007351
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Zs.A 6745: Show issues

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Article ; Online: Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.

Johnson, James A / Kim, Soong-Hoon / Jiang, Ji / Phillips, Monique / Schumacher, William A / Bostwick, Jeffrey S / Gargalovic, Peter S / Onorato, Joelle M / Luk, Chiuwa E / Generaux, Claudia / He, Yan / Chen, Xue-Qing / Xu, Carrie / Galella, Michael A / Wang, Tao / Gordon, David A / Wexler, Ruth R / Finlay, Heather J

Journal of medicinal chemistry

2021 Volume 64, Issue 6, Page(s) 3086–3099

Abstract: Apelin-13 is an endogenous peptidic agonist of the apelin receptor (APJ) receptor with the potential for improving cardiac function in heart failure patients. However, the low plasma stability of apelin-13 necessitates continuous intravenous infusion for ...

Abstract	Apelin-13 is an endogenous peptidic agonist of the apelin receptor (APJ) receptor with the potential for improving cardiac function in heart failure patients. However, the low plasma stability of apelin-13 necessitates continuous intravenous infusion for therapeutic use. There are several approaches to increase the stability of apelin-13 including attachment of pharmacokinetic enhancing groups, stabilized peptides, and Fc-fusion approaches. We sought a small-molecule APJ receptor agonist approach to target a compound with a pharmacokinetic profile amenable for chronic oral administration. This manuscript describes sequential optimization of the pyrimidinone series, leading to pyridinone
MeSH term(s)	Animals ; Apelin Receptors/agonists ; Apelin Receptors/metabolism ; Dogs ; Drug Discovery ; Haplorhini ; Humans ; Intercellular Signaling Peptides and Proteins/metabolism ; Male ; Models, Molecular ; Pyridones/chemistry ; Pyridones/pharmacokinetics ; Pyridones/pharmacology ; Rats ; Rats, Sprague-Dawley
Chemical Substances	Apelin Receptors ; Intercellular Signaling Peptides and Proteins ; Pyridones ; apelin-13 peptide
Language	English
Publishing date	2021-03-09
Publishing country	United States
Document type	Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.0c01878
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Zs.B 151: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular ab Jg. 2022: Lesesaal (EG)
Zs.MB 1: Show issues

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Article: Caveolins and macrophage lipid metabolism.

Gargalovic, Peter / Dory, Ladislav

Journal of lipid research

2003 Volume 44, Issue 1, Page(s) 11–21

Abstract: The identification of caveolin-1 more than a decade ago initiated active research into its role in the formation of caveolae, membrane trafficking, signal transduction pathways, and lipid homeostasis. Although caveolins are ubiquitously expressed, the ... ...

Abstract	The identification of caveolin-1 more than a decade ago initiated active research into its role in the formation of caveolae, membrane trafficking, signal transduction pathways, and lipid homeostasis. Although caveolins are ubiquitously expressed, the majority of the available information comes from differentiated cells rich in caveolins, such as fibroblasts, adipocytes, and endothelial cells. During the development of atherosclerosis, macrophages play a pivotal role in the formation of the fatty streak lesions. They take up large amounts of lipids and accumulate in the subendothelial space, forming foam cells that fill up the lesion area. Since caveolins have been implicated in the regulation of cellular cholesterol metabolism in several cell types, it is of interest to examine their potential function in macrophages. In this review, we attempt to summarize current knowledge and views on the role of caveolins in cholesterol metabolism with emphasis on macrophages.
MeSH term(s)	Animals ; Caveolae/metabolism ; Caveolins/genetics ; Caveolins/metabolism ; Cholesterol/metabolism ; Gene Expression Regulation ; Humans ; Lipid Metabolism ; Macrophages/cytology ; Macrophages/metabolism
Chemical Substances	Caveolins ; Cholesterol (97C5T2UQ7J)
Language	English
Publishing date	2003-01
Publishing country	United States
Document type	Journal Article ; Research Support, U.S. Gov't, P.H.S. ; Review
ZDB-ID	80154-9
ISSN	1539-7262 ; 0022-2275
ISSN (online)	1539-7262
ISSN	0022-2275
DOI	10.1194/jlr.r200005-jlr200
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Zs.A 175: Show issues

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Article: Cellular apoptosis is associated with increased caveolin-1 expression in macrophages.

Gargalovic, Peter / Dory, Ladislav

Journal of lipid research

2003 Volume 44, Issue 9, Page(s) 1622–1632

Abstract: Macrophage apoptosis is an important factor in determining the efficiency of the immune response, atherosclerotic lesion stability, and clearance of aged cells by phagocytosis. The involvement of caveolin-1 in the regulation of apoptosis has been ... ...

Abstract	Macrophage apoptosis is an important factor in determining the efficiency of the immune response, atherosclerotic lesion stability, and clearance of aged cells by phagocytosis. The involvement of caveolin-1 in the regulation of apoptosis has been previously suggested in fibroblasts and epithelial cells. Here we show that treatment of thioglycollate-elicited mouse peritoneal macrophages with various unrelated apoptotic agents, including simvastatin, camptothecin, or glucose deprivation, is associated with a specific and large increase in caveolin-1 expression. In contrast, caveolin-2 levels remain unaffected. Induction of apoptosis was measured by changes in cell morphology, annexin V-labeling, and DNA fragmentation. We demonstrate that caveolin-1 in macrophages is present in lipid rafts and colocalizes with phosphatidylserine (PS) at the cell surface of apoptotic macrophages. Our data suggest that caveolin-1 increase is an early event, closely accompanied by PS externalization and independent of caspase activation and nuclear DNA fragmentation. The increase in caveolin-1 levels does not require new protein synthesis, as cycloheximide does not prevent the apoptosis-mediated increase in caveolin-1 levels. We propose that increased levels of caveolin-1 characterize the apoptotic phenotype of macrophages. Caveolin-1 may be involved in the efficient externalization of PS at the surface of the apoptotic cells.
MeSH term(s)	Animals ; Apoptosis/drug effects ; Apoptosis/physiology ; Caspases/metabolism ; Caveolin 1 ; Caveolin 2 ; Caveolins/genetics ; Caveolins/metabolism ; Cells, Cultured ; Enzyme Activation ; Gene Expression Regulation/drug effects ; Macrophages/cytology ; Macrophages/drug effects ; Macrophages/enzymology ; Macrophages/metabolism ; Membrane Microdomains/metabolism ; Mice ; Protein Biosynthesis ; Simvastatin/pharmacology ; Up-Regulation
Chemical Substances	Cav1 protein, mouse ; Caveolin 1 ; Caveolin 2 ; Caveolins ; Simvastatin (AGG2FN16EV) ; Caspases (EC 3.4.22.-)
Language	English
Publishing date	2003-06-01
Publishing country	United States
Document type	Journal Article ; Research Support, U.S. Gov't, P.H.S.
ZDB-ID	80154-9
ISSN	1539-7262 ; 0022-2275
ISSN (online)	1539-7262
ISSN	0022-2275
DOI	10.1194/jlr.M300140-JLR200
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