Research Topics
| Ester Carballo JaneSummaryAffiliation: Merck Research Laboratories Country: USA Publications
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Detail Information
Publications
ApoA-I mimetic peptides promote pre-β HDL formation in vivo causing remodeling of HDL and triglyceride accumulation at higher doseEster Carballo-Jane
Merck Research Laboratories, 126 East Lincoln Avenue, RY80Y 140, Rahway, NJ 07065, USA
Bioorg Med Chem 18:8669-78. 2010..These results suggest our peptide design confers activities that are potentially anti-atherogenic. However a dosing regimen which maximizes their therapeutic properties while minimizing adverse effects needs to be established...
Potential role for epidermal Langerhans cells in nicotinic acid-induced vasodilatation in the mouseE Carballo-Jane
Department of Pharmacology, Merck Research Laboratories, Rahway, PO Box 2000, RY80Y 140, Rahway, New Jersey 07065, USA
Inflamm Res 56:254-61. 2007..Our objective is to study the role of cutaneous Langerhans cells on a mouse model of nicotinic acid-induced vasodilatation...- Comparison of rat and dog models of vasodilatation and lipolysis for the calculation of a therapeutic index for GPR109A agonistsEster Carballo-Jane
Department of Pharmacology, Merck Research Laboratories, Rahway, NJ, USA
J Pharmacol Toxicol Methods 56:308-16. 2007..The rat and the dog have previously been used to study the antilipolytic effects of nicotinic acid, but no optimal vasodilatation model exits in either species... - Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemiaDarby Schmidt
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 19:4768-72. 2009..One analog, 23, showed improved potency and lacked flushing at doses that effectively altered the lipid profile of rats... - Molecular modeling aided design of nicotinic acid receptor GPR109A agonistsQiaolin Deng
Department of Molecular Systems, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 18:4963-7. 2008..The designed compounds were synthesized, and showed significantly improved binding affinity and activation of GPR109A... - Discovery of betamethasone 17alpha-carbamates as dissociated glucocorticoid receptor modulators in the ratAmjad Ali
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, United States
Bioorg Med Chem 16:7535-42. 2008..Taken together, these results indicate that dissociated glucocorticoid receptor modulators can be identified in rodents... - Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109AHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 17:6723-8. 2007..Compound 1a displayed good PK, better in vivo efficacy in reducing FFA in mouse than niacin, and no vasodilation in a mouse model. Compound 1q demonstrated equal affinity to GPR109A as niacin... - Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptorHong C Shen
Merck Research Laboratories, Merck and Co, Inc, Rahway, New Jersey 07065 0900, USA
J Med Chem 50:6303-6. 2007..Compound 2i exhibited good in vivo antilipolytic efficacy while providing a significantly improved therapeutic index over vasodilation (flushing) with respect to niacin in the mouse model... - Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammationSTEPHEN J O'KEEFE
Department of Immunology, Merck Research Laboratories, Rahway, New Jersey 07065, USA
J Biol Chem 282:34663-71. 2007..Similarly, p38beta knock-out mice respond normally to inflammatory stimuli. These results demonstrate conclusively that specific inhibition of the p38alpha isoform is necessary and sufficient for anti-inflammatory efficacy in vivo... - Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experimentsChristopher F Thompson
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 17:3354-61. 2007..Two compounds were profiled in vivo and shown to reduce inflammation in a mouse model. An active metabolite is suspected in one case... - p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffoldSwaminathan R Natarajan
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 16:5468-71. 2006..Compound 16 reduced inflammation in animal disease models at EC(50) doses as low as 0.2mpk... - Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activityCameron J Smith
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 15:2926-31. 2005..Of these compounds, 27, 28, and 35 were evaluated further in a mouse LPS-induced TNF-alpha secretion model. Compound 28 had an ED(50) of 14.1 mg/kg compared with 0.5 mg/kg for prednisolone in the same assay... - Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacyChristopher F Thompson
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 15:2163-7. 2005..These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse... - Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activityAmjad Ali
Departments of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, New Jersey 07065, USA
J Med Chem 47:2441-52. 2004..The thiophenyl analogue 25 was evaluated in vivo in the mouse LPS challenge model and showed an ED(50) = 4.0 mg/kg, compared to 0.5 mg/kg for prednisolone in the same assay... - Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidateHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, Rahway, New Jersey 07065 0900, USA mail
J Med Chem 53:2666-70. 2010.... - Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)Songnian Lin
Merck Research Laboratories, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 19:3238-42. 2009..The synthesis, structure-activity relationship (SAR), and biological evaluation of these compounds are discussed... - Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in ratsHong C Shen
Departments of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, Rahway, New Jersey 07065 0900, USA
J Med Chem 52:2587-602. 2009.... - GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109aJason E Imbriglio
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, Rahway, NJ 07065 0900, United States
Bioorg Med Chem Lett 19:2121-4. 2009..5-Alkyl and aryl-pyrazole-tetrazoles have been identified as a new class of selective, small-molecule, agonists of the human G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid... - Altered lipoprotein metabolism in P2Y(13) knockout miceDaniel Blom
Department of Cardiovascular Diseases, Merck and Co, Inc, Rahway, NJ 07065, USA
Biochim Biophys Acta 1801:1349-60. 2010..Taken together, our experiments assess a role for the purinergic receptor P2Y(13) in the regulation of lipoprotein metabolism and demonstrate that modulating its activity could be of benefit to the treatment of dyslipidemia in people... - GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109aJason E Imbriglio
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 20:4472-4. 2010..5-Alkyl and aryl-pyrazole-acids have been identified as a new class of selective, small-molecule, agonists of the human orphan G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid... - Anthranilic acid replacements in a niacin receptor agonistDarby Schmidt
Department of Medicinal Chemistry, Merck and Co, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 20:3426-30. 2010..In order to improve efficacy and provide structural diversity, replacements for the anthranilic acid were investigated and several compounds with improved properties were identified... - Skeletal muscle: a dual system to measure glucocorticoid-dependent transactivation and transrepression of gene regulationEster Carballo-Jane
Merck Research Laboratories, Department of Pharmacology, P.O. Box 2000, Rahway, NJ 07065, USA
J Steroid Biochem Mol Biol 88:191-201. 2004..Thus, skeletal muscle cells and tissues present a novel system for the identification of selective GR-binding ligands, which simultaneously inhibit cytokine expression in the absence of GS induction... - 3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in miceGraeme Semple
Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, California 92121, USA
J Med Chem 51:5101-8. 2008..Moreover, preadministration of 5a blocked the flushing effect induced by nicotinic acid but not that induced by PGD2. This profile made 5a a suitable candidate for further study for the treatment of dyslipidemia...