Search Results - "Lupisella, John A."
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Preservation of Post-Infarction Cardiac Structure and Function via Long-Term Oral Formyl Peptide Receptor Agonist Treatment
Published in JACC. Basic to translational science (01-12-2019)“…[Display omitted] •Myocardial infarction leads to recruitment of monocyte/macrophages to the injured myocardium to drive infarct healing.•Activation of formyl…”
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2
11β-hydroxysteroid dehydrogenase type 1 gene knockout attenuates atherosclerosis and in vivo foam cell formation in hyperlipidemic apoE⁻/⁻ mice
Published in PloS one (01-02-2013)“…Chronic glucocorticoid excess has been linked to increased atherosclerosis and general cardiovascular risk in humans. The enzyme 11β-hydroxysteroid…”
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3
Formyl peptide receptor 2 and heart disease
Published in Seminars in immunology (01-01-2022)“…Formyl peptide receptor type 2 (FPR2) regulates the initiation and resolution phases of the inflammatory response. In the setting of heart injury and disease,…”
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4
Discovery of Potent, Orally-Active, and Muscle-Selective Androgen Receptor Modulators Based on an N-Aryl-hydroxybicyclohydantoin Scaffold
Published in Journal of medicinal chemistry (28-12-2006)“…A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered through structure-guided modifications of androgen receptor…”
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5
Discovery and Optimization of Aryl Piperidinone Ureas as Selective Formyl Peptide Receptor 2 Agonists
Published in ACS medicinal chemistry letters (12-09-2024)“…We report the discovery and optimization of aryl piperidinone urea formyl peptide receptor 2 (FPR2) agonists from a weakly active high-throughput screening…”
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6
Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists
Published in ACS medicinal chemistry letters (09-06-2022)“…Formyl peptide receptor 2 (FPR2) agonists have shown efficacy in inflammatory-driven animal disease models and have the potential to treat a range of diseases…”
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Selective FPR2 Agonism Promotes a Proresolution Macrophage Phenotype and Improves Cardiac Structure-Function Post Myocardial Infarction
Published in JACC. Basic to translational science (01-08-2021)“…[Display omitted] •MI leads to ischemic damage of myocardium and activation of inflammatory programs as part of the wound healing response.•Selective…”
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8
Inhibition of disease progression by a novel retinoid antagonist in animal models of arthritis
Published in Journal of rheumatology (01-02-2003)“…OBJECTIVE: To investigate the usefulness of a novel retinoic acid receptor (RAR) antagonist (BMS-189453) in animal models of arthritis. METHODS: BMS-189453 was…”
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Pharmacological and X-Ray Structural Characterization of a Novel Selective Androgen Receptor Modulator: Potent Hyperanabolic Stimulation of Skeletal Muscle with Hypostimulation of Prostate in Rats
Published in Endocrinology (Philadelphia) (01-01-2007)“…A novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator (BMS-564929) has been identified, and this compound has…”
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10
N-Aryl-oxazolidin-2-imine Muscle Selective Androgen Receptor Modulators Enhance Potency through Pharmacophore Reorientation
Published in Journal of medicinal chemistry (14-05-2009)“…A novel selective androgen receptor modulator (SARM) scaffold was discovered as a byproduct obtained during synthesis of our earlier series of…”
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11
Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators
Published in Bioorganic & medicinal chemistry letters (01-04-2007)“…SAR relating to the optimization of androgen receptor agonist activity and elimination of mutagenic potential is reported. Pharmacokinetic studies in…”
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12
11[beta]-Hydroxysteroid Dehydrogenase Type 1 Gene Knockout Attenuates Atherosclerosis and In Vivo Foam Cell Formation in Hyperlipidemic apoE.sup.-/- Mice
Published in PloS one (01-02-2013)“…Background Chronic glucocorticoid excess has been linked to increased atherosclerosis and general cardiovascular risk in humans. The enzyme…”
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13
Ligand-induced Conformational Changes in the Human Retinoic Acid Receptor γ Detected Using Monoclonal Antibodies
Published in The Journal of biological chemistry (20-09-1996)“…The mechanism by which the naturally occurring ligand for a nuclear hormone receptor regulates transcription remains largely unknown. One approach combines the…”
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14
The Ligand Binding Domain of the Human Retinoic Acid Receptor γ Is Predominantly α-Helical with a Trp Residue in the Ligand Binding Site (∗)
Published in The Journal of biological chemistry (20-10-1995)“…Retinoic acid exerts its many biological effects by interaction with a nuclear protein, the retinoic acid receptor (RAR). The details of this interaction are…”
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15
The Ligand Binding Domain of the Human Retinoic Acid Receptor Is Predominantly -Helical with a Trp Residue in the Ligand Binding Site
Published in The Journal of biological chemistry (20-10-1995)“…Retinoic acid exerts its many biological effects by interaction with a nuclear protein, the retinoic acid receptor (RAR). The details of this interaction are…”
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16
Ligand-induced Conformational Changes in the Human Retinoic Acid Receptor γ Detected Using Monoclonal Antibodies
Published in The Journal of biological chemistry (20-09-1996)Get full text
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17
Protein synthesis in yeast. Structural and functional analysis of the gene encoding elongation factor 3
Published in The Journal of biological chemistry (15-09-1990)“…The yeast translational elongation factor 3 (EF-3) stimulates EF-1 alpha-dependent binding of aminoacyl-tRNA by the ribosome. The requirement for EF-3 is…”
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