Donna L. Hreniuk

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Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective human β3 adrenergic receptor agonists

Gregori J. Morriello, Harvey R. Wendt, Alka Bansal, Jerry Di Salvo, more

Bioorganic & Medicinal Chemistry Letters > 2011 > 21 > 6 > 1865-1870

A novel class of human β ₃ -adrenergic receptor agonists was designed in effort to improve selectivity and metabolic stability versus previous disclosed β ₃ -AR agonists. As observed, many of the β ₃ -AR agonists seem to need the acyclic ethanolamine core for agonist activity. We have synthesized derivatives that constrained this moiety by introduction of a pyrrolidine. This...

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Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists

Alexander Pasternak, Stephen D. Goble, Reynalda K. deJesus, Donna L. Hreniuk, more

Bioorganic & Medicinal Chemistry Letters > 2009 > 19 > 21 > 6237-6240

This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit.

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2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists

Jinlong Jiang, Myle Hoang, Jonathan R. Young, Danny Chaung, more

Bioorganic & Medicinal Chemistry Letters > 2006 > 16 > 20 > 5270-5274

A series of 2-aminoquinoline compounds was prepared and evaluated in MCH1R binding and functional antagonist assays. Small dialkyl, methylalkyl, methylcycloalkyl, and cyclic amines were tolerated at the quinoline 2-position. The in vivo efficacy of compound 12 was explored and compared to that of a related inactive analog to determine their effects on food intake and body weight in rodents.

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4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists

Jinlong Jiang, Peter Lin, Myle Hoang, Lehua Chang, more

Bioorganic & Medicinal Chemistry Letters > 2006 > 16 > 20 > 5275-5279

Structure–activity relationships of a 4-aminoquinoline MCH1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group...

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Characterization of the bombesin-like peptide receptor family in primates

Hideki Sano, Scott D. Feighner, Donna L. Hreniuk, Hisashi Iwaasa, more

Genomics > 2004 > 84 > 1 > 139-146

In mammals, bombesin-like peptides mediate a broad range of physiological functions through binding to three highly conserved G-protein-coupled receptors: the neuromedin B-preferring, the gastrin-releasing peptide-preferring, and the bombesin-receptor subtype 3. Selective modulation of these receptors presents opportunities for the development of novel therapeutics. To ascertain if rhesus monkey could...

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Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats

Lauren P. Shearman, Ramon E. Camacho, D. Sloan Stribling, Dan Zhou, more

European Journal of Pharmacology > 2003 > 475 > 1-3 > 37-47

Central administration of the neuropeptide melanin-concentrating hormone (MCH) stimulates feeding in rodents. We studied the effects of intracerebroventricular (i.c.v.) administration of an MCH-1 receptor agonist (Compound A) and an MCH-1 receptor antagonist (Compound B) on feeding in satiated rats. Compound B (10 μg, i.c.v.) blocked the acute orexigenic effect of Compound A (5 μg, i.c.v.). In an...

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Melanin-Concentrating Hormone Receptor Subtypes 1 and 2: Species-Specific Gene Expression

Carina P. Tan, Hideki Sano, Hisashi Iwaasa, Jie Pan, more

Genomics > 2002 > 79 > 6 > 785-792

To assess the contribution of potential central nervous system pathways implicated in the control of appetite regulation and energy metabolism, it is essential to first identify appropriate animal models. Melanin-concentrating hormone (MCH), a conserved cyclic neuropeptide implicated in the modulation of food intake, has been shown to bind and activate two G-protein-coupled receptors, called GPR24...

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Synthesis and Biological Evaluation in Vitro of Selective, High Affinity Peptide Antagonists of Human Melanin-Concentrating Hormone Action at Human Melanin-Concentrating Hormone Receptor 1

Maria A. Bednarek, Donna L. Hreniuk, Carina Tan, Oksana C. Palyha, more

Biochemistry > 2002 > 41 > 20 > 6383 - 6390

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Short Segment of Human Melanin-Concentrating Hormone That Is Sufficient for Full Activation of Human Melanin-Concentrating Hormone Receptors 1 and 2

Maria A. Bednarek, Scott D. Feighner, Donna L. Hreniuk, Oksana C. Palyha, more

Biochemistry > 2001 > 40 > 31 > 9379 - 9386

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Spiro(indoline-3,4′-piperidine) growth hormone secretagogues as ghrelin mimetics

Brenda L. Palucki, Scott D. Feighner, Sheng-Shung Pong, Karen Kulju McKee, more

Bioorganic & Medicinal Chemistry Letters > 2001 > 11 > 14 > 1955-1957

A series of small molecules derived from MK-0677, a potent synthetic GHS, mimicking the N-terminal Gly-Ser-O-(n-octanoyl)-l-Ser-Phe segment of ghrelin was synthesized and tested in a binding and in a functional assay measuring intracellular calcium elevation in HEK-293 cells expressing hGHSR1a. Replacement of Phe in this tetrapeptide with a spiro(indoline-3,4′-piperidine) group, Gly-Ser with 2-aminoisobutyric...

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Molecular analysis of a new splice variant of the human melanocortin-1 receptor

Carina P. Tan, Karen Kulju McKee, David H. Weinberg, Tanya MacNeil, more

FEBS Letters > 1999 > 451 > 2 > 137-141

The primary hormonal regulator of pigmentation is melanocyte stimulating hormone derived from proopiomelanocortin by proteolytic processing. The melanocortin-1 receptor serves a key role in the regulation of pigmentation. We describe the identification of the first intron within a melanocortin receptor. A new melanocortin-1 receptor isoform, generated by alternative mRNA splicing, encodes an additional...

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Cloning and Characterization of a Human and Murine T-Cell Orphan G-Protein-Coupled Receptor Similar to the Growth Hormone Secretagogue and Neurotensin Receptors

Carina P. Tan, Karen Kulju McKee, Qingyun Liu, Oksana C. Palyha, more

Genomics > 1998 > 52 > 2 > 223-229

Growth hormone secretagogues (GHS) are a group of synthetic peptide and nonpeptide molecules that potently stimulate the release of GH from the anterior pituitary gland through the activation of a novel G-protein-coupled receptor (GPC-R), the GHS-R. In our search for GHS-R family members, we recently described the cloning of two related GPC-Rs, GPR38 and 39. In the present report, we detail the isolation...

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Cloning and Characterization of Two Human G Protein-Coupled Receptor Genes (GPR38 and GPR39) Related to the Growth Hormone Secretagogue and Neurotensin Receptors

Karen Kulju McKee, Carina P. Tan, Oksana C. Palyha, Jim Liu, more

Genomics > 1997 > 46 > 3 > 426-434

The recent cloning of a growth hormone secretagogue receptor (GHS-R) from human pituitary gland and brain identified a third G protein-coupled receptor (GPC-R) involved in the control of growth hormone release. The nucleotide sequence of the GHS-R is most closely related to the neurotensin receptor-1 (NT-R1) (35% overall protein identity). Two human GPC-Rs related to both the type 1a GHS-R and NT-Rs...

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Detection of intracellular calcium elevations in Xenopus laevis oocytes: aequorin luminescence versus electrophysiology

Ryszard Grygorczyk, Scott D. Feighner, Mohammed Adam, K. Liu Ken, more

Journal of Neuroscience Methods > 1996 > 67 > 1 > 19-25

Detection of receptor expression in Xenopus oocytes often relies upon functional coupling to second messengers such as Ca ² ⁺ or cyclic adenosine monophosphate. To detect intracellular Ca ² ⁺ , electrophysiological measurement of the endogenous Ca ² ⁺ -activated chloride current (I _C _I (Ca)) is often used (Dascal, 1987). An alternative utilizes the...

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Search results for: Donna L. Hreniuk

Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective human β3 adrenergic receptor agonists

Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists

2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists

4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists

Characterization of the bombesin-like peptide receptor family in primates

Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats

Melanin-Concentrating Hormone Receptor Subtypes 1 and 2: Species-Specific Gene Expression

Synthesis and Biological Evaluation in Vitro of Selective, High Affinity Peptide Antagonists of Human Melanin-Concentrating Hormone Action at Human Melanin-Concentrating Hormone Receptor 1

Short Segment of Human Melanin-Concentrating Hormone That Is Sufficient for Full Activation of Human Melanin-Concentrating Hormone Receptors 1 and 2

Spiro(indoline-3,4′-piperidine) growth hormone secretagogues as ghrelin mimetics

Molecular analysis of a new splice variant of the human melanocortin-1 receptor

Cloning and Characterization of a Human and Murine T-Cell Orphan G-Protein-Coupled Receptor Similar to the Growth Hormone Secretagogue and Neurotensin Receptors

Cloning and Characterization of Two Human G Protein-Coupled Receptor Genes (GPR38 and GPR39) Related to the Growth Hormone Secretagogue and Neurotensin Receptors

Detection of intracellular calcium elevations in Xenopus laevis oocytes: aequorin luminescence versus electrophysiology

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