Search results for: Scott D. Feighner

Items from 1 to 20 out of 25 results

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Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists

Shuwen He, Peter H. Dobbelaar, Jian Liu, Tianying Jian, more

Bioorganic & Medicinal Chemistry Letters > 2010 > 20 > 6 > 1913-1917

We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3.

article

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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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...

article

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...

article

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...

article

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

article

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

article

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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Delay of Intracellular Calcium Transients Using a Calcium Chelator: Application to High-Throughput Screening of the Capsaicin Receptor Ion Channel and G-Protein-Coupled Receptors

Stephan K. Grant, Alka Bansal, Anjalee Mitra, Scott D. Feighner, more

Analytical Biochemistry > 2001 > 294 > 1 > 27-35

Whole-cell functional assays are often used for high-throughput screening (HTS) of molecular targets such as ion channels and G-protein-coupled receptors. A common method for assaying the activity of these membrane proteins is to measure the change in intracellular calcium concentration upon receptor stimulation. These changes in calcium concentration are typically transient and therefore not readily...

article

Orphan G-protein-coupled receptors and natural ligand discovery

Andrew D. Howard, George McAllister, Scott D. Feighner, Qingyun Liu, more

Trends in Pharmacological Sciences > 2001 > 22 > 3 > 132-140

The superfamily of seven-transmembrane-domain G-protein-coupled receptors (GPCRs) is the largest and most diverse group of transmembrane proteins involved in signal transduction. Each of the ~1000 family members found in vertebrates responds to stimuli as diverse as hormones, neurotransmitters, odorants and light, which selectively activate intracellular signaling events mediated by heterotrimeric...

article

Adenosine: A Partial Agonist of the Growth Hormone Secretagogue Receptor

Roy G. Smith, Patrick R. Griffin, Yuan Xu, Alexander G. A. Smith, more

Biochemical and Biophysical Research Communications > 2000 > 276 > 3 > 1306-1313

The growth hormone secretagogue receptor (GHS-R) is involved in the regulation of pulsatile GH release. However, until recently, natural endogenous ligands for the receptor were unknown. We fractionated porcine hypothalamic extracts and assayed fractions for activity on HEK293 cells expressing GHS-R and aequorin. A partial agonist was isolated and identified using microspray tandem mass spectrometry...

article

Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues

Zhixiong Ye, Yingduo Gao, Raman K. Bakshi, Meng-Hsin Chen, more

Bioorganic & Medicinal Chemistry Letters > 2000 > 10 > 1 > 5-8

Quinazolinone derivatives were synthesized and evaluated as non-peptidic growth hormone secretagogues. Modeling guided design of quinazolinone compound 21Scheme 2(a) DMAP, Et₃N, DMF; (b) Gly-OMe (8), heat; (c) NaOH, H₂O, THF; (d) NH₂(CH₂)_nNHBoc, HOBt, EDC, NMM; (e) PhB(OH)₂, Pd(PPh₃)₄, Na₂CO₃; (f) HCl. led to a potency enhancement of greater than 200-fold compared to human growth hormone secretagogue...

article

Reply

Christopher P. Austin, David J. Figueroa, Scott D. Feighner, Andrew D. Howard

Gastroenterology > 1999 > 117 > 6 > 1504

GASTROENTEROLOGY 1999;117:1504

article

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...

article

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...

article

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...

article

Molecular cloning and characterization of a new receptor for galanin

Andrew D Howard, Carina Tan, Lin-Lin Shiao, Oksana C Palyha, more

FEBS Letters > 1997 > 405 > 3 > 285-290

Galanin (GAL) is a widely distributed neuropeptide with diverse biological effects including modulation of hormone release, antinociception and modification of feeding behavior. Its effects are mediated through G-protein-coupled receptors (GPCR) for which only a single type has been cloned, GAL receptor 1 (GALR1). We describe the cloning of a second galanin receptor type, GALR2, from rat hypothalamus...

article

Eimeria tenella 16S RDNA probes

Prasanta R Chakraborty, Michael Dashkevicz, Alex Elbrecht, Scott D Feighner, more

Biotechnology Advances > 1997 > 15 > 2 > 460

Unique species-specific Eimeria tenella DNA probes comprising divergent DNA sequences are disclosed. The probes are complementary to a small subunit ribosomal RNA gene of Eimeria tenella.

article

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...

article

Eimeria praecox 16s rDNA probes

Prasanta R Chakraborty, Michael Dashkevicz, Alex Elbrecht, Scott D Feighner, more

Biotechnology Advances > 1996 > 14 > 4 > 478

Unique species-specific Eimeria praecox DNA probes comprising divergent DNA sequences are disclosed. The probes are complementary to a small subunit ribosomal RNA gene of Eimeria praecox.

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Search results for: Scott D. Feighner

Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists

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

Delay of Intracellular Calcium Transients Using a Calcium Chelator: Application to High-Throughput Screening of the Capsaicin Receptor Ion Channel and G-Protein-Coupled Receptors

Orphan G-protein-coupled receptors and natural ligand discovery

Adenosine: A Partial Agonist of the Growth Hormone Secretagogue Receptor

Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues

Reply

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

Molecular cloning and characterization of a new receptor for galanin

Eimeria tenella 16S RDNA probes

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

Eimeria praecox 16s rDNA probes

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