Search results for: Carina Tan

Items from 1 to 7 out of 7 results

article

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

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.

article

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...

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

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...

article

Growth hormone secretagogue receptor family members and ligands

Roy G. Smith, Reid Leonard, Alex R. T. Bailey, Oksana Palyha, more

Endocrine > 2001 > 14 > 1 > 9-14

We have previously reported the cloning and characterization of a new orphan G-protein-coupled receptor (GPC-R), the growth hormone secretagogue receptor (GHS-R), and shown that this receptor mediates the activity of the growth hormone-releasing peptides (GHRPs) and nonpeptide ligands such as L-692,429 and MK-0677. Because the GHS-R obviously does not belong to any of the known GPC-R subfamilies,...

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...

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Search results for: Carina Tan

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

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

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

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

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

Growth hormone secretagogue receptor family members and ligands

Molecular cloning and characterization of a new receptor for galanin

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