GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists

Parker, Eric M.; Babij, Carol K; Balasubramaniam, Ambikaipakan; Burrier, Robert E.; Guzzi, M.; Hamud, Fozia; Mukhopadhyay, Gauranga; Rudinski, Mark S; Zou, Tao; Tice, Melissa A.B.; Ling, Xinsheng; Mullins, Deborra; Salisbury, Brian

doi:10.1016/s0014-2999(98)00171-x

Cited by 112 publications

(95 citation statements)

References 27 publications

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“…Crude membrane fractions were isolated from BT-549 cells as previously described (25,26). Membrane fractions were incubated in the binding buffer as described in our previous report (17).…”

Section: Receptor Binding Studies In Bt-549 Cellsmentioning

confidence: 99%

Neuropeptide Y Y5 Receptor Promotes Cell Growth through Extracellular Signal-Regulated Kinase Signaling and Cyclic AMP Inhibition in a Human Breast Cancer Cell Line

Sheriff

Ali

Yahya

et al. 2010

Molecular Cancer Research

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Overexpression of neuropeptide Y (NPY) and its receptor system has been reported in various types of cancers. NPY Y5 receptor (Y5R) has been implicated in cell growth and angiogenesis. However, the role of Y5R in breast cancer is unknown. To identify the role of Y5R in breast cancer, we screened several breast cancer cell lines to examine the expression of Y5R and its function in breast cancer. All screened cell lines express both Y1 receptor and Y5R except BT-549, which expresses mainly Y5R. Binding studies showed that NPY, Y5R-selective agonist peptide, and Y5R-selective antagonist (CGP71683A) displaced

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“…Crude membrane fractions were isolated from BT-549 cells as previously described (25,26). Membrane fractions were incubated in the binding buffer as described in our previous report (17).…”

Section: Receptor Binding Studies In Bt-549 Cellsmentioning

confidence: 99%

Neuropeptide Y Y5 Receptor Promotes Cell Growth through Extracellular Signal-Regulated Kinase Signaling and Cyclic AMP Inhibition in a Human Breast Cancer Cell Line

Sheriff

Ali

Yahya

et al. 2010

Molecular Cancer Research

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“…Cells were harvested 24 hours post-transfection and membranes were prepared as described previously [19], with minor modifications. Briefly, cells were washed twice with PBS and collected in ice cold 50 mM HEPES-KOH, pH 7.4, supplemented with 1X protease inhibitor cocktail (Boehringer Mannheim).…”

Section: Preparation Of Cell Particulatesmentioning

confidence: 99%

“…Radioligand binding assays were performed as described before [19] with minor modifications. The assay buffer contained 20 mM HEPES-NaOH (pH 7.4), 4 mM CaCl 2 , 2 mM MgCl 2 , 50 μM ATP, 0.025%of bacitracin, 10 μg/ml each of leupeptin, pepstatin, aprotinin, chymostatin and antipain, 1 mM phenylmethylsufonyl fluoride, and 2 mg/ml of proteinase-free bovine serum albumin.…”

Section: I-ppyy and 125 I-ppyy 3-36 Binding Assaysmentioning

confidence: 99%

Interaction of NPY compounds with the rat glucocorticoid-induced receptor (GIR) reveals similarity to the NPY–Y2 receptor

et al. 2007

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The rat glucocorticoid induced receptor (rGIR) is an orphan G protein-coupled receptor awaiting pharmacological characterization. Among known receptors, rGIR exhibits highest sequence similarity to the Neuropeptide Y (NPY) -Y 2 receptor (38-40%). The pharmacological profile of rGIR was investigated using 125 I-PYY 3-36 , a Y 2 -preferring radioligand and several NPY analogs. rGIR displayed a similar displacement profile as reported for the Y 2 receptor, in that the Y 2 -selective C terminus fragments of NPY and PYY (NPY 3-36 and PYY 3-36 ) showed high affinity binding and activation of rGIR (low nanomolar range). The rank order potency for displacement was NPY

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“…For example, [Nle 30 ]hPP [25][26][27][28][29][30][31][32][33][34][35][36] and [Leu 34 ]pNPY [25][26][27][28][29][30][31][32][33][34][35][36] were found to be Y 4 R selective partial agonists, 10 and a nonapeptide based on the C-terminal fragment of NPY, Ile-Asn-Pro-Ile-Tyr-Arg-Leu-Arg- [28][29][30][31][32][33][34][35][36] ], also known as 1229U91, showed enhanced potency at both receptor subtypes but is in particular the most potent known Y 1 R antagonist. [13][14][15][16][17] Another of several highly potent Y receptor ligands based upon dimeric C-terminal sequences is D/L-2,7-diaminooctanedioyl-bis(YRLRY-NH 2 ), 1 (BVD-74D) 18 ( Figure 1). …”

Section: Introductionmentioning

confidence: 99%

Optically Pure, Structural, and Fluorescent Analogues of a Dimeric Y₄ Receptor Agonist Derived by an Olefin Metathesis Approach

et al. 2016

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(2016) Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach. Journal of Medicinal Chemistry . ISSN 1520-4804 Access from the University of Nottingham repository: http://eprints.nottingham.ac.uk/34144/1/acs.jmedchem.6b00310.pdf Copyright and reuse:The Nottingham ePrints service makes this work by researchers of the University of Nottingham available open access under the following conditions. This article is made available under the University of Nottingham End User licence and may be reused according to the conditions of the licence. For more details see: http://eprints.nottingham.ac.uk/end_user_agreement.pdf A note on versions:The version presented here may differ from the published version or from the version of record. If you wish to cite this item you are advised to consult the publisher's version. Please see the repository url above for details on accessing the published version and note that access may require a subscription.For more information, please contact eprints@nottingham.ac.uk Just Accepted "Just Accepted" manuscripts have been peer-reviewed and accepted for publication. They are posted online prior to technical editing, formatting for publication and author proofing. The American Chemical Society provides "Just Accepted" as a free service to the research community to expedite the dissemination of scientific material as soon as possible after acceptance. "Just Accepted" manuscripts appear in full in PDF format accompanied by an HTML abstract. "Just Accepted" manuscripts have been fully peer reviewed, but should not be considered the official version of record. They are accessible to all readers and citable by the Digital Object Identifier (DOI®). "Just Accepted" is an optional service offered to authors. Therefore, the "Just Accepted" Web site may not include all articles that will be published in the journal. After a manuscript is technically edited and formatted, it will be removed from the "Just Accepted" Web site and published as an ASAP article. Note that technical editing may introduce minor changes to the manuscript text and/or graphics which could affect content, and all legal disclaimers and ethical guidelines that apply to the journal pertain. ACS cannot be held responsible for errors or consequences arising from the use of information contained in these "Just Accepted" manuscripts. 1Optically pure, structural and fluorescent analogues of a dimeric Y 4 receptor agonist derived by an olefin metathesis approach. 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59

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GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists

Cited by 112 publications

References 27 publications

Neuropeptide Y Y5 Receptor Promotes Cell Growth through Extracellular Signal-Regulated Kinase Signaling and Cyclic AMP Inhibition in a Human Breast Cancer Cell Line

Neuropeptide Y Y5 Receptor Promotes Cell Growth through Extracellular Signal-Regulated Kinase Signaling and Cyclic AMP Inhibition in a Human Breast Cancer Cell Line

Interaction of NPY compounds with the rat glucocorticoid-induced receptor (GIR) reveals similarity to the NPY–Y2 receptor

Optically Pure, Structural, and Fluorescent Analogues of a Dimeric Y₄ Receptor Agonist Derived by an Olefin Metathesis Approach

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GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists

Cited by 112 publications

References 27 publications

Neuropeptide Y Y5 Receptor Promotes Cell Growth through Extracellular Signal-Regulated Kinase Signaling and Cyclic AMP Inhibition in a Human Breast Cancer Cell Line

Neuropeptide Y Y5 Receptor Promotes Cell Growth through Extracellular Signal-Regulated Kinase Signaling and Cyclic AMP Inhibition in a Human Breast Cancer Cell Line

Interaction of NPY compounds with the rat glucocorticoid-induced receptor (GIR) reveals similarity to the NPY–Y2 receptor

Optically Pure, Structural, and Fluorescent Analogues of a Dimeric Y4 Receptor Agonist Derived by an Olefin Metathesis Approach

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Optically Pure, Structural, and Fluorescent Analogues of a Dimeric Y₄ Receptor Agonist Derived by an Olefin Metathesis Approach