Neuropeptide Y 3–36 is an endogenous ligand selective for Y2 receptors

Grandt, Daniel; Schimiczek, M.; Rascher, Wolfgang; Feth, Friedhelm; Shively, John E.; Lee, T.D; Davis, Michael T.; Reeve, Joseph R.; Michel, Martin C.

doi:10.1016/s0167-0115(96)00104-8

Cited by 58 publications

(40 citation statements)

References 22 publications

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“…The observed IC 50 value for Y 2 agonist, NPY 3-36 in our study (3.36 nM) is similar to affinity values reported for the Y 2 receptor expressed in vitro [23,27]. The affinity of NPY for rGIR, however, is 3-30 fold lower than that reported for the Y 2 receptors in in vitro expression systems [7][8][9]23]. Thus, rGIR is distinct from Y 2 receptors in its preference for N-truncated fragments of NPY, over the NPY holopeptide.…”

Section: Pharmacological Specificities Of Rgir: Analogy To the Npy-y supporting

confidence: 85%

“…rGIR binds NPY C-terminus fragments with high affinity. Presence of truncated forms of NPY (NPY ) and PYY (PYY ) have been reported to exist endogenously [9,14,17]. Recent studies have described the importance of N terminal dipeptide cleavage of NPY in regulation of the functional effects of NPY [14].…”

Section: Physiological Implications Of Interaction Between Npy Ligandmentioning

confidence: 99%

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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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Section: Pharmacological Specificities Of Rgir: Analogy To the Npy-y supporting

confidence: 85%

Section: Physiological Implications Of Interaction Between Npy Ligandmentioning

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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“…8,12,24 Y2R is highly expressed in the arcuate nucleus, a major integrator of appetite control in the hypothalamus, but also in other hypothalamic areas, dorsal root ganglia, hippocampus, as well as in peripheral neurons, the intestine and certain blood vessels. [25][26][27][28] Y2R mediates presynaptic actions involving suppression of neurotransmitter release 29 through inhibition of adenylyl activation via Gi.…”

Section: Discussionmentioning

confidence: 99%

“…10,11 In the fasting state, PYY is the dominating form. 9 While PYY and NPY 12 can activate NPY receptors Y1, Y2 and Y5, PYY 3-36 is a selective agonist for the Y2 receptor. 13 Y2R is a seven transmembrane domain G-protein-coupled presynaptic inhibitory autoreceptor, 14 which is highly expressed in NPY neurons within the hypothalamic arcuate nucleus, a key brain area regulating appetite.…”

Section: Introductionmentioning

confidence: 99%

Common neuropeptide Y2 receptor gene variant is protective against obesity among Swedish men

et al. 2005

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Background: Gut hormones and their receptors are considered important in the control of feeding behavior. The gut hormone peptide-YY (PYY) has anorexic effects via the inhibitory neuropeptide Y2 receptor (Y2R) highly expressed in orexigenic NPY/ AGRP neurons within the arcuate nucleus, a major integrator of appetite control in the hypothalamus. Design: Genetic case-control association study of single nucleotide polymorphisms (SNPs) in Y2R and PYY. Subjects: Swedish Caucasians comprising 148 lean, 129 overweight/obese and 226 morbidly obese men. Measurements: Genotypes of the common, silent and conserved SNP Y2R 585T4C and the common SNP PYY Arg72Thr, as well as various obesity-related clinical parameters. Results: Obese men had a lower allele and homozygosity frequency of the common allele 585T4C:T which was particularly evident comparing morbidly obese with lean men (P ¼ 0.002), and analyzing dependence between continuous body mass index (BMI) and genotype (P ¼ 0.002). In agreement, systolic blood pressure tended to be lower in those homozygous for allele T, which was not explained by the BMI -genotype dependence. We found no association to obesity for the PYY Arg72Thr polymorphism, which is located nearby the essential carboxy terminal. Conclusion: A common and conserved variant of the PYY and NPY receptor Y2R is less prevalent among obese compared to among lean Swedish men. This suggests that the common Y2R variant is protective against obesity. Our findings further implicate Y2R in food intake regulation.

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“…Similarly, endogenous NPY 3-36 has been isolated recently from porcine brain tissue extracts (Grandt et al 1996). Of note, human neonates and infants have elevated cord and peripheral blood levels of PYY-LI and, on gel permeation chromatography, the majority of this plasma PYY-LI appears to be of a similar size as PYY 1-36 (Adrian et al 1986).…”

Section: Discussionmentioning

confidence: 99%

Human placenta and fetal membranes contain peptide YY1-36 and peptide YY3-36

Xiao

Han²,

Arany³

et al. 1998

Journal of Endocrinology

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Extracts of human term amniotic, placental, and chorion/ decidua tissue contained, respectively, 4·36 2·79 (pmol/g wet wt; mean ...; n=5), 2·78 0·5 (n=5) and 0·68 0·68 (n=5) peptide YY (PYY)-like immunoreactivity. Using a specific PYY antiserum, gel filtration chromatography and reverse-phase high performance liquid chromatography (HLPC), amniotic, placental and fetal intestinal tissue extracts were demonstrated to contain PYY-like immunoreactivity consisting of equal amounts of PYY 1-36 and PYY . The presence of pancreatic polypeptide was not detected in any of the extracts.Positive immunohistochemical staining for PYY was seen in extravillous trophoblasts in the decidual septa and fetal membranes, the syncytiotrophoblast and cytotrophoblasts, amniotic epithelial cells and in maternal decidual stromal cells. Positive staining for PYY was found at the earliest date examined (9·5 weeks) and remained present throughout pregnancy to term. PYY and PYY 3-36 may play important roles in human pregnancy, acting via endocrine or paracrine mechanisms.

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Neuropeptide Y 3–36 is an endogenous ligand selective for Y2 receptors

Cited by 58 publications

References 22 publications

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

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

Common neuropeptide Y2 receptor gene variant is protective against obesity among Swedish men

Human placenta and fetal membranes contain peptide YY1-36 and peptide YY3-36

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