Functional characterization of the modified melanocortin peptides responsible for ligand selectivity at the human melanocortin receptors.

Abstract:

:The melanocortin system plays an important role in energy homeostasis as well as skin pigmentation, steroidogenesis and exocrine gland function. In this study, we examined eight Ac-His-Phe-Arg-Trp-NH(2) tetrapeptides that were modified at the Phe position and pharmacologically characterized their activities at the human MCR wild-types and their mutants. Our results indicate that at the hMC1R, all D stereochemical modified residues at the Phe position of peptides increase cAMP production in a dose-dependent manner. At the hMC3R, the DPhe peptide dose dependently increases cAMP production but all other three tetrapeptides were not. At the hMC4R, both the DPhe and DNal(1') peptides induce cAMP production. However, both DTyr and DNal(2') were not able to induce cAMP production. Further studies indicated that at the hMC1R M128L mutant receptor, the all D-configured tetrapeptides reduce their potencies as compared to that of hMC1R wild-type. However, at the hMC3R and hMC4R L165M and L133M mutant receptors, the DNal(2') and DTyr tetrapeptides possess agonist activity. These findings indicate that DPhe in tetrapeptide plays an important role in ligand selectivity and specific residue TM3 of the melanocortin receptors is crucial for ligand selectivity.

journal_name

Peptides

journal_title

Peptides

authors

Chen M,Georgeson KE,Harmon CM,Haskell-Luevano C,Yang Y

doi

10.1016/j.peptides.2006.04.012

subject

Has Abstract

pub_date

2006-11-01 00:00:00

pages

2836-45

issue

11

eissn

0196-9781

issn

1873-5169

pii

S0196-9781(06)00202-6

journal_volume

27

pub_type

杂志文章

相关文献

PEPTIDES文献大全
  • Secondary structure of antisauvagine analogues is important for CRF receptor antagonism: development of antagonists with increased potency and receptor selectivity.

    abstract::Antisauvagine-30 (aSVG) is the only high-affinity antagonist for the corticotropin-releasing factor (CRF) type 2 (CRF(2)) receptor. A structure-activity relationship study was performed to pinpoint residues conferring aSVG's selectivity. The aSVG-analogues being N-terminally extended by one or two residues or containi...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/s0196-9781(02)00139-0

    authors: Brauns O,Brauns S,Jenke M,Zimmermann B,Dautzenberg FM

    更新日期:2002-10-01 00:00:00

  • Conformational states of the corticotropin releasing factor 1 (CRF1) receptor: detection, and pharmacological evaluation by peptide ligands.

    abstract::Previous corticotropin releasing factor 1 (CRF1) receptor characterization has been performed using radiolabeled agonists, which bind predominantly the receptor-G-protein complex. The pharmacological profile of other receptor states, and their abundance, remain poorly characterized. Here we investigated the affinity s...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2003.09.002

    authors: Hoare SR,Sullivan SK,Pahuja A,Ling N,Crowe PD,Grigoriadis DE

    更新日期:2003-12-01 00:00:00

  • Marked ion dependence of 125I-angiotensin I binding to atypical sites on Mycoplasma hyorhinis.

    abstract::125I-Ang I binding to atypical sites on Mycoplasma hyorhinis-contaminated IEC-18 cell membranes increased with increasing pH and [NaCl] (ED50 at 500 mM; maximal 13-fold increase at 2 M NaCl). Alkali metal chlorides and sodium halides increased binding with rank orders of Na+ < K+ < Rb+ < Cs+ = Li+ and F- < Cl- < Br < ...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/s0196-9781(98)00163-6

    authors: Smith RD

    更新日期:1999-01-01 00:00:00

  • Multiple Y receptors mediate pancreatic polypeptide responses in mouse colon mucosa.

    abstract::A functional study has been performed to characterise the Y receptors responsible for NPY, PYY and PP-stimulated responses in mouse colonic mucosal preparations. Electrogenic ion secretion was stimulated with VIP following which NPY, PYY and PP analogues were, to varying degrees, inhibitory. PYY(3-36), hPP, Gln(23)hPP...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/s0196-9781(01)00355-2

    authors: Cox HM,Pollock EL,Tough IR,Herzog H

    更新日期:2001-03-01 00:00:00

  • The role of caudate nucleus in dermorphin-induced catalepsy in rats.

    abstract::Bilateral electrolytic lesions of caudate nucleus were observed to potentiate the cataleptic response, and to prevent the muscular rigidity produced by intracerebroventricular injection or infusion of dermorphin. These results suggest that caudate nucleus plays an inhibitory role in controlling the cataleptic response...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(85)90368-7

    authors: Improta G,Guglietta A

    更新日期:1985-01-01 00:00:00

  • Sauvagine: effects on gastric acid secretion in rats.

    abstract::Intracerebroventricular (ICV) and subcutaneous (SC) injections of sauvagine powerfully inhibited gastric acid secretion stimulated by gastric distension and by 2-deoxy-D-glucose, but not by histamine in pylorus-ligated rats. Naloxone failed to antagonize the antisecretory effects of SC and ICV sauvagine. Intravenous i...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(88)90131-3

    authors: Improta G,Broccardo M

    更新日期:1988-07-01 00:00:00

  • The Y1 receptor for NPY: a key modulator of the adaptive immune system.

    abstract::Growing evidence suggests that the neuropeptide Y (NPY) system plays an important role in the immune system. Yet, little is known about the expression of NPY and receptors in the immune system. Moreover, original contradicting results have confused the picture and hampered a clear understanding of its role in the immu...

    journal_title:Peptides

    pub_type: 杂志文章,评审

    doi:10.1016/j.peptides.2006.09.030

    authors: Wheway J,Herzog H,Mackay F

    更新日期:2007-02-01 00:00:00

  • Oxyntomodulin and its C-terminal octapeptide inhibit liquid meal-stimulated acid secretion.

    abstract::Oxyntomodulin (OXM), a 37-amino acid glucagon-containing peptide produced mainly in intestine and endocrine pancreas, is present in rat plasma and inhibits pentagastrin-stimulated gastric acid secretion in both the anesthetized and the conscious rat. In order to investigate the modifications in acid and water secretio...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(86)90196-8

    authors: Jarrousse C,Niel H,Audousset-Puech MP,Martinez J,Bataille D

    更新日期:1986-01-01 00:00:00

  • A comparison of leptin and ghrelin levels in plasma and saliva of young healthy subjects.

    abstract::In the last 10 years, saliva has been increasingly used as a diagnostic fluid and in predictions of disease progression. Leptin and ghrelin are synthesized in several tissues including the salivary glands. The action of ghrelin is antagonistic to that of leptin. This study was undertaken to measure and compare the sal...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2004.11.008

    authors: Aydin S,Halifeoglu I,Ozercan IH,Erman F,Kilic N,Aydin S,Ilhan N,Ilhan N,Ozkan Y,Akpolat N,Sert L,Caylak E

    更新日期:2005-04-01 00:00:00

  • Determination of the site of action of calcitonin gene-related peptide in the alteration of intracellular calcium levels in adult and neonatal rodent myocytes.

    abstract::The purpose of this study is to elucidate the mechanism of action and site of action of calcitonin gene-related peptide (CGRP) and its effects on calcium concentrations in two types of cardiomyocytes, neonatal and adult, by employing real-time fluorescence imaging. CGRP caused an increase in intramyocytic calcium with...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2005.04.021

    authors: Bick RJ,Poindexter BJ,Davis RA,Schiess MC

    更新日期:2005-11-01 00:00:00

  • Water intake modifications induced by tachykinins, bombesins and opioid peptides.

    abstract::Nonmammalian peptides of the tachykinin, bombesin and opioid families, injected into the brain ventricles, potently and specifically affect drinking behaviour of rats and pigeons. These peptides, or at least their counterparts, have been found in the brain of mammals and birds. It has been hypothesized that these endo...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(85)90372-9

    authors: de Caro G,Massi M

    更新日期:1985-01-01 00:00:00

  • Relationship of alpha MSH-specific neurons to the arcuate opiocortin neuronal system as determined by dual antigen immunocytochemical procedures.

    abstract::The cross-immunoreactivity, topography, and fiber projections of the alpha MSH-immunoreactive specific neurons in the forebrain of the rat appear to be distinctly different from that of the neurons in the hypothalamic arcuate opiocortin system. The cell bodies, immunoreactive only to alpha-MSH, have a specific pattern...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(84)90176-1

    authors: Piekut DT,Knigge KM

    更新日期:1984-11-01 00:00:00

  • C-type natriuretic peptide and its relation to non-invasive indices of left ventricular function in patients with chronic heart failure.

    abstract::C-type natriuretic peptide (CNP) significantly increases in chronic heart failure (CHF) patients as a function of clinical severity. Aim of this study was to evaluate in CHF patients the relationship between circulating CNP concentrations and echo-Doppler conventional indices of left ventricular (LV) function as well ...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2007.10.022

    authors: Del Ry S,Maltinti M,Cabiati M,Emdin M,Giannessi D,Morales MA

    更新日期:2008-01-01 00:00:00

  • Detection of neuropeptides in vivo and open questions for current and upcoming fluorescent sensors for neuropeptides.

    abstract::During a stress response, various neuropeptides are secreted in a spatiotemporally coordinated way in the brain. For a precise understanding of peptide functions in a stress response, it is important to investigate when and where they are released, how they diffuse, and how they are broken down in the brain. In the pa...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2020.170456

    authors: Inutsuka A,Ino D,Onaka T

    更新日期:2020-11-24 00:00:00

  • Amylin brain circuitry.

    abstract::Amylin is a peptide hormone that is mainly known to be produced by pancreatic β-cells in response to a meal but amylin is also produced by brain cells in discrete brain areas albeit in a lesser amount. Amylin receptor (AMY) is composed of the calcitonin core-receptor (CTR) and one of the 3 receptor activity modifying ...

    journal_title:Peptides

    pub_type: 杂志文章,评审

    doi:10.1016/j.peptides.2020.170366

    authors: Boccia L,Gamakharia S,Coester B,Whiting L,Lutz TA,Le Foll C

    更新日期:2020-10-01 00:00:00

  • The effect of halogenation on the antimicrobial activity, antibiofilm activity, cytotoxicity and proteolytic stability of the antimicrobial peptide Jelleine-I.

    abstract::Antimicrobial peptides (AMPs) are believed to be a promising class of antimicrobial agents against bacteria and fungi. To promote the clinical use of AMPs, their antimicrobial activity and susceptibility to protease degradation should be further improved. The antimicrobial peptide Jelleine-I was originally isolated fr...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2018.11.006

    authors: Jia F,Zhang Y,Wang J,Peng J,Zhao P,Zhang L,Yao H,Ni J,Wang K

    更新日期:2019-02-01 00:00:00

  • Scorpion venom peptides with no disulfide bridges: a review.

    abstract::Scorpion venoms are rich sources of biologically active peptides that are classified into disulfide-bridged peptides (DBPs) and non-disulfide-bridged peptides (NDBPs). DBPs are the main scorpion venom components responsible for the neurotoxic effects observed during scorpion envenomation as they usually target membran...

    journal_title:Peptides

    pub_type: 杂志文章,评审

    doi:10.1016/j.peptides.2013.10.021

    authors: Almaaytah A,Albalas Q

    更新日期:2014-01-01 00:00:00

  • Bioactivities and secondary structure of mast cell degranulating (MCD) peptide analogs.

    abstract::Three analogs of Mast Cell Degranulating (MCD) peptide with C-terminal and one analog with N- and C-terminal deletions were synthesized and assayed for histamine-releasing activity in mast cells. Des(20-22)-MCD and des(21)-MCD markedly decreased this activity. In des(16-17,21)-MCD this activity was completely abolishe...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/s0196-9781(97)00253-2

    authors: Buku A,Maulik G,Hook WA

    更新日期:1998-01-01 00:00:00

  • Thermoregulatory, behavioral and seizure modulatory effects of AVP in the gerbil.

    abstract::Recent reports suggest that arginine vasopressin (AVP) may be an endogenous antipyretic peptide and a mediator of febrile convulsions [10,12]. The spontaneously seizing Mongolian gerbil was used to investigate the thermoregulatory, behavioral and seizure modulatory effects of AVP. Injection of AVP (1.0 and 5.0 microgr...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(83)90070-0

    authors: Lee RJ,Lomax P

    更新日期:1983-11-01 00:00:00

  • Dynamics of diapause hormone and prothoracicotropic hormone transcript expression at diapause termination in pupae of the corn earworm, Helicoverpa zea.

    abstract::Both diapause hormone (DH) and ecdysone (E) are capable of terminating pupal diapause in members of the Helicoverpa/Heliothis complex. In this study we examine how the transcript encoding prothoracicotropic hormone (PTTH), the neuropeptide that stimulates the prothoracic gland to produce E, and the transcript encoding...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2011.05.019

    authors: Zhang Q,Denlinger DL

    更新日期:2012-03-01 00:00:00

  • Secretion of neurophysins during luteal regression in the goat.

    abstract::In non-pregnant goats, ovariectomy on day 12 of oestrous cycle resulted in parallel decrease of oxytocin and progesterone jugular concentration. Similarly, luteolysis, indicated by decreasing progesterone concentration, was accompanied by simultaneous release of oxytocin and oxytocin-associated neurophysins (mean of n...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(87)90063-5

    authors: Homeida AM

    更新日期:1987-09-01 00:00:00

  • Neuropeptide Y microinjected into the suprachiasmatic region phase shifts circadian rhythms in constant darkness.

    abstract::The geniculohypothalamic tract (GHT) is a projection from the intergeniculate leaflet to the suprachiasmatic nucleus (SCN). The GHT exhibits neuropeptide Y (NPY) immunoreactivity and appears to communicate photic information to the SCN. Microinjection of NPY into the SCN has been found to phase shift circadian rhythms...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(94)90126-0

    authors: Huhman KL,Albers HE

    更新日期:1994-01-01 00:00:00

  • Apelin alleviates diabetes-associated endoplasmic reticulum stress in the pancreas of Akita mice.

    abstract::Apelin, a newly identified bioactive adipokine, has been found to play important roles in multiple diseases, including diabetes, hypertension and cardiovascular diseases with unclear molecular mechanisms. The present study aimed to investigate the effects of apelin on endoplasmic reticulum (ER) stress in the pancreas ...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2011.06.025

    authors: Chen H,Zheng C,Zhang X,Li J,Li J,Zheng L,Huang K

    更新日期:2011-08-01 00:00:00

  • Blockade of dynorphin A(1-13) overt psychomotor effects by naloxone.

    abstract::Each of the dynorphin A(1-13) or dynorphin (dyn) treatment groups receiving naloxone showed a significant overall reduction of overt signs compared with the dyn controls. The data suggested that the overt psychomotor effects of dyn in the rhesus monkey were especially prone to blockade by naloxone, and probably involv...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(92)90196-a

    authors: Aceto MD,Bowman ER

    更新日期:1992-07-01 00:00:00

  • Urotensin II inhibits the proliferation but not the differentiation of cardiac side population cells.

    abstract::Urotensin II (UII) induces the development of cardiac remodeling and atherosclerosis by promoting hypertrophy of cardiomyocytes and mitogenesis of fibroblasts and vascular smooth muscle cells. But its effect on cardiac side population cells (CSPs), one of somatic stem cells, is unclear. The present study examined the ...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2011.01.024

    authors: Gong H,Ma H,Liu M,Zhou B,Zhang G,Chen Z,Jiang G,Yan Y,Yang C,Kanda M,Wu J,Yuan J,Li L,Nagai T,Komuro I,Ge J,Zou Y

    更新日期:2011-05-01 00:00:00

  • Blood pressure modulation following activation of mast cells by cationic cell penetrating peptides.

    abstract::Short cell penetrating peptides (CPP) are widely used in vitro to transduce agents into cells. But their systemic effect has not been yet studied in detail. We studied the systemic effect of the cell penetrating peptides, penetratin, transportan and pro-rich, on rat hemodynamic functions. Intra-arterial monitoring of ...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2011.09.017

    authors: Basheer M,Schwalb H,Shefler I,Levdansky L,Mekori YA,Gorodetsky R

    更新日期:2011-12-01 00:00:00

  • Central effects of the peptides, SchistoFLRFamide and proctolin, on locust oviduct contraction.

    abstract::We have developed a semi-intact preparation-consisting of an isolated oviduct with abdominal ganglia VII and VIII intact and attached-with which to characterize the effects on oviduct contraction, of peptides that are bath applied to CNS tissues. The work presented here offers a qualitative analysis of the central eff...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/s0196-9781(02)00173-0

    authors: Kwok R,Orchard I

    更新日期:2002-11-01 00:00:00

  • Production of VIP- and PHM (human PHI)-related peptides in human neuroblastoma cells.

    abstract::We demonstrated the production and release of a peptide structurally identical with porcine and bovine VIP-28 in human neuroblastoma NB-OK-1 cell line. In the cells, VIP-like immunoreactive (IR-VIP) components of 8 K dalton (Kd), 11 Kd, 18 Kd and 30 Kd were also detected and the 8 Kd and 18 Kd components were apparent...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(84)90199-2

    authors: Hoshino M,Yanaihara C,Ogino K,Iguchi K,Sato H,Suzuki T,Yanaihara N

    更新日期:1984-03-01 00:00:00

  • Effect of Met-enkephalin and opioid antagonists on rat macrophages.

    abstract::Effects of Met-enkephalin (Met-ENK) and opioid antagonists on H2O2 release by peritoneal macrophages from DA and AO rats were investigated. Met-ENK increased and decreased H2O2 production by macrophages of DA and AO rats, respectively. These effects were antagonized by low, but not high, concentrations of naloxone and...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/0196-9781(95)02003-f

    authors: Radulović J,Dimitrijević M,Laban O,Stanojević S,Vasiljević T,Kovacević-Jovanović V,Marković BM

    更新日期:1995-01-01 00:00:00

  • Transcriptional regulation of guanylyl cyclase/natriuretic peptide receptor-A gene.

    abstract::Activation of natriuretic peptide receptor-A (NPRA) produces the second messenger cGMP, which plays a pivotal role in maintaining blood pressure and cardiovascular homeostasis. In the present study, we have examined the role of trans-acting factor Ets-1 in transcriptional regulation of Npr1 gene (coding for NPRA). Usi...

    journal_title:Peptides

    pub_type: 杂志文章

    doi:10.1016/j.peptides.2006.01.004

    authors: Kumar P,Arise KK,Pandey KN

    更新日期:2006-07-01 00:00:00