Abstract：
:Recently we have demonstrated that replacing His(6) by constrained amino acids(2) in the well-known antagonist SHU-9119 resulted in potent and selective antagonist ligands especially at the hMC3R and hMC5 receptors. With the aim to further explore position 6 in the sequence of SHU-9119 and MT-II, we have designed, synthesized, and pharmacologically characterized a series of peptide analogues of MT-II and SHU-9119 at the human melanocortin receptors subtypes MC3R, MC4R and MC5R. All these peptides were modified at position 6 with constrained amino acids which are commercially available. In this study, we have identified new selective ligands for the hMC4R, and an antagonist for the hMC3/hMC4 receptors. Additionally, we have discovered an interesting new selective antagonist at the hMC3R, Ac-Nle-c[Asp-betaAla-DNal(2')-Arg-Trp-Lys]-NH(2) (2, PG-106) which represents an important tool in further biological investigations of the hMC3R. PG-106 will be useful in further efforts to differentiate the substructural features responsible for selectivity at the hMC3R, hMC4R, and hMC5R.
journal_name
Peptidesjournal_title
Peptidesauthors
Grieco P,Cai M,Han G,Trivedi D,Campiglia P,Novellino E,Hruby VJdoi
10.1016/j.peptides.2007.02.012subject
Has Abstractpub_date
2007-06-01 00:00:00pages
1191-6issue
6eissn
0196-9781issn
1873-5169pii
S0196-9781(07)00094-0journal_volume
28pub_type
杂志文章相关文献
PEPTIDES文献大全abstract：:alpha-MSH immunoreactive peptides were fractionated and characterized in rat and human brain and rat pituitary by reversed phase high pressure liquid chromatographic techniques. alpha-MSH and deacetylated alpha-MSH were two major naturally existing peptides in both brain and pituitary gland. Subsequent experiments exa...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(81)80126-x
更新日期：1981-10-01 00:00:00
abstract：:CR 1409, a glutaramic acid derivative with competitive cholecystokinin-antagonistic activity, was administered IP and evaluated in comparison with proglumide (the model CCK-receptor antagonist), gabexate (protease inhibitor) and PGE2 (cytoprotective) on two different models of experimental pancreatitis. Acute pancreat...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(86)90147-6
更新日期：1986-11-01 00:00:00
abstract：:Catestatin (CST) is an endogenous neuropeptide with multiple cardiovascular activities. The study is to investigate circulating CST levels in heart failure (HF) patients and to evaluate the role of CST as a biomarker for HF. Plasma CST concentrations were measured by enzyme-linked immunosorbent assay in 228 HF patient...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2013.05.003
更新日期：2013-08-01 00:00:00
abstract：:Previously, calcitonin gene-related peptide (CGRP) decreased food intake when administered ICV but not when administered peripherally to rats. Amylin, which has a close structural homology to CGRP, reduced food intake administered IP at concentrations higher than those previously tested for CGRP. We examined the effec...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(96)00015-0
更新日期：1996-01-01 00:00:00
abstract：:The UII and urotensin II-related peptide (URP) genes belong to the same superfamily as the somatostatin gene. It has been previously shown that somatostatin activates the UII-receptor (UTR). In contrast, the possible interaction between UII and URP and somatostatin receptors has remained scarcely analyzed. Herein, we ...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2007.12.015
更新日期：2008-05-01 00:00:00
abstract：:The hypothalamic neuropeptide orexin A (hypocretin-1) is a key signal in sleep/wake regulation and promotes food intake. We investigated the relationship between cerebrospinal fluid orexin A concentrations and body composition in non-narcoleptic human subjects with a wide range of body weight to gain insight into the ...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2018.02.005
更新日期：2018-04-01 00:00:00
abstract：:Substance P (SP) has been implicated in the pathophysiology of ulcerative colitis (UC) and it has been suggested that blocking of its effect would be advantageous in this disease. Eosinophils have also been implicated in the pathophysiology of UC. In the present study, specimens from the sigmoid colon of UC patients w...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2004.12.018
更新日期：2005-05-01 00:00:00
abstract：:The peptidome of the central nervous system of adult cabbage root fly, Delia radicum (L) was investigated using matrix assisted laser desorption ionization time of flight mass spectrometry (MALDI-TOF MS). Over twenty neuropeptides were identified from three different tissue sources, the combined brain/suboesophageal g...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2010.08.028
更新日期：2011-03-01 00:00:00
abstract：:A novel 6.6 kDa antifungal peptide (NFAP) from the culture supernatant of the mold, Neosartorya fischeri (anamorf: Aspergillus fischerianus), and its encoding gene were isolated in this study. NFAP is a small, basic and cysteine-rich protein consisting of 57 amino acid residues. It shows 37.9-50% homology to similar p...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2011.06.022
更新日期：2011-08-01 00:00:00
abstract：:Bradykinin (BK) has been proposed as the principal mediator of hypersensitivity reactions (HSR) in patients dialyzed using negatively charged membranes and concomitantly treated with angiotensin-converting enzyme (ACE) inhibitors. We investigated the metabolism of exogenous BK added to the sera of 13 patients dialyzed...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(99)00020-0
更新日期：1999-01-01 00:00:00
abstract：:Generally, biomacromolecules, such as DNA, RNA, and proteins, cannot freely permeate into cells from outside the membrane. Protein transduction domains (PTDs) are peptides containing a large number of basic amino acids that can deliver macromolecules into living cells. Arginine-rich intracellular delivery (AID) peptid...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2009.06.006
更新日期：2009-09-01 00:00:00
abstract：:The cholecystokinin receptor-type 1 (CCK1R) is a G-protein coupled receptor localized in the animal gastrointestinal tract. Receptor activation by the natural peptide ligand CCK leads to a feeling of satiety. In this study, hydrolysates from soy and milk proteins were evaluated for their potential to activate the CCK1...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2011.11.019
更新日期：2012-03-01 00:00:00
abstract：:Endothelial neutral endopeptidase (EC 3.4.24.11, NEP) contributes to the inactivation of vasoactive and inflammatory peptides such as f-Met-Leu-Phe, substance P, atrial natriuretic peptide, and bradykinin. The aim of the present study was to investigate the cellular regulation of NEP expression in human endothelial ce...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(95)00077-w
更新日期：1995-01-01 00:00:00
abstract：:The very first step in the study of the endocrine control of insect molting was taken in 1922. Stefan Kopec characterized a factor in the brain of the gypsy moth, Lymantria dispar which appeared to be essential for metamorphosis. This factor was later identified as the neuropeptide prothoracicotropic hormone (PTTH), t...
journal_title：Peptides
pub_type： 杂志文章,评审
doi：10.1016/j.peptides.2009.08.020
更新日期：2010-03-01 00:00:00
abstract：:It is well known that glucoprivation induces the release of counterregulatory hormones such as glucagon, and that the response is attenuated when the stimuli are repeated. Glucoprivation also activates orexigenic neurons and induces hyperphagic responses, although it remains unclear whether these responses are attenua...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2010.12.009
更新日期：2011-04-01 00:00:00
abstract：:Trefoil factors family 2 (TFF2), also known as spasmolytic polypeptide, is primarily expressed in the mucus neck cells of gastrointestinal tracts. It has been proposed that TFF2 plays an important physiological role in protection, repair, and healing of gastrointestinal mucosa. To investigate the cis-acting regulatory...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2003.11.022
更新日期：2004-05-01 00:00:00
abstract：:Intracerebroventricular injections of rat hypothalamic growth hormone-releasing factor (rhGRF) were examined for effects on food intake in free-feeding rats. It was found that, in picomole doses, rhGRF had a stimulatory effect on food intake. Examination of higher doses of rhGRF revealed a decrease in the facilitatory...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(88)90220-3
更新日期：1988-01-01 00:00:00
abstract：:As the frequent emergence of the resistant bacteria, the development of new agents with a new action mode attracts a great deal of interest. It is now widely accepted that antimicrobial peptides (AMPs) are promising alternatives to conventional antibiotics. In this study, antimicrobial peptide polybia-MPI and its anal...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2012.11.002
更新日期：2013-01-01 00:00:00
abstract：:The objective of this study was to investigate absorption enhancing approaches for systemic delivery of methionine enkephalin via the nose. Absorption promotion of methionine enkephalin in the presence of protease inhibitors (bestatin, puromycin) and absorption enhancers (glycocholate, dimethyl-beta-cyclodextrin) were...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2004.02.019
更新日期：2004-04-01 00:00:00
abstract：:NPFF receptors are expressed in several brain regions directly or indirectly involved in cognition and behavior. However, the cognitive effects of the NPFF system have been poorly studied. Therefore, the aim of our study was to analyze the effects of i.c.v. injections of 1 DMe, a stable agonist of NPFF receptors, on b...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2009.11.009
更新日期：2010-02-01 00:00:00
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
更新日期：2020-10-01 00:00:00
abstract：:While neuropeptides of the allatostatin family inhibit in vitro production of juvenile hormone, which modulates aspects of development and reproduction in the cockroach, Diploptera punctata, they are susceptible to inactivation by peptidases in the hemolymph, gut, and bound to internal tissues. Patterns of peptidase c...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(98)00149-1
更新日期：1999-01-01 00:00:00
abstract：:There is a well-documented association between cyclic changes to food intake and the changing ovarian hormone levels of the reproductive cycle in female mammals. Limited research on appetite-controlling gastrointestinal peptides has taken place in females, simply because regular reproductive changes in steroid hormone...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2017.02.010
更新日期：2017-04-01 00:00:00
abstract：:Obestatin regulates fluid and electrolyte homeostasis mainly by opposing the action of vasopressin (AVP). We measured plasma concentration of obestatin and AVP in patients with cardiorenal syndrome (CRS). Plasma AVP and obestatin concentration were measured in 34 patients with type II CRS. The data were compared to th...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2012.08.022
更新日期：2012-12-01 00:00:00
abstract：:Effects of spantide ([D-Arg1,D-Trp7,9,Leu11]substance P) on coronary resistance vessels were studied in isolated guinea pig hearts perfused at constant rate with isotonic buffer containing 20 or 40 mM KCl. Spantide (1 microM) caused a 20-fold rightward shift of the substance P (SP) dose-response curve for vasodilation...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(91)90047-s
更新日期：1991-09-01 00:00:00
abstract：:Numerous works associate the MCH peptide, and the hypothalamic neurons that produce it, to the feeding behavior and energy homeostasis. It is commonly admitted that MCH is an orexigenic peptide, and MCH neurons could be under the control of arcuate NPY and POMC neurons. However, the literature data is not always conco...
journal_title：Peptides
pub_type： 杂志文章,评审
doi：10.1016/j.peptides.2009.07.008
更新日期：2009-11-01 00:00:00
abstract：:Our previous findings that the degree of endotoxin-induced hypotension in the dog is inversely related to ambient temperature (19 degrees through 30 degrees C) and that only increased doses of naloxone are effective at 19 degrees C suggested that opioid activity is also influenced by ambient temperature, increasing in...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(85)90007-5
更新日期：1985-01-01 00:00:00
abstract：:Orexin is one of the orexigenic neuropeptides in the hypothalamus. Orexin neurons in the lateral hypothalamus (LH) project into the cerebral cortex and hippocampus in which the receptors are distributed in high concentrations. Therefore, to elucidate the actions of orexin in the cerebral cortex, we examined its effect...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2008.05.002
更新日期：2008-09-01 00:00:00
abstract：:More than 40 peptides belonging to the -Y/FXFGL-NH(2) allatostatin superfamily have been isolated and identified from the central nervous system (CNS) of the tiger prawn, Penaeus monodon (Crustacea: Penaeidea). The peptides can be arranged in seven sub-groups according to the variable post-tyrosyl residue represented ...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(02)00035-9
更新日期：2002-06-01 00:00:00
abstract：:Increased plasma levels of neuropeptide Y (NPY)-like immunoreactivity (p-NPY-LI) have been described in hemodialysis (HD) patients. In this investigation the effect of a standard HD on p-NPY-LI, analyzed by radioimmunoassay and reverse-phase high performance liquid chromatography (HPLC), was studied. During dialysis p...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(94)00206-l
更新日期：1995-01-01 00:00:00
