Abstract:
:Pharmacological study of Phe-Met-Leu-Phe-amide (FMRFa) receptors is hindered by the lack of selective ligands. The classification of these selective ligands is further hampered by the limited availability of functional assays. In this study, we evaluated several synthetic FMRFa analogs for agonist and antagonist activity by measuring their abilities to produce [35-S]-GTP-gamma-S stimulation or to inhibit FMRFa-induced [35S]-GTP-gamma-S binding in squid optic lobes. Analogs included acetyl-Phe-norLeu-Arg-Phe-amide (acFnLRFa), desamino-Tyr-Phe-Leu-Arg-amide (daYFLRa), desamino Tyr-Phe-norLeu-Arg-Phe-amide (daYFnLRFa), desamino Tyr-Phe-norLeu-Arg-[TIC]-amide (daYFnLR[TIC]a), desamino Tyr-Trp-norLeu-Arg-amide (daYWnLRa), (D)-Tyr-Phe-norLeu-Arg-Phe-amide (D)-YFnLRFa), Phe-Leu-Arg-Phe-amide (FLRFa), and the D-amino acid analogs of FMRFa (D-FMRFa, F-(D)-MRFa and FM-(D)-RFa). For agonist studies, full dose-response curves were generated and analyzed for potency and efficacy (maximal percent effect). FMRFamide as well as analogs ac-FnLRFa, daYFnLRFa, daYFnLR[TIC]a, D-YFnLRFa, FLRFa, and (D)-FMRFa stimulated [35S]-GTP-gamma-S binding. Analogs daYWnLRa, daYFLRa, F-(D)-MRFa, and FM-(D)-RFa failed to stimulate either [35S]-GTP-gamma-S binding or to inhibit FMRFa-induced [35S]-GTP-gamma-S binding. The rank order of potency was daYFnLRFa > or = daYFnLRF[TIC]a > acFnLRFa > (D)YFnLRFa > FLRFa > or = FMRFa > (D)-FMRFa. The order of efficacy was daYFnLRFa = acFnLRFa = (D)-YFnLRFa > FLRFa = FMRFa > or = (D)-FMRFa > or = daYFnLRF[TIC]a. Peptide analog daYFnLR[TIC]a was less efficacious (59% maximal stimulation) than analogs daYFnLRFa, acFnLRFa, and (D)-YFnLRFa (113-146% maximal stimulation). A maximal concentration of daYFnLR[TIC]a (10 microM) reduced daYFnLRFa, acFnLRFa, and (D)-YFnLRFa induced [35S]-GTP-gamma-S stimulation, indicating that daYFnLR[TIC]a is a partial agonist at the receptor stimulated by the FMRFamide analogs. Analysis of the structural requirements needed for promoting [35S]-GTP-gamma-S binding show that elongation (i.e., daYFnLRFa, D-YFnLRFa) or modification of Phe1 (ac-FnLRFa) leads to increased efficacy and potency. Moreover, elimination of the C-terminal Phe (daYWnLRa, daYFLRa,) leads to a loss of biological activity. However, substitution with L-1,2,3,4 tetrahydroisoquinoline-3-carboxylic acid, a rigid analog of the C-terminal Phe (daYFnLR[TIC]a), leads to decreased efficacy but not loss of potency. The data suggest that immobilization or modification of the C-terminal Phe may produce highly selective and potent FMRFamide antagonists. These results agree with published receptor radioligand studies and indicate that the [35S]GTP-gamma-S assay may be useful in classifying novel FMRFamide-selective ligands.
journal_name
Peptidesjournal_title
Peptidesauthors
Heyliger SO,Payza K,Rothman RBdoi
10.1016/s0196-9781(97)00481-6subject
Has Abstractpub_date
1998-01-01 00:00:00pages
739-47issue
4eissn
0196-9781issn
1873-5169pii
S0196978197004816journal_volume
19pub_type
杂志文章相关文献
PEPTIDES文献大全abstract::As a class of peptides with 10 cysteine residues (-C-CC-C-CC-C-C-C-C-), D-superfamily conotoxins (D-conotoxins) can specifically act on nicotinic acetylcholine receptors (nAChRs). According to the conserved signal peptides of D-conotoxins, seven D-conotoxin precursor sequences with a previously undescribed Cys arrange...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2017.06.008
更新日期:2017-08-01 00:00:00
abstract::Bombesin (BBS) at doses of 0.1, 1.0, 10.0 and 100.0 nM stimulated chemiluminescence (CL) production by phagocytic cells (monocytes, macrophages and polymorphonuclear leucocytes) in mice in the presence of ZAP (opsonized zymosan particles containing luminol). These data suggest that BBS increased the phagocytic functio...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(90)90098-p
更新日期:1990-03-01 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::Capsaicin-sensitive sensory nerves participate in the regulation of cardiovascular functions both in the normal state and the pathophysiology of hypertension through the actions of potent vasodilator neuropeptides, including calcitonin gene-related peptide (CGRP). CGRP, a very potent vasodilator, is the predominant ne...
journal_title:Peptides
pub_type: 杂志文章,评审
doi:10.1016/j.peptides.2005.02.002
更新日期:2005-09-01 00:00:00
abstract::A neuropeptide F (NPF) was isolated from the fruit fly, Drosophila mellanogaster, based on a radioimmunoassay for a gut peptide from the corn earworm, Helicoverpa zea. A partial sequence was obtained from the fly peptide, and a genomic sequence coding for NPF was cloned after inverse polymerase chain reaction and show...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(99)00097-2
更新日期:1999-01-01 00:00:00
abstract::Adjacent tissue sections through the rat median eminence were examined for the distribution of gonadotropin-releasing hormone (GnRH) and catecholamines (CA). A simultaneous visualization technique was employed for this correlative neuroanatomical analysis. At rostral and mid-central levels of the median eminence the m...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(80)90037-6
更新日期:1980-04-01 00:00:00
abstract::The functional help provided by four cross-linked synthetic peptides from HIV-1 Gag structural proteins was investigated in the mouse model. These peptides, selected upon non-self-criteria, are not predicted as T epitopes by classical prediction methods such as the Rothbard consensus or the amphipathy rule. Priming mi...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(94)90055-8
更新日期:1994-01-01 00:00:00
abstract::Bradykinin-potentiating peptides from Bothrops jararaca (Bj) discovered in the early 1960s, were the first natural inhibitors of the angiotensin-converting enzyme (ACE). These peptides belong to a large family of snake venom proline-rich oligopeptides (PROs). One of these peptides, Bj-PRO-9a, was essential for definin...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2013.07.016
更新日期:2013-10-01 00:00:00
abstract::Crustacean hyperglycemic hormone (CHH) not only plays an important role in the modulation of hemolymph glucose level but also functions in other biological events including molting, reproduction and stress response. Of the six CHHs characterized in Marsupenaeus japonicus, an expression system for recombinant Pej-SGP-V...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2008.07.017
更新日期:2009-03-01 00:00:00
abstract::Urocortin is a newly identified member of the CRF neuropeptide family. Urocortin has been found to bind with high affinity to CRF receptors. The present study investigated urocortin and CRF receptor expression in human colonic mucosa. Non-pathologic sections of adult colorectal tissues were obtained from patients with...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(00)00335-1
更新日期:2000-12-01 00:00:00
abstract::We investigated the effect of synthetic antimicrobial decapeptide KSL-W (KKVVFWVKFK) on normal human gingival fibroblast growth, migration, collagen gel contraction, and α-smooth muscle actin protein expression. Results show that in addition to promoting fibroblast adhesion by increasing F-actin production, peptide KS...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2017.05.003
更新日期:2017-07-01 00:00:00
abstract::The leucosulfakinins (LSKs), isolated from head extracts of the cockroach Leucophaea maderae, are sulfated neuropeptides with homology to gastrin and cholecystokinin. The undecapeptide LSK and decapeptide LSK-II stimulate contractions of the isolated cockroach hindgut. Several structural aspects of the two gastrin/CCK...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(88)90237-9
更新日期:1988-01-01 00:00:00
abstract::Salusins originally identified using bioinformatics analyses have been shown to act on the cardiovascular and endocrine systems. Although the hypotensive activity of salusin-alpha is limited, it exerts a significant anti-atherosclerotic effect via suppression of foam cell formation in human monocyte-derived macrophage...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2008.08.015
更新日期:2008-12-01 00:00:00
abstract::Calcitonin gene-related peptide (CGRP) immunoreactive material has been found in extracts of the intestine, however, the structure of intestinal CGRP is not known. Analytical reverse phase HPLC and ion-exchange FPLC revealed one predominant immunoreactive CGRP peak in rabbit intestinal extracts. This material was puri...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(91)90014-g
更新日期:1991-03-01 00:00:00
abstract::Neural input to distinct and separate populations of CRF-immunoreactive (ir) neurons in rat forebrain was investigated. The relationship of opiocortin and/or catecholamine fibers to different groups of CRF-containing neurons was elucidated using single and dual labeling immunocytochemical procedures. Antibodies to CRF...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(89)90005-3
更新日期:1989-11-01 00:00:00
abstract::The effect of EGF on the incorporation of [3H]TdR into DNA (DNA synthesis) was determined in the esophagus, liver, pancreas, and kidney in mice standardized to 12 hours (hr) of light alternating with 12 hr of darkness. A question asked was whether intraperitoneally administered EGF could alter the circadian patterns o...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(87)90110-0
更新日期:1987-03-01 00:00:00
abstract::To identify male-specific genes that could be involved in male development, we screened a subtracted male reproductive tract library and isolated a novel gene named Mar-Mrr (M. rosenbergii male reproduction-related gene). The Mar-Mrr cDNA sequence consists of 683 nucleotides with a 333 nucleotide open reading frame, e...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2005.09.004
更新日期:2006-04-01 00:00:00
abstract::Endokinins are novel tachykinins encoded on the human TAC4 and consist of Endokinin A (EKA), B (EKB), C (EKC) and D (EKD). To date, the function of Endokinins in pain processing was not fully understood. Therefore the aim of this study was to investigate the effects of Endokinin A/B (EKA/B, the common C-terminal decap...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2009.10.013
更新日期:2010-01-01 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::We studied the effects of calcitonin gene-related peptide (CGRP) on ciliary beat frequency (CBF) and electrical properties of canine tracheal epithelium by a photoelectric method and Ussing's short-circuit technique, respectively. CGRP dose dependently increased CBF, an effect that was accompanied by elevation of intr...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(89)90183-6
更新日期:1989-09-01 00:00:00
abstract::The incretin hormones, glucose dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 1 (GLP-1), potentiate insulin secretion and are responsible for the majority of insulin secretion that occurs after a meal. They may also, however, have a fundamental role in pancreatic beta cell development and functio...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2016.03.012
更新日期:2016-05-01 00:00:00
abstract::N-hydroxysuccinimide (NHS) esters of biotin are reported to react specifically with amino groups of peptides and proteins. However, we have found that these reagents can readily acylate other functional groups in specific peptide sequences under relatively mild conditions. We have extended our inquiry of sequence-depe...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(97)00225-8
更新日期:1997-01-01 00:00:00
abstract::Given the importance of G-protein coupled receptors in the regulation of many physiological functions, deciphering the relationships between genotype and phenotype in past and present hominin GPCRs is of main interest to understand the evolutionary process that contributed to the present-day variability in human trait...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2019.170154
更新日期:2019-12-01 00:00:00
abstract::We investigated the plasma concentration of ghrelin peptide during pregnancy and lactation in rats. Plasma ghrelin levels on days 10 and 15 of pregnancy were significantly lower than those of the non-pregnant rats. Thereafter, the plasma ghrelin levels on day 20 of pregnancy sharply increased to levels comparable with...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2004.01.011
更新日期:2004-02-01 00:00:00
abstract::Bradykinin-potentiating peptides (BPPs) are an important group of toxins present in Lachesis muta rhombeata venom. They act directly at renin-angiotensin-aldosterone system, through the inhibition of angiotensin-converting enzyme (ACE). This action may contribute to the hypotensive shock observed during the envenoming...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2018.01.015
更新日期:2018-04-01 00:00:00
abstract::The actions of a behaviorally active luteinizing hormone-releasing hormone fragment, Ac-LHRH(5-10), on CA1 pyramidal cells were studied utilizing conventional intracellular recordings from the in vitro rat hippocampal slice preparation. The behaviorally active fragment (10(-7) M) and the natural decapeptide [LHRH(1-10...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(93)90090-4
更新日期:1993-09-01 00:00:00
abstract::Using a one-bottle taste aversion conditioning paradigm, sulfated cholecystokinin(26-33) (CCK-8) has again been shown to induce taste aversion conditioning in rats. Even though the effective doses of CCK-8 are relatively high, they do not induce as strong an aversion as has been demonstrated with LiCl. This pharmacody...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(95)00001-z
更新日期:1995-01-01 00:00:00
abstract::We applied computational biology to identify the linear amino acid sequence recognized by a mouse monoclonal antibody raised against the full length HPV16 E7 oncoprotein. Computer-assisted search for the epitopic peptide used two parameters: the capability of E7 peptides to bind to MHC class II molecules, and the simi...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(01)00539-3
更新日期:2001-12-01 00:00:00
abstract::We have studied the in vitro effect of VIP and histamine on ultrastructure of the parietal cells in isolated guinea pig fundic glands. The morphological changes induced by histamine in the parietal cells can be compared to those observed after histamine stimulation in vivo or in vitro on gastric mucosa preparations. I...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(84)90219-5
更新日期:1984-03-01 00:00:00
abstract::We examined the effects of tumor necrosis factor (TNF)-alpha on the expression and functionality of adrenomedullin (AM) receptors in cultured human coronary artery smooth muscle cells. Analysis of real-time quantitative polymerase chain reactions showed that these cells abundantly express two AM receptors comprised of...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2004.04.010
更新日期:2004-07-01 00:00:00