LH-RH analogue carrying a cytotoxic radical is internalized by rat pituitary cells in vitro.


:The binding and internalization of a cytotoxic analogue of luteinizing hormone-releasing hormone (LH-RH), T-98 (agonist [D-Lys6]LH-RH linked to glutaryl-2-(hydroxymethyl)anthraquinone), by rat anterior pituitary cells was investigated. Analogue T-98 was bound to pituitary membrane binding sites for LH-RH with a high affinity (Kd = 1.2 nM) and was 17 times more potent in releasing luteinizing hormone (LH) from superfused rat pituitary cells than LH-RH. The labeling of this cytotoxic LH-RH analogue was carried out both with radioactive (125I) and nonradioactive iodine. Monoiodination of the Tyr5 residue of T-98 did not significantly affect its binding affinity but greatly decreased its LH-releasing activity to about 3% of the original value. Di-iodination in the same position lowered binding affinity twenty-threefold and further diminished LH-releasing potency. [125I]T-98 was found to bind very strongly to polystyrene, which precluded the use of regular tissue culture plasticware in our experiments. In pituitary cells cultured in glass vials, binding and internalization of [125I]T-98 were observed, which were time and temperature dependent, and which could be inhibited by excess unlabeled analogue. No enzymatic degradation of labeled T-98 was detected in the culture medium during the incubation. Our results indicate that T-98 is internalized by pituitary gonadotropes through receptor-mediated endocytosis. Because this new class of compounds was designed as anticancer drugs, our findings also suggest that this cytotoxic LH-RH agonist may also be internalized by LH-RH receptors present in breast, prostate, ovarian, and other tumors.






Szöke B,Horváth J,Halmos G,Rékási Z,Groot K,Nagy A,Schally AV




Has Abstract


1994-01-01 00:00:00
















  • Antinociceptive action of intrathecal neurotensin in mice.

    abstract::Neurotensin has been demonstrated to be analgesic in rodents. This study used intrathecal injection of neurotensin in unanesthetized mice to evaluate the effect of the peptide at the spinal level on unconditioned behavior. Intrathecal administration of neurotensin produced dose-related inhibition of locomotor activity...


    pub_type: 杂志文章


    authors: Hylden JL,Wilcox GL

    更新日期:1983-07-01 00:00:00

  • Chromatographic identification of Met- and Leu-enkephalin in the human fetal spinal cord.

    abstract::Using the indirect immunofluorescence method, enkephalin-like immunoreactivity was visualized on human fetus spinal cord sections (gestational age from 17 to 25 weeks). Immunolabeled varicose fibers and terminal-like structures were seen through the whole length fetal spinal cord principally in the dorsal gray, in the...


    pub_type: 杂志文章


    authors: Rougeot C,Charnay Y,Dray F,Dubois PM

    更新日期:1988-01-01 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 ...


    pub_type: 杂志文章


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

    更新日期:2008-01-01 00:00:00

  • Thirst impairment elicited by intraventricular administration of vasopressin antagonists.

    abstract::To determine whether centrally released vasopressin influences thirst, observations of osmotic thirst threshold, osmotic load excretion and postloading restitution of plasma osmolality were made in dogs in control experiments and during infusion of AVP antagonists into the third ventricle. Significant elevation of osm...


    pub_type: 杂志文章


    authors: Szczepanska-Sadowska E,Sobocinska J,Kozłowski S

    更新日期:1987-11-01 00:00:00

  • Apelin attenuates TGF-β1-induced epithelial to mesenchymal transition via activation of PKC-ε in human renal tubular epithelial cells.

    abstract::Epithelial to mesenchymal transition (EMT), a process whereby fully differentiated epithelial cells transition to a mesenchymal phenotype, has been implicated in the pathogenesis of renal fibrosis. Apelin, a bioactive peptide, has recently been recognized to protect against renal profibrotic activity, but the underlyi...


    pub_type: 杂志文章


    authors: Wang LY,Diao ZL,Zheng JF,Wu YR,Zhang QD,Liu WH

    更新日期:2017-10-01 00:00:00

  • Cardiorenovascular effects of urotensin II and the relevance of the UT receptor.

    abstract::Urotensin II (U-II) is a vasoactive peptide with many potent effects in the cardiorenovascular system. U-II activates a G-protein-coupled receptor termed UT. UT and U-II are highly expressed in the cardiovascular and renal system. Patients with various cardiovascular diseases show high U-II plasma levels. It was demon...


    pub_type: 杂志文章,评审


    authors: Tölle M,van der Giet M

    更新日期:2008-05-01 00:00:00

  • Regulation of hepcidin in HepG2 and RINm5F cells.

    abstract::Despite the high impact of the antimicrobial peptide hepcidin in iron homeostasis, the regulation of this hormone is still not completely understood. Studies concerning hepcidin regulation are performed at the mRNA level. For the first time we analyzed the regulation of hepcidin not only at mRNA, but also at protein l...


    pub_type: 杂志文章


    authors: Fein E,Merle U,Ehehalt R,Herrmann T,Kulaksiz H

    更新日期:2007-05-01 00:00:00

  • Gonadotropin-releasing hormone neuropeptides and receptor in human breast cancer: correlation to poor prognosis parameters.

    abstract::Expression of the two gonadotropin-releasing hormone homologue peptides GnRHI and GnRHII and their receptor GnRHR has been demonstrated in a number of malignancies. In hormone-dependent breast cancer, GnRH analogs are used for therapy in premenopausal women. Gene expression of GnRHI, II and R was studied in breast bio...


    pub_type: 杂志文章


    authors: Pazaitou-Panayiotou K,Chemonidou C,Poupi A,Koureta M,Kaprara A,Lambropoulou M,Constantinidis TC,Galaktidou G,Koffa M,Kiziridou A,Kakolyris S,Kolios G,Kortsaris A,Chatzaki E

    更新日期:2013-04-01 00:00:00

  • Protein phosphorylation in snail cardiocytes stimulated with molluscan peptide SCPb.

    abstract::Dissociated muscle cells prepared from hearts of the pulmonate snail Helix aspersa were used to study signal transduction induced by molluscan cardioactive peptides. The effects of SCPb on the cAMP levels of whole hearts and the cell preparation were compared. The cells responded to SCPb with a dose-dependent increase...


    pub_type: 杂志文章


    authors: Reich G,Doble KE,Greenberg MJ

    更新日期:1997-01-01 00:00:00

  • Molecular cloning and sequence analyses of preprotemporin mRNAs containing premature stop codons from extradermal tissues of Rana tagoi.

    abstract::The temporins are a family of hydrophobic, C-terminally alpha-amidated antimicrobial peptides that are synthesized in the skins of a wide range of species of frogs belonging to the genus Rana. In the present study, we investigated using RT-PCR the expression of preprotemporin mRNAs in extradermal tissues of Tago's bro...


    pub_type: 杂志文章


    authors: Iwamuro S,Nakamura M,Ohnuma A,Conlon JM

    更新日期:2006-09-01 00:00:00

  • cis-peptide bond mimetic tetrazole analogs of the insect kinins identify the active conformation.

    abstract::The insect kinin neuropeptides have been implicated in the regulation of water balance, digestive organ contraction, and energy mobilization in a number of insect species. A previous solution conformation study of an active, restricted-conformation cyclic analog, identified two possible turn conformations as the likel...


    pub_type: 杂志文章


    authors: Nachman RJ,Zabrocki J,Olczak J,Williams HJ,Moyna G,Ian Scott A,Coast GM

    更新日期:2002-04-01 00:00:00

  • The effect of pea albumin 1F on glucose metabolism in mice.

    abstract::Pea albumin 1F (PA1F), a plant peptide isolated from pea seeds, can dramatically increase blood glucose concentration by subcutaneous injection with a dosage of 5 or 10 microg/g (body weight) in normal and type II diabetic mice (KK/upj-Ay). The voltage-dependent anion channel 1 (VDAC-1) has been identified as the PA1F...


    pub_type: 杂志文章


    authors: Dun XP,Li FF,Wang JH,Chen ZW

    更新日期:2008-06-01 00:00:00

  • Arginine vasotocin and aggression in rats.

    abstract::Pinealectomized (PX) and sham animals were administered either AVT (1 ng/kg) or vehicle (1 ml H20). Boxing-kicking-biting episodes were significantly reduced by administration of AVT, F(1,21) = 8.09, p less than 0.009. Crawling under behavior was increased in PXH20 animals (p less than 0.05). Non-aggressive rearing wa...


    pub_type: 杂志文章


    authors: Brown R,King MG

    更新日期:1984-11-01 00:00:00

  • Neuropeptide K-(1-24)-peptide: storage and release by carcinoid tumors.

    abstract::An antiserum directed against the COOH-terminal region of neuropeptide K-(1-24)-peptide that shows only 0.5% reactivity with neuropeptide K has been used in radioimmunoassay to study the posttranslation processing of human beta-preprotachykinin. A primary midgut carcinoid tumor contained high concentration of substanc...


    pub_type: 杂志文章


    authors: Conlon JM,Deacon CF,Grimelius L,Cedermark B,Murphy RF,Thim L,Creutzfeldt W

    更新日期:1988-07-01 00:00:00

  • Effect of central injection of bradykinin and bradykinin potentiating factor upon release of anterior pituitary hormones in ovariectomized female rats.

    abstract::The effects of third ventricular (IVT) injection of 25 micrograms of bradykinin (BK) upon plasma levels of LH, FSH, TSH, GH and prolactin were investigated in conscious ovariectomized female rats bearing indwelling jugular cannulae. Some animals were pretreated with bradykinin potentiating factor (BPF). Intravenous ad...


    pub_type: 杂志文章


    authors: Steele MK,Negro-Vilar A,McCann SM

    更新日期:1980-10-01 00:00:00

  • Prognostic value of leptin: 6-month outcome in patients with intracerebral hemorrhage.

    abstract::Leptin has recently been discussed as a novel biomarker for the clinical outcome of critical illness. This study aims to investigate the prognostic value of leptin with regard to long-term clinical outcomes in patients with intracerebral hemorrhage. In 50 healthy controls and 92 patients with acute spontaneous basal g...


    pub_type: 杂志文章


    authors: Zhang X,Lu XM,Huang LF,Li X

    更新日期:2013-05-01 00:00:00

  • Somatostatin binding to dissociated cells from rat cerebral cortex.

    abstract::A method has been developed for the study of somatostatin (SS) binding to dissociated cells from rat cerebral cortex. Binding of [125I] [Tyr11]SS to cells obtained by mechanical dissociation of rat cerebral cortex was dependent on time and temperature, saturable, reversible and highly specific. Under conditions of equ...


    pub_type: 杂志文章


    authors: Colas B,Prieto JC,Arilla E

    更新日期:1990-11-01 00:00:00

  • Neuropeptide Y, ubiquitous and elusive.

    abstract::This paper reviews aspects of NPY research that were emerging in 1985, shortly after the isolation and characterization of the peptide. NPY had become known for its widespread distribution especially in the central and peripheral nervous systems, but also in the gastro-intestinal and respiratory tracts and in fibers i...


    pub_type: 杂志文章,评审


    authors: Chronwall BM,Zukowska Z

    更新日期:2004-03-01 00:00:00

  • Multiple cleavage sites of cholecystokinin heptapeptide by "enkephalinase".

    abstract::Degradation of Boc CCK7 (Boc Tyr1 (SO3H)-Met2-Gly3-Trp4-Met5-Asp6-Phe7-NH2), a fully active analog of CCK8, by purified rabbit kidney neutral metalloendopeptidase (enkephalinase) was studied as a basis for the rational design of potent peptidases-resistant analogs of cholecystokinin. Characterization of the metabolite...


    pub_type: 杂志文章


    authors: Durieux C,Charpentier B,Fellion E,Gacel G,Pelaprat D,Roques BP

    更新日期:1985-05-01 00:00:00

  • C-terminal amide to alcohol conversion changes the cardiovascular effects of endomorphins in anesthetized rats.

    abstract::Endomorphin1-ol (Tyr-Pro-Trp-Phe-ol, EM1-ol) and endomorphin2-ol (Tyr-Pro-Phe-Phe-ol, EM2-ol), with C-terminal alcohol (-ol) containing, have been shown to exhibit higher affinity and lower intrinsic efficacy in vitro than endomorphins. In the present study, in order to investigate the alterations of systemic hemodyna...


    pub_type: 杂志文章


    authors: Yu Y,Wang CL,Cui Y,Fan YZ,Liu J,Shao X,Liu HM,Wang R

    更新日期:2006-01-01 00:00:00

  • Exenatide and feeding: possible peripheral neuronal pathways.

    abstract::Intraperitoneal (i.p.) administration of the synthetic agonist of the glucagon like peptide-1 (GLP-1) receptor exenatide reduces food intake. Here, we evaluated possible peripheral pathways for this reduction. Exenatide (0.5 μg/kg, i.p.) was given to three, overnight food-deprived, groups of rats: total subdiaphragmat...


    pub_type: 杂志文章


    authors: Hunt JV,Washington MC,Sayegh AI

    更新日期:2012-02-01 00:00:00

  • Osmotic stimulation affects neurohypophysial corticotropin releasing factor-41 content: effect of dexamethasone.

    abstract::In this study we examined the effects of 2% saline loading (S), partial restriction of water consumption (R) or a combination of S or R with dexamethasone (DEX) treatment for 14 days on corticotropin releasing factor (CRF)-41 content of the neurointermediate lobe (NIL) and supraoptic nuclei (SON) of male Wistar rats. ...


    pub_type: 杂志文章


    authors: Dohanics J,Linton EA,Lowry PJ,Makara GB

    更新日期:1990-01-01 00:00:00

  • Lack of CCK-like pancreatic stimulation by intraduodenal amino acids in the anesthetized cat.

    abstract::We have attempted to demonstrate a pancreatic secretory response to intraduodenal amino acids in the anesthetized cat. In four cats stimulated with supramaximal doses of secretin, protein concentrations in pancreatic juice were measured after intraduodenal bolus injection of various amino acids, IV CCK, or electrical ...


    pub_type: 杂志文章


    authors: Johnson C,Jeanningros R,Sarles H

    更新日期:1982-03-01 00:00:00

  • Episodic secretion of ACTH in rats.

    abstract::While the circadian rhythm of pituitary adrenocorticotropin (ACTH) secretion has been well characterized, the ultradian rhythm has been less thoroughly investigated. To study the episodic nature of ACTH secretion, unrestrained, unanesthetized rats were bled continuously through indwelling jugular venous cannulae and b...


    pub_type: 杂志文章


    authors: Carnes M,Brownfield MS,Kalin NH,Lent S,Barksdale CM

    更新日期:1986-03-01 00:00:00

  • The state versus amyloid-beta: the trial of the most wanted criminal in Alzheimer disease.

    abstract::Investigators studying the primary culprit responsible for Alzheimer disease have, for the past two decades, primarily focused on amyloid-beta (Abeta). Here, we put Abeta on trial and review evidence amassed by the prosecution that implicate Abeta and also consider arguments and evidence gathered by the defense team w...


    pub_type: 杂志文章,评审


    authors: Rottkamp CA,Atwood CS,Joseph JA,Nunomura A,Perry G,Smith MA

    更新日期:2002-07-01 00:00:00

  • Bolus administration of obestatin does not change glucose and insulin levels neither in the systemic nor in the portal circulation of the rat.

    abstract::Obestatin is a second peptide derived from the preproghrelin polypeptide. It was originally thought to have anorexigenic effects, thereby functioning as an antagonist of ghrelin. However, this has been a subject of debate ever since. Since acylated ghrelin strongly induces insulin resistance, it could be hypothesized ...


    pub_type: 杂志文章


    authors: Kiewiet RM,Gauna C,van Aken MO,van de Zande B,van der Lely AJ

    更新日期:2008-12-01 00:00:00

  • Continuous intraventricular infusion of neuropeptide Y evokes episodic food intake in satiated female rats: effects of adrenalectomy and cholecystokinin.

    abstract::In these studies the pattern of feeding behavior during continuous intraventricular (IVT) infusion of NPY for 4 hr in the satiated female rat was monitored. Whereas saline infusion was ineffective, each of the three doses of NPY (117, 470 or 1175 pmol/hr) increased feeding during the entire 4 hr infusion and 2 hr post...


    pub_type: 杂志文章


    authors: Kalra SP,Dube MG,Kalra PS

    更新日期:1988-07-01 00:00:00

  • Role of neuropeptides in cardiomyopathies.

    abstract::The role of neuropeptides in cardiomyopathy-associated heart failure has been garnering more attention. Several neuropeptides--Neuropeptide Y (NPY), vasoactive intestinal peptide (VIP), calcitonin gene related peptide (CGRP), substance P (SP) and their receptors have been studied in the various types of cardiomyopathi...


    pub_type: 杂志文章,评审


    authors: Dvorakova MC,Kruzliak P,Rabkin SW

    更新日期:2014-11-01 00:00:00

  • Immunohistochemical mapping of galanin-like immunoreactivity in the brain of the dogfish Scyliorhinus canicula.

    abstract::The distribution of galanin-like immunoreactivity in the brain of the dogfish Scyliorhinus canicula was investigated using the indirect immunofluorescence technique. In the telencephalon, positive cells and fibers were located in the mid-caudal part of the area superficialis basalis, the n. septi caudoventralis and in...


    pub_type: 杂志文章


    authors: Vallarino M,Feuilloley M,Vandesande F,Vaudry H

    更新日期:1991-03-01 00:00:00

  • Investigation of gastrin-releasing peptide as a mediator for 5'-guanidinonaltrindole-induced compulsive scratching in mice.

    abstract::Gastrin-releasing peptide (GRP) has been implicated in the itch-scratch cycle. We investigated if this gut-brain-skin peptide plays a role in the compulsive, hindleg scratching of the neck of mice by 5'-guanidinonaltrindole (GNTI), the kappa opioid receptor antagonist, and in the antipruritic activity of nalfurafine, ...


    pub_type: 杂志文章


    authors: Inan S,Dun NJ,Cowan A

    更新日期:2011-02-01 00:00:00