BioAssay record AID 74411 submitted by ChEMBL: Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor.

The Caenorhabditis elegans genome is known to code for at least 1149 G protein-coupled receptors (GPCRs), but the GPCR(s) critical to the regulation of reproduction in this nematode are not yet known. This study examined whether GPCRs orthologous to human gonadotropin-releasing hormone receptor (GnRHR) exist in C. elegans. Our sequence analyses indicated the presence of two proteins in C. elegans, one of 401 amino acids [GenBank: NP_491453; WormBase: F54D7.3] and another of 379 amino acids [GenBank: NP_506566; WormBase: C15H11.2] with 46.9% and 44.7% nucleotide similarity to human GnRHR1 and GnRHR2, respectively. Like human GnRHR1, structural analysis of the C. elegans GnRHR1 orthologue (Ce-GnRHR) predicted a rhodopsin family member with 7 transmembrane domains, G protein coupling sites and phosphorylation sites for protein kinase C. Of the functionally important amino acids in human GnRHR1, 56% were conserved in the C. elegans orthologue. Ce-GnRHR was actively transcribed in adult worms and

TY - JOUR. T1 - Peripubertal decline in ovarian LHRH receptor content. T2 - Characterization and distribution. AU - White, S. S.. AU - Ojeda, S. R.. N1 - Copyright: Copyright 2018 Elsevier B.V., All rights reserved.. PY - 1983. Y1 - 1983. N2 - In the rat, ovarian LHRH receptor content, as measured by the binding of 125I-D-Ala6, Pro9-LHRH (A-LHRH) to ovarian membranes, decreases markedly during the days preceding the first preovulatory gonadotropin surge. The present study shows that the decrease in LHRH receptor number occurs exclusively in granulosa cells, and that the greatest rate of decline takes place between the juvenile period and the early proestrous phase of puberty. In contrast to granulosa cells, membranes prepared from ovarian tissues after removal of these cells demonstrated no significant change in LHRH binding capacity throughout puberty. Scatchard analysis of competition curves, constructed using membranes from whole ovaries, revealed that receptor affinity remains unchanged ...

Biology of Reproduction contains original scientific research on a broad range of topics in the field of reproductive biology, as well as minireviews.

Descriptive coverage of pipeline development activities for Gonadotropin-Releasing Hormone (GnRH) Receptor (LHRH Receptor) Antagonist - Pipeline therapeutics development coverage provides descriptive product profiles including (but not limited to) drug description, product development and R&D activities encompassing clinical and pre-clinical studies, designations, collaborations, licensing deals, grants, technologies and patent details ...

Differential usage of several transcription start sites in the human GnRH receptor gene was evident in human brain and pituitary. To locate the promoter responsible for a cluster of the 3′ CAP sites from -635 to -578 (relative to ATG) found in the pituitary, a proximal promoter element was identified at -677/-558 by 5′ and 3′ deletion mutant analysis. The promoter element drove a 13.1 ± 0.6-fold increase in reporter gene activity in an orientation-dependent manner in the mouse gonadotrope-derived αT3-1 cells. Within the core promoter element, two functional AT-rich Inr motifs, interacting with the same protein factor with different affinities, were identified. By Southwestern blot analysis and competitive gel mobility shift assays, multiple nuclear factors (36-150 kDa) were found to interact specifically with the core promoter element. Interestingly, these nuclear proteins also interacted with a previously identified distal promoter of the human GnRH receptor gene. Taken together, our ...

Administration of a potent gonadotropin-releasing hormone (GnRH) antagonist [Nac-L-Ala1,pCl-D-Phe2,D-Trp3,6]GnRH as a single subcutaneous injection to castrated adult male rats reduced, by more than 90 percent, both serum luteinizing hormone concentrations and specific pituitary GnRH receptor binding. This effect persisted for 24 hours. The dissociation rate of the antagonist from pituitary membrane homogenates was fourfold slower than the dissociation rate of a potent agonist. The prolonged in vivo inhibition of pituitary GnRH receptor binding and luteinizing hormone secretion by the GnRH antagonist may be mediated by the slower dissociation rate of the antagonist from its specific pituitary membrane receptor site. ...

Shop a large selection of products and learn more about Thermo Scientific Lab Vision GnRH Receptor/LH-RH Receptor Ab-3, Mouse Monoclonal 1mL; Unlabeled; Ready-to-use format.

Data Availability StatementAll datasets generated because of this research are contained in the content/supplementary material. assessed bodyweight and performed behavioral checks to look for the ramifications of fluoxetine and pressure on depressive-like behaviors. Real-time PCR and traditional western blotting were utilized to gauge the mRNA and proteins manifestation degrees of GRPR in the hypothalamus. After that, Flag-tagged proteins (pcmv-Flag-5HT2aR) and Myc-tagged proteins (pcmv-Myc-GRPR) manifestation vectors were built, determined, and transfected into human being embryo kidney 293 (HEK293) cells. The interaction between 5-HT2aR and GRPR was recognized by double-label and coimmunoprecipitation immunofluorescence. Outcomes The rats put through four weeks of CUMS demonstrated depressive-like behaviors, including reduced bodyweight, sucrose choice, and distance journeyed, rearing rate of recurrence and speed on view field ensure that you improved immobility amount of time in the pressured ...

CD8+ T cell responses are thought to play an important role during HIV infection, particularly in HIV controllers (HIC) in whom viral replication is spontaneously controlled without any treatment. of HIV-specific CD8+ T cells were observed only in a subset of HLA-B*57+ subjects. They were tightly associated with the ability to suppress viral replication to kill virally infected autologous CD4+ T cells and therefore suppress viral replication (15, 16). However, this CD8+ T cell viral suppression activity is not present in all HIC (17). Most studies have been performed with HLA-B*57+ or HLA-B*27+ patients, since they represent a large. ...

The principle of targeted chemotherapy is based on a concept by Paul Ehrlich, who postulated ,100 years ago that antibodies could deliver toxic compounds to specific antigens on cancer cells (41) . This targeting was conceived to eradicate mainly the tumors, thus sparing the normal tissue (41) . In the search for cytotoxic hybrids with clinical potential, we developed a new class of targeted antitumor conjugates by linking agonistic analogues of LH-RH, which have a high affinity for LH-RH receptors, to a variety of chemotherapeutic agents (15 , 16 , 30) . The rationale for using LH-RH for targeted chemotherapy is based on the presence of specific high-affinity binding sites for this peptide hormone on various human tumors, including breast, ovarian, endometrial, and prostatic carcinomas (4 , 15, 16, 17 , 19, 20, 21) . We found LH-RH receptors and their mRNA in 86% of clinical specimens of prostate cancer (17) . The expression of mRNA for LH-RH receptors is significantly higher in hormone ...

BioAssay record AID 102693 submitted by ChEMBL: Compounds were tested for the effective dose to induce luteinizing hormone (LH) release in rat pituitary receptors.

Markers of alleles for three physiological candidate genes for reproductive traits, growth hormone (GHR), gonadotropin-releasing hormone receptor (GNRHR) and neuropeptide Y (NPY) were assessed for the association with the total egg production, number of double-yolked eggs and age at first egg in a single generation of a broiler breeder (Gallus gallus) pedigree dam line. Single-nucleotide polymorphisms and deletions were detected in the GHR, GNRHR and NPY genes. Genotypes were identified using a PCR-RFLP assay. The frequency of restriction enzyme+/-alleles in the population was for GHR 0.68 (NspI-) and 0.32 (NspI+), for NPY 0.78 (DraI+) and 0.22 (DraI-) and for GNRHR 0.54 (Bpu11021+) and 0.46 (Bpu11021-). Trait data from a total of 772 hens in 67 sire families from one generation of the pedigree dam line were recorded. However, the analysis used only the offspring of heterozygous sires to reduce the influence of selection and genetic background (n = 33 sire families for GHR; n = 14 sire families ...

Based on molecular modeling and site-directed mutagenesis studies, a C6.47-N7.45 hydrogen bond interaction has recently been proposed in the gonadotropin-releasing hormone receptor [59]. Since all receptors with available structures feature N7.45 (66% conserved) except bRho/sRho (contain S:12%) and CXCR4 (contains H:8%) we assessed, by conducting systematic analysis on the available crystal structures, if this interaction was likely to exist in other GPCRs.. Available crystal structures differ in the assignment of CO and NH2 groups for N7.45 (see Table 1). This it is not surprising because even at 1.8 Å resolution (the highest obtained for a GPCR structure; see Table 1) it is not possible to correctly assign all side chain rotamers. Since it is unlikely that the orientation of the CO/NH2 groups of N7.45 is not the same in all receptors (this position is surrounded by many conserved residues) we evaluated the two possible orientations using NQ-Flipper (see Methods) [60]. The results revealed ...

Plenaxis (abarelix) is a protein pharmaceutical. Abarelix was first approved as Plenaxis on 2003-11-25. The pharmaceutical is active against gonadotropin-releasing hormone receptor.

抗体名称：GNRHR抗体,Anti-GNRHR抗体背景资料：GNRHR,alsonamedasGRHR,belongstotheG-proteincoupledreceptor1family.GNRHRisareceptorforgonadotropinreleasinghormone(GnRH)thatmediatestheactionofGnRHtostimulatethesecretiono

CHO-Anti-Human GNRHR MAb stable cell line is clonally-derived from a CHO cell line, which has been transfected with an Anti-human GNRHR MAb gene to allow expression of the MAb. It is an example of a cell line transfected using our proprietary CBTGS gene screening and amplification system.

Order GNRHR ELISA Kits for many Reactivities. Cow, Dog, Goat and more. Compare GNRHR ELISA Kits and find the right product on antibodies-online.com.

Alfa Chemistry is the worlds leading provider for special chemicals. We offer qualified products for 218433-98-8((BIOTINYL-GLN1)-LHRH),please inquire us for 218433-98-8((BIOTINYL-GLN1)-LHRH).

Chemotherapie met AN-152 and AN-207 remt sterk de groei van vergevorderde vormen van kanker ontstaan vanuit endometriose met LHRH receptoren. Nieuwe studies toegevoegd die goede resultaten van gerichte aanpak bevestigen. Artikel update 7 november 2012

TY - JOUR. T1 - Gonadotropin-releasing hormone receptor expression in xenopus oocytes. AU - Sealfon, Stuart C.. AU - Gillo, Boaz. AU - Mundamattom, Shirley. AU - Mellon, Pamela L.. AU - Windle, Jolene J.. AU - Landau, Emmanuel. AU - Roberts, James L.. N1 - Copyright: Copyright 2016 Elsevier B.V., All rights reserved.. PY - 1990/1. Y1 - 1990/1. N2 - The rodent GnRH receptor was characterized in Xenopus oocytes injected with RNA isolated from rat pituitary and from a gonadotrope cell line, αT3, derived from a transgenic mouse. Three to 4 days after 150-200 ng RNA injection, 93% of the oocytes, which were recorded by voltage clamp, responded to 10-7 m GnRH. The mean inward currents obtained after RNA injection were 620 ± 88 nA (n = 22) with pituitary RNA and 1415 ± 598 (n = 4) with αT3 RNA. The threshold GnRH concentration able to evoke the dose dependent current after pituitary RNA injection was 3 x 10-9 m GnRH. The GnRH receptor response of the oocyte was antagonized by [D-Phe2, 6, Pro3] GnRH ...

TY - JOUR. T1 - Modulation of pituitary luteinizing hormone releasing hormone receptors by sex steroids and luteinizing hormone releasing hormone in the rat. AU - Marchetti, B.. AU - Reeves, J. J.. AU - Pelletier, G.. AU - Labrie, F.. PY - 1982. Y1 - 1982. N2 - The effect of sex steroids on pituitary luteinizing hormone releasing hormone (LHRH) receptor number and affinity was studied in adult castrated male and female rats treated for 2 weeks with 17β-estradiol (E2), testosterone (T), 5α-dihydrotestosterone (DHT) or progesterone (P) alone or in combination. The effect of chronic treatment with the potent LHRH agonist [D-Ser(TBU)6, des-Gly-NH210] LHRH ethylamide, Buserelin, was studied in intact and castrated animals. [125I]-Buserelin was used as tracer to measure LHRH receptors in individual pituitaries. Daily treatment of intact male rats for 2 weeks with Buserelin (200 ng) increased pituitary LHRH receptor concentration while the same treatment in castrated animals reversed by 60% the ...

Purpose: In addition to their expression on pituitary cells, receptors for luteinizing hormone-releasing hormone (LH-RH) are found on most prostate cancer cells. These tumoral LH-RH receptors mediate the direct cytotoxic effects of LH-RH analogs and are potential therapeutic targets. Although pituitary LH-RH receptors are downregulated following prolonged exposure to LH-RH agonists, there is no evidence that tumoral receptors behave in a similar manner. To better characterize expression of tumoral LH-RH receptors, specimens of prostate cancer from various cohorts of patients were analyzed.. Experimental Design: Surgical specimens were obtained from untreated patients with prostate cancer and from patients with metastatic castration-resistant prostate cancer previously treated with bilateral orchiectomy. To address the possibility of receptor downregulation, two additional cohorts of patients who had been previously treated with LH-RH agonists were included. One group received neoadjuvant therapy ...

The integrated functions of the hypothalamus, anterior pituitary gland, and ovaries serve to regulate normal female reproductive function. The hypothalamus secretes Gonadotropin-Releasing Hormone (GnRH), a peptide hormone, in a pulsatile manner. GnRH stimulates the anterior pituitary gland via binding to specific, high-affinity receptors on the plasma membrane of gonadotrophs. GnRH binding initiates a cascade of intracellular events resulting in synthesis and secretion of the gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and also synthesis and insertion of its own receptors into the plasma membrane. When gonadotropins are released into circulation, they exert their primary biological effects at the gonads. Ovarian hormones, progesterone, inhibin, and estradiol, feedback effects at both the hypothalamus and pituitary gland. Progesterone reduces the pulse frequency and amplitude of GnRH being released from the hypothalamus, thus, decreasing gonadotropin secretion. It is

Complementar Deoxyribonucleic Acid Cloning, Gene Expression, and Ligand Selectivity of a Novel Gonadotropin-Releasing Hormone Receptor Expressed in the Pituitary and Midbrain of ,I,Xenopus Laevis,/I ...

To investigate the mechanism controlling the fall in maternal pituitary responsiveness to GnRH, LH synthesis and pituitary GnRH receptor content during pregnancy, maternal pituitaries were collected from sheep on days 35, 45, 60, 90, 110, 125 and 135 of pregnancy. Circulating steroids and gonadotrophins were determined in blood samples collected from these ewes immediately before death. Pituitary blocks from each ewe were perifused with either medium alone (control) or medium supplemented with oestradiol, oestradiol plus progesterone or oestradiol plus RU486, for 150 min before administration of two 15 s GnRH pulses 90 min apart. The amounts of mRNA encoding LHβ and GnRH receptor were determined in pituitary tissue fragments snap-frozen in liquid N2 at the time of collection from the ewes. While basal LH secretion fell during pregnancy, pituitary responsiveness to GnRH remained high (up to seven times basal LH concentrations). After day 90, the first GnRH pulse elicited LH peaks equivalent to ...

TY - CHAP. T1 - Exploring Dynamics and Noise in Gonadotropin-Releasing Hormone (GnRH) Signaling. AU - Voliotis, Margaritis. AU - Garner, Kathryn L. AU - Alobaid, Hussah. AU - Tsaneva-Atanasova, Krasimira. AU - McArdle, Craig A. PY - 2018. Y1 - 2018. N2 - Gonadotropin-releasing hormone (GnRH) acts via G-protein coupled receptors on pituitary gonadotropes. These are Gq-coupled receptors that mediate acute effects of GnRH on the exocytotic secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), as well as the chronic regulation of their synthesis. FSH and LH control steroidogenesis and gametogenesis in the gonads so GnRH mediates control of reproduction by the central nervous system. GnRH is secreted in short pulses and the effects of GnRH on its target cells are dependent on the dynamics of these pulses. Here we provide a brief overview of the signaling network activated by GnRH with emphasis on the use of high content imaging for their examination. We also describe ...

GnRH (gonadotropin-releasing hormone) plays a pivotal role in the regulation of reproduction in vertebrates through interaction with a specific receptor. Previously, we isolated a GnRH homo-logue, oct-GnRH, from the common octopus (Octopus vulgaris). In the present study, we have identified a GnRH receptor (oct-GnRHR) specific for oct-GnRH from Octopus brain. Oct-GnRHR includes domains and motifs typical of vertebrate GnRH receptors. The intron-inserted positions are conserved between oct-GnRHR and the chordate GnRHR genes. The oct-GnRHR expressed in Xenopus (South African clawed frog) oocytes was responsive to oct-GnRH, but not to any other HPLC fractions of the Octopus brain extract. These results show that oct-GnRHR is an authentic receptor for oct-GnRH. Southern blotting of reverse-transcription PCR products revealed that the oct-GnRHR mRNA was widely distributed in the central and peripheral nervous systems and in several peripheral tissues. In situ hybridiz-ation showed that oct-GnRHR mRNA ...

TY - JOUR. T1 - Effect of N-methyl-D,L-aspartate (NMA) on gonadotropin-releasing hormone (GnRH) gene expression in male mice. AU - Wu, T. J.. AU - Gibson, Marie J.. AU - Roberts, James L.. N1 - Funding Information: This project was supported by DK39029 (JLR), NS20335 (MJG) and T32-DK07645 (TJW). The authors wish to thank Dr. Areta Dobrjansky for assistance with the LH RIA, and Dr. Yuhua Sun for helpful discussions and Ms. Alice Elste for reading the manuscript.. PY - 2000/4/17. Y1 - 2000/4/17. N2 - The glutamate analog N-methyl-D,L-aspartate (NMA) affects the regulation of GnRH and LH release in mammals. Several laboratories have reported a rapid and transient increase in GnRH mRNA levels of male rats after NMA injection. Studies employing the simultaneous measurements of nuclear GnRH primary transcript RNA, a reflection of gene transcription, and GnRH mRNA suggest that NMAs effect on GnRH gene expression in the rat is likely due to post-transcriptional regulation. Despite the increasingly ...

gonadotropin-releasing hormone (GnRH): GnRH a neurohormone consisting of 10 amino acids that is produced in the arcuate nuclei of the hypothalamus. GnRH stimulates the synthesis and secretion of the two gonadotropins...

Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013. - Mechanism of Action & Protocol.

GNRHR2 Antibody (monoclonal) (M01), Mouse monoclonal antibody raised against a partial recombinant GNRHR2. validated in WB, E (AT2234a), Abcepta

Image by Joel Ito and P. Michael Conn The first clinical trials to test protein misfolding therapies are so new that researchers havent yet agreed on a collective name for the compounds being administered. Variously dubbed chemical chaperones, pharmacological chaperones, and pharmacoperones, these small molecules correct the misfolding of proteins that recent research has implicated in a host of diseases, both rare and prevalent. In such conformational diseases, misfolded proteins may lose

Gonadotropin-Releasing Hormone-Associated Peptide (Human, 34-56) Antiserum Anti Gonadotropin-Releasing Hormone-Associated Peptide (Human, ...

Mouse monoclonal antibody raised against a partial recombinant GNRHR2. GNRHR2 (NP_001457, 237 a.a. ~ 292 a.a) partial recombinant protein with GST tag. MW of the GST tag alone is 26 KDa. (H00114814-M01) - Products - Abnova

கருவகவூக்கி வெளியிடு இயக்குநீர் (Gonadotropin-releasing hormone; GnRH) என்பது, எந்த திசுக்களின் மீது செயலாற்றுகிறதோ, அவற்றின் வளர்ச்சியைத் தூண்டக்கூடிய, உயிரணுக்களை மிகைப்பெருக்கம் அல்லது மிகை வளர்ச்சிச் செய்யக்கூடிய தூண்டும் இயக்குநீர் (trophic hormone)[1] வகைகளுள் ஒன்றாகும். இது லூட்டினைசிங் இயக்குநீர்- வெளியிடு இயக்குநீர், லூலிபெரின் என்றும் அழைக்கப்படுகின்றது. முற்பகுதி பிட்யூட்டரியிலிருந்து ...

余白の削除などで一部分だけ印刷したい場合、または画像が薄すぎる、暗すぎる場合は、下の「詳細設定」をお試しください ...

He employs molecular, cellular, transgenic animal and human tissue models to understand the biology of these commonly encountered hormone-secreting adenomas. He tests pituitary receptor signaling to develop novel peptide analog treatments for these tumors secreting growth hormone, prolactin, ACTH or gonadotropins. ...

Antagonist til gonadotropin-releasing hormone (GnRH). Polypeptid. Hæmmer udskillelsen af det luteiniserende hormon (LH) og det follikelstimulerende hormon (FSH).

Multiple gonadotropin-releasing hormone receptors (GnRHRs) are present in vertebrates, but their differential physiological relevances remain to be clarified. In the present study, we identified three GnRH ligands GnRH1 (pjGnRH), GnRH2 (cGnRH-II), and GnRH3 (sGnRH) from the brain, and two GnRH receptors GnRHR1 (GnRHR IIa) and GnRHR2 (GnRHR IIb) from the pituitary of the ricefield eel Monopterus albus. GnRH1 and GnRH3 but not GnRH2 immunoreactive neurons were detected in the pre-optic area, hypothalamus, and pituitary, suggesting that GnRH1 and GnRH3 may exert hypophysiotropic roles in ricefield eels. gnrhr1 mRNA was mainly detected in the pituitary, whereas gnrhr2 mRNA broadly in tissues of both females and males. In the pituitary, GnRHR1 and GnRHR2 immunoreactive cells were differentially distributed, with GnRHR1 immunoreactive cells mainly in peripheral areas of the adenohypophysis whereas GnRHR2 immunoreactive cells in the multicellular layers of adenohypophysis adjacent to the neurohypophysis. Dual

Gonadotropin-releasing hormone antagonists (GnRH antagonists) are a class of medications that antagonize the gonadotropin-releasing hormone receptor (GnRH receptor) and thus the action of gonadotropin-releasing hormone (GnRH). Some are similar in structure to natural GnRH (a hormone made by neurons in the hypothalamus) but that have an antagonistic effect. These GnRH antagonists are peptide molecules that are made up multiple, often synthetically produced amino acids. Others are small-molecule, non-peptide compounds. GnRH antagonists compete with natural GnRH for binding to GnRH receptors, thus decreasing or blocking GnRH action in the body. Testosterone promotes growth of many prostate tumors and therefore reducing circulating testosterone to very low (castration) levels is often the treatment goal in the management of men with advanced prostate cancer. GnRH antagonists are used to provide fast suppression of testosterone without the surge in testosterone levels that is seen when treating ...

https://doi.org/10.18632/oncotarget.1379 Andrea Treszl, Zita Steiber, Andrew V Schally, Norman L Block, Balazs Dezso, Gabor Olah, Bernadett Rozsa, Klara Fodor, Armin Buglyo, Janos Gardi, Andras...

TY - JOUR. T1 - Induction of apoptosis by AN-152, a cytotoxic analog of luteinizing hormone-releasing hormone (LHRH), in LHRH-R positive human breast cancer cells is independent of multidrug resistance-1 (MDR-1) system. AU - Günthert, Andreas R.. AU - Gründker, Carsten. AU - Bongertz, Till. AU - Nagy, Attila. AU - Schally, Andrew V.. AU - Emons, Günter. PY - 2004/10/1. Y1 - 2004/10/1. N2 - Objective. More than 50% of human breast cancers express receptors for luteinizing hormone-releasing hormone (LHRH-R). These receptors can be used for targeted chemotherapy with agents like AN-152, in which doxorubicin is linked to analog [D-Lys 6]LHRH. We compared the effects of AN-152 and doxorubicin in human breast cancer cells. Methods. MCF-7, T47D, HCC-70 and ZR-75-1 cells were analysed for expression of LHRH-R using RT-PCR, immunostaining and flow cytometry. Apoptosis and expression of MDR-1 gene product Pgp were measured by flow cytometry. Cleavage of doxorubicin from AN-152 by serum carboxylesterase ...

The highly conserved DRY motif located at the end of the third transmembrane of G-protein-coupled receptors has been described as a key motif for several aspects of GPCR functions. However, in the case of the vertebrate gonadotropin-releasing hormone receptor (GnRHR), the amino acid in the third position in the DRY motif is variable. In the lamprey, a most basal vertebrate, the third amino acid of the DRY in lamprey (lGnRHR-1) is His, while it is most often His/Gln in the type II GnRHR. To investigate the functional significance of the substitution of DRY to DRH in the GnRHR-1, second messenger signaling, ligand binding and internalization of the wild-type and mutant lGnRH receptors were characterized with site-directed mutagenesis. Treatment of the DRE151 and DRS151 mutant receptors with lamprey GnRH-I significantly reduced inositol phosphate compared to wild-type (DRH151) and DRY151 receptors. The Log IC50 of wild-type receptor (-9.554 +/- 0.049) was similar to the Log IC50 of DRE151, DRS151 and

Xenopus laevis (X) GnRHRs ( approximately 40%). This distinction is retained at comparable whole cell expression levels, and the hGnRHR PCSE is increased by addition of the XGnRHR C-tail (h.XGnRHR) or by a membrane-permeant pharmacological chaperone (IN3). The IN3 effect is concentration- and time-dependent and IN3 also enhances the hGnRHR-mediated (but not h.XGnRHR- or mouse GnRHR-mediated) stimulation of [(3)H]inositol phosphate accumulation and the hGnRHR-mediated reduction in cell number. We also find that the PCSE for hGnRHRs and h.XGnRHRs is low and is greatly increased by IN3 in two hormone-dependent cancer lines, but is higher and less sensitive to IN3 in a gonadotrope line. Finally, we show that the effect of IN3 on hGnRHR PCSE is not mimicked or blocked by two peptide antagonists although they do increase the PCSE for h.XGnRHRs, revealing that an antagonist-occupied cell surface GnRHR conformation can differ from that of the unoccupied receptor. The low PCSE of hGnRHRs and this novel ...

Ozarelix (developmental code names D-63153, SPI-153) is a peptide gonadotropin-releasing hormone antagonist (GnRH antagonist) which is under development by AEterna Zentaris Inc. and Spectrum Pharmaceuticals as a long-acting injection formulation for the treatment of prostate cancer. It has also been under investigation for the treatment of endometriosis, but no development has been reported. The drug was previously under investigation for the treatment of benign prostatic hyperplasia and Alzheimers disease as well, but development for these indications was discontinued. As of December 2017, it is in phase II clinical trials for prostate cancer. Gonadotropin-releasing hormone receptor § Antagonists List of investigational hormonal agents § GnRH/gonadotropins http://adisinsight.springer.com/drugs/800013299 Festuccia C, Dondi D, Piccolella M, Locatelli A, Gravina GL, Tombolini V, Motta M (2010). Ozarelix, a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen ...

QUÉBEC CITY, Feb. 4, 2014 /PRNewswire/ - Aeterna Zentaris Inc. (NASDAQ: AEZS) (TSX: AEZ) (the Company) today announced that an article on Phase 2 results for zoptarelin doxorubicin (AEZS-108) in endometrial cancer has been published in the February issue of the International Journal of Gynecological Cancer. Zoptarelin doxorubicin, is the Companys cytotoxic peptide conjugate which specifically targets luteinizing hormone-releasing hormone (LHRH) receptors. The article, Efficacy and Safety of AEZS-108 (LHRH Agonist Linked to Doxorubicin) in Women With Advanced or Recurrent Endometrial Cancer Expressing LHRH Receptors: A Multicenter Phase 2 Trial (AGO-GYN5), Emons G., Gorchev G., Harter P., Wimberger P., Stähle A., Hanker L., Hilpert F., Beckmann M.W., Dall P., Gründker C., Sindermann H., Sehouli J., outlines results of this study which had been previously presented at the European Society of Gynaecological Oncologys (ESGO) annual meeting in September 2011. The article is currently ...

TY - JOUR. T1 - Increased potency and sustained suppressive actions of a new gonadotropin-releasing hormone (GnRH) antagonist peptide in man.. AU - Urban, R. J.. AU - Pavlou, S. N.. AU - Rivier, J. E.. AU - Vale, W. W.. AU - Dufau, M. L.. AU - Veldhuis, J. D.. PY - 1988. Y1 - 1988. N2 - We have used a new potent GnRH antagonist to assess the efficacy of suppression of gonadotropin secretion in healthy postmenopausal women at three different doses. The Nal-Glu antagonist produced significant suppression of immunoactive and bioactive LH at a 300 micrograms/kg dose throughout the 30-hr sampling interval with only minimal local (skin) histamine release. This increased potency and decreased skin reactivity of the Nal-Glu antagonist make it a drug with potential clinical use similar to the GnRH agonist, but with the advantage of immediate gonadotropin suppression.. AB - We have used a new potent GnRH antagonist to assess the efficacy of suppression of gonadotropin secretion in healthy postmenopausal ...

TY - JOUR. T1 - Involvement of headless myosin X in the motility of immortalized gonadotropin-releasing hormone neuronal cells. AU - Wang, Jun Jie. AU - Fu, Xiu Qing. AU - Guo, Yu Guang. AU - Yuan, Lin. AU - Gao, Qian Qian. AU - Yu, Hua Li. AU - Shi, Heng Liang. AU - Wang, Xing Zhi. AU - Xiong, Wen Cheng. AU - Zhu, Xiao Juan. N1 - Funding Information: This work was supported by the National Natural Science Foundation of China (30670689) and the Program for New Century Excellent Talents in University (NCET-07-0173), Specialized Research Fund for the Doctoral Program of High Education (20060200008) and Scientific Research Foundation for the Returned Overseas Chinese Scholars from the Ministry of Education of China.. PY - 2009/5. Y1 - 2009/5. N2 - Myosin X (Myo X), an unconventional myosin with a tail homology 4-band 4.1/ezrin/radixin/moesin (MyTH4-FERM) tail, is expressed ubiquitously in various mammalian tissues. In addition to the full-length Myo X (Myo X FL), a headless form is synthesized in ...

Gonadotropin-releasing hormone (GnRH) is considered to stimulate LH secretion from the pituitary. This antibody is raised against an GnRH analog (GnRHa).

Gonadotropin-releasing hormone (GnRH) is a neurohormone central to initiation of the reproductive hormone cascade. Pulsatile secretion of GnRH from the hypothalamus is key in establishing and maintaining normal gonadal function.

Gonadotropin-releasing hormone (GnRH) is a neurohormone central to initiation of the reproductive hormone cascade. Pulsatile secretion of GnRH from the hypothalamus is key in establishing and maintaining normal gonadal function.

The research focus of Dr. Shlomo Melmed is molecular pathogenesis of pituitary tumors and pituitary receptor signaling. He employs molecular, cellular, transgenic animal and human tissue models to understand the biology of these commonly encountered hormone-secreting adenomas. He tests pituitary receptor signaling to develop novel peptide analog treatments for these tumors secreting growth hormone, prolactin, ACTH or gonadotropins.. ...

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Degarelix (INN) or degarelix acetate (USAN) (trade name Firmagon) has an immediate onset of action, binding to gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland and blocking their interaction with GnRH. Reference can be found at ...

Professional guide for Cetrorelix. Includes: pharmacology, pharmacokinetics, contraindications, interactions, adverse reactions and more.

Stacys fitness journey started when her son, Marcus, was very young. Originally, it was something for her to do to reconnect with herself outside of being a mom. Sometimes, Stacy would exercise while Marcus would sleep and other times Marcus and his sisters would exercise alongside her. Her ultimate dream was to reach Ironman distance, and she knew that she wanted to set an example for Marcus and her three girls: that anything is possible. She cant think of anything more rewarding than being a part of #TeamNDSS and working towards raising $10,000 to help fund advocacy and outreach programs.. - Stacy DeLeon Learn More ...