G protein‐coupled receptors of the hypothalamic–pituitary–gonadal axis: A case for gnrh, LH, FSH, and GPR54 receptor ligands

Heitman, Laura H.; IJzerman, Adriaan P.

doi:10.1002/med.20129

Cited by 53 publications

(34 citation statements)

References 114 publications

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“…Many pathways including cAMP and cAMP-dependent protein kinase A are reported to be involved in regulating this process (Downs et al, 2002;Homa, 1988). FSH stimulates germinal-vesicle breakdown (GVBD) and resumption of oocyte maturation both in vitro and in vivo (Assidi et al, 2008(Assidi et al, , 2010Sirard et al, 2007) through binding to FSH receptors on granulosa cells or cumulus cells which are G-protein-coupled receptors (Heitman and Ijzerman, 2008;Segaloff et al, 1990) and results in a signalling cascade involving increasing intracellular cAMP concentrations (Dekel, 1988) and stimulation of prostaglandin E synthesis (Shimada et al, 2006;Yamashita et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Role of PTGS2-generated PGE2 during gonadotrophin-induced bovine oocyte maturation and cumulus cell expansion

Marei

Abayasekara

Wathes

et al. 2014

Reproductive BioMedicine Online

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(AA Fouladi-Nashta).Waleed Fawzy A Marei is a veterinarian and graduated from Cairo University, Egypt in 2001. He started his academic career in theriogenology in 2002 and obtained his MSc degree in 2005. He joined the reproduction research group at the Royal Veterinary College, London, UK and investigated the effects of fatty acids on oocyte quality and early embryo development for his PhD, awarded in 2010. He then pursued post-doctoral research in the same group, working on early embryo development and implantation. Currently, he is a lecturer on theriogenology at Cairo University. His interests are clinical applications of assisted reproduction technologies and feed additives to improve reproductive performance in farm animals.Abstract Prostaglandin E 2 (PGE 2 ) is an autocrine/paracrine factor which mediates gonadotrophin (Gn) stimulation of cumulus expansion and oocyte maturation in rodents. Its role in bovine oocyte maturation is less characterized. This study detected PTGS2 (COX2) and PGE synthases (PTGES1, PTGES2 and PTGES3) in bovine cumulus-oocyte complexes (COC). Only PTGS2 and PTGES1 expression changed during maturation. In Gn-free media, no cumulus expansion and $45% nuclear maturation was achieved, while Gn-induced maturation showed full cumulus expansion (score 3) and $87% maturation. PGE 2 supplementation without Gn induced mild cumulus expansion (score 0.5-1) but increased nuclear maturation to levels similar to those obtained with Gn alone. In the presence of Gn, exogenous PGE 2 did not affect expansion or nuclear maturation and subsequent embryo development. Treatment with PTGS2 selective inhibitor (NS398), PTGS2-specific siRNA or PTGER2-receptor antagonist (AH6809) resulted in $20-25% reduction in nuclear maturation. NS398 and AH6809 did not affect cumulus expansion. Most oocytes not reaching metaphase of second meiosis (MII) following NS398, AH6809 and PTGS2-specific siRNA treatments were at MI. After longer maturation, NS398-treated oocytes had normal MII rate and uncompromised embryo development. PGE 2 has a limited role in cumulus expansion in bovine COC but is important for the timing of Gn-induced nuclear maturation. RBMOnline

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Section: Introductionmentioning

confidence: 99%

Role of PTGS2-generated PGE2 during gonadotrophin-induced bovine oocyte maturation and cumulus cell expansion

Marei

Abayasekara

Wathes

et al. 2014

Reproductive BioMedicine Online

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“…Hypergeometric tests of gene ontology terms and pathways revealed significant (P < 0.01) overrepresentation of genes involved with olfactory and G-protein coupled receptor functions near the SNP affecting puberty, follicle count, and pregnancy (Table 3). The olfactory system is high in G-protein coupled receptors, and G-protein coupled receptors regulate the hypothalamic-pituitary-gonadal axis, affecting reproduction and sex hormone-dependent diseases (Heitman and Ijzerman, 2008). The set of genes involved with the overrepresented olfactory and G-protein receptor functions were used to identify a set of 55,421 BovineHD SNP for further evaluation in Cycle VII heifers.…”

Section: Evaluation Of Large and Reduced Snp Sets From The Bovinehd Bmentioning

confidence: 99%

PHYSIOLOGY AND ENDOCRINOLOGY SYMPOSIUM: How single nucleotide polymorphism chips will advance our knowledge of factors controlling puberty and aid in selecting replacement beef females1,2,3,4

Snelling

Cushman

Fortes

et al. 2012

Journal of Animal Science

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ABSTRACT:The promise of genomic selection is accurate prediction of the genetic potential of animals from their genotypes. Simple DNA tests might replace low-accuracy predictions for expensive or lowly heritable measures of puberty and fertility based on performance and pedigree. Knowing with some certainty which DNA variants (e.g., SNP) affect puberty and fertility is the best way to fulfill the promise. Several SNP from the BovineSNP50 assay have tentatively been associated with reproductive traits including age at puberty, antral follicle count, and pregnancy observed on different sets of heifers. However, sample sizes are too small and SNP density is too sparse to definitively determine genomic regions harboring causal variants affecting reproductive success. Additionally, associations between individual SNP and similar phenotypes are inconsistent across data sets, and genomic predictions do not appear to be globally applicable to cattle of different breeds. Discrepancies may be a result of different QTL segregating in the sampled populations, differences in linkage disequilibrium (LD) patterns such that the same SNP are not correlated with the same QTL, and spurious correlations with phenotype. Several approaches can be used independently or in combination to improve detection of genomic factors affecting heifer puberty and fertility. Larger samples and denser SNP will increase power to detect real associations with SNP having more consistent LD with underlying QTL. Meta-analysis combining results from different studies can also be used to effectively increase sample size. Highdensity genotyping with heifers pooled by pregnancy status or early and late puberty can be a cost-effective means to sample large numbers. Networks of genes, implicated by associations with multiple traits correlated with puberty and fertility, could provide insight into the complex nature of these traits, especially if corroborated by functional annotation, established gene interaction pathways, and transcript expression. Example analyses are provided to demonstrate how integrating information about gene function and regulation with statistical associations from whole-genome SNP genotyping assays might enhance knowledge of genomic mechanisms affecting puberty and fertility, enabling reliable DNA tests to guide heifer selection decisions.

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“…Вещество 9 стимулирует АЦ со значением EC 50 1,2 нМ, являясь частичным агонистом рецептора ФСГ. В настоящее время получены и другие агонисты рецептора ФСГ на основе тетрагидрохинолина, гексагидрохинолина, карбазола, тиено [2,3-D]пиримидина, изоксазолилтиазола и пиразола [22]. Наиболее эффективные из них запатентованы фармацевтическими компаниями ("Organon Biosciences", "Serono RBI", "ARS Holding", "Arena").…”

Section: рисунок 3 низкомолекулярные агонисты рецептора фолликулостиunclassified

“…Поскольку как вещество 11, так и вещество 10 не способны сами стимулировать активность АЦ, то можно предположить, что они блокируют активацию серпантинного домена эктодоменом, но не способны, в отличие от агонистов, вызывать в серпантинном домене такие конформационные изменения, которые ведут к активации им G s -белка [39]. В настоящее время запатентованы четыре антагониста, которые относятся к классам аминоалкиламидов, пиперазинов, пиррол[2,1-c]-бензодиазепинов и индола [22]. Следует отметить, что все антагонисты, исключая производные пиперазина, содержат бифенильные радикалы, которые являются, как полагают важнейшей структурной детерминантой, необходимой для эффективного взаимодействия низкомолекулярных лигандов с серпантинным доменом рецептора ФСГ.…”

Section: рисунок 3 низкомолекулярные агонисты рецептора фолликулостиunclassified

“…Вещество Org43553 также активно в условиях in vivo, как индуктор овуляции, и сопоставимо по эффективности действия с чХГ. Org41841 и Org43553 запатентованы фирмой "Organon Biosciences" и предполагаются для широкого применения в качестве агонистов рецепторов гонадотропинов [22].…”

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Low-molecular regulators of polypeptide hormones receptors containing LGR-repeats

Шпаков

Shpakova

2010

BIOMED KHIM

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During the last years the low-molecular non-peptidic regulators of the polypeptide hormones receptors containing LGR-repeats were identified. In the review the data on the structure and the molecular mechanisms of action of these regulators as agonists and antagonists of the luteinizing, follicle-stimulating and thyrotropin hormones are analyzed and systematized. The regulators interact with the serpentine domain of LGR-receptor and trigger the signaling cascades coupled with the receptor. Low-molecular agonists and antagonists of the LGR-receptors are considered as a new generation of the drugs that regulates the functional activity of sensitive to pituitary glycoprotein hormones signaling systems with high efficiency and selectivity. These regulators are more accessible compared to the hormones and can be use orally.

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G protein‐coupled receptors of the hypothalamic–pituitary–gonadal axis: A case for gnrh, LH, FSH, and GPR54 receptor ligands

Cited by 53 publications

References 114 publications

Role of PTGS2-generated PGE2 during gonadotrophin-induced bovine oocyte maturation and cumulus cell expansion

Role of PTGS2-generated PGE2 during gonadotrophin-induced bovine oocyte maturation and cumulus cell expansion

PHYSIOLOGY AND ENDOCRINOLOGY SYMPOSIUM: How single nucleotide polymorphism chips will advance our knowledge of factors controlling puberty and aid in selecting replacement beef females1,2,3,4

Low-molecular regulators of polypeptide hormones receptors containing LGR-repeats

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