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Prolactin receptor

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https://www.readbyqxmd.com/read/28425851/altered-structure-and-function-of-adipose-tissue-in-long-lived-mice-with-growth-hormone-related-mutations
#1
Justin Darcy, Samuel McFadden, Andrzej Bartke
A major focus of biogerontology is elucidating the role(s) of the endocrine system in aging and the accumulation of age-related diseases. Endocrine control of mammalian longevity was first reported in Ames dwarf (Prop1(df)) mice, which are long-lived due to a recessive Prop1 loss-of-function mutation resulting in deficiency of growth hormone (GH), thyroid-stimulating hormone, and prolactin. Following this report, several other GH-related mutants with altered longevity have been described including long-lived Snell dwarf and growth hormone receptor knockout mice, and short-lived GH overexpressing transgenic mice...
March 21, 2017: Adipocyte
https://www.readbyqxmd.com/read/28425631/restraint-stress-increases-prolactin-mediated-phosphorylation-of-signal-transducer-and-activator-of-transcription-5-in-the-hypothalamus-and-adrenal-cortex-in-the-male-mouse
#2
S E Kirk, T Y Xie, F J Steyn, D R Grattan, S J Bunn
Prolactin is a pleiotropic peptide hormone produced by the lactotrophs in the anterior pituitary. Its rate of secretion is primarily regulated by a negative feedback mechanism whereby prolactin stimulates the activity of the tuberoinfundibular dopaminergic (TIDA) neurons, increasing their release of dopamine which accesses the pituitary via the median eminence to suppress further prolactin secretion. In addition to its well established role in lactation, circulating prolactin is secreted in response to stress, although the mechanism by which this is achieved or its cellular targets are unknown...
April 20, 2017: Journal of Neuroendocrinology
https://www.readbyqxmd.com/read/28423697/essential-role-of-endogenous-prolactin-and-cdk7-in-estrogen-induced-upregulation-of-the-prolactin-receptor-in-breast-cancer-cells
#3
Raghuveer Kavarthapu, Maria L Dufau
Our early studies have shown that Estradiol (E2)/Estrogen Receptor α (ER) in a non-DNA dependent manner through complex formation with C/EBPβ/SP1 induced transcriptional activation of the generic hPIII promoter and expression of the Prolactin Receptor (PRLR) receptor in MCF-7 cells. Subsequent studies demonstrated effects of unliganded ERα with requisite participation of endogenous PRL on the activation of PRLR transcription. Also, EGF/ERBB1 in the absence of PRL and E2 effectively induced upregulation of the PRLR...
March 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28412548/internal-image-anti-idiotypic-antibody-a-new-strategy-for-the-development-a-new-category-of-prolactin-receptor-prlr-antagonist
#4
Hainan Lan, Pan Hong, Ruonan Li, Suo L, Shan Anshan, Steven Li, Xin Zheng
Over the past decades, a number of prolactin receptor (PRLR) antagonists have been developed, which can be divided into two categories, PRLR analogue and anti-PRLR antibody. However, until now, there have been no commercially available PRLR antagonists. Here, we described a new approach for the preparation of PRLR antagonist, namely internal image anti-idiotypic antibody strategy. The hybridoma technique was used to generate anti-idiotypic antibodies to PRL. Competitive ELISA, competitive receptor-binding analysis and immunofluorescence assay (IFA) were then used to screen and characterize anti-idiotypic antibodies to PRL...
April 13, 2017: Molecular Immunology
https://www.readbyqxmd.com/read/28412388/prolactin-modulates-luteal-activity-in-the-short-nosed-fruit-bat-cynopterus-sphinx-during-delayed-embryonic-development
#5
Anuradha, Amitabh Krishna
The aim of this study was to evaluate the role of prolactin as a modulator of luteal steroidogenesis during the period of delayed embryonic development in Cynopterus sphinx. A marked decline in circulating prolactin levels was noted during the months of November through December coinciding with the period of decreased serum progesterone and delayed embryonic development. The seasonal changes in serum prolactin levels correlated positively with circulating progesterone (P) level, but inversely with circulating melatonin level during first pregnancy showing delayed development in Cynopterus sphinx...
April 12, 2017: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28407852/establishment-and-characterization-of-a-telomerase-immortalized-porcine-luteal-cells
#6
Liang Zhang, Yong Huang, Zhenyu Wang, Xiaomao Luo, Hongling Zhang, Qian Du, Lingling Chang, Xiaomin Zhao, Dewen Tong
Luteal cells play a crucial role in pregnancy through secreting progesterone to maintain pregnancy and support of fetus. However, low cellular yields and inability to passage primary porcine luteal cells (PLCs) in vitro limit the luteal cell study. Therefore, developing an immortalized porcine luteal cell line is necessary for studying luteal cells activity and function in different diseases. In this study, primary PLCs were obtained from gilts at day 30 to day 50 of gestation and immortalized by human telomerase reverse transcriptase (hTERT)...
May 2017: Theriogenology
https://www.readbyqxmd.com/read/28405133/risperidone-induced-adverse-drug-reactions-and-role-of-drd2-141-c-ins-del-and-5htr2c-759-c-t-genetic-polymorphisms-in-patients-with-schizophrenia
#7
Charanraj Goud Alladi, Anbarasan Mohan, Deepak Gopal Shewade, Ravi Philip Rajkumar, Surendiran Adithan, Karthick Subramanian
OBJECTIVE: To determine the adverse drug reaction (ADR) profile of risperidone and their association with dopamine (DRD2 - 141 C Ins/Del/rs1799732) and serotonin receptor (5HTR2C -759 C>T/rs3813929) gene polymorphisms in patients with schizophrenia. MATERIALS AND METHODS: The study was conducted among 289 patients who were diagnosed with schizophrenia and were on treatment with risperidone (4-8 mg/day)-based therapy for a minimum of 4 weeks. Genotyping was carried by real-time quantitative polymerase chain reaction...
January 2017: Journal of Pharmacology & Pharmacotherapeutics
https://www.readbyqxmd.com/read/28404690/pharmacologic-characterization-of-valbenazine-nbi-98854-and-its-metabolites
#8
Dimitri E Grigoriadis, Evan Smith, Sam R J Hoare, Ajay Madan, Haig Bozigian
The vesicular monoamine transporter 2 (VMAT2) is an integral presynaptic protein that regulates the packaging and subsequent release of dopamine and other monoamines from neuronal vesicles into the synapse. Valbenazine (NBI-98854), a novel compound that selectively inhibits VMAT2, is being developed for the treatment of tardive dyskinesia. Valbenazine is converted to two significant circulating metabolites in vivo, namely, (+)-α-dihydrotetrabenazine (R,R,R-DHTBZ) and a mono-oxy metabolite, NBI-136110. Radioligand binding studies were conducted to assess and compare valbenazine, tetrabenazine and their respective metabolites in their abilities to selectively and potently inhibit [(3)H]-DHTBZ binding to VMAT2 in rat striatal, rat forebrain, and human platelet homogenates...
April 12, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28396166/paeoniflorin-and-liquiritin-two-major-constituents-in-chinese-herbal-formulas-used-to-treat-hyperprolactinemia-associated-disorders-inhibits-prolactin-secretion-in-prolactinoma-cells-by-different-mechanisms
#9
Yuanyi Wei, Lei La, Lili Wang, Robert Batey, Yuhao Li, Chunxia Wang
ETHNOPHARMACOLOGICAL RELEVANCE: Paeoniflorin and liquiritin are major constituents in some Chinese herbal formulas, such as Yiru Tiaojing (YRTJ) Granule (a hospitalized preparation) and Peony-Glycyrrhiza Decoction, used for hyperprolactinemia-associated disorders. AIM OF THE STUDY: To investigate the effect of paeoniflorin and liquiritin on prolactin secretion. MATERIALS AND METHODS: The effect of YRTJ Granule on metoclopramide-induced hyperprolactinemia was tested in rats...
April 7, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28390952/hypothyroidism-decreases-jak-stat-signaling-pathway-in-lactating-rat-mammary-gland
#10
Fiorella Campo Verde Arboccó, Fabio Andres Persia, María Belén Hapon, Graciela A Jahn
Thyroid pathologies have deleterious effects on lactation. Especially hypothyroidism (HypoT) induces premature mammary involution at the end of lactation and decreases milk production and quality in mid lactation. Milk synthesis is controlled by JAK2/STAT5 signaling pathway and prolactin (PRL), which activates the pathway. In this work we analyzed the effect of chronic 6-propyl-2- thiouracil (PTU)-induced HypoT on PRL signaling pathway on mammary glands from rats on lactation (L) days 2, 7 and 14. HypoT decreased prolactin receptor expression, and expression and activation of Stat5a/b protein...
April 5, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28387824/alpha-estrogen-and-progesterone-receptors-modulate-kisspeptin-effects-on-prolactin-role-in-estradiol-induced-prolactin-surge-in-female-rats
#11
Nayara S S Aquino, Roberta Araujo-Lopes, Patricia C Henriques, Felipe E F Lopes, Daniela O Gusmao, Candido C Coimbra, Celso R Franci, Adelina M Reis, Raphael E Szawka
Kisspeptin regulates prolactin (PRL) in an estradiol-dependent manner. We investigated the interaction between ovarian-steroid receptors and kisspeptin in the control of PRL secretion. Intracerebroventricular injections of kisspeptin-10 (Kp-10) or kisspeptin-234 (Kp-234) were performed in ovariectomized (OVX) rats under different hormonal treatments. Kp-10 increased PRL release and decreased 3,4-dihydroxyphenylacet acid (DOPAC) levels in the median eminence (ME) of OVX rats treated with estradiol (OVX+E), which was prevented by tamoxifen...
April 6, 2017: Endocrinology
https://www.readbyqxmd.com/read/28378505/prolactin-receptors-in-rip-cre-cells-but-not-in-agrp-neurons-are-involved-in-energy-homeostasis
#12
S R Ladyman, M A MacLeod, Z Khant Aung, P Knowles, H R Phillipps, R S E Brown, D R Grattan
Among its many functions, prolactin has been implicated in energy homeostasis, particularly during pregnancy and lactation. The arcuate nucleus is a key site in the regulation of energy balance. The aim of this study was to examine whether arcuate nucleus neuronal populations involved in energy homeostasis are prolactin responsive and if they can mediate the effects of prolactin on energy homeostasis. To determine if Agrp neurons or Rip-Cre neurons are prolactin responsive, transgenic mice expressing the reporter td-tomato in Agrp neurons (td-tomato/AgRP-Cre) or Rip-Cre neurons (td-tomato/Rip-Cre) were treated with prolactin and perfused 45 minutes later...
April 4, 2017: Journal of Neuroendocrinology
https://www.readbyqxmd.com/read/28377489/preclinical-activity-of-the-novel-anti-prolactin-receptor-prlr-antibody-drug-conjugate-regn2878-dm1-in-prlr-positive-breast-cancers
#13
Marcus P Kelly, Carlos Hickey, Sosina Makonnen, Sandra Coetzee, Sumreen Jalal, Yu Wang, Frank Delfino, Jing Shan, Terra B Potocky, Ishita Chatterjee, Julian Andreev, Arthur Kunz, Christopher D'Souza, Jason T Giurleo, Thomas Nittoli, Pamela A Trail, Gavin Thurston, Jessica R Kirshner
The Prolactin Receptor (PRLR) is a type 1 cytokine receptor that is expressed in a subset of breast cancers and may contribute to its pathogenesis. It is relatively over-expressed in ~25% of human breast tumors while expressed at low levels in some normal human tissues including the mammary gland. We developed an anti-PRLR antibody-drug conjugate (ADC), to target PRLR positive breast cancer. REGN2878-DM1 is comprised of a fully human high affinity function-blocking anti-PRLR IgG1 antibody (REGN2878) conjugated via a non-cleavable SMCC linker to the cytotoxic maytansine derivative DM1...
April 4, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28364216/prolactin-androgen-inducible-carboxypeptidase-d-increases-with-nitrotyrosine-and-ki67-for-breast-cancer-progression-in-vivo-and-upregulates-progression-markers-vegf-c-and-runx2-in-vitro
#14
Lynn N Thomas, Emily R Chedrawe, Penelope J Barnes, Catherine K L Too
PURPOSE: Carboxypeptidase-D (CPD) cleaves C-terminal arginine (Arg) to produce nitric oxide (NO). Upregulation of CPD and NO by 17β-estradiol, prolactin (PRL), and androgen increases survival of human breast cancer (BCa) cells in vitro. To demonstrate similar events in vivo, CPD, nitrotyrosine (NT, hallmark of NO action), androgen receptor (AR), prolactin receptor (PRLR), and phospho-Stat5a (for activated PRLR) levels were evaluated in benign and malignant human breast tissues, and correlated with cell proliferation (Ki67) and BCa progression (Cullin-3) biomarkers...
March 31, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28339753/in-ovo-monochromatic-green-light-photostimulation-enhances-embryonic-somatotropic-axis-activity
#15
L Dishon, N Avital-Cohen, D Malamud, R Heiblum, S Druyan, T E Porter, M Gumulka, I Rozenboim
Previous studies demonstrated that in ovo photostimulation with monochromatic green light increases body weight and accelerates muscle development in broilers. The mechanism in which in ovo photostimulation accelerates growth and muscle development is not clearly understood. The objective of the current study was to define development of the somatotropic axis in the broiler embryo associated with in ovo green light photostimulation. Two-hundred-forty fertile broiler eggs were divided into 2 groups. The first group was incubated under intermittent monochromatic green light using light-emitting diode (LED) lamps with an intensity of 0...
February 23, 2017: Poultry Science
https://www.readbyqxmd.com/read/28338740/the-role-of-vip-in-social-behavior-neural-hotspots-for-the-modulation-of-affiliation-aggression-and-parental-care
#16
Marcy A Kingsbury, Leah C Wilson
Although the modulation of social behaviors by most major neurochemical systems has been explored, there are still standouts, including the study of vasoactive intestinal polypeptide (VIP). VIP is a modulator of circadian, reproductive, and seasonal rhythms and is well known for its role in reproductive behavior, as it is the main vertebrate prolactin-releasing hormone. Originally isolated as a gut peptide, VIP and its cognate receptors are present in virtually every brain area that is important for social behavior, including all nodes of the core "social behavior network" (SBN)...
December 16, 2016: Integrative and Comparative Biology
https://www.readbyqxmd.com/read/28337596/prolactin-regulation-of-the-hpa-axis-is-not-mediated-by-a-direct-action-upon-crh-neurons-evidence-from-the-rat-and-mouse
#17
Papillon Gustafson, Ilona Kokay, Tony Sapsford, Stephen Bunn, David Grattan
Centrally acting prolactin has been shown to have anti-stress effects by modulating the activity of the hypothalamic-pituitary-adrenal axis. We tested the hypothesis that prolactin directly targets hypothalamic corticotropin-releasing hormone (CRH) neurons. In situ hybridisation confirmed expression of mRNA encoding the long, but not the short, isoform of the prolactin receptor (PRLR) within the paraventricular nucleus (PVN) of the virgin rat; however, only 6% of CRH neurons expressed long-form Prlr mRNA. Examination of the functional response of CRH neurons to intracerebroventricular prolactin (500 ng) showed that these neurons did not respond with activation of phosphorylated signal transducer and activator of transcription 5 (pSTAT5), a marker of long-form PRLR activation...
March 23, 2017: Brain Structure & Function
https://www.readbyqxmd.com/read/28333280/hcg-activates-the-erk1-2-mitogen-activated-protein-kinase-pathway-in-human-endometrial-stromal-cells-transiently-increasing-the-progesterone-receptor-and-regulating-genes-associated-with-endometrial-receptivity
#18
Alejandro Tapia-Pizarro, Sebastián Archiles, Felipe Argandoña, Cecilia Valencia, Keyla Zavaleta, María Cecilia Johnson, Reinaldo González-Ramos, Luigi Devoto
STUDY QUESTION: How does hCG signal in human endometrial stromal cells (ESCs) and what is its role in regulating ESC function? SUMMARY ANSWER: CG signaling in ESCs activates the extracellular signal-regulated protein kinases 1 and 2 (Erk1/2) pathway through exchange protein activated by cAMP (Epac) and transiently increases progesterone receptor (PR) transcript and protein expression and its transcriptional function. WHAT IS KNOWN ALREADY: hCG is one of the earliest embryo-derived secreted signals in the endometrium, which abundantly expresses LH/hCG receptors...
March 14, 2017: Molecular Human Reproduction
https://www.readbyqxmd.com/read/28331050/first-in-human-clinical-trial-of-oral-onc201-in-patients-with-refractory-solid-tumors
#19
Mark N Stein, Joseph R Bertino, Howard L Kaufman, Tina Mayer, Rebecca Moss, Ann Silk, Nancy Chan, Jyoti Malhotra, Lorna Rodriguez-Rodriguez, Joseph Aisner, Robert D Aiken, Bruce G Haffty, Robert S DiPaola, Tracie Saunders, Andrew Zloza, Sherri Damare, Yasmeen Beckett, Bangning Yu, Saltanat Najmi, Christian Gabel, Siobhan Dickerson, Ling Zheng, Wafik S El-Deiry, Joshua E Allen, Martin Stogniew, Wolfgang Oster, Janice M Mehnert
Purpose ONC201 is a small molecule selective antagonist of the G protein-coupled receptor DRD2 that is the founding member of the imipridone class of compounds. A first-in-human phase I study of ONC201 was conducted to determine its recommended phase II dose (RP2D). Experimental Design This open-label study treated 10 patients during dose escalation with histologically-confirmed advanced solid tumors. Patients received ONC201 orally once every 3 weeks, defined as one cycle, at doses from 125 to 625 mg using an accelerated titration design...
March 22, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28330858/prolactin-up-regulates-female-predominant-cyp-gene-expressions-and-down-regulates-male-predominant-gene-expressions-in-mice-liver
#20
Yuya Sato, Yoshikatsu Kaneko, Takamasa Cho, Kei Goto, Tadashi Otsuka, Suguru Yamamoto, Shin Goto, Hiroki Maruyama, Ichiei Narita
Prolactin is a polypeptide hormone with over 300 separate biological activities and its serum level is increased during pregnancy and lactation. It has been described that pregnancy and lactation affect drug and steroid metabolism in mice and humans. Several studies reported that pregnancy or lactation influences liver cytochrome P450 (Cyp) expression and its activity, affecting the biosynthesis of steroids and xenobiotics through growth hormone or sex hormones; however, the role of prolactin as the regulator of liver Cyp expression has not been elucidated so far...
March 22, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
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