9,851 results match your criteria Molecular and cellular endocrinology[Journal]


Relaxin and fibrosis: Emerging targets, challenges, and future directions.

Mol Cell Endocrinol 2019 Feb 14. Epub 2019 Feb 14.

Cardiovascular Disease Theme, Monash Biomedicine Discovery Institute and Department of Pharmacology, Monash University, Clayton, VIC, Australia; Central Clinical School, Monash University, Prahran, VIC, Australia. Electronic address:

The peptide hormone relaxin is well-known for its anti-fibrotic actions in several organs, particularly from numerous studies conducted in animals. Acting through its cognate G protein-coupled receptor, relaxin family peptide receptor 1 (RXFP1), serelaxin (recombinant human relaxin) has been shown to consistently inhibit the excessive extracellular matrix production (fibrosis) that results from the aberrant wound-healing response to tissue injury and/or chronic inflammation, and at multiple levels. Furthermore, it can reduce established scarring by promoting the degradation of aberrant extracellular matrix components. Read More

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http://dx.doi.org/10.1016/j.mce.2019.02.005DOI Listing
February 2019

Emerging roles for the relaxin/RXFP1 system in cancer therapy.

Mol Cell Endocrinol 2019 Feb 11. Epub 2019 Feb 11.

Department of Human Anatomy and Cell Science, College of Medicine, University of Manitoba, Winnipeg, Canada. Electronic address:

A role for the hormone relaxin in cancer was described well before the receptor was identified. Relaxin predominantly increases the growth and invasive potential in cancers of different origins. However, relaxin was also shown to promote cell differentiation and to act in a dose-and time-dependent manner in different cancer cell models used. Read More

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http://dx.doi.org/10.1016/j.mce.2019.02.001DOI Listing
February 2019

Galectin-3 plays an important role in endometriosis development and is a target to endometriosis treatment.

Mol Cell Endocrinol 2019 Feb 9. Epub 2019 Feb 9.

Morphological Sciences Program, Biomedical Sciences Institute, Federal University of Rio de Janeiro - UFRJ, Rio de Janeiro, RJ, Brazil.

This study aimed to analyze galectin-3 importance in endometriotic lesions development and the effect of recombinant Gal-3 carbohydrate recognition domain (Gal3C) in experimental endometriosis treatment. Experimental endometriosis was induced in WT and Gal-3-/- mice. Initially developed lesions were macroscopically and histologically analyzed, including immunohistochemical analysis. Read More

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http://dx.doi.org/10.1016/j.mce.2019.02.007DOI Listing
February 2019

Effects of stanniocalcin hormones on rat brown adipose tissue metabolism under fed and fasted conditions.

Mol Cell Endocrinol 2019 Feb 7. Epub 2019 Feb 7.

Department of Physiology, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.

In this study we determined the effect of fed and fasting (48 h) states on the expression of stanniocalcin-1 (Stc1) and stanniocalcin-2 (Stc2) in rat brown adipose tissue (BAT), as well as the in vitro effects of human stanniocalcin 1 and 2 (hSTC-1 and hSTC-2) hormones on lipid and glucose metabolism. In addition, lactate, glycogen levels and hexokinase (HK) activity were determined. In fasting Stc2 expression increased markedly. Read More

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http://dx.doi.org/10.1016/j.mce.2019.02.004DOI Listing
February 2019

Binding kinetics of ligands acting at GPCRs.

Mol Cell Endocrinol 2019 Feb 7. Epub 2019 Feb 7.

Cell Signalling and Pharmacology Research Group, Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, UK; Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK. Electronic address:

The influence of drug-receptor binding kinetics has often been overlooked during the development of new therapeutics that target G protein-coupled receptors (GPCRs). Over the last decade there has been a growing understanding that an in-depth knowledge of binding kinetics at GPCRs is required to successfully target this class of proteins. Ligand binding to a GPCR is often not a simple single step process with ligand freely diffusing in solution. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.018DOI Listing
February 2019

ETV5 regulates GOAT/ghrelin system in an mTORC1-dependent manner.

Mol Cell Endocrinol 2019 Feb 5. Epub 2019 Feb 5.

Center for Diabetes, Obesity and Metabolism, Department of Physiology, Shenzhen University Health Science Center, Shenzhen, Guangdong province, 518000, China; Department of Physiology and Pathophysiology, School of Basic Science, Peking University Health Science Center, Beijing, 100191, China. Electronic address:

Ghrelin, a 28 amino acid peptide hormone, regulates multiple important metabolic functions. Its acylation by ghrelin-O-acyl-transferase enzyme (GOAT) is required for binding to and activating its receptor, the growth hormone secretagogue receptor 1a. Mechanism underlying the regulation of GOAT and acyl ghrelin remains unclear. Read More

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http://dx.doi.org/10.1016/j.mce.2019.02.003DOI Listing
February 2019
4.405 Impact Factor

Clinical applications of small molecule inhibitors of Pregnane X receptor.

Mol Cell Endocrinol 2019 Feb 3. Epub 2019 Feb 3.

Basic Sciences, Kansas City University of Medicine and Biosciences, Joplin, MO, USA. Electronic address:

The canonical effect of Pregnane X Receptor (PXR, NR1I2) agonism includes enhanced hepatic uptake and a concomitant increase in the first-pass metabolism and efflux of drugs in mammalian liver and intestine. In patients undergoing combination therapy, PXR-mediated gene regulation represents the molecular basis of numerous food-drug, herb-drug, and drug-drug interactions. Moreover, PXR activation promotes chemotherapeutic resistance in certain malignancies. Read More

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http://dx.doi.org/10.1016/j.mce.2019.02.002DOI Listing
February 2019
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The impact of sensory and motor enrichment on the epigenetic control of steroidogenic-related genes in rat hippocampus.

Mol Cell Endocrinol 2019 Feb 2. Epub 2019 Feb 2.

Departamento de Bioquímica Clínica y Cuantitativa, Facultad de Bioquímica y Ciencias Biológicas, Universidad Nacional del Litoral, Santa Fe, Argentina; Instituto de Salud y Ambiente del Litoral(ISAL), Facultad de Bioquímica y Ciencias Biológicas, Universidad Nacional del Litoral-CONICET, Santa Fe, Argentina. Electronic address:

In the present study, we analyzed the effects of a short-term environmental enrichment on the mRNA expression and DNA methylation of steroidogenic enzymes in the hippocampus. Thus, young adult (80-day-old) and middle-aged (350-day-old) Wistar female rats were exposed to sensory (SE) or motor (ME) enrichment during 10 days and compared to animals housed under standard conditions. SE was provided by an assortment of objects that included plastic tubes and toys; for ME, rodent wheels were provided. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.025DOI Listing
February 2019

Regulation of Gpr173 expression, a putative phoenixin receptor, by saturated fatty acid palmitate and endocrine-disrupting chemical bisphenol A through a p38-mediated mechanism in immortalized hypothalamic neurons.

Mol Cell Endocrinol 2019 Feb 1. Epub 2019 Feb 1.

Department of Physiology, University of Toronto, Toronto, ON, Canada; Departments of Obstetrics and Gynaecology and Medicine, University of Toronto, Toronto, ON, Canada. Electronic address:

GPR173 is a highly conserved G protein coupled receptor associated with the hypothalamic-pituitary-gonadal reproductive axis. It is expressed in the brain and ovaries, however considerable knowledge about its function remains unknown. One putative ligand for this receptor is phoenixin (PNX), a newly identified reproductive peptide involved in hypothalamic coordination of the estrous cycle. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.026DOI Listing
February 2019
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Rapid effect of bisphenol A on glutamate-induced Ca influx in hippocampal neurons of rats.

Mol Cell Endocrinol 2019 Jan 29. Epub 2019 Jan 29.

Chemistry and Life Sciences College, Key Laboratory of Wildlife Biotechnology and Conservation and Utilization of Zhejiang Province, Zhejiang Provincial Key Laboratory of Ecology, Zhejiang Normal University, PR China. Electronic address:

Intracellular Ca signaling plays an essential role in synaptic plasticity. This study examined the effect of BPA on concentration of intracellular Ca ([Ca]) by measuring fluorescence intensity of Ca in hippocampal neurons in vitro. The results showed that BPA for 30 min exerted dose-dependently dual effects on glutamate-elevated [Ca]: BPA at 1-10 μM suppressed but at 1-100 nM enhanced glutamate-raised [Ca]. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.024DOI Listing
January 2019

The structural basis of the arrestin binding to GPCRs.

Mol Cell Endocrinol 2019 Mar 28;484:34-41. Epub 2019 Jan 28.

Department of Pharmacology, Vanderbilt University, Nashville, TN, 37232, USA.

G protein-coupled receptors (GPCRs) are the largest family of signaling proteins targeted by more clinically used drugs than any other protein family. GPCR signaling via G proteins is quenched (desensitized) by the phosphorylation of the active receptor by specific GPCR kinases (GRKs) followed by tight binding of arrestins to active phosphorylated receptors. Thus, arrestins engage two types of receptor elements: those that contain GRK-added phosphates and those that change conformation upon activation. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.019DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6377262PMC

Allosteric small molecule modulators of nuclear receptors.

Mol Cell Endocrinol 2019 Jan 28. Epub 2019 Jan 28.

Laboratory of Chemical Biology, Department of Biomedical Engineering and Institute for Complex Molecular Systems, Technische Universiteit Eindhoven, Den Dolech 2, 5612AZ, Eindhoven, the Netherlands. Electronic address:

Nuclear Receptors (NRs) are multi-domain proteins, whose natural regulation occurs via ligands for a classical, orthosteric, binding pocket and via intra- and inter-domain allosteric mechanisms. Allosteric modulation of NRs via synthetic small molecules has recently emerged as an interesting entry to address the need for small molecules targeting NRs in pathology, via novel modes of action and with beneficial profiles. In this review the general concept of allosteric modulation in drug discovery is first discussed, serving as a background and inspiration for NRs. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.022DOI Listing
January 2019

Modulation of nuclear receptor function: Targeting the protein-DNA interface.

Mol Cell Endocrinol 2019 Mar 28;484:1-14. Epub 2019 Jan 28.

Brazilian Biosciences National Laboratory (LNBio), Brazilian Center for Research in Energy and Materials (CNPEM), Campinas, SP, 13083-970, Brazil. Electronic address:

Nuclear receptors (NRs) are a superfamily of ligand-dependent transcription factors that modulate several biological processes. Traditionally, modulation of NRs has been focused on the development of ligands that recognize and bind to the ligand binding domain (LBD), resulting in activation or repression of transcription through the recruitment of coregulators. However, for more severe diseases, such as breast and prostate cancer, the conventional treatment addressing LBD modulation is not always successful, due to tumor resistance. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.023DOI Listing
March 2019
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Japanese medaka as a model for studying the relaxin family genes involved in neuroendocrine regulation: Insights from the expression of fish-specific rln3 and insl5 and rxfp3/4-type receptor paralogues.

Mol Cell Endocrinol 2019 Jan 28. Epub 2019 Jan 28.

Department of Biology, The University of Winnipeg, Winnipeg, MB, Canada; Department of Biology, The University of Manitoba, Winnipeg, MB, Canada. Electronic address:

The goal of this paper is to establish Japanese medaka (Oryzias latipes) as a model for relaxin family peptide research, particularly for studying the functions of RLN3 and INSL5, hormones playing roles in neuroendocrine regulation. Medaka, like other teleosts, retained duplicate copies of rln3, insl5 and their rxfp3/4-type receptors following fish-specific whole genome duplication (WGD) and paralogous copies of these genes may have sub-functionalised providing an intuitive model for teasing apart the pleiotropic roles of the corresponding genes in mammals. To this end, we provide experimental evidence for the expression of the relaxin family genes in medaka that had previously only been identified in-silico, confirm the gene structure of five of the ligand genes, characterise gene expression across multiple tissues and during embryonic development, perform in situ hybridization with anti-sense insl5a on embryos and in adult brain and intestinal samples, and compare these results to the data available in zebrafish. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.017DOI Listing
January 2019
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Nanobodies: New avenues for imaging, stabilizing and modulating GPCRs.

Mol Cell Endocrinol 2019 Mar 26;484:15-24. Epub 2019 Jan 26.

Amsterdam Institute for Molecules, Medicines and Systems (AIMMS), Division of Medicinal Chemistry, Faculty of Sciences, Vrije Universiteit, De Boelelaan 1108, 1081 HZ, Amsterdam, the Netherlands. Electronic address:

The family of G protein-coupled receptors (GPCRs) is the largest class of membrane proteins and an important drug target due to their role in many (patho)physiological processes. Besides small molecules, GPCRs can be targeted by biologicals including antibodies and antibody fragments. This review describes the use of antibodies and in particular antibody fragments from camelid-derived heavy chain-only antibodies (nanobodies/VHHs/sdAbs) for detecting, stabilizing, modulating and therapeutically targeting GPCRs. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.021DOI Listing
March 2019
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NMR analysis of GPCR conformational landscapes and dynamics.

Mol Cell Endocrinol 2019 Mar 25;484:69-77. Epub 2019 Jan 25.

Laboratoire de Biologie Physico-Chimique des Protéines Membranaires, UMR7099, CNRS/Université; Paris Diderot, Sorbonne Paris Cité, Institut de Biologie Physico-Chimique (FRC 550), 13 rue Pierre et Marie Curie, 75005, Paris, France. Electronic address:

Understanding the signal transduction mechanism mediated by the G Protein-Coupled Receptors (GPCRs) in eukaryote cells represents one of the main issues in modern biology. At the molecular level, various biophysical approaches have provided important insights on the functional plasticity of these complex allosteric machines. In this context, X-ray crystal structures published during the last decade represent a major breakthrough in GPCR structural biology, delivering important information on the activation process of these receptors through the description of the three-dimensional organization of their active and inactive states. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.019DOI Listing
March 2019
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Oxidative stress increases the 17,20-lyase-catalyzing activity of adrenal P450c17 through p38α in the development of hyperandrogenism.

Mol Cell Endocrinol 2019 Mar 23;484:25-33. Epub 2019 Jan 23.

Department of Endocrinology, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, 639 Zhizaoju Road, Shanghai, 200011, China. Electronic address:

Unexplained hyperandrogenic oligoanovulation is a main feature of polycystic ovary syndrome (PCOS). P450c17 phosphorylation selectively increases 17,20-lyase activity and androgen biosynthesis but minimally affects 17α-hydroxylase. Studies have recently identified mitogen-activated protein kinase 14 (MAPK14, p38α) as the kinase responsible for enhancing 17,20-lyase activity through P450c17 phosphorylation. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03037207193002
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http://dx.doi.org/10.1016/j.mce.2019.01.020DOI Listing
March 2019
5 Reads

Estrogen receptors localization and signaling pathways in DU-145 human prostate cancer cells.

Mol Cell Endocrinol 2019 Mar 17;483:11-23. Epub 2019 Jan 17.

Laboratory of Experimental Endocrinology, Department of Pharmacology, Escola Paulista de Medicina, Universidade Federal de São Paulo, Rua Pedro de Toledo 669, Vila Clementino, São Paulo, SP, 04039-032, Brazil. Electronic address:

The aim of the present study was to investigate the subcellular localization of estrogen receptors ERα and ERβ in androgen-independent prostate cancer cell line DU-145, and the possible role of exportin CRM1 on ERs distribution. In addition, we evaluated the ERs contribution to activation of ERK1/2 and AKT. Immunostaining of ERα and ERβ was predominantly found in the extranuclear regions of DU-145 cells. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.015DOI Listing
March 2019
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Oxysterols and nuclear receptors.

Mol Cell Endocrinol 2019 Mar 18;484:42-51. Epub 2019 Jan 18.

Department of Molecular and Integrative Physiology, University of Illinois at Urbana-Champaign, Urbana, IL, United States; University of Illinois Cancer Center, Chicago, IL, United States; Division of Nutritional Sciences, University of Illinois at Urbana-Champaign, Urbana, IL, United States; Carl R. Woese Institute for Genomic Biology, Anticancer Discovery from Pets to People Theme, University of Illinois at Urbana Champaign, Urbana, IL, United States; Cancer Center at Illinois, University of Illinois at Urbana-Champaign, IL, United States. Electronic address:

Oxysterols are derivatives of cholesterol and an important regulator of cholesterol metabolism, in part due to their role as ligands for nuclear receptors, such as the liver X receptors. Oxysterols are also known to be ligands for the RAR-related orphan receptors, involved in normal T cell differentiation. However, increasing evidence supports a role for oxysterols in the progression of several diseases. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03037207193002
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http://dx.doi.org/10.1016/j.mce.2019.01.016DOI Listing
March 2019
4 Reads

Effect of the TYK-2/STAT-3 pathway on lipid accumulation induced by mono-2-ethylhexyl phthalate.

Mol Cell Endocrinol 2019 Mar 17;484:52-58. Epub 2019 Jan 17.

Department of Occupational and Environmental Health, School of Public Health, Jilin University, Changchun, China. Electronic address:

Background: Mono-2-ethylhexyl phthalate (MEHP), an important metabolite of di (2-ethylhexyl) phthalate (DEHP), can induce lipid metabolic disorder. Previous studies have shown that MEHP promotes 3T3-L1 cell differentiation; however, the underlying mechanism is unclear. The present study was performed to investigate the effect of the TYK-2/STAT-3 pathway on lipid accumulation induced by MEHP. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.012DOI Listing

Relaxin and extracellular matrix remodeling: Mechanisms and signaling pathways.

Mol Cell Endocrinol 2019 Jan 17. Epub 2019 Jan 17.

Research Service, VA Nebraska-Western Iowa Health Care System, Departments of Internal Medicine and Biochemistry & Molecular Biology, University of Nebraska Medical Center, Omaha, NE, USA. Electronic address:

Fibrosis is associated with accumulation of excess fibrillar collagen, leading to tissue dysfunction. Numerous processes, including inflammation, myofibroblast activation, and endothelial-to-mesenchymal transition, play a role in the establishment and progression of fibrosis. Relaxin is a peptide hormone with well-known antifibrotic properties that result from its action on numerous cellular targets to reduce fibrosis. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.015DOI Listing
January 2019
5 Reads

Insights into how phosphorylation of estrogen receptor at serine 305 modulates tamoxifen activity in breast cancer.

Mol Cell Endocrinol 2019 Mar 16;483:97-101. Epub 2019 Jan 16.

Department of Physiology and Biophysics, University of Illinois at Chicago, Chicago, IL, USA.

Estrogen receptor (ER) is the most important factor in the pathophysiology of breast cancer. Consequently, modulation of ER activity has been exploited to develop drugs against ER + breast cancer, such as tamoxifen, referred to as endocrine therapies. With deeper understanding of ER mechanism of action, posttranslational modifications (PTMs) are increasingly recognized as important in mediating ER activity. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.014DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6368394PMC
March 2019
2 Reads

Relaxin-2 for heart failure with preserved ejection fraction (HFpEF): Rationale for future clinical trials.

Mol Cell Endocrinol 2019 Jan 16. Epub 2019 Jan 16.

Relaxera Pharmazeutische Gesellschaft mbH & Co. KG, Stubenwald-Allee 8a, 64625, Bensheim, Germany. Electronic address:

Heart Failure with preserved Ejection Fraction (HFpEF), a distinct sub-entity of chronic heart failure characterized by generalized inflammatory non-compliance of the cardio-vascular system, is associated with high mortality and still an unmet medical need. Many novel and promising therapeutic approaches have failed in large studies. This review focuses on basic research, pre-clinical and clinical findings that may account for the potential benefit of relaxin-2 in HFpEF. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.013DOI Listing
January 2019

Alternative binding sites at the vitamin D receptor and their ligands.

Mol Cell Endocrinol 2019 Jan 14. Epub 2019 Jan 14.

Department of Chemistry and Biochemistry and Milwaukee Institute for Drug Discovery (MIDD), University of Wisconsin, Milwaukee, WI, 53211, USA. Electronic address:

In recent decades, the majority of ligands developed for the vitamin D receptor (VDR) bind at its deeply buried genomic ligand binding pocket. Theses ligands can be categorized into agonists and partial agonists/antagonists. A limited number of ligands, most of them peptides, bind the VDR‒coactivator binding site that is formed in the presence of an agonist and inhibit coactivator recruitment, and therefore transcription. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.011DOI Listing
January 2019

Bisphenol S increases EZRIN expression and the detrimental effects induced by dehydroepiandrosterone in rat endometrium.

Mol Cell Endocrinol 2019 Mar 14;483:64-73. Epub 2019 Jan 14.

National Atomic Energy Commission of Argentina (CNEA), National Research Council of Argentina (CONICET), Department of Radiobiology, Av. General Paz 1499 (1650), San Martín, Buenos Aires, Argentina. Electronic address:

The use of Bisphenol S (BPS) was proposed as an alternative to Bisphenol A (BPA), a chemical employed in the production of polycarbonate plastics and epoxy resins. BPA is a xenoestrogen that affects normal physiology in several species. It was reported that BPS may also act as a xenoestrogen with harmful effects in the reproductive system. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.006DOI Listing
March 2019
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The role of Slit2 as a tumor suppressor in thyroid cancer.

Mol Cell Endocrinol 2019 Mar 12;483:87-96. Epub 2019 Jan 12.

Department of Internal Medicine, Asan Medical Center, University of Ulsan College of Medicine, 88, Olympic-ro 43-gil, Songpa-gu, Seoul, 05505, South Korea. Electronic address:

Slits, representative axon guidance molecules, and their Roundabout (Robo) transmembrane receptors play roles in the progression of many cancers. We investigated the effects of Slit2 on the proliferation, migration, and invasion of thyroid cancer cells, and on the prognosis of papillary thyroid cancer (PTC). Slit2 overexpression inhibited the proliferation, migration and invasion of thyroid cancer cells by inhibiting transcriptional activity of beta-catenin and regulating Rho GTPase activity. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.010DOI Listing
March 2019
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Single chain peptide agonists of relaxin receptors.

Mol Cell Endocrinol 2019 Jan 11. Epub 2019 Jan 11.

Florey Institute for Neuroscience & Mental Health, VIC, Australia; School of Chemistry and Bio21, University of Melbourne, University of Melbourne, VIC, Australia. Electronic address:

There are seven human relaxin family peptides that have two chains (A and B) and three disulfide bonds. The target receptors for four of these peptides are known as relaxin family peptide receptors, RXFP1-RXFP4. Detailed structure-activity relationship (SAR) studies of relaxin family peptides have been reported over the years and have led to the design of new analogs with agonistic and antagonistic properties. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.008DOI Listing
January 2019

Mannose receptor C type 2 mediates 1,25(OH)D/vitamin D receptor-regulated collagen metabolism through collagen type 5, alpha 2 chain and matrix metalloproteinase 13 in murine MC3T3-E1 cells.

Mol Cell Endocrinol 2019 Mar 11;483:74-86. Epub 2019 Jan 11.

Department of Pediatric Orthopedic, Shengjing Hospital of China Medical University, Shenyang, Liaoning, 110004, China; Key Laboratory of Health Ministry for Congenital Malformation, Shengjing Hospital of China Medical University, Benxi, Liaoning, 117004, China. Electronic address:

Vitamin D plays an important role in maintaining skeletal development and bone homeostasis. Although vitamin D has been extensively researched, the direct effect of 1,25(OH)D on osteoblasts is unclear. To explore the 1,25(OH)D action on murine osteoblasts, we performed tandem mass tag experiments on MC3T3-E1 cells treated with and without 1,25(OH)D. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.007DOI Listing

Relaxin gene therapy: A promising new treatment option for various diseases with aberrant fibrosis or irregular angiogenesis.

Mol Cell Endocrinol 2019 Jan 11. Epub 2019 Jan 11.

Department of Bioengineering, College of Engineering, Hanyang University, 222 Wangsimni-ro, Seongdong-gu, 133-791, Seoul, Republic of Korea; Institute of Nano Science and Technology (INST), Hanyang University, Republic of Korea. Electronic address:

Relaxin (RLX) is an insulin-like polypeptide hormone that was initially introduced for its pregnancy-related function. Subsequent studies revealed that RLX possesses anti-fibrotic functions in tumors and nonreproductive tissues, such as skin, lungs, and others. This aspect of the RLX has been explored for the treatment of various illnesses, such as cardiac fibrosis, liver fibrosis, and solid tumors. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.009DOI Listing
January 2019
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PTHrP treatment of colon cancer cells promotes tumor associated-angiogenesis by the effect of VEGF.

Mol Cell Endocrinol 2019 Mar 11;483:50-63. Epub 2019 Jan 11.

Dept. Biología Bioquímica y Farmacia-INBIOSUR, Universidad Nacional del Sur, Bahía Blanca, Argentina.

We showed that Parathyroid Hormone-related Peptide (PTHrP) induces proliferation, migration, survival and chemoresistance via MAPKs and PI3K/AKT pathways in colorectal cancer (CRC) cells. The objective of this study was to investigate if PTHrP is also involved in tumor angiogenesis. PTHrP increased VEGF expression and the number of structures with characteristics of neoformed vessels in xenografts tumor. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.005DOI Listing

Commercial immunoassays for human relaxin-2.

Authors:
Dennis R Stewart

Mol Cell Endocrinol 2019 Jan 8. Epub 2019 Jan 8.

Molecular Medicine Research Institute, 428 Oakmead Pkwy, Sunnyvale, CA, 94085, USA. Electronic address:

Several different immunoassays have been used in the commercial pharmaceutical development of serelaxin. These assays have been well validated for submission of GLP preclinical and clinical studies to the FDA and EU regulatory bodies. The requirements for these assays exceed that of most research assays commonly developed in academic research but have been and are currently available to academic researchers. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.004DOI Listing
January 2019

Relaxin and the 'Milky Way': The lactocrine hypothesis and maternal programming of development.

Mol Cell Endocrinol 2019 Jan 8. Epub 2019 Jan 8.

Department of Anatomy, Physiology and Pharmacology, Cellular and Molecular Biosciences Program, College of Veterinary Medicine, Auburn University, Auburn, AL, 36849-5517, USA.

Maternal effects on early postnatal development in mammals are mediated, in part, by milk-borne bioactive factors transmitted from mother to nursing offspring. The term 'lactocrine' was coined to describe this mode of signaling. Relaxin (RLX), one of a family of neohormones found in mammals, is detectable in milk from multiple species. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.003DOI Listing
January 2019
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INSL3 in the muscolo-skeletal system.

Mol Cell Endocrinol 2019 Jan 6. Epub 2019 Jan 6.

Unit of Endocrinology, Department of Clinical and Experimental Sciences, University of Brescia, Viale Europa 11, 25123, Brescia, Italy. Electronic address:

Bone and skeletal muscle are currently considered a unified functional unit, showing complementary regulation at mechanical, biochemical, paracrine and metabolic levels. This functional unit undergoes a central hormonal regulation which is mainly ascribed to sex steroids and, in particular, androgens. However, recent evidence suggest that another testicular hormone lines the classical anabolic effect of testosterone on bone and muscle, the insulin-like peptide 3 (INSL3) acting on its specific receptor RXFP2. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03037207183038
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http://dx.doi.org/10.1016/j.mce.2018.12.021DOI Listing
January 2019
2 Reads

Cardioprotective actions of relaxin.

Mol Cell Endocrinol 2019 Jan 6. Epub 2019 Jan 6.

Department of Medicine, Heart and Vascular Institute, University of Pittsburgh, Pittsburgh, PA, 15261, USA; McGowan Institute for Regenerative Medicine, University of Pittsburgh, Pittsburgh, PA, 15261, USA. Electronic address:

Relaxin is a hormone of pregnancy first discovered for its ability to induce ligament relaxation in nonpregnant guinea pig and is important for softening of the birth canal during parturition, decidualization, implantation, nipple development and increased maternal renal perfusion, glomerular filtration, and cardiac output. Subsequently, relaxin has been shown to exert multiple beneficial cardiovascular effects during pathological events such as hypertension, atrial fibrillation, heart failure and myocardial infarction, including suppression of arrhythmia and inflammation, and reversal of fibrosis. Despite extensive studies, the mechanisms underlying relaxin's effects are not well understood. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03037207183037
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http://dx.doi.org/10.1016/j.mce.2018.12.016DOI Listing
January 2019
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The Gata2 repression during 3T3-L1 preadipocyte differentiation is dependent on a rapid decrease in histone acetylation in response to glucocorticoid receptor activation.

Mol Cell Endocrinol 2019 Mar 4;483:39-49. Epub 2019 Jan 4.

Department of Pharmacy, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki, Japan. Electronic address:

The transcription factor GATA2 is an anti-adipogenic factor whose expression is downregulated during adipocyte differentiation. The present study attempted to clarify the molecular mechanism underlying the GATA2 repression and found that the repression is dependent on the activation of the glucocorticoid receptor (GR) during 3T3-L1 preadipocyte differentiation. Although several recognition sequences for GR were found in both the proximal and distal regions of the Gata2 locus, the promoter activity was not affected by the GR activation in the reporter assays, and the CRISPR-Cas9-mediated deletion of the two distal regions of the Gata2 locus was not involved in the GR-mediated Gata2 repression. Read More

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http://dx.doi.org/10.1016/j.mce.2019.01.002DOI Listing

Bisphenol A induces human uterine leiomyoma cell proliferation through membrane-associated ERα36 via nongenomic signaling pathways.

Mol Cell Endocrinol 2019 Mar 4;484:59-68. Epub 2019 Jan 4.

Molecular Pathogenesis Group, National Toxicology Program Laboratory (NTPL), Division of the NTP (DNTP), Research Triangle Park, NC, 27709, USA. Electronic address:

The role of ERα36 in regulating BPA's effects and its potential as a risk factor for human uterine fibroids were evaluated. BPA at low concentrations (10 μM - 10 μM) increased proliferation by facilitating progression of hormonally regulated, immortalized human uterine leiomyoma (ht-UtLM; fibroid) cells from G-G into S phase of the cell cycle; whereas, higher concentrations (100 μM-200 μM) decreased growth. BPA upregulated ERα36 gene and protein expression, and induced increased SOS1 and Grb2 protein expression, both of which are mediators of the MAPK/ERK1/2 pathway. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03037207193000
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http://dx.doi.org/10.1016/j.mce.2019.01.001DOI Listing
March 2019
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Somatostatin analogs regulate tumor corticotrophs growth by reducing ERK1/2 activity.

Mol Cell Endocrinol 2019 Mar 3;483:31-38. Epub 2019 Jan 3.

Fondazione IRCCS Ca' Granda Ospedale Maggiore Policlinico, Endocrine Unit, Department of Clinical Sciences and Community Health, University of Milan, Milan, Italy.

Pasireotide has been associated with tumor shrinkage in patients with Cushing's disease subjected to long term treatment. However, to date the implicated molecular mechanisms are poorly elucidated. Here, we tested pasireotide-mediated cytostatic and cytotoxic effects in ACTH-secreting primary tumor cultures and murine corticotroph tumor cell line, AtT-20 cells. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.022DOI Listing

The subcellular dynamics of GPCR signaling.

Mol Cell Endocrinol 2019 Mar 2;483:24-30. Epub 2019 Jan 2.

Institute of Metabolism and Systems Research, University of Birmingham, Birmingham, UK; Centre of Membrane Proteins and Receptors (COMPARE), Universities of Birmingham and Nottingham, UK.

G protein-coupled receptors (GPCRs) are the largest family of membrane receptors and mediate the effects of a multitude of extracellular cues, such as hormones, neurotransmitters, odorants and light. Because of their involvement in numerous physiological and pathological processes and their accessibility, they are extensively exploited as pharmacological targets. Biochemical and structural biology investigations have clarified the molecular basis of GPCR signaling to a high level of detail. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.020DOI Listing

Understanding relaxin signalling at the cellular level.

Mol Cell Endocrinol 2018 Dec 25. Epub 2018 Dec 25.

Florey Institute of Neuroscience and Mental Health, University of Melbourne, Parkville, Victoria, 3010, Australia. Electronic address:

The peptide hormone relaxin mediates many biological actions including anti-fibrotic, vasodilatory, angiogenic, anti-inflammatory, anti-apoptotic, and organ protective effects across a range of tissues. At the cellular level, relaxin binds to the G protein-coupled receptor relaxin family peptide receptor 1 (RXFP1) to activate a variety of downstream signal transduction pathways. This signalling cascade is complex and also varies in diverse cellular backgrounds. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.017DOI Listing
December 2018
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Targeting the relaxin/insulin-like family peptide receptor 1 and 2 with small molecule compounds.

Mol Cell Endocrinol 2018 Dec 24. Epub 2018 Dec 24.

Department of Human and Molecular Genetics, Herbert Wertheim College of Medicine, Florida International University, Miami, FL, 33199, USA. Electronic address:

The peptide hormone relaxin has beneficial roles in several organs through its action on its cognate G protein-coupled receptor, RXFP1. Relaxin administration is limited to intravenous, subcutaneous, intramuscular, or spinal injection. Another drawback of peptide-based therapy is the short half-life, which requires continuous delivery of the drug to achieve efficient concentration in target organs. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.013DOI Listing
December 2018

The influence of oxytocin on eating behaviours and stress in women with bulimia nervosa and binge eating disorder.

Mol Cell Endocrinol 2018 Dec 21. Epub 2018 Dec 21.

Institute of Psychiatry, Psychology and Neuroscience (IoPPN) - King's College London (KCL), London, United Kingdom.

The current study aimed to test the influence of oxytocin on palatable food intake, 24-h caloric consumption, and stress in women with bulimia nervosa and binge eating disorder. We recruited 25 women with DSM-5 bulimia nervosa or binge eating disorder, and 27 weight-matched comparison women without history of an eating disorder. We employed a double-blind, placebo-controlled crossover design in which each participant attended the lab for two experimental sessions, receiving a divided dose of 64IU intranasal oxytocin in one session and equivalent volume of placebo nasal spray in the opposite session. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.014DOI Listing
December 2018
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Testosterone augments FSH signaling by upregulating the expression and activity of FSH-Receptor in Pubertal Primate Sertoli cells.

Mol Cell Endocrinol 2019 Feb 21;482:70-80. Epub 2018 Dec 21.

Cellular Endocrinology Laboratory, National Institute of Immunology, New Delhi, 110067, India; Primate Research Center, National Institute of Immunology, New Delhi, India; National Institute of Animal Biotechnology, Hyderabad, Telangana, India. Electronic address:

The synergistic actions of Testosterone (T) and FSH via testicular Sertoli cells (Sc) regulate male fertility. We have previously reported that the actions of these hormones (T and FSH) in infant monkey testes are restricted only to the expansion of Sc and spermatogonial cells. The robust differentiation of male Germ cells (Gc) occurs after pubertal maturation of testis. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.012DOI Listing
February 2019
4.405 Impact Factor

Dual inhibition of ERK1/2 and AKT pathways is required to suppress the growth and survival of endometriotic cells and lesions.

Mol Cell Endocrinol 2019 Mar 20;484:78-92. Epub 2018 Dec 20.

Reproductive Endocrinology and Cell Signaling Laboratory, Department of Integrative Biosciences, College of Veterinary Medicine and Biomedical Sciences, Texas A&M University, TX, 77843, College Station, USA.

Endometriosis is an estrogen-dependent and progesterone-resistant gynecological inflammatory disease of reproductive-age women. Current hormonal therapies targeting estrogen can be prescribed only for a short time. It indicates a need for non-hormonal therapy. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.011DOI Listing
March 2019
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4.405 Impact Factor

The role of TCPTP on leptin effects on astrocyte morphology.

Mol Cell Endocrinol 2019 Feb 17;482:62-69. Epub 2018 Dec 17.

Department of Physiology, Ribeirao Preto Medical School, University of Sao Paulo, Sao Paulo, Brazil.

Leptin and LPS has been implicated in the development of hypothalamic astrogliosis in rodents. Astrocytes, which are interconnected by gap junction proteins, have emerged as important players in the control of energy homeostasis exerted by the hypothalamus. To investigate the hypothesis of action of T-cell protein tyrosine phosphatase (TCPTP) on the astrocyte morphology, astrocytes from the hypothalamus of one-day-old rats were stimulated with leptin and LPS (used as a positive control). Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.010DOI Listing
February 2019
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Stress hormones and eating disorders.

Mol Cell Endocrinol 2018 Dec 14. Epub 2018 Dec 14.

Department of Psychiatry, University of Naples SUN, Naples, Italy.

Aims: The aim of this paper is to emphasize the role of stress processes in the aetiology of eating disorders.

Methods: We have examined the literature for evidence that people with eating disorders might exhibit markers of stress and show signs of the "maltreated ecophenotype".

Results: Early adversity is more common among people with binge eating behaviours. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03037207183036
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http://dx.doi.org/10.1016/j.mce.2018.12.009DOI Listing
December 2018
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Amino acid residue L112 in the ACTH receptor plays a key role in ACTH or α-MSH selectivity.

Mol Cell Endocrinol 2019 Feb 13;482:11-17. Epub 2018 Dec 13.

Department of Surgery, State University of New York at Buffalo, United States.

The adrenocorticotropic hormone (ACTH) receptor, known as the melanocortin-2 receptor (MC2R), plays a key role in regulating adrenocortical function. MC2R is a subtype of the melanocortin receptor family and ACTH is only agonist for MC2R. Our previous result indicates that ACTH1-17 is the minimal peptide required for MC2R activation but DPhe7-ACTH1-17 has no activity at MC2R. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03037207183034
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http://dx.doi.org/10.1016/j.mce.2018.12.002DOI Listing
February 2019
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Administration of eicosapentaenoic and docosahexaenoic acids may improve the remodeling and browning in subcutaneous white adipose tissue and thermogenic markers in brown adipose tissue in mice.

Mol Cell Endocrinol 2019 Feb 12;482:18-27. Epub 2018 Dec 12.

Laboratory of Morphometry, Metabolism and Cardiovascular Diseases, Biomedical Center, Institute of Biology, State University of Rio de Janeiro, Rio de Janeiro, Brazil. Electronic address:

The role of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in browning and thermogenesis has not been fully elucidated. Thus, we meant to evaluate the effect of EPA and DHA, administered alone or combined, with the activation of browning markers in subcutaneous white adipose tissue (sWAT), and thermogenic markers in brown adipose tissue (BAT). C57BL/6 adult male mice received a control diet or a high-fructose diet (HFru) for eight weeks, but after the first three weeks, HFru was divided into new groups: HFru, HFru + EPA, HFru + DHA, and HFru-EPA + DHA. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.003DOI Listing
February 2019

Relaxin in liver transplantation: A personal perspective.

Mol Cell Endocrinol 2019 Feb 11;482:57-61. Epub 2018 Dec 11.

The Dumont-UCLA Transplant Center, Department of Surgery, Division of Liver and Pancreas Transplantation, David Geffen School of Medicine at University of California, Los Angeles, CA, 90095, USA. Electronic address:

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http://dx.doi.org/10.1016/j.mce.2018.12.008DOI Listing
February 2019

Neonatal exposure to a glyphosate-based herbicide alters the histofunctional differentiation of the ovaries and uterus in lambs.

Mol Cell Endocrinol 2019 Feb 11;482:45-56. Epub 2018 Dec 11.

Instituto de Salud y Ambiente del Litoral (ISAL), Facultad de Bioquímica y Ciencias Biológicas, Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Universidad Nacional del Litoral, Santa Fe, Argentina. Electronic address:

The aim of the present study was to compare the effect of oral and subcutaneous exposure to a glyphosate-based herbicide (GBH) on the female reproductive system, specifically in the ovaries and uterus of prepubertal lambs. To this end, ewe lambs were exposed to a s.c. Read More

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http://dx.doi.org/10.1016/j.mce.2018.12.007DOI Listing
February 2019
5 Reads