Search results for " antagonist"
showing 10 items of 1421 documents
mcr-1- like detection in commensal Escherichia coli and Salmonella spp. from food-producing animals at slaughter in Europe
2017
International audience; We evaluate here the presence of the mcr-1-like and mcr-2 genes in Escherichia coli and Salmonella spp. isolated from healthy food-producing animals at slaughter between 2002 and 2014 in Europe. Isolates were retrieved from cattle, pig and chicken from 11 European countries of production. The susceptibility to colistin and antibiotics used in human medicine was determined by agar dilution. Colistin-resistant isolates were PCR-screened for mcr genes. mcr-positive isolates were typed by Pulsed-Field Gel Electrophoresis (PFGE) and Multi-Locus Sequence Typing. Among the 10,206 E. coli and 1774 Salmonella spp. isolated from cattle, pigs and chickens, 148 E. coli and 92 Sa…
Glucagon-Like Peptide 1 and Taste Perception: From Molecular Mechanisms to Potential Clinical Implications
2021
Preclinical studies provided some important insights into the action of glucagon-like peptide 1 (GLP-1) in taste perception. This review examines the literature to uncover some molecular mechanisms and connections between GLP-1 and the gustatory coding. Local GLP-1 production in the taste bud cells, the expression of GLP-1 receptor on the adjacent nerves, a functional continuum in the perception of sweet chemicals from the gut to the tongue and an identification of GLP-1 induced signaling pathways in peripheral and central gustatory coding all strongly suggest that GLP-1 is involved in the taste perception, especially sweet. However, the impact of GLP-1 based therapies on gustatory coding i…
Antiproliferative and pro-apoptotic activity of melatonin analogues on melanoma and breast cancer cells
2017
// Giuliana Gatti 1, * , Valeria Lucini 2, * , Silvana Dugnani 2 , Angela Calastretti 1 , Gilberto Spadoni 3 , Annalida Bedini 3 , Silvia Rivara 4 , Marco Mor 4 , Gianfranco Canti 1 , Francesco Scaglione 2 and Annamaria Bevilacqua 1 1 Department of Medical Biotechnology and Translational Medicine, Universita degli Studi di Milano, Milan, Italy 2 Department of Oncology and Hemato-oncology, Universita degli Studi di Milano, Milan, Italy 3 Department of Biomolecular Sciences, Universita degli Studi di Urbino “Carlo Bo”, Urbino, Italy 4 Department of Food and Drug, Universita degli Studi di Parma, Parma, Italy * Authors contributed equally to this work Correspondence to: Annamaria Bevilacqua, e…
Blocking oestradiol synthesis pathways with potent and selective coumarin derivatives
2018
A comprehensive set of 3-phenylcoumarin analogues with polar substituents was synthesised for blocking oestradiol synthesis by 17-b-hydroxysteroid dehydrogenase 1 (HSD1) in the latter part of the sulphatase pathway. Five analogues produced 62% HSD1 inhibition at 5 mM and, furthermore, three of them produced 68% inhibition at 1 mM. A docking-based structure-activity relationship analysis was done to determine the molecular basis of the inhibition and the cross-reactivity of the analogues was tested against oestrogen receptor, aromatase, cytochrome P450 1A2, and monoamine oxidases. Most of the analogues are only modestly active with 17-b-hydroxysteroid dehydrogenase 2 – a requirement for lowe…
Bisphenolic compounds alter gene expression in MCF-7 cells through interaction with estrogen receptor α
2020
Plasticizers released from microplastic are increasingly viewed with concern. While adverse health effects induced by bisphenol A and its analogues on marine animals are well documented in the literature, the endocrine potential of bisphenolic compounds on human health remains elusive. We applied next generation sequencing (NGS) with the estrogen receptor α (ERα) positive human breast cancer cell line MCF-7 treated with 17-β-estradiol (E2), bisphenol A (BPA), bisphenol B (BPB), bisphenol Z (BPZ) and tetramethyl bisphenol A (4MeBPA). We used molecular docking, microscale thermophoresis, ERα activation assay, and cell cycle experiments on MCF-7 and ERα overexpressing HEK293 cells to verify th…
Activin and inhibin A in predicting outcome of pregnancies of unknown location after ART
2018
Abstract The aim was to investigate the predictive value of a single serum determination of activin A and inhibin A for classifying pregnancies of unknown location (PUL) after IVF cycles in both own fresh and donated oocytes. A case–control study conducted in a University-affiliated IVF center. Pregnancy outcomes after own fresh oocytes included 12 failing PUL, 12 ectopic pregnancies (EP) and a control group of 24 singleton intrauterine pregnancies (IUP). The same scheme was followed for the oocyte donation recipients. Inhibin A, activin A, β-hCG and Progesterone (P) were determined. In the own fresh oocytes IVF, the AUC for predicting EP vs. f failing PUL were: Activin A: 0.458 and Inhibin…
Evidence That Graves' Ophthalmopathy Immunoglobulins Do Not Directly Activate IGF-1 Receptors
2018
Background: Graves' ophthalmopathy (GO) pathogenesis involves thyrotropin (TSH) receptor (TSHR)-stimulating autoantibodies. Whether there are autoantibodies that directly stimulate insulin-like growth factor 1 receptors (IGF-1Rs), stimulating insulin-like growth factor receptor antibodies (IGFRAbs), remains controversial. This study attempted to determine whether there are stimulating IGFRAbs in patients with GO. Methods: Immunoglobulins (Igs) were purified from normal volunteers (NV-Igs) and patients with GO (GO-Igs). The effects of TSH, IGF-1, NV-Igs, and GO-Igs on pAKT and pERK1/2, members of pathways used by IGF-1R and TSHR, were compared in orbital fibroblasts from GO patients (GOFs) a…
microRNA Expression Profile in Single Hormone Receptor-Positive Breast Cancers is Mainly Dependent on HER2 Status—A Pilot Study
2020
Estrogen (ER) and progesterone (PgR) receptors and HER2 are crucial in the assessment of breast cancer specimens due to their prognostic and predictive significance. Single hormone receptor-positive breast cancers are less common and their clinical course is less favorable than ER(+)/PgR(+) tumors. Their molecular features, especially microRNA (miRNA) profiles, have not been investigated to date. Tumor specimens from 36 chemonaive breast cancer patients with known ER and PgR status (18 ER(+)/PgR(&minus
The Severity of Acute Stress Is Represented by Increased Synchronous Activity and Recruitment of Hypothalamic CRH Neurons
2016
The hypothalamo-pituitary-adrenocortical (HPA) axis regulates stress physiology and behavior. To achieve an optimally tuned adaptive response, it is critical that the magnitude of the stress response matches the severity of the threat. Corticotropin-releasing hormone (CRH) released from the paraventricular nucleus of the hypothalamus is a major regulator of the HPA axis. However, how CRH-producing neurons in an intact animal respond to different stressor intensities is currently not known. Using two-photon calcium imaging on intact larval zebrafish, we recorded the activity of CRH cells, while the larvae were exposed to stressors of varying intensity. By combining behavioral and physiologic…
Influence of glucagon-like peptide 2 on energy homeostasis
2016
Glucagon like peptide-2 (GLP-2) is a gastrointestinal hormone released from enteroendocrine L-type cells together with glucagon like peptide-1 in response to dietary nutrients. GLP-2 acts through a specific receptor, the GLP-2 receptor, mainly located in the gut and in the brain. Classically, GLP-2 is considered a trophic hormone involved in the maintenance of intestinal epithelial morphology and function. This role has been targeted for therapies promoting repair and adaptive growth of the intestinal mucosa. Recently, GLP-2 has been shown to exert beneficial effects on glucose metabolism specially in conditions related to increased uptake of energy, such as obesity. Several actions of GLP-…