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Related publications (32)

Cyclic peptide therapeutics: past, present and future

Christian Heinis, Alessandro Zorzi, Kaycie Marie Butler

Cyclic peptides combine several favorable properties such as good binding affinity, target selectivity and low toxicity that make them an attractive modality for the development of therapeutics. Over 40 cyclic peptide drugs are currently in clinical use an ...

2017

Systems Phytohormone Responses to Mitochondrial Proteotoxic Stress

Johan Auwerx, Xu Wang

Mitochondrial function is controlled by two separate genomes. This feature makes mitochondria prone to proteotoxic stress when a stoichiometric imbalance occurs in the protein complexes that perform oxidative phosphorylation, which consist of both nucleara ...

Cell Press2017

Development of an albumin-binding ligand for prolonging the plasma half-life of peptide therapeutics

Alessandro Zorzi

Peptides represent a promising format for the development of therapeutics since they combine the advantages of proteins and small molecules. Several techniques based on rational design or in vitro evolution can be used to develop peptides as therapeutics. ...

EPFL2017

Potent Prearranged Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor

Rosario Scopelliti, Johannes Broichhagen

Drugs that allosterically modulate G protein-coupled receptor (GPCR) activity display higher specificity and may improve disease treatment. However, the rational design of compounds that target the allosteric site is difficult, as conformations required fo ...

Wiley-V C H Verlag Gmbh2017

Extensive Regulation of Diurnal Transcription and Metabolism by Glucocorticoids

Cédric Gobet, Meltem Weger, Frédéric Bruno Martin Gachon, Benjamin Dieter Weger

Altered daily patterns of hormone action are suspected to contribute to metabolic disease. It is poorly understood how the adrenal glucocorticoid hormones contribute to the coordination of daily global patterns of transcription and metabolism. Here, we exa ...

Public Library Science2016

A Preclinical Model for ERα-Positive Breast Cancer Points to the Epithelial Microenvironment as Determinant of Luminal Phenotype and Hormone Response

Cathrin Brisken, Georgios Sflomos, Valentina Scabia, Ayyakkannu Ayyanan, Rachel Marcone, Laura Battista, Maryse Fiche, Valérian Charles Robert Dormoy

Seventy-five percent of breast cancers are estrogen receptor α positive (ER(+)). Research on these tumors is hampered by lack of adequate in vivo models; cell line xenografts require non-physiological hormone supplements, and patient-derived xenografts (PD ...

Elsevier2016

Allosteric Optical Control of a Class B G-Protein-Coupled Receptor

Johannes Broichhagen

Allosteric regulation promises to open up new therapeutic avenues by increasing drug specificity at G-protein-coupled receptors (GPCRs). However, drug discovery efforts are at present hampered by an inability to precisely control the allosteric site. Herei ...

Wiley-VCH Verlag GmbH2016

Murine ovarian follicle culture in PEG-hydrogel: Effects of mechanical properties and the hormones FSH and LH on development

Jeffrey Alan Hubbell, Seung Tae Lee, Jong Eun Ihm

The development of an in vitro culture system, comparable to the in vivo environment in terms of effects on oocyte growth and development, could provide a valuable experimental tool for studying the mechanisms governing oocyte development as well as practi ...

Polymer Soc Korea2015

Anti-Obesity and Anti-Hyperglycemic Effects of Cinnamaldehyde via altered Ghrelin Secretion and Functional impact on Food Intake and Gastric Emptying

Henry Markram, Julie Meystre, Maurizio Ferdinando Pezzoli, Johannes Le Coutre, Susana Camacho Romero

Cinnamon extract is associated to different health benefits but the active ingredients or pathways are unknown. Cinnamaldehyde (CIN) imparts the characteristic flavor to cinnamon and is known to be the main agonist of transient receptor potential-ankyrin r ...

Nature Publishing Group2015

Progesterone and Wnt4 control mammary stem cells via myoepithelial crosstalk

Cathrin Brisken, Jacques Rougemont, Ayyakkannu Ayyanan, Marian Caikovski, Duje Buric, Renuga Devi Rajaram

Ovarian hormones increase breast cancer risk by poorly understood mechanisms. We assess the role of progesterone on global stem cell function by serially transplanting mouse mammary epithelia. Progesterone receptor (PR) deletion severely reduces the regene ...

Wiley-Blackwell2015

Influence of MCHR2 and MCHR2-AS1 Genetic Polymorphisms on Body Mass Index in Psychiatric Patients and In Population-Based Subjects with Present or Past Atypical Depression

Pierre Magistretti, Aurélie Delacrétaz

Obesity development during psychotropic treatments represents a major health issue in psychiatry. Melanin-concentrating hormone receptor 2 (MCHR2) is a central receptor involved in energy homeostasis. MCHR2 shares its promoter region with MCHR2-AS1, a long ...

Public Library of Science2015

NR5A2 Regulates Lhb and Fshb Transcription in Gonadotrope-Like Cells In Vitro, but Is Dispensable for Gonadotropin Synthesis and Fertility In Vivo

Johan Auwerx, Kristina Schoonjans, Yiping Wang, Xin Zhou, Vikas Kumar

Successful mammalian reproduction depends on proper synthesis of the pituitary-derived glycoprotein hormones, luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Several transcription factors cooperate to activate cell-specific and hormone-reg ...

Public Library of Science2013

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