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Membrane-tethered peptides derived from intracellular loops 2 and 3 of the urotensin II receptor act as allosteric biased ligands [article]

Hassan Nassour, Tuan Anh Hoang, Ryan D Martin, Juliana C.C. Dallagnol, Etienne Billard, Myriam Létourneau, Ettore Novellino, Alfonso Carotenuto, Bruce G. Allen, Jason C. Tanny, Alain Fournier, Terence E. Hébert (+1 others)
2020 bioRxiv   pre-print
Therefore, pepducins derived from the human urotensin II receptor might represent unique tools to generate signaling bias and study UT signaling networks.  ...  Pepducins and other lipidated peptides have been used as both mechanistic probes and potential therapeutics.  ...  Conflict of interest: The authors declare that they have no conflicts of interest.  ... 
doi:10.1101/2020.11.23.394270 fatcat:r6xrra2qwjfetpfvwn2abwo7rm

A Role for a Helical Connector between Two Receptor Binding Sites of a Long-chain Peptide Hormone

Michael Beyermann, Sven Rothemund, Nadja Heinrich, Klaus Fechner, Jens Furkert, Margitta Dathe, Rüdiger Winter, Eberhard Krause, Michael Bienert
2000 Journal of Biological Chemistry  
Connection of the two sites by an appropriate helical peptide led to a very potent analogue, which adopted, in contrast to CRF itself, a stable, monomer conformation in aqueous solution.  ...  conformation, and thus hampers insights into the mechanism of ligand-receptor interaction.  ...  Vogelreiter, and for critical reading of the manuscript, J. Dickson.  ... 
doi:10.1074/jbc.275.8.5702 pmid:10681555 fatcat:2nngv6roozcxbf7ncwsudi2ubi

Prediction of the Three-Dimensional Structure for the Rat Urotensin II Receptor, and Comparison of the Antagonist Binding Sites and Binding Selectivity between Human and Rat Receptors from Atomistic Simulations

Soo-Kyung Kim, Youyong Li, Changmoon Park, Ravinder Abrol, William A. Goddard
2010 ChemMedChem  
In addition, the computational resources used here were provided by grants from ARO-DURIP and ONR-DURIP. We thank Ms.  ...  Acknowledgements This work was funded partially by Boehringer-Ingelheim and by the National Institutes of Health (USA).  ...  Introduction Urotensin-II (U-II) is a C-terminal conserved disulfide-bridged cyclic peptide (ETPDCFWKYCA).  ... 
doi:10.1002/cmdc.201000175 pmid:20683923 pmcid:PMC3517062 fatcat:ot6hw3kwvvgnjltoqgjktreacu

Current understanding of the structure and function of family B GPCRs to design novel drugs

Vlasios Karageorgos, Maria Venihaki, Stelios Sakellaris, Michail Pardalos, George Kontakis, Minos-Timotheos Matsoukas, Achille Gravanis, Andreas Margioris, George Liapakis
The C-terminal region of peptides first binds to the Ndomain of receptors.  ...  Family B of G-protein-coupled receptors (GPCRs) and their ligands play a central role in a number of homeostatic mechanisms in the endocrine, gastrointestinal, skeletal, immune, cardiovascular and central  ...  In contrast, in aqueous solutions, these peptides are generally disordered.  ... 
doi:10.1007/s42000-018-0009-5 pmid:29858864 fatcat:upmmg5zxezc2nmvaudsvvceuj4

Cardiovascular Activity [chapter]

Hans Gerhard Vogel
2007 Drug Discovery and Evaluation  
MODIFICATIONS OF THE METHOD Ito et al. (1990) measured glucose utilization in the mouse brain by the simultaneous use of [ 14 C]2-deoxyglucose and [ 3 H]3-O-methylglucose.  ...  Hawkins et al. (1993) developed a method for evaluating tumor glycolytic rates in vivo with nude mice injected with 2-[ 18 F]fluoro-2-deoxy-D-glucose and a dedicated animal positron emission tomography  ...  Brkovic et al. (2003) performed functional and binding characterizations of urotensin-II-related peptides in human and rat urotensin II receptor assays.  ... 
doi:10.1007/978-3-540-70995-4_2 fatcat:z75tsqr3nzhpric5ftzldlabra

Fluorescent approaches for understanding interactions of ligands with G protein coupled receptors

Rajashri Sridharan, Jeffrey Zuber, Sara M. Connelly, Elizabeth Mathew, Mark E. Dumont
2014 Biochimica et Biophysica Acta - Biomembranes  
In addition, we discuss the use of fluorescence spectroscopy for detecting and characterizing conformational changes in receptors induced by the binding of ligands.  ...  The use of fluorescence spectroscopy can provide important information about the process of ligand binding and ligand dependent conformational changes in receptors, especially kinetic aspects of these  ...  Fred Naider of the College of Staten Island of the City University of New York for many years of invaluable discussions on the use of fluorescent peptide ligands for GPCRs and for synthesizing many of  ... 
doi:10.1016/j.bbamem.2013.09.005 pmid:24055822 pmcid:PMC3926105 fatcat:ihdcthsmmzgarh5jc7j3w5scsa

B-Type Natriuretic Peptide Signal Peptide Circulates in Human Blood: Evaluation as a Potential Biomarker of Cardiac Ischemia

M. Siriwardena, T. Kleffmann, P. Ruygrok, V. A. Cameron, T. G. Yandle, M. G. Nicholls, A. M. Richards, C. J. Pemberton
2010 Circulation  
Methods and Results-Using specific immunoassay and tandem mass spectrometry, we show that a fragment derived from the signal peptide of B-type natriuretic peptide (BNPsp) not only is detectable in cytosolic  ...  Conclusion-Our results demonstrate for the first time that BNPsp exists as a distinct entity in the human circulation and could serve as a new class of circulating biomarker with the potential to accelerate  ...  One microlitre of peptide solution was premixed with 2 µl of matrix (10 mg/ml {alpha}cyano-4-hydroxycinnamic acid dissolved in 65% [v/v] aqueous acetonitrile containing 0.1% TFA and 10 mM ammonium dihydrogen  ... 
doi:10.1161/circulationaha.109.909937 pmid:20606123 fatcat:max7g2woujetnl2nfaw6yilxoq

13th IIS(UK group) symposium

Stephen Caddick, Sharon Stone-Elander, Simon G. Patching, Richard B. Herbert, Peter J. F. Henderson, Adrian R. Brough, David A. Middleton, Gregory S. Coumbarides, Jason Eames, Stephanos Ghilagaber, Michael J. Suggate, Neluka Weerasooriya (+74 others)
2004 Journal of labelled compounds & radiopharmaceuticals  
The aim of our work is to understand the role of these vasoactive peptides and their receptor sub-types in the human cardiovascular system and to quantify changes associated with disease.  ...  We have discovered in the human vasculature a number of these novel peptide receptor systems, originally predicted from the human genome, that may become targets for new therapies.  ...  apelin, ghrelin and urotensin II facilitating the rapid translation of information from the human genome into function.  ... 
doi:10.1002/jlcr.819 fatcat:teb2p43jjraqhbkbqilbpzl67i

Developing Actively Targeted Nanoparticles to Fight Cancer: Focus on Italian Research

Monica Argenziano, Silvia Arpicco, Paola Brusa, Roberta Cavalli, Daniela Chirio, Franco Dosio, Marina Gallarate, Elena Peira, Barbara Stella, Elena Ugazio
2021 Pharmaceutics  
Active targeting is a valuable and promising approach with which to enhance the therapeutic efficacy of nanodelivery systems, and the development of tumor-targeted nanoparticles has therefore attracted  ...  In addition, solid lipid nanoparticles, squalene nanoparticles and nanobubbles have also been successfully proposed.  ...  solutes in an aqueous solution (Figure 1 ).  ... 
doi:10.3390/pharmaceutics13101538 pmid:34683830 fatcat:aupaegywrjhgte52rxtrtkiixy

The Combinatorial Nature of Osmosensing in Fishes

Dietmar Kültz
2012 Physiology  
Input from numerous osmosensors is integrated to encode magnitude, direction, and ionic basis of osmolality change. This combinatorial nature of osmosensing is discussed with emphasis on fishes.  ...  Such osmosensing comprises a complex physiological process involving many elements at organismal and cellular levels of organization.  ...  Urotensin II and its receptor in the killifish gill: regulators of NaCl extrusion. J Exp Biol 214: 3985-3991, 2011. 47. Evans TG, Somero GN.  ... 
doi:10.1152/physiol.00014.2012 pmid:22875456 fatcat:josd4rvlpbgixozesqz5uacvme

The Corticotropin-Releasing Factor Family: Physiology of the Stress Response

Jan M. Deussing, Alon Chen
2018 Physiological Reviews  
A: alignment of amino acid sequences of mature CRF-related peptides from vertebrates and of diuretic hormone (DH) from insects. The NH 2 -terminal activating domain is highlighted in light green.  ...  This review focuses on the physiology of CRF-related peptides and their cognate receptors with the aim of providing a comprehensive up-to-date overview of the field.  ...  Chen is the head of the Max Planck Society-Weizmann Institute of Science Laboratory for Experimental Neuropsychiatry and Behavioral Neurogenetics.  ... 
doi:10.1152/physrev.00042.2017 pmid:30109816 fatcat:7uvifc2l7baahbt2lb4udn2cvy

NMR spectroscopy: a useful tool for drugs development and monitoring biological reactions [article]

Antonio Limatola
, including frogs, rats, mice, pigs, monkeys, and humans. 6 In 2003, a paralogue of U-II, known as urotensin-related peptide (URP), was isolated in mammals. 7 The U-II and URP genes are mostly expressed  ...  , human Urotensin-II peptide; h-UTR, human Urotensin II receptor; IL, intracellular loop; LC, liquid chromatography; MD, molecular dynamic; Nal, Naphtylalanine; NMR, nuclear magnetic resonance; NOE, nuclear  ... 
doi:10.6093/unina/fedoa/10433 fatcat:fxrbwags2zblbbv3clekkj7q6a


1985 FEBS Letters  
Sci. 22, 129 NMR studies of conformational states and dynamics of DNA Keams D R (1984) CRC Crit. Rev.  ...  in plants Electrochemical properties of flavins in aqueous solutions Ksenzek 0 S & Petrova S A (1983) Bioelectrochem.  ...  Immunol. 2.493 Freeze The toxicology of molecular oxygen  ... 
doi:10.1016/0014-5793(85)81322-3 fatcat:3jtzvopzhrhlblb5xrbekaxafi

Interaction of peptides and small molecules with biological targets

Diego Brancaccio
In particular, I investigated the conformational behaviour of peptide analogues of Urotensin, Melanocortin and Somatostatin in water solution and membrane mimetic environment (SDS and DPC micelles).  ...  During my PhD course, I focused my attention on the conformational analysis of peptides that interact with GPCR and ligand-receptor interactions from NMR spectroscopy with possible application to cytotoxic  ...  Recently, an analogue of U-II, called urotensin-related peptide (URP), has been identified in mammals.  ... 
doi:10.6092/unina/fedoa/8816 fatcat:i6a7c7pzandtzjqvae6vhj75xu

Receptor Databases and Computational Websites for Ligand Binding [chapter]

Brinda K. Rana, Philip E. Bourne, Paul A. Insel
2012 Msphere  
This method involves the docking of molecules in multiple conformations into receptor-binding sites to find potential ligands.  ...  Further, with the recent influx of human genetic variation data in pharmacogenomic studies, as well as data from mutational analyses, knowledge of amino acid residues important in ligand-receptor binding  ...  Acknowledgments We thank Jenny Eichhorst for excellent technical assistance, Brunhilde Oczko for assistance in analyzing of the microscopic data, Tim Plant for reading the manuscript and providing helpful  ... 
doi:10.1007/978-1-61779-909-9_1 pmid:22674158 fatcat:qf26fmaftndn3dlb5vpfflsabi
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