A5082434067- Neuropeptides and Animal Physiology
- Receptor Mechanisms and Signaling
- Peptidase Inhibition and Analysis
- Lipid Membrane Structure and Behavior
- Pharmacological Receptor Mechanisms and Effects
- Monoclonal and Polyclonal Antibodies Research
- Phytase and its Applications
- Signaling Pathways in Disease
- Hormonal Regulation and Hypertension
- Chemical Synthesis and Analysis
- Neuroendocrine regulation and behavior
- Neuroscience and Neuropharmacology Research
- Diabetes Treatment and Management
- Glycosylation and Glycoproteins Research
- Ion channel regulation and function
- Neuroendocrine Tumor Research Advances
- Protein Kinase Regulation and GTPase Signaling
- Pancreatic function and diabetes
- Migraine and Headache Studies
- Hypothalamic control of reproductive hormones
- Nicotinic Acetylcholine Receptors Study
- Trace Elements in Health
- Nitric Oxide and Endothelin Effects
- PI3K/AKT/mTOR signaling in cancer
- Pituitary Gland Disorders and Treatments
Aston University
2016-2025
Utrecht University
2023
Pharmabridge (United States)
2023
Makerere University
2023
University of Birmingham
2001-2021
University of Nottingham
2020-2021
Laboratoire de Biologie Physico-Chimique des Protéines Membranaires
2020
University of Auckland
2008
Douglas Mental Health University Institute
2002-2008
University of Warwick
2008
Calcitonin (CT) receptors dimerize with receptor activity-modifying proteins (RAMPs) to create high-affinity amylin (AMY) receptors, but there is no reliable means of pharmacologically distinguishing these receptors. We used agonists and antagonists define their pharmacology, expressing the CT<sub>(a)</sub> alone or RAMPs in COS-7 cells measuring cAMP accumulation. Intermedin short, otherwise known as adrenomedullin 2, mirrored action αCGRP, being a weak agonist at CT<sub>(a)</sub>,...
G-protein coupled receptors (GPCRs) constitute the largest class of membrane proteins and are a major drug target. A serious obstacle to studying GPCR structure/function characteristics is requirement extract from their native environment in plasma membrane, with inherent instability GPCRs detergents required for solubilization. In present study, we report first solubilization purification functional [human adenosine A2A receptor (A2AR)], total absence detergent at any stage, by exploiting...
Abstract Muscarinic acetylcholine receptors were purified from rat forebrain and labeled with [3H]N-(2-chloroethyl)N-(2',3'-[3H2]propyl)-2-aminoethylbenzilate. Cleavage of the muscarinic a lysine-specific protease yielded labeled, glycosylated peptides about 130 200 residues in length, which came different receptor sequences. The probable cleavage sites are second intracellular loop extracellular or third loop. N-terminal disulfide-bonded to another part structure, supporting presence link...
1. The ability of myo-inositol polyphosphates to inhibit iron-catalysed hydroxyl radical formation was studied in a hypoxanthine/xanthine oxidase system [Graf, Empson and Eaton (1987) J. Biol. Chem. 262, 11647-11650]. Fe3+ present the assay reagents supported some formation, standard assay, with 5 microM added, used investigate specificity compounds which could generation. 2. InsP6 (phytic acid) able this completely. In respect it similar effects high affinity chelator Desferral, dissimilar...
Adrenomedullin (AM) has two known receptors formed by the calcitonin receptor-like receptor (CL) and activity-modifying protein (RAMP) 2 or 3: we report effects of antagonist fragments human AM CGRP (AM22-52 CGRP8-37) in inhibiting at (h), rat (r) mixed species CL/RAMP2 CL/RAMP3 transiently expressed Cos 7 cells endogenously as rCL/rRAMP2 complexes Rat L6 cells. AM22-52 (10 microM) antagonised all (apparent pA2 values: 7.34+/-0.14 (hCL/hRAMP2), 7.28+/-0.06 (Rat 2), 7.00+/-0.05 (L6),...
The glucagon and glucagon-like peptide-1 (GLP-1) receptors play important, opposing roles in regulating blood glucose levels. Consequently, these have been identified as targets for novel diabetes treatments. However, drugs acting at the GLP-1 receptor, although having clinical efficacy, associated with severe adverse side-effects, targeting of receptor has yet to be successful. Here we use a combination yeast reporter assays mammalian systems provide more complete understanding signaling,...
1. Standard and high-performance anion-exchange-chromatographic techniques have been used to purify myo-[3H]inositol pentakisphosphates from various myo-[3H]inositol-prelabelled cells. Slime mould (Dictyostelium discoideum) contained 8 microM-myo-[3H]inositol 1,3,4,5,6-pentakisphosphate, 16 1,2,3,4,6-pentakisphosphate 36 microM-D-myo-[3H]inositol 1,2,4,5,6-pentakisphosphate [calculated intracellular concentrations; Stephens & Irvine (1990) Nature (London) 346, 580-583]; germinating mung-bean...
Although it is established that the receptor activity modifying proteins (RAMPs) can interact with a number of GPCRs, little known about consequences these interactions. Here interaction RAMPs glucagon-like peptide 1 (GLP-1 receptor), human vasoactive intestinal polypeptide/pituitary AC-activating 2 (VPAC(2)) and type corticotrophin releasing factor (CRF(1)) has been examined.GPCRs were co-transfected in HEK 293S CHO-K1 cells. Cell surface expression GPCRs was examined by ELISA. Where there...
Abstract G protein-coupled receptors are allosteric proteins that control transmission of external signals to regulate cellular response. Although agonist binding promotes canonical protein signalling transmitted through conformational changes, also interact with other proteins. These include receptors, and channels, regulatory receptor-modifying proteins, notably receptor activity-modifying (RAMPs). RAMPs have at least 11 partners, including many class B receptors. Prototypic is the...