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AMY1 receptors

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https://www.readbyqxmd.com/read/27139251/synthesis-and-amylin-receptor-activity-of-glycomimetics-of-pramlintide-using-click-chemistry
#1
Lauren R Yule, Rebekah L Bower, Harveen Kaur, Renata Kowalczyk, Debbie L Hay, Margaret A Brimble
Pramlintide (Symlin®), a synthetic analogue of the neuroendocrine hormone amylin, is devoid of the tendency to form cytotoxic amyloid fibrils and is currently used in patients with type I and type II diabetes mellitus as an adjunctive therapy with insulin or insulin analogues. As part of an on-going search for a pramlintide analogue with improved pharmacokinetic properties, we herein report the synthesis of mono- and di-glycosylated analogues of pramlintide and their activity at the AMY1(a) receptor. Introduction of N-glycosylated amino acids into the pramlintide sequence afforded the native N-linked glycomimetics whilst use of Cu(i)-catalysed azide-alkyne 1,3-dipolar cycloaddition (click) chemistry delivered 1,2,3-triazole linked glycomimetics...
June 21, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/27081662/reply-to-comment-on-a-second-trigeminal-cgrp-receptor-function-and-expression-of-the-amy1-receptor
#2
Christopher S Walker, Debbie L Hay
No abstract text is available yet for this article.
April 2016: Annals of Clinical and Translational Neurology
https://www.readbyqxmd.com/read/27081661/comment-on-a-second-trigeminal-cgrp-receptor-function-and-expression-of-the-amy1-receptor
#3
Kristian Agmund Haanes, Ka Yi Chan, Antoinette MaassenVanDenBrink
No abstract text is available yet for this article.
April 2016: Annals of Clinical and Translational Neurology
https://www.readbyqxmd.com/read/26125036/a-second-trigeminal-cgrp-receptor-function-and-expression-of-the-amy1-receptor
#4
Christopher S Walker, Sajedeh Eftekhari, Rebekah L Bower, Andrea Wilderman, Paul A Insel, Lars Edvinsson, Henry J Waldvogel, Muhammad A Jamaluddin, Andrew F Russo, Debbie L Hay
OBJECTIVE: The trigeminovascular system plays a central role in migraine, a condition in need of new treatments. The neuropeptide, calcitonin gene-related peptide (CGRP), is proposed as causative in migraine and is the subject of intensive drug discovery efforts. This study explores the expression and functionality of two CGRP receptor candidates in the sensory trigeminal system. METHODS: Receptor expression was determined using Taqman G protein-coupled receptor arrays and immunohistochemistry in trigeminal ganglia (TG) and the spinal trigeminal complex of the brainstem in rat and human...
June 2015: Annals of Clinical and Translational Neurology
https://www.readbyqxmd.com/read/25563409/insights-into-hominin-phenotypic-and-dietary-evolution-from-ancient-dna-sequence-data
#5
George H Perry, Logan Kistler, Mary A Kelaita, Aaron J Sams
Nuclear genome sequence data from Neandertals, Denisovans, and archaic anatomically modern humans can be used to complement our understanding of hominin evolutionary biology and ecology through i) direct inference of archaic hominin phenotypes, ii) indirect inference of those phenotypes by identifying the effects of previously-introgressed alleles still present among modern humans, or iii) determining the evolutionary timing of relevant hominin-specific genetic changes. Here we review and reanalyze published Neandertal and Denisovan genome sequence data to illustrate an example of the third approach...
February 2015: Journal of Human Evolution
https://www.readbyqxmd.com/read/24647952/antipsychotic-like-actions-of-the-satiety-peptide-amylin-in-ventral-striatal-regions-marked-by-overlapping-calcitonin-receptor-and-ramp-1-gene-expression
#6
Sarah K Baisley, Quentin Z Bremer, Vaishali P Bakshi, Brian A Baldo
Amylin is a calcitonin-related peptide co-secreted with insulin, which produces satiety through brainstem-localized receptors; however, its effects in forebrain are poorly understood. The nucleus accumbens shell (AcbSh) exhibits among the densest concentrations of high-affinity amylin binding; nevertheless, these receptors have not been explored beyond one study showing dopamine antagonist-like effects of intra-Acb amylin on feeding and associated behavior (Baldo and Kelley, 2001). Here, we investigated whether intra-Acb amylin signaling modulates prepulse inhibition (PPI), a measure of sensorimotor gating deficient in several illnesses including schizophrenia...
March 19, 2014: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/24169554/activity-of-pramlintide-rat-and-human-amylin-but-not-a%C3%AE-1-42-at-human-amylin-receptors
#7
Joseph J Gingell, Erica R Burns, Debbie L Hay
Amylin is a neuroendocrine hormone involved in glucose regulation. An amylin analog, pramlintide, is used to treat insulin-requiring diabetes. Its anorexigenic actions give it potential as an obesity treatment. There are 3 amylin receptors (AMY1, AMY2, AMY3), comprising the calcitonin receptor and receptor activity-modifying proteins 1, 2, and 3, respectively. The pharmacology of pramlintide at each subtype has not been determined whereas the unrelated peptide β-amyloid 1-42 (Aβ1-42) has recently been proposed to be a specific agonist of the AMY3 receptor...
January 2014: Endocrinology
https://www.readbyqxmd.com/read/18599553/receptor-activity-modifying-proteins-differentially-modulate-the-g-protein-coupling-efficiency-of-amylin-receptors
#8
Maria Morfis, Nanda Tilakaratne, Sebastian G B Furness, George Christopoulos, Tim D Werry, Arthur Christopoulos, Patrick M Sexton
Receptor activity-modifying proteins (RAMPs) 1, 2, and 3 are prototypic G protein-coupled receptor accessory proteins that can alter not only receptor trafficking but also receptor phenotype. Specific RAMP interaction with the calcitonin receptor (CTR) generates novel and distinct receptors for the peptide amylin; however, the role of RAMPs in receptor signaling is not understood. The current study demonstrates that RAMP interaction with the CTRa in COS-7 or HEK-293 cells leads to selective modulation of signaling pathways activated by the receptor complex...
November 2008: Endocrinology
https://www.readbyqxmd.com/read/18593822/identification-of-n-terminal-receptor-activity-modifying-protein-residues-important-for-calcitonin-gene-related-peptide-adrenomedullin-and-amylin-receptor-function
#9
Tao Qi, George Christopoulos, Richard J Bailey, Arthur Christopoulos, Patrick M Sexton, Debbie L Hay
Calcitonin-family receptors comprise calcitonin receptor-like receptor (CL) or calcitonin receptor and receptor activity-modifying protein (RAMP) pairings. Calcitonin gene-related peptide (CGRP) receptors are CL/RAMP1, whereas adrenomedullin (AM) receptors are CL/RAMP2 (AM1 receptor) or CL/RAMP3 (AM2 receptor). Amylin (Amy) receptors are RAMP hetero-oligomers with the calcitonin receptor (AMY1, AMY2, and AMY3, respectively). How RAMPs change G protein-coupled receptor pharmacology is not fully understood. We exploited sequence differences between RAMP1 and RAMP3 to identify individual residues capable of altering receptor pharmacology...
October 2008: Molecular Pharmacology
https://www.readbyqxmd.com/read/18434892/procalcitonin-has-bioactivity-at-calcitonin-receptor-family-complexes-potential-mediator-implications-in-sepsis
#10
Patrick M Sexton, George Christopoulos, Arthur Christopoulos, Eric S Nylen, Richard H Snider, Kenneth L Becker
CONTEXT: Sepsis is a major cause of death in the United States and accounts for approximately 50% of the fatalities in intensive care units. Serum procalcitonin (ProCT) levels are markedly elevated in sepsis and correlate positively with severity of the illness and mortality, however, little is known about the biological activity of ProCT. OBJECTIVE: To explore the biological activity of purified human ProCT at the calcitonin (CT) family of receptors. DESIGN: Human ProCT was purified from the TT medullary thyroid carcinoma cell line...
May 2008: Critical Care Medicine
https://www.readbyqxmd.com/read/8001974/syntenic-assignment-of-human-chromosome-1-homologous-loci-in-the-bovine
#11
COMPARATIVE STUDY
D S Threadgill, D W Threadgill, Y D Moll, J A Weiss, N Zhang, H W Davey, A G Wildeman, J E Womack
Three mouse chromosomes (MMU 1, 3, and 4) carry homologs of human chromosome 1 (HSA 1) genes. A similar situation is found in the bovine, where five bovine chromosomes (BTA 2, 3, 5, 16, and unassigned syntenic group U25) contain homologs of HSA 1 loci. To evaluate further the syntenic relationship of HSA 1 homologs in cattle, 10 loci have been physically mapped through segregation analysis in bovine-rodent hybrid somatic cells. These loci, chosen for their location on HSA 1, are antithrombin 3 (AT3), renin (REN), complement component receptor 2 (CR2), phosphofructokinase muscle type (PFKM), Gardner-Rasheed feline sarcoma viral (v-fgr) oncogene homolog (FGR), alpha fucosidase (FUCA1), G-protein beta 1 subunit (GNB1), alpha 1A amylase, (AMY1), the neuroblastoma RAS viral (v-ras) oncogene homolog (NRAS), and alpha skeletal actin (ACTA1)...
August 1994: Genomics
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