Exploring Ligand Binding to Calcitonin Gene-Related Peptide Receptors
Class B1 G protein-coupled receptors (GPCRs) are important targets for many diseases, including cancer, diabetes, and heart disease. All the approved drugs for this receptor family are peptides that mimic the endogenous activating hormones.
Giuseppe Deganutti +7 more
doaj +1 more source
Crystal structure of the human receptor activity‐modifying protein 1 extracellular domain [PDF]
AbstractReceptor activity‐modifying protein (RAMP) 1 forms a heterodimer with calcitonin receptor‐like receptor (CRLR) and regulates its transport to the cell surface. The CRLR·RAMP1 heterodimer functions as a specific receptor for calcitonin gene‐related peptide (CGRP). Here, we report the crystal structure of the human RAMP1 extracellular domain. The
Seisuke, Kusano +7 more
openaire +2 more sources
Receptor Activity-modifying Protein (RAMP) Isoform-specific Regulation of Adrenomedullin Receptor Trafficking by NHERF-1 [PDF]
Receptor activity-modifying proteins (RAMPs 1-3) are single transmembrane accessory proteins critical to various G-protein coupled receptors for plasma membrane expression and receptor phenotype. A functional receptor for the vasodilatory ligand, adrenomedullin (AM), is comprised of RAMP2 or RAMP3 and calcitonin receptor-like receptor (CRLR). It is now
Jennifer M, Bomberger +4 more
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Receptor Activity-modifying Protein 1 Determines the Species Selectivity of Non-peptide CGRP Receptor Antagonists [PDF]
The heterodimeric CGRP receptor requires co-expression of calcitonin receptor-like receptor (CRLR) and an accessory protein called receptor activity-modifying protein (RAMP) 1 (McLatchie, L. M., Fraser, N. J., Main, M. J., Wise, A., Brown, J., Thompson, N., Solari, R., Lee, M. G., and Foord, S. M. (1998) Nature 393, 333-339).
John J, Mallee +6 more
openaire +2 more sources
Pharmacological levels of withaferin A (Withania somnifera) trigger clinically relevant anticancer effects specific to triple negative breast cancer cells [PDF]
Withaferin A (WA) isolated from Withania somnifera (Ashwagandha) has recently become an attractive phytochemical under investigation in various preclinical studies for treatment of different cancer types. In the present study, a comparative pathway-based
A Albini +74 more
core +6 more sources
The Extracellular Domain of Receptor Activity-modifying Protein 1 Is Sufficient for Calcitonin Receptor-like Receptor Function [PDF]
A functional calcitonin gene-related peptide (CGRP) receptor requires dimerization of calcitonin receptor-like receptor (CRLR) with receptor activity-modifying protein 1 (RAMP 1). To determine the function of the three domains (extracellular, ECD; transmembrane, TM; and tail domains) of human RAMP 1, three mutants were constructed: RAMP 1 without the ...
Timothy J, Fitzsimmons +2 more
openaire +2 more sources
Genetic analysis and cAMP measurement: comparison between lean and obese anovulating mice [PDF]
PURPOSE: To evaluate genes differentially expressed in ovaries from lean (wild type) and obese (ob/ob) female mice and cyclic AMP production in both groups.METHODS: The expression on messenger RNA levels of 84 genes concerning obesity was analyzed ...
Daniela Berguio Vidotti +5 more
doaj +2 more sources
Receptor-activity-modifying protein 1 forms heterodimers with two G-protein-coupled receptors to define ligand recognition [PDF]
Receptor-activity-modifying proteins (RAMPs) with single transmembrane domains define the function of two G-protein-coupled receptors of the B family. Cell-surface complexes of human RAMP1 (hRAMP1) and human calcitonin (CT) receptor isotype 2 (hCTR2) or rat CT-receptor-like receptor (rCRLR) have now been identified through protein cross-linking, co ...
K, Leuthäuser +6 more
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Procalcitonin and Adrenomedullin in Infectious Diseases
Calcitonin (CT) and adrenomedullin (ADM) are members of the CT family. Procalcitonin (PCT) is a prohormone of CT. Elevations in serum PCT and ADM levels are associated with severe sepsis and coronavirus disease 2019 (COVID-19).
Yoshimitsu Kiriyama, Hiromi Nochi
doaj +1 more source
An Amylin Receptor Is Revealed Following Co-Transfection of a Calcitonin Receptor with Receptor Activity Modifying Proteins-1 or -3 [PDF]
Human receptor activity modifying proteins (RAMP) regulate the ligand specificity of the calcitonin-receptor-like-receptor (McLatchie et al., Nature 393:333-339 (1998)). Here we have investigated binding of [125I]-labeled human (h) calcitonin ([125I]hCT) and rat amylin ([125I]amylin) to rabbit aortic endothelial cells (RAEC) co-transfected with the hCT
R, Muff +3 more
openaire +3 more sources

