Discovery of a first-in-class small molecule antagonist against the adrenomedullin-2 receptor: structure–activity relationships and optimization
JO Zirimwabagabo, ABA Jailani… - Journal of Medicinal …, 2021 - ACS Publications
Class B G-protein-coupled receptors (GPCRs) remain an underexploited target for drug
development. The calcitonin receptor (CTR) family is particularly challenging, as its …
development. The calcitonin receptor (CTR) family is particularly challenging, as its …
Elucidating the Interactome of G Protein-Coupled Receptors (GPCRs) and Receptor Activity-Modifying Proteins (RAMPs)
IB Kotliar, E Lorenzen, JM Schwenk, DL Hay… - Pharmacological …, 2022 - ASPET
G protein-coupled receptors (GPCRs) are known to interact with several other classes of
integral membrane proteins that modulate their biology and pharmacology. However, the …
integral membrane proteins that modulate their biology and pharmacology. However, the …
Virtual drug repurposing study for the CGRPR identifies pentagastrin and leuprorelin as putative candidates
B Aksoydan, S Durdagi - Journal of Molecular Graphics and Modelling, 2022 - Elsevier
Calcitonin gene-related peptide receptor (CGRPR) is a heterodimer consisting of CLR and
RAMP1 proteins. Activation of the CGRPR with the endogenous peptide CGRP is known to …
RAMP1 proteins. Activation of the CGRPR with the endogenous peptide CGRP is known to …
Calcitonin gene-related peptide-induced phosphorylation of STAT3 in arcuate neurons is a link in the metabolic benefits of portal glucose
M Soty, J Vily-Petit, A Castellanos-Jankiewicz… - …, 2021 - karger.com
Introduction: Intestinal gluconeogenesis (IGN) exerts metabolic benefits in energy
homeostasis via the neural sensing of portal glucose. Objective: The aim of this work was to …
homeostasis via the neural sensing of portal glucose. Objective: The aim of this work was to …
Family BG protein-coupled receptors and their ligands: from structure to function
G Liapakis, MT Matsoukas… - Current Medicinal …, 2017 - ingentaconnect.com
Background: Family BG protein-coupled receptors (GPCRs) play an important role in many
physiological and pathophysiological processes. They are plasma-membrane proteins …
physiological and pathophysiological processes. They are plasma-membrane proteins …
CGRP receptor biology: is there more than one receptor?
DL Hay - Calcitonin Gene-Related Peptide (CGRP) Mechanisms …, 2019 - Springer
Calcitonin gene-related peptide (CGRP) has many reported pharmacological actions. Can a
single receptor explain all of these? This chapter outlines the molecular nature of reported …
single receptor explain all of these? This chapter outlines the molecular nature of reported …
Pharmacological characterization and investigation of N-terminal loop amino acids of adrenomedullin 2 that are important for receptor activation
Adrenomedullin 2 (AM2) is a peptide hormone with potent effects in the cardiovascular
system. The N-terminal disulfide loop of AM2 is thought to be important for interacting with its …
system. The N-terminal disulfide loop of AM2 is thought to be important for interacting with its …
Targeting temperature-sensitive transient receptor potential channels in hypertension: Far beyond the perception of hot and cold
Transient receptor potential (TRP) channels are nonselective cation channels and
participate in various physiological roles. Thus, changes in TRP channel function or …
participate in various physiological roles. Thus, changes in TRP channel function or …
Biochemical characterization of G protein coupling to calcitonin gene–related peptide and adrenomedullin receptors using a native PAGE assay
AM Roehrkasse, ML Warner, JM Booe… - Journal of Biological …, 2020 - ASBMB
Calcitonin gene-related peptide (CGRP), adrenomedullin (AM), and adrenomedullin
2/intermedin (AM2/IMD) have overlapping and unique functions in the nervous and …
2/intermedin (AM2/IMD) have overlapping and unique functions in the nervous and …
Receptor activity modifying proteins have limited effects on the Class BG protein-coupled receptor calcitonin receptor-like receptor stalk
ML Garelja, CA Walker, A Siow, SH Yang… - Biochemistry, 2018 - ACS Publications
The calcitonin receptor-like receptor (CLR) is a class BG protein-coupled receptor (GPCR)
that forms the basis of three pharmacologically distinct receptors, the calcitonin gene-related …
that forms the basis of three pharmacologically distinct receptors, the calcitonin gene-related …