Adrenomedullin–current perspective on a peptide hormone with significant therapeutic potential

JP Fischer, S Els-Heindl, AG Beck-Sickinger - Peptides, 2020 - Elsevier
The peptide hormone adrenomedullin (ADM) consists of 52 amino acids and plays a pivotal
role in the regulation of many physiological processes, particularly those of the …

Determining the Effects of Differential Expression of GRKs and β-arrestins on CLR-RAMP Agonist Bias

A Pearce, T Redfern-Nichols, M Harris… - Frontiers in …, 2022 - frontiersin.org
Signalling of the calcitonin-like receptor (CLR) is multifaceted, due to its interaction with
receptor activity modifying proteins (RAMPs), and three endogenous peptide agonists …

Pharmacological characterisation of mouse calcitonin and calcitonin receptor‐like receptors reveals differences compared with human receptors

ML Garelja, RL Bower, MA Brimble… - British journal of …, 2022 - Wiley Online Library
Background and Purpose The calcitonin (CT) receptor family is complex, comprising two
receptors (the CT receptor [CTR] and the CTR‐like receptor [CLR]), three accessory proteins …

[HTML][HTML] Receptor activity-modifying protein dependent and independent activation mechanisms in the coupling of calcitonin gene-related peptide and adrenomedullin …

MJ Woolley, CA Reynolds, J Simms, CS Walker… - Biochemical …, 2017 - Elsevier
Calcitonin gene-related peptide (CGRP) or adrenomedullin (AM) receptors are heteromers
of the calcitonin receptor-like receptor (CLR), a class BG protein-coupled receptor, and one …

Differential Influences of Endogenous and Exogenous Sensory Neuropeptides on the ATP Metabolism by Soluble Ectonucleotidases in the Murine Bladder Lamina …

A Gutierrez Cruz, MSL Aresta Branco… - International Journal of …, 2023 - mdpi.com
Bladder urothelium and suburothelium/lamina propria (LP) have prominent sensory and
transducer functions with the active participation of afferent neurons and urothelium-derived …

[HTML][HTML] Modelling and simulation of biased agonism dynamics at a G protein-coupled receptor

LJ Bridge, J Mead, E Frattini, I Winfield… - Journal of theoretical …, 2018 - Elsevier
Theoretical models of G protein-coupled receptor (GPCR) concentration-response
relationships often assume an agonist producing a single functional response via a single …

RAMP2 influences glucagon receptor pharmacology via trafficking and signaling

J Cegla, BJ Jones, JV Gardiner, DJ Hodson… - …, 2017 - academic.oup.com
Endogenous satiety hormones provide an attractive target for obesity drugs. Glucagon
causes weight loss by reducing food intake and increasing energy expenditure. To further …

Discovery of a first-in-class potent small molecule antagonist against the adrenomedullin-2 receptor

P Avgoustou, ABA Jailani… - ACS pharmacology & …, 2020 - ACS Publications
The hormone adrenomedullin has both physiological and pathological roles in biology. As a
potent vasodilator, adrenomedullin is critically important in the regulation of blood pressure …

Elevated intracellular cAMP concentration mediates growth suppression in glioma cells

D Safitri, M Harris, H Potter, HY Yeung, I Winfield… - Biochemical …, 2020 - Elsevier
Supressed levels of intracellular cAMP have been associated with malignancy. Thus,
elevating cAMP through activation of adenylyl cyclase (AC) or by inhibition of …

Adrenomedullin 2/intermedin is a slow off-rate, long-acting endogenous agonist of the adrenomedullin2 G protein–coupled receptor

KM Babin, JA Karim, PH Gordon, J Lennon… - Journal of Biological …, 2023 - ASBMB
Adrenomedullin 2/intermedin (AM2/IMD), adrenomedullin (AM), and calcitonin gene-related
peptide (CGRP) have functions in the cardiovascular, lymphatic, and nervous systems by …