User profiles for Madeleine M. Fletcher

Madeleine Fletcher

GSK
Verified email at gsk.com
Cited by 787

Glucagon-like peptide-1 and its class BG protein–coupled receptors: a long march to therapeutic successes

…, LJ Miller, JM Ahn, J Liao, MM Fletcher… - Pharmacological …, 2016 - ASPET
The glucagon-like peptide (GLP)-1 receptor (GLP-1R) is a class BG protein–coupled receptor
(GPCR) that mediates the action of GLP-1, a peptide hormone secreted from three major …

Activation of the GLP-1 receptor by a non-peptidic agonist

…, YL Liang, MJ Belousoff, G Deganutti, MM Fletcher… - Nature, 2020 - nature.com
Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases,
including diabetes and obesity 1 . Structures of active receptors reveal peptide agonists …

[PDF][PDF] Toward a structural understanding of class B GPCR peptide binding and activation

YL Liang, MJ Belousoff, P Zhao, C Koole, MM Fletcher… - Molecular cell, 2020 - cell.com
Class BG protein-coupled receptors (GPCRs) are important therapeutic targets for major
diseases. Here, we present structures of peptide and Gs-bound pituitary adenylate cyclase-…

A structural basis for amylin receptor phenotype

…, YL Liang, RM Johnson, TM Josephs, MM Fletcher… - Science, 2022 - science.org
Amylin receptors (AMYRs) are heterodimers of the calcitonin (CT) receptor (CTR) and one
of three receptor activity–modifying proteins (RAMPs), AMY 1 R, AMY 2 R, and AMY 3 R. …

Structure and Dynamics of Adrenomedullin Receptors AM1 and AM2 Reveal Key Mechanisms in the Control of Receptor Phenotype by Receptor Activity-Modifying …

…, MM Fletcher, X Zhang, M Khoshouei… - ACS pharmacology & …, 2020 - ACS Publications
Adrenomedullin (AM) and calcitonin gene-related peptide (CGRP) receptors are critically
important for metabolism, vascular tone, and inflammatory response. AM receptors are also …

Structural insight into selectivity of amylin and calcitonin receptor agonists

…, E Gerrard, R Danev, MM Fletcher… - Nature Chemical …, 2023 - nature.com
Amylin receptors (AMYRs), heterodimers of the calcitonin receptor (CTR) and one of three
receptor activity-modifying proteins, are promising obesity targets. A hallmark of AMYR …

Glucagon-like peptide-1 receptor internalisation controls spatiotemporal signalling mediated by biased agonists

MM Fletcher, ML Halls, P Zhao, L Clydesdale… - Biochemical …, 2018 - Elsevier
The glucagon-like peptide-1 receptor (GLP-1R) is a major therapeutic target in the treatment
of type 2 diabetes due to its roles in regulating blood glucose and in promoting weight loss. …

AM833 is a novel agonist of calcitonin family G protein–coupled receptors: pharmacological comparison with six selective and nonselective agonists

MM Fletcher, P Keov, TT Truong, G Mennen… - … of Pharmacology and …, 2021 - ASPET
Obesity and associated comorbidities are a major health burden, and novel therapeutics to
help treat obesity are urgently needed. There is increasing evidence that targeting the amylin …

The complexity of signalling mediated by the glucagon-like peptide-1 receptor

MM Fletcher, ML Halls, A Christopoulos… - Biochemical Society …, 2016 - portlandpress.com
The glucagon-like peptide-1 receptor (GLP-1R) is a class B GPCR that is a major therapeutic
target for the treatment of type 2 diabetes. The receptor is activated by the incretin peptide …

[HTML][HTML] Understanding VPAC receptor family peptide binding and selectivity

…, J Lu, P Zhao, YL Liang, Y Lu, MM Fletcher… - Nature …, 2022 - nature.com
The vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating polypeptide
(PACAP) receptors are key regulators of neurological processes. Despite recent structural …