User profiles for Madeleine M. Fletcher
Madeleine FletcherGSK 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
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 …
(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
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 …
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
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-…
diseases. Here, we present structures of peptide and Gs-bound pituitary adenylate cyclase-…
A structural basis for amylin receptor phenotype
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. …
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 …
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 …
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
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. …
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 …
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
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 …
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
The vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating polypeptide
(PACAP) receptors are key regulators of neurological processes. Despite recent structural …
(PACAP) receptors are key regulators of neurological processes. Despite recent structural …