[HTML][HTML] GLP-1 physiology informs the pharmacotherapy of obesity

DJ Drucker - Molecular metabolism, 2022 - Elsevier
Background Glucagon-like peptide-1 receptor agonists (GLP1RA) augment glucose-
dependent insulin release and reduce glucagon secretion and gastric emptying, enabling …

[HTML][HTML] An update on peptide-based therapies for type 2 diabetes and obesity

CJ Bailey, PR Flatt, JM Conlon - Peptides, 2023 - Elsevier
Long-acting analogues of the naturally occurring incretin, glucagon-like peptide-1 (GLP-1)
and those modified to interact also with receptors for glucose-dependent insulinotropic …

Once-weekly cagrilintide for weight management in people with overweight and obesity: a multicentre, randomised, double-blind, placebo-controlled and active …

DCW Lau, L Erichsen, AM Francisco, A Satylganova… - The Lancet, 2021 - thelancet.com
Background Natural amylin is a pancreatic hormone that induces satiety. Cagrilintide is a
long-acting amylin analogue under investigation for weight management. We assessed the …

Derivatization with fatty acids in peptide and protein drug discovery

P Kurtzhals, S Østergaard, E Nishimura… - Nature Reviews Drug …, 2023 - nature.com
Peptides and proteins are widely used to treat a range of medical conditions; however, they
often have to be injected and their effects are short-lived. These shortcomings of the native …

Elucidating the interactome of G protein-coupled receptors and receptor activity-modifying proteins

IB Kotliar, E Lorenzen, JM Schwenk, DL Hay… - Pharmacological …, 2023 - 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 …

A structural basis for amylin receptor phenotype

J Cao, MJ Belousoff, YL Liang, RM Johnson… - Science, 2022 - science.org
Amylin receptors (AMYRs) are heterodimers of the calcitonin (CT) receptor (CTR) and one of
three receptor activity–modifying proteins (RAMPs), AMY1R, AMY2R, and AMY3R. Selective …

[HTML][HTML] Anti-obesity medications and investigational agents: an obesity medicine association (OMA) clinical practice statement (CPS) 2022

HE Bays, A Fitch, S Christensen, K Burridge, J Tondt - Obesity Pillars, 2022 - Elsevier
Abstract Background This “Anti-Obesity Medications and Investigational Agents: An Obesity
Medicine Association Clinical Practice Statement 2022” is intended to provide clinicians an …

Structural insight into selectivity of amylin and calcitonin receptor agonists

J Cao, MJ Belousoff, E Gerrard, R Danev… - Nature Chemical …, 2024 - 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 …

Recent advances in the development of therapeutic peptides

J Fetse, S Kandel, UF Mamani, K Cheng - Trends in Pharmacological …, 2023 - cell.com
Peptides have unique characteristics that make them highly desirable as therapeutic agents.
The physicochemical and proteolytic stability profiles determine the therapeutic potential of …

Preclinical evaluation of a protracted GLP-1/glucagon receptor co-agonist: translational difficulties and pitfalls

L Simonsen, J Lau, T Kruse, T Guo, J McGuire… - PLoS …, 2022 - journals.plos.org
During recent years combining GLP-1 and glucagon receptor agonism with the purpose of
achieving superior weight loss and metabolic control compared to GLP-1 alone has …