Advances in therapeutic peptides targeting G protein-coupled receptors

AP Davenport, CCG Scully, C de Graaf… - Nature Reviews Drug …, 2020 - nature.com
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …

Mechanistic links between obesity, diabetes, and blood pressure: role of perivascular adipose tissue

SN Saxton, BJ Clark, SB Withers… - Physiological …, 2019 - journals.physiology.org
Obesity is increasingly prevalent and is associated with substantial cardiovascular risk.
Adipose tissue distribution and morphology play a key role in determining the degree of …

The Concise Guide to PHARMACOLOGY 2013/14: G protein‐coupled receptors

SPH Alexander, HE Benson… - British journal of …, 2013 - Wiley Online Library
Abstract The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of
the key properties of over 2000 human drug targets with their pharmacology, plus links to an …

The role of apelin–APJ system in diabetes and obesity

C Li, H Cheng, BK Adhikari, S Wang, N Yang… - Frontiers in …, 2022 - frontiersin.org
Nowadays, diabetes and obesity are two main health-threatening metabolic disorders in the
world, which increase the risk for many chronic diseases. Apelin, a peptide hormone, exerts …

Elabela/toddler is an endogenous agonist of the apelin APJ receptor in the adult cardiovascular system, and exogenous administration of the peptide compensates for …

P Yang, C Read, RE Kuc, G Buonincontri… - Circulation, 2017 - Am Heart Assoc
Background: Elabela/toddler (ELA) is a critical cardiac developmental peptide that acts
through the G-protein–coupled apelin receptor, despite lack of sequence similarity to the …

The therapeutic potential of apelin in kidney disease

FA Chapman, D Nyimanu, JJ Maguire… - Nature Reviews …, 2021 - nature.com
Chronic kidney disease (CKD) is a leading cause of global morbidity and mortality and is
independently associated with cardiovascular disease. The mainstay of treatment for CKD is …

Involvement of novel adipokines, chemerin, visfatin, resistin and apelin in reproductive functions in normal and pathological conditions in humans and animal models

A Estienne, A Bongrani, M Reverchon, C Ramé… - International journal of …, 2019 - mdpi.com
It is well known that adipokines are endocrine factors that are mainly secreted by white
adipose tissue. Their central role in energy metabolism is currently accepted. More recently …

Angiotensin-converting enzyme 2 metabolizes and partially inactivates pyr-apelin-13 and apelin-17: physiological effects in the cardiovascular system

W Wang, SMK McKinnie, M Farhan, M Paul… - …, 2016 - Am Heart Assoc
Apelin peptides mediate beneficial effects on the cardiovascular system and are being
targeted as potential new drugs. However, apelin peptides have extremely short biological …

Apelin, diabetes, and obesity

I Castan-Laurell, C Dray, C Attané, T Duparc, C Knauf… - Endocrine, 2011 - Springer
Apelin is a peptide known as the ligand of the G-protein-coupled receptor APJ. Several
active apelin forms exist such as apelin-36, apelin-17, apelin-13, and the pyroglutamated …

The apelin receptor: physiology, pathology, cell signalling, and ligand modulation of a peptide-activated class A GPCR

NA Chapman, DJ Dupré… - Biochemistry and cell …, 2014 - cdnsciencepub.com
The apelin receptor (AR or APJ) is a class A (rhodopsin-like) G-protein-coupled receptor
with wide distribution throughout the human body. Activation of the AR by its cognate …