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 …

[HTML][HTML] Therapeutic potential of apelin and Elabela in cardiovascular disease

S Gao, H Chen - Biomedicine & Pharmacotherapy, 2023 - Elsevier
Abstract Apelin and Elabela (Ela) are peptides encoded by APLN and APELA, respectively,
which act on their receptor APJ and play crucial roles in the body. Recent research has …

Apelin pathway in cardiovascular, kidney, and metabolic diseases: Therapeutic role of apelin analogs and apelin receptor agonists

AA de Oliveira, A Vergara, X Wang, JC Vederas… - Peptides, 2022 - Elsevier
The apelin/apelin receptor (ApelinR) signal transduction pathway exerts essential biological
roles, particularly in the cardiovascular system. Disturbances in the apelin/ApelinR axis are …

Cardiovascular and renal effects of apelin in chronic kidney disease: a randomised, double-blind, placebo-controlled, crossover study

FA Chapman, V Melville, E Godden, B Morrison… - Nature …, 2024 - nature.com
Chronic kidney disease (CKD) affects~ 10% of the population and cardiovascular disease is
its commonest complication. Despite treatment, patient outcomes remain poor and newer …

Therapeutic approaches for treating pulmonary arterial hypertension by correcting imbalanced TGF-β superfamily signaling

P Andre, SR Joshi, SD Briscoe, MJ Alexander… - Frontiers in …, 2022 - frontiersin.org
Pulmonary arterial hypertension (PAH) is a rare disease characterized by high blood
pressure in the pulmonary circulation driven by pathological remodeling of distal pulmonary …

[HTML][HTML] A promising therapeutic peptide and preventive/diagnostic biomarker for age-related diseases: The Elabela/Apela/Toddler peptide

R Monastero, D Magro, M Venezia, C Pisano… - Ageing research …, 2023 - Elsevier
ABSTRACT Elabela (ELA), Apela or Toddler peptide is a hormone peptide belonging to the
adipokine group and a component of apelinergic system, discovered in 2013-2014. Given its …

Therapy for pulmonary arterial hypertension: Glance on nitric oxide pathway

A Tettey, Y Jiang, X Li, Y Li - Frontiers in pharmacology, 2021 - frontiersin.org
Pulmonary arterial hypertension (PAH) is a severe disease with a resultant increase of the
mean pulmonary arterial pressure, right ventricular hypertrophy and eventual death …

Structure–function relationship and physiological role of apelin and its G protein coupled receptor

S Murali, GK Aradhyam - Biophysical reviews, 2023 - Springer
Apelin receptor (APJR) is a class A peptide (apelin) binding G protein-coupled receptor
(GPCR) that plays a significant role in regulating blood pressure, cardiac output, and …

Targeting the apelin system for the treatment of cardiovascular diseases

FA Chapman, JJ Maguire, DE Newby… - Cardiovascular …, 2023 - academic.oup.com
Cardiovascular disease is the leading cause of death worldwide. Its prevalence is rising due
to ageing populations and the increasing incidence of diseases such as chronic kidney …

Size-Reduced Macrocyclic Analogues of [Pyr1]-apelin-13 Showing Negative Gα12 Bias Still Produce Prolonged Cardiac Effects

K Tran, X Sainsily, J Cote, D Coquerel… - Journal of medicinal …, 2022 - ACS Publications
We previously reported a series of macrocyclic analogues of [Pyr1]-apelin-13 (Ape13) with
increased plasma stability and potent APJ agonist properties. Based on the most promising …