Prostacyclin mimetics inhibit DRP1-mediated pro-proliferative mitochondrial fragmentation in pulmonary arterial hypertension
In this study, we confirmed the previously reported increase in DRP1-mediated mitochondrial hyper-fragmentation in PAH PASMCs. We then showed that the prostacyclin mimetic treprostinil signals via either the Gs-coupled IP or EP2 receptor to inhibit mitochondrial fragmentation and the associated hyper-proliferation in a manner analogous to the DRP1 inhibitor Mdivi-1. We also showed that treprostinil recruits either the IP or EP2 receptor to activate PKA and induce the phosphorylation of DRP1 at the inhibitory residue S637 and inhibit that at the stimulatory residue S616, both of which are suggestive of reduced DRP1 fission ...
Source: Vascular Pharmacology - July 13, 2023 Category: Drugs & Pharmacology Authors: Jeries Abu-Hanna Evangelos Anastasakis Jigisha A Patel Mohammad Mahmoud Rajab Eddama Christopher P Denton Jan-Willem Taanman David Abraham Lucie H Clapp Source Type: research

Prostacyclin mimetics inhibit DRP1-mediated pro-proliferative mitochondrial fragmentation in pulmonary arterial hypertension
In this study, we confirmed the previously reported increase in DRP1-mediated mitochondrial hyper-fragmentation in PAH PASMCs. We then showed that the prostacyclin mimetic treprostinil signals via either the Gs-coupled IP or EP2 receptor to inhibit mitochondrial fragmentation and the associated hyper-proliferation in a manner analogous to the DRP1 inhibitor Mdivi-1. We also showed that treprostinil recruits either the IP or EP2 receptor to activate PKA and induce the phosphorylation of DRP1 at the inhibitory residue S637 and inhibit that at the stimulatory residue S616, both of which are suggestive of reduced DRP1 fission ...
Source: Vascular Pharmacology - July 13, 2023 Category: Drugs & Pharmacology Authors: Jeries Abu-Hanna Evangelos Anastasakis Jigisha A Patel Mohammad Mahmoud Rajab Eddama Christopher P Denton Jan-Willem Taanman David Abraham Lucie H Clapp Source Type: research

Cardiovascular aspects of ELABELA: A potential diagnostic biomarker and therapeutic target
Vascul Pharmacol. 2023 Jul 9:107193. doi: 10.1016/j.vph.2023.107193. Online ahead of print.ABSTRACTELABELA, an early endogenous ligand for the G protein-coupled receptor APJ (apelin peptide jejunum, apelin receptor), has been known as an important regulator in cardiovascular homeostasis and may be a novel therapeutic target for multiple cardiovascular diseases (CVDs). At the physiological level, ELABELA exhibits angiogenic and vasorelaxant effects and is essential for heart development. At the pathological level, circulating ELABELA levels may be a novel diagnostic biomarker for various CVDs. ELABELA peripherally displays ...
Source: Vascular Pharmacology - July 11, 2023 Category: Drugs & Pharmacology Authors: Chuanming Xu Source Type: research

Cardiovascular aspects of ELABELA: A potential diagnostic biomarker and therapeutic target
Vascul Pharmacol. 2023 Jul 9:107193. doi: 10.1016/j.vph.2023.107193. Online ahead of print.ABSTRACTELABELA, an early endogenous ligand for the G protein-coupled receptor APJ (apelin peptide jejunum, apelin receptor), has been known as an important regulator in cardiovascular homeostasis and may be a novel therapeutic target for multiple cardiovascular diseases (CVDs). At the physiological level, ELABELA exhibits angiogenic and vasorelaxant effects and is essential for heart development. At the pathological level, circulating ELABELA levels may be a novel diagnostic biomarker for various CVDs. ELABELA peripherally displays ...
Source: Vascular Pharmacology - July 11, 2023 Category: Drugs & Pharmacology Authors: Chuanming Xu Source Type: research

Cardiovascular aspects of ELABELA: A potential diagnostic biomarker and therapeutic target
Vascul Pharmacol. 2023 Jul 9:107193. doi: 10.1016/j.vph.2023.107193. Online ahead of print.ABSTRACTELABELA, an early endogenous ligand for the G protein-coupled receptor APJ (apelin peptide jejunum, apelin receptor), has been known as an important regulator in cardiovascular homeostasis and may be a novel therapeutic target for multiple cardiovascular diseases (CVDs). At the physiological level, ELABELA exhibits angiogenic and vasorelaxant effects and is essential for heart development. At the pathological level, circulating ELABELA levels may be a novel diagnostic biomarker for various CVDs. ELABELA peripherally displays ...
Source: Vascular Pharmacology - July 11, 2023 Category: Drugs & Pharmacology Authors: Chuanming Xu Source Type: research