Chemical Blockage of the Mitochondrial Rhomboid Protease PARL by Novel Ketoamide Inhibitors Reveals Its Role in PINK1/Parkin-Dependent Mitophagy
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01092
Abstract: The mitochondrial rhomboid protease PARL regulates mitophagy by balancing intramembrane proteolysis of PINK1 and PGAM5. It has been implicated in the pathogenesis of Parkinson’s disease, but its investigation as a possible therapeutic target is challenging… read more here.
Keywords: ketoamide inhibitors; parl; rhomboid protease; mitochondrial rhomboid ... See more keywords
4-Oxo-β-lactams as Covalent Inhibitors of the Mitochondrial Intramembrane Protease PARL.
Sign Up to like & getrecommendations! Published in 2024 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.4c00384
Abstract: Rhomboid proteases play a variety of physiological roles, but rhomboid protease inhibitors have been mostly developed for the E. coli model rhomboid GlpG. In this work, we screened different electrophilic scaffolds against the human mitochondrial… read more here.
Keywords: oxo lactams; parl; covalent inhibitors; inhibitors mitochondrial ... See more keywords
L-carnitine alleviates cardiac microvascular dysfunction in diabetic cardiomyopathy by enhancing PINK1-Parkin-dependent mitophagy through the CPT1a-PHB2-PARL pathways.
Sign Up to like & getrecommendations! Published in 2023 at "Acta physiologica"
DOI: 10.1111/apha.13975
Abstract: AIM To explore the beneficial effects of L-carnitine on cardiac microvascular dysfunction in diabetic cardiomyopathy from the perspectives of mitophagy and mitochondrial integrity. METHODS Male db/db and db/m mice were randomly assigned to groups and… read more here.
Keywords: cardiac microvascular; parl; cpt1a; mitophagy ... See more keywords