Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Exploring Hypertension: The Role of AT1 Receptors, Sartans, and Lipid Bilayers
Δημιουργός/Συγγραφέας:	Georgiou, Nikitas Chontzopoulou, Eleni Routsi, Efthymios Alexandros Stavrakaki, Irene Georgia Petsas, Errikos Zoupanou, Nikoletta Kakava, Margarita Georgia [EL] Τζέλη, Δήμητρα[EN] Tzeli, Demeter [EL] Μαυρομούστακος, Θωμάς[EN] Mavromoustakos, Thomas Kiriakidi, Sofia
Ημερομηνία:	2024
Γλώσσα:	Αγγλικά
ISSN:	2470-1343 2470-1343
DOI:	10.1021/acsomega.4c06351
Περίληψη:	The rational design of AT1 receptor antagonists represents a pivotal approach in the development of therapeutic agents targeting cardiovascular pathophysiology. Sartans, a class of compounds engineered to inhibit the binding and activation of Angiotensin II on the AT1 receptor, have demonstrated significant clinical efficacy. This review explores the multifaceted role of sartans in mitigating hypertension and related complications. We highlight the integration of crystallography, computational simulations, and NMR spectroscopy to elucidate sartan-AT1 receptor interactions, providing a foundation for the next-generation antagonist design. The review also delves into the challenges posed by the high lipophilicity and suboptimal bioavailability of sartans, emphasizing advancements in nanotechnology and novel drug delivery systems. Additionally, we discuss the impact of lipid bilayers on the AT1 receptor conformation and drug binding, underscoring the importance of the lipidic environment in receptor-drug interactions. We suggest that optimizing drug design to account for these factors could enhance the therapeutic potential of AT1 receptor antagonists, paving the way for improved cardiovascular health outcomes.
Τίτλος πηγής δημοσίευσης:	ACS Omega
Τόμος/Κεφάλαιο:	9
Τεύχος:	45
Θεματική Κατηγορία:	[EL] Δομική Βιολογία[EN] Structural Biology [EL] Θεραπευτική. Φαρμακολογία[EN] Therapeutics.Pharmacology [EL] Κρυσταλλογραφία[EN] Crystallography [EL] Φαρμακευτική χημεία[EN] Pharmaceutical chemistry
Λέξεις-Κλειδιά:	AT1 receptor antagonists drug design drug delivery NMR spectroscopy
Κάτοχος πνευματικών δικαιωμάτων:	© 2024 The Authors. Published by American Chemical Society
Ηλεκτρονική διεύθυνση στον εκδότη (link):	https://doi.org/10.1021/acsomega.4c06351
Εμφανίζεται στις συλλογές:	Ινστιτούτο Θεωρητικής και Φυσικής Χημείας (ΙΘΦΧ) - Επιστημονικό έργο