Sartans and Bisartans: Expanding Therapeutic Horizons Through Broad Receptor Interactions and Repurposing Potential
9 affiliations
- 1Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, 15771 Athens, Greece
- 2School of Health and Biomedical Sciences, RMIT University, Melbourne, VIC 3000, Australia
- 3NewDrug PC, Patras Science Park, 26504 Patras, Greece
- 4THERAmolecular, LLC., Rodeo, NM 88056, USA
- 5Institute for Sustainable Industries and Liveable Cities, Victoria University, Melbourne, VIC 8001, Australia
- 6Pepmetics Inc., 772 Murphy Place, Victoria, BC V8Y 3H4, Canada
- 7Institute for Health and Sport, Victoria University, Melbourne, VIC 3030, Australia
- 8Department of Chemistry, University of Patras, 26504 Patras, Greece
- 9Department of Physiology and Pharmacology, Cumming School of Medicine, University of Calgary, Calgary, AB T2N 1N4, Canada
Abstract
Angiotensin receptor blockers (ARBs), also known as sartans, are a family of highly selective angiotensin II type 1 receptor antagonists commonly prescribed to individuals with hypertension, heart failure, and chronic kidney disease. Additionally, the discovery and facile synthesis of bisartans, a novel class of ARB antihypertensives, have shown therapeutic promise for cardiovascular diseases. Recent computational and network pharmacology studies have shown a broader receptor interactome, encompassing alpha-adrenergic receptors, and delta- and mu-opioid receptors, highlighting the polypharmacology of ARBs. Herein, we combine molecular docking, molecular dynamics, and protein–protein interaction analyses to characterize the binding profiles of sartans and bisartans, as well as conformational impacts across multiple G-protein-coupled receptors. Emphasis is placed on their potential to modulate receptor desensitization states and influence pathways involved in neuropsychiatric disorders, addiction, viral infections, and cardiovascular diseases. Limitations of current computational approaches are discussed alongside the need for experimental proteomic validation. Collectively, this evidence positions sartans and bisartans as structurally privileged scaffolds for multi-target drug repurposing and precision medicine applications.
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BibTeX
@article{petsas2026sartans,
title = {{Sartans and Bisartans: Expanding Therapeutic Horizons Through Broad Receptor Interactions and Repurposing Potential}},
author = {Errikos Petsas and Vasso Apostolopoulos and Despoina P. Kiouri and Konstantinos Kelaidonis and Harry Ridgway and Graham J. Moore and Thomas Mavromoustakos and Laura Kate Gadanec and John M. Matsoukas and Christos T. Chasapis},
journal = {International Journal of Molecular Sciences},
year = {2026},
month = oct,
doi = {10.3390/ijms27198883},
url = {https://www.mdpi.com/1422-0067/27/19/8883},
note = {CC BY 4.0},
}
RIS
TY - JOUR
TI - Sartans and Bisartans: Expanding Therapeutic Horizons Through Broad Receptor Interactions and Repurposing Potential
AU - Errikos Petsas
AU - Vasso Apostolopoulos
AU - Despoina P. Kiouri
AU - Konstantinos Kelaidonis
AU - Harry Ridgway
AU - Graham J. Moore
AU - Thomas Mavromoustakos
AU - Laura Kate Gadanec
AU - John M. Matsoukas
AU - Christos T. Chasapis
PY - 2026
DA - 2026/10/06
JO - International Journal of Molecular Sciences
DO - 10.3390/ijms27198883
UR - https://www.mdpi.com/1422-0067/27/19/8883
AB - Angiotensin receptor blockers (ARBs), also known as sartans, are a family of highly selective angiotensin II type 1 receptor antagonists commonly prescribed to individuals with hypertension, heart failure, and chronic kidney disease. Additionally, the discovery and facile synthesis of bisartans, a novel class of ARB antihypertensives, have shown therapeutic promise for cardiovascular diseases. Recent computational and network pharmacology studies have shown a broader receptor interactome, encompassing alpha-adrenergic receptors, and delta- and mu-opioid receptors, highlighting the polypharmacology of ARBs. Herein, we combine molecular docking, molecular dynamics, and protein–protein interaction analyses to characterize the binding profiles of sartans and bisartans, as well as conformational impacts across multiple G-protein-coupled receptors. Emphasis is placed on their potential to modulate receptor desensitization states and influence pathways involved in neuropsychiatric disorders, addiction, viral infections, and cardiovascular diseases. Limitations of current computational approaches are discussed alongside the need for experimental proteomic validation. Collectively, this evidence positions sartans and bisartans as structurally privileged scaffolds for multi-target drug repurposing and precision medicine applications.
SN - 1422-0067
ER -