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Targeting the activated allosteric conformation of the endothelin receptor B in melanoma with an antibody-drug conjugate: mechanisms and therapeutic efficacy.
BJC Rep
January 2025
Université Paris-Saclay, CEA, INRAE, Médicaments et Technologies pour la Santé (MTS), SPI, Laboratoire d'Etude de l'Unité Neurovasculaire et Innovation Thérapeutique (LENIT), Gif-sur-Yvette, France.
Background: Endothelin 1 receptors are one of the drivers of tumor progression in many cancers. Inhibition of their signaling pathways with antagonist drugs has been the subject of numerous clinical trials, but the results have not met expectations probably due to the high endothelin concentrations in the tumor microenvironment and their unusually high affinity for their receptors.
Methods: We previously reported the rendomab B49 antibody (RB49) exhibiting a preferential affinity for the activated conformation of human endothelin B receptor (ET), not displaced by high endothelin levels, and without any pharmacological properties that could inhibit the division of melanoma cells.
[Biomarkers of atherothrombotic and cardioembolic subtypes of acute ischemic stroke].
Zh Nevrol Psikhiatr Im S S Korsakova
January 2025
Imannuel Kant Baltic Federal University, Kaliningrad, Russia.
Objective: To evaluate the concentrations of CC-chemokines and stable metabolites of nitric oxide (NO) and endothelin-1 (ET-1) in patients with atherothrombotic (AT) and cardioembolic (CE) subtypes of ischemic stroke (IS) in the acute period.
Material And Methods: Sixty patients diagnosed with IS in the carotid basin were examined. Group 1 included 30 patients with AT, group 2 - 30 patients with CE subtype of IS.
Repurposing bosentan as an anticancer agent: EGFR/ERK/c-Jun modulation inhibits NSCLC tumor growth.
Fundam Clin Pharmacol
February 2025
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, 62514, Egypt.
Drug repurposing of well-established drugs to be targeted against lung cancer has been a promising strategy. Bosentan is an endothelin 1 (ET-1) blocker widely used in pulmonary hypertension. The current experiment intends to inspect the anticancer and antiangiogenic mechanism of bosentan targeting epidermal growth factor receptor (EGFR) /extra-cellular Signal Regulated Kinase (ERK) /c-Jun/vascular endothelial growth factor (VEGF) carcinogenic pathway.
View Article and Find Full Text PDFRelationship Between the Biomarkers of Collagen Regulation and Echocardiography Parameters in Patients With Heart Failure With Preserved Ejection Fraction.
Kardiologiia
December 2024
Tyumen Cardiological Research Center, Tomsk National Research Medical Center of the Russian Academy of Sciences, Tomsk.
Aim: To study the relationship between laboratory markers and echocardiography (EchoCG) parameters in heart failure with preserved ejection fraction (HFpEF) depending on the results of the diastolic stress test (DST).
Material And Methods: The diagnostic algorithm provided by the current guidelines for the assessment of left ventricular (LV) diastolic function was used to select patients. If there were not enough criteria to make a conclusion about increased LV filling pressure (FP) based on standard resting echocardiography data in patients with arterial hypertension and ischemic heart disease, DST was performed to detect HFpEF.
Clearing Amyloid-Beta by Astrocytes: The Role of Rho GTPases Signaling Pathways as Potential Therapeutic Targets.
Brain Sci
December 2024
Department of Anatomy and Neurobiology, University of Tennessee Health Science Center, Memphis, TN 38163, USA.
Astrocytes, vital support cells in the central nervous system (CNS), are crucial for maintaining neuronal health. In neurodegenerative diseases such as Alzheimer's disease (AD), astrocytes play a key role in clearing toxic amyloid-β (Aβ) peptides. Aβ, a potent neuroinflammatory trigger, stimulates astrocytes to release excessive glutamate and inflammatory factors, exacerbating neuronal dysfunction and death.
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