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Transport and action of sesame protein-derived ACE inhibitory peptides ITAPHW and IRPNGL.
Food Chem
January 2025
State Key Laboratory of Food Science and Resources, Nanchang University, No. 235 Nanjing East Road, Nanchang, Jiangxi, 330047, PR China; School of Food Science and Technology, Nanchang University, No. 235 Nanjing East Road, Nanchang, Jiangxi, 330047, PR China.
Vascular endothelial dysfunction is an important pathogenic factor in hypertension, in which angiotensin-converting enzyme (ACE) plays an important role. Peptides that bind to ACE may attenuate vascular endothelial dysfunction by altering the structure of ACE. This study demonstrated that ITAPHW and IRPNGL were resistant to simulated gastrointestinal fluid and were transported across the Caco-2 monolayer via the intercellular space, with ITAPHW showing a high apparent permeability coefficient of (1.
View Article and Find Full Text PDFTargeting 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.
Pharmacological profiling of small molecule modulators of the TMEM16A channel and their implications for the control of artery and capillary function.
Br J Pharmacol
January 2025
Department of Pharmacology, University of Oxford, Oxford, UK.
Background And Purpose: TMEM16A chloride channels constitute a depolarising mechanism in arterial smooth muscle cells (SMCs) and contractile cerebral pericytes. TMEM16A pharmacology is incompletely defined. We elucidated the mode of action and selectivity of a recently identified positive allosteric modulator of TMEM16A (PAM_16A) and of a range of TMEM16A inhibitors.
View Article and Find Full Text PDFComparative Pharmacokinetics and Bioequivalence of 2 Formulations of Bosentan Dispersible Tablets in Healthy Chinese Volunteers Under Fasting and Fed Conditions.
Clin Pharmacol Drug Dev
January 2025
Department of Pathology, Xianning Central Hospital, The First Affiliated Hosptial of Hubei University of Science and Technology, Xianning, Hubei, P.R. China.
Bosentan is a dual endothelin receptor antagonist widely used in the treatment of pulmonary artery hypertension. However, there are few reports on the pharmacokinetics (PK) and bioequivalence of bosentan dispersible tablets (32 mg) in the Chinese population. This study aimed to evaluate the PK characteristics and bioequivalence of the test and reference formulations of bosentan dispersible tablets in healthy Chinese volunteers under fasting and fed conditions.
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