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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.
Assessing candidate DLX-regulated genes in the first pharyngeal arch of chick embryos.
Dev Dyn
January 2025
Department of Molecular and Cellular Biology, University of Guelph, Guelph, Ontario, Canada.
Background: Insights into the development and evolution of asymmetrical jaws will require an understanding of the gene regulatory networks that underpin the differential morphogenesis of the maxillary and mandibular domains of the first pharyngeal arch in a variety of gnathostomes. While a robust relationship has been demonstrated between jaw patterning and the Endothelin-Dlx gene axis, much less is known of the next level of genes in the jaw patterning hierarchy.
Results: Several genes, whose expression depends on Dlx5 and/or Dlx6, have been identified in mice.
Investigation of the protective effect of cilostazol on acute lung injury-mediated inflammation and in silico molecular modelling studies of inflammatory signalling pathway: a repurposing study.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Dr. Babasaheb Ambedkar Technological University, Lonere, Raigad, 402103, India.
Acute lung injury i.e. ALI and its serious form acute respiratory distress syndrome (ARDS) are incurable medical conditions associated with significant global mortality and morbidity.
View Article and Find Full Text PDFIndependent prognostic value of lipocalin-2 in congenital heart disease-associated pulmonary artery hypertension.
World J Cardiol
December 2024
Department of Tumor and Immunology, Beijing Pediatric Research Institute, Beijing Children's Hospital, Capital Medical University, National Center for Children's Health, Beijing 100045, China.
Background: Timely and accurate evaluation of the patient's pulmonary arterial pressure (PAP) is of great significance for the treatment of congenital heart disease. Currently, there is no non-invasive gold standard method for evaluating PAP.
Aim: To assess the prognostic value of lipocalin-2 (LCN2) in relation to PAP in patients with congenital heart disease associated with pulmonary artery hypertension.
Sodium valproate reverses aortic hypercontractility in acute myocardial infarction in rabbits.
Eur J Pharmacol
February 2025
Department of Physiology, School of Medicine, University of Valencia, Spain; Institute of Health Research INCLIVA, Valencia, Spain; Center for Biomedical Research Network on Cardiovascular Diseases (CIBER-CV), Madrid, Spain. Electronic address:
Sympathetic nervous system (SNS), endothelin 1 (ET-1) and angiotensin II (Ang II) are involved in the pathophysiology of acute myocardial infarction (AMI). Valproic acid (VPA) is under study for the treatment against AMI due to its beneficial cardiac effects. However, the vascular effects of VPA on the activation of the SNS, ET-1 and Ang II after AMI are not fully studied.
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