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Effective Treatment With Oral Propranolol for Congenital Intracranial Hemangioma in a Neonate: A Case Report and Literature Review.
Cureus
December 2024
Department of Pediatrics, The Jikei University School of Medicine, Tokyo, JPN.
Congenital intracranial hemangiomas are rare benign vascular tumors that develop before birth. Although various treatments, including surgery, steroids, interferon-α, thalidomide, bevacizumab, or propranolol, have been reported, no standard therapy has been established. We report the case of a neonate with congenital intracranial hemangioma and central nervous system symptoms requiring therapeutic intervention.
View Article and Find Full Text PDFEvaluation of Cereblon-Directing Warheads for the Development of Orally Bioavailable PROTACs.
J Med Chem
January 2025
Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
PROTACs usually occupy physicochemical space outside the one defined by classical drug-like molecules, which often presents considerable challenges in their optimization and development for oral administration. We have previously reported phenyl glutarimide (PG)-based BET PROTAC SJ995973, with improved overall degradation and antiproliferative activities compared to its direct thalidomide-based analogue dBET1, but similarly poor pharmacokinetic profile. To further demonstrate the PG utility, we describe here optimization efforts that led to the discovery of an orally bioavailable BET-PROTAC SJ44236 (), and results of a comprehensive comparative study with analogues containing alternative CRBN-directing warheads.
View Article and Find Full Text PDFSuccessful Treatment of a Case of Scleromyxedema With Intravenous Immunoglobulin and Thalidomide and a Two-and-a-Half-Year Follow-Up.
Australas J Dermatol
January 2025
Department of Dermatology and Venereology, All India Institute of Medical Sciences (AIIMS), Bhubaneswar, India.
Inhalation of crystalline silica particles causes silicosis, which is a severe inflammatory lung disease that is associated with granulomatous and fibrotic responses. We investigated whether silica-induced silicosis might promote airway hyperreactivity (AHR) and the role of TNF-α and thalidomide in this process. Mice received an intranasal instillation of silica particles (1.
View Article and Find Full Text PDFMechanisms and pharmacotherapy of cancer cachexia-associated anorexia.
Pharmacol Res Perspect
February 2025
Department of Cardiology and Pneumology, University of Göttingen Medical Center, Göttingen, Germany.
Cachexia is a multifactorial metabolic syndrome characterized by weight and skeletal muscle loss caused by underlying illnesses such as cancer, heart failure, and renal failure. Inflammation, insulin resistance, increased muscle protein degradation, decreased food intake, and anorexia are the primary pathophysiological drivers of cachexia. Cachexia causes physical deterioration and functional impairment, loss of quality of life, lower response to active treatment, and ultimately morbidity and mortality, while the difficulties in tackling cachexia in its advanced phases and the heterogeneity of the syndrome among patients require an individualized and multidisciplinary approach from an early stage.
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