RESUMEN
This article describes the synthesis and photophysical properties of a series of BODIPY photosensitisers that feature tellurophene motifs appended at the boron centre. These compounds were obtained via nucleophilic substitution of various F-BODIPYs with lithiated tellurophene. The synthetic scope, photophysical characteristics and photosensitisation properties are discussed. Structural modifications around the BODIPY core resulted in an eight-fold improvement in light IC50 values compared to previous designs.
RESUMEN
Chronic graft-versus-host disease (cGvHD) is a multisystem disease that is diagnosed in up to 70% of patients following allogeneic hematopoietic cell transplantation. In cGvHD, the donor immune cells attack the patient's cells, resulting in inflammation and fibrosis in multiple tissues. cGvHD can affect almost any organ and is the major cause of morbidity and mortality in transplant survivors. Rho-associated coiled-coil-containing protein kinase (ROCK) is a signaling pathway that modulates inflammatory response and fibrotic processes and is dysregulated in autoimmune disorders. Many inhibitors targeting the ROCK pathway have been studied, but most lack isoform selectivity resulting in dose-limiting effects. Belumosudil mesylate is a selective oral ROCK2 inhibitor that has demonstrated safety and efficacy for cGvHD. It has been approved by the U.S. Food and Drug Administration (FDA) for the treatment of adult and pediatric patients 12 years and older with cGvHD after failure of at least two prior lines of systemic therapy, becoming the first and only approved therapy targeting ROCK2. This review examines the preclinical and clinical studies leading to the first approval of the novel drug belumosudil for cGvHD.
Asunto(s)
Enfermedad Injerto contra Huésped , Trasplante de Células Madre Hematopoyéticas , Acetamidas/uso terapéutico , Adulto , Niño , Enfermedad Crónica , Enfermedad Injerto contra Huésped/tratamiento farmacológico , Trasplante de Células Madre Hematopoyéticas/efectos adversos , Humanos , Quinasas Asociadas a rhoRESUMEN
Oligodendrogliomas are slow-growing tumors that account for 15-20% of gliomas. This case report describes the case of an adult male patient diagnosed initially with tumefactive demyelination and multiple sclerosis, which was subsequently found to be a well-differentiated low-grade oligodendroglioma. This case emphasizes the importance of timely diagnosis in oligodendrogliomas and other brain tumors for the prompt initiation of appropriate therapy, to minimize the likelihood of disease progression, ensure symptom management and escalation of unnecessary treatments for multiple sclerosis.