RIPK1 inhibitors: A key to unlocking the potential of necroptosis in drug development

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 265, P. 116123 - 116123

Published: Jan. 3, 2024

Language: Английский

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How to Use the Cuprizone Model to Study De- and Remyelination

International Journal of Molecular Sciences, Journal Year: 2024, Volume and Issue: 25(3), P. 1445 - 1445

Published: Jan. 24, 2024

Multiple sclerosis (MS) is an autoimmune and inflammatory disorder affecting the central nervous system whose cause still largely unknown. Oligodendrocyte degeneration results in demyelination of axons, which can eventually be repaired by a mechanism called remyelination. Prevention pharmacological support remyelination are two promising strategies to ameliorate disease progression MS patients. The cuprizone model commonly employed investigate oligodendrocyte mechanisms or explore pathways. During last decades, several different protocols have been applied, all their pros cons. This article intends offer guidance for conducting pre-clinical trials using mice, focusing on discovering new treatment approaches prevent enhance

Language: Английский

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Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors as Potential Treatment for Several Inflammatory and Neurodegenerative Diseases

ACS Medicinal Chemistry Letters, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 27, 2025

The invention in this patent application relates to 2-amino-[1,2,4]triazolo[1,5-a]pyridin derivatives represented generally herein as formula 1. These compounds have activities receptor-interacting protein kinase 1 (RIPK1) inhibitors and may potentially provide treatment and/or prophylaxis of inflammatory neurodegenerative diseases associated with aberrant RIPK1 activity such ulcerative colitis, Crohn's disease, psoriasis, NASH, heart failure, multiple sclerosis, amyotrophic lateral sclerosis (ALS), Alzheimer's disease.

Language: Английский

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1,2,3-Triazole appended Schiff base functionalized silanes: A colorimetric sensor of Al (III) and a potent inhibitor of butyrylcholinesterase in Alzheimer’s diseases via molecular docking

Inorganica Chimica Acta, Journal Year: 2024, Volume and Issue: 572, P. 122269 - 122269

Published: July 20, 2024

Language: Английский

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Serum RIPK1, Acute Lung Injury, and Outcomes in Severe Traumatic Brain Injury: A Multicenter Prospective Study

Therapeutics and Clinical Risk Management, Journal Year: 2025, Volume and Issue: Volume 21, P. 385 - 405

Published: March 1, 2025

Receptor-interacting protein kinase-1 (RIPK1), a regulator of necroptosis, is involved in acute brain injury and lung (ALI). Here, serum RIPK1 levels were measured after severe traumatic (sTBI), with an endeavor to unveil its prognostic implications mediation effects ALI. In this multicenter prospective study, gauged 100 healthy individuals 158 sTBI patients need decompressive craniectomy for herniation. The collected materials encompassed the Glasgow Coma Scale (GCS), pupil enlargement status, basal cisternal shapes, ALI, etc. extended outcome scale (GOSE) was employed estimating neurological impairments at posttraumatic 180-day mark. Multifactorial analytical methods applied assess relevancies. Patients, as opposed controls, had markedly raised levels, even substantially higher those lower GCS scores, bilateral or obliterated cisterns. Using restricted cubic spline, linearly related occurrent risks four variables interest, that death, overall survival, poor prognosis (GOSE scores 1-4) independently predicted these variables. noninteractional age, sex, hypertension, diabetes, smoking alcohol habits terms association exhibited high discriminatory efficiency under receiver operating characteristic curve. via partial by associated death patients. Elevated may be highly trauma severity, outcomes ALI; ALI partially explains links between prognosis, substantializing serological predictor good prospect sTBI.

Language: Английский

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Design, synthesis, and biological evaluation of RIPK1-targeting PROTACs

Molecular Diversity, Journal Year: 2025, Volume and Issue: unknown

Published: March 24, 2025

Language: Английский

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Novel Isoxazolidines as RIPK1 Inhibitors for Treating Alzheimer’s Disease, Multiple Sclerosis, and Amyotrophic Lateral Sclerosis

ACS Medicinal Chemistry Letters, Journal Year: 2024, Volume and Issue: 15(4), P. 447 - 448

Published: April 2, 2024

Provided herein are novel isoxazolidines as RIPK1 inhibitors, pharmaceutical compositions, use of such compounds in treating Alzheimer's disease, multiple sclerosis, and amyotrophic lateral sclerosis (ALS), processes for preparing compounds.

Language: Английский

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Recent advancements in the understanding of the alterations in mitochondrial biogenesis in Alzheimer’s disease

Molecular Biology Reports, Journal Year: 2025, Volume and Issue: 52(1)

Published: Jan. 29, 2025

Language: Английский

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Novel Fused Triazole Compounds as RIPK1 Inhibitors for Treating Neurodegenerative, Autoimmune, and Inflammatory Diseases

ACS Medicinal Chemistry Letters, Journal Year: 2024, Volume and Issue: 15(2), P. 177 - 178

Published: Jan. 26, 2024

Provided herein are novel fused triazole compounds as RIPK1 inhibitors, pharmaceutical compositions, use of such in treating neurodegenerative, autoimmune, and inflammatory diseases, processes for preparing compounds.

Language: Английский

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The role of RIPK1 in chronic obstructive pulmonary disease

Drug Discovery Today, Journal Year: 2024, Volume and Issue: 29(7), P. 104020 - 104020

Published: May 11, 2024

Language: Английский

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