Inside Perspective of the Synthetic and Computational Toolbox of JAK Inhibitors: Recent Updates
Copyright policy )Inside Perspective of the Synthetic and Computational Toolbox of JAK Inhibitors: Recent Updates
The mechanisms of inflammation and cancer are intertwined by complex networks of signaling pathways. Dysregulations in the Janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway underlie several pathogenic conditions related to chronic inflammatory states, autoimmune diseases and cancer. Historically, the potential application of JAK inhibition has been thoroughly explored, thus triggering an escalation of favorable results in this field. So far, five JAK inhibitors have been approved by the Food and Drug Administration (FDA) for the treatment of different diseases. Considering the complexity of JAK-depending processes and their involvement in multiple disorders, JAK inhibitors are the perfect candidates for drug repurposing and for the assessment of multitarget strategies. Herein we reviewed the recent progress concerning JAK inhibition, including the innovations provided by the release of JAKs crystal structures and the improvement of synthetic strategies aimed to simplify of the industrial scale-up.
- Magna Graecia University Italy
- University of Cagliari Italy
Protein Conformation, Anti-Inflammatory Agents, Organic chemistry, Antineoplastic Agents, Review, Autoimmune Diseases, QD241-441, Piperidines, Neoplasms, Nitriles, cancer, synthetic strategies, Humans, Janus Kinase Inhibitors, multitarget, Drug Approval, Janus Kinases, Inflammation, tofacitinib, United States Food and Drug Administration, Cancer; Inflammation; Janus kinase (JAK); Multitarget; Ruxolitinib; Synthetic strategies; Tofacitinib, Janus kinase (JAK), United States, Pyrimidines, inflammation, Drug Design, Pyrazoles, Protein Binding
Protein Conformation, Anti-Inflammatory Agents, Organic chemistry, Antineoplastic Agents, Review, Autoimmune Diseases, QD241-441, Piperidines, Neoplasms, Nitriles, cancer, synthetic strategies, Humans, Janus Kinase Inhibitors, multitarget, Drug Approval, Janus Kinases, Inflammation, tofacitinib, United States Food and Drug Administration, Cancer; Inflammation; Janus kinase (JAK); Multitarget; Ruxolitinib; Synthetic strategies; Tofacitinib, Janus kinase (JAK), United States, Pyrimidines, inflammation, Drug Design, Pyrazoles, Protein Binding
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