SCH 900271
SCH 900271 is a pharmacological compound of significant interest in the field of medicine and biochemistry. It is a potent and selective inhibitor of the enzyme glycogen synthase kinase 3 (GSK-3), which plays a crucial role in cellular processes such as glycogen metabolism, cell division, and cell differentiation.
History
The compound SCH 900271 was first synthesized and characterized by scientists at Schering-Plough, a pharmaceutical company now part of Merck & Co.. The development of this compound was part of a broader effort to discover and develop novel inhibitors of GSK-3, a key target in the treatment of several diseases, including Alzheimer's disease, bipolar disorder, and diabetes.
Pharmacology
SCH 900271 is a potent inhibitor of GSK-3, with a half-maximal inhibitory concentration (IC50) in the nanomolar range. It acts by binding to the ATP-binding pocket of the enzyme, thereby preventing the phosphorylation of its substrates. This leads to alterations in various cellular processes, including glycogen metabolism, cell division, and cell differentiation.
Clinical significance
Due to its potent inhibitory activity against GSK-3, SCH 900271 has potential therapeutic applications in several diseases. For instance, it could be used in the treatment of Alzheimer's disease, where GSK-3 is known to contribute to the formation of neurofibrillary tangles, one of the hallmarks of the disease. Similarly, it could be used in the treatment of bipolar disorder, where GSK-3 has been implicated in the pathophysiology of the disease. Finally, it could be used in the treatment of diabetes, where GSK-3 is involved in the regulation of glucose metabolism.
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Contributors: Prab R. Tumpati, MD