Published TCIMAIL newest issue No.197
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Protein Kinase Inhibitor: Indirubin
No.175(October 2017)
Indirubin (1) is an inhibitor of protein kinases (Table).1,2) According to a crystal structure study of CDK2 in complexation with indirubin derivatives has shown that 1 interacts with the ATP-binding site of the kinase.1) 1 also was reported to have high binding affinity with the aryl hydrocarbon receptor (AhR).3)
In DNCB-induced mice, 1 inhibited allergic contact dermatitis by regulating T helper mediated immune system.4)
CDK: cyclin-dependent kinase
DNCB: 1-chloro-2,4-dinitrobenzene
DNCB: 1-chloro-2,4-dinitrobenzene
References
- 1)Indirubin, the active constituent of a chinese antileukaemia medicine, inhibits cyclin-dependent kinases
- 2)Indirubins inhibit glycogen synthase kinase-3β and CDK5/P25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer’s disease
- 3)Indirubin and indigo are potent aryl hydrocarbon receptor ligands present in human urine
- 4)Indirubin, a purple 3,2- bisindole, inhibited allergic contact dermatitis via regulating T helper (Th)-mediated immune system in DNCB-induced model
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