| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T69085 | ||||
| Target Name | Transcription factor AP-1 | ||||
| Target Type | Discontinued |
||||
| Drug Potency against Target | TWS-119 | Drug Info | IC50 = 15000 nM | [527964] | |
| Action against Disease Model | T-5224 | The in vivo ED50 of T-5224 corresponds to a Cmax of 0.03-0.5 uM, a figure that is substantially lower than the in vitro IC50 of ~10 uM. | [552835] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | Genetically modified mice have provided important insights into the biological functions of the dimeric transcription factor complex AP-1. Extensive analyses of mice and cells with genetically modified Fos or Jun proteins provide novel insights into the physiological functions of AP-1 proteins. Using knock-out strategies it was found that some components, such as c-Fos, FosBand JunD are dispensable, whereas others, like c-Jun, JunB and Fra-1 are essential in embryonic development and/or in the adult organism. Besides the specific roles of AP-1 proteins in developmental processes, we are beginning to obtain a better molecular understanding of the cell-context dependent function of AP-1 in cell proliferation and apoptosis, in bone biology as well as in multistep t uMorigenesis. | [527964] | |||
| References | |||||
| Ref 527964 | Nat Chem Biol. 2005 Jul;1(2):74-84.Diversity-oriented synthesis: exploring the intersections between chemistry and biology. | ||||
| Ref 552835 | Treatment of arthritis with a selective inhibitor of c-Fos/activator protein-1. Nat Biotechnol. 2008 Jul;26(7):817-23. doi: 10.1038/nbt1412. Epub 2008 Jun 29. | ||||
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