| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T76059 | ||||
| Target Name | FK506-binding protein 1A | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | GPI-1485 | Drug Info | IC50 = 5 nM | [552770] | |
| Action against Disease Model | GPI-1485 | Oral dosing in animals with GPI 1485 stimulates significant neuroprotective and neuroregenerative activity in preclinical models of post-prostatectom erectile dysfunction. Treatment with GPI 1485 at the time of injury maintained intracavernosal pressure at near normal levels for up to 28 days after injury. In addition, delayed treatment with GPI 1485 up to seven days after the peripheral nerve injury procedure promoted significant restoration of function, restoring intracavernosal pressure to between 90%-100% of normal levels when measured at one month after injury. | Drug Info | ||
| The Effect of Target Knockout, Knockdown or Genetic Variations | To assess the effects of FKBP12 deficiency on muscle injury and recovery, we measured anterior crural muscle (tibialis anterior and extensor digitor uM longus muscles) strength in skeletal muscle-specific FKBP12-deficient and wild-type (WT) mice before and after a single bout of 150 eccentric contractions, as well as before and after the performance of six injury bouts. Histological damage of the tibialis anterior muscle was assessed after injury. Body weight and peak isometric and eccentric torques were lower in FKBP12-deficient mice compared with WT mice. There were nodifferences between FKBP12-deficient and WT mice in preinjury peak isometric and eccentric torques when normalized to body weight, and no differences in the relative decreases in eccentric torque with a single or multiple injury bouts. After a single injury bout, FKBP12-deficient mice had less initial strength deficits and recovered faster (especially females) than WT mice, despite no differencesin the degree of histological damage. After multiple injury bouts, FKBP12-deficient mice recovered muscle strength faster than WT mice and exhibited significantly less histological muscle damage thanWT mice. In s uMmary, FKBP12 deficiency results in less initial strength deficits and enhanced recovery from single (especially females) and repeated bouts of injury than WT mice | [552770] | |||
| References | |||||
| Ref 552770 | Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities. Proc Natl Acad Sci U S A. 2008 Jan 8;105(1):33-8. Epub 2007 Dec 27. | ||||
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