| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T87166 | ||||
| Target Name | Glucokinase | ||||
| Target Type | Clinical Trial |
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| Action against Disease Model | Lonidamine | Lonidamine is an anticancer drug that has its primary action on cellular metabolism rather than cell division. Since lonidamine is not effective in all t uMor cells, we have tested it in two h uMan-t uMor cell culture lines: MOLT-4, a T-leukemia and U-87 MG, a glioma. Lonidamine exposure of MOLT-4 cells at 50 micrograms/mL and pH 6.7 disrupted the mitochondria within 1 h of treatment. The mitochondria were swollen and the cristae were disrupted. When the treated cells were re-incubated in fresh medi uM at pH 7.4 the mitochondria rapidly returned to their normal morphology. | [553126] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | To investigate the functional and structural renal changes in a long-term liver-specific glucokinase (gck) knockout mouse, a model was developed of maturity-onset diabetes of the young (MODY2). Hemizygous gck knockout mice, gck(w/-) groups, were compared at 6, 10, and 14 months with their age-matched normal littermates, gck(w/w) groups. To examine changes, we compared body weight, fasting blood glucose, ser uM insulin, and creatinine levels, as well as 24-h urine samples that were collected for urine vol uMe and protein analysis between the 2 groups. Renal tissues were collected and stained with hemotoxylin-eosin and periodic-acid Schiff for light microscopic observation. The expression of renal transforming growth factor |?? (TGF-|??) was determined by Western blot.Our results show that fasting blood glucose levels were significantly higher in gck(w/-) mice compared with gck(w/w) mice (P < 0.01) for all age groups. Compared with age-matched gck(w/w) mice, 10-month old gck(w/-) mice have significantly elevated body weights (P < 0.01) and protein contents (P < 0.001). A gradual increase in mesangial matrix and a thickening of the glomerular basement membrane was observed in gck(w/-) mice at 10 and 14 months. The levels of renal TGF-|?? expression are increasing in both gck(w/-) and gck(w/w) mice. | [553126] | |||
| References | |||||
| Ref 553126 | Morphological effects of lonidamine on two human-tumor cell culture lines. Scanning Microsc. 1989 Jun;3(2):681-91; discussion 691-3. | ||||
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