F0604 | Mitochondrial protein translation
| Compound |
Dose |
Time |
Species |
Model |
Method |
Action |
Result |
Positive criterion |
Reference |
| tetracyclines |
|
|
|
|
|
decrease |
Positive |
|
307 |
| Zidovudine |
|
|
|
|
|
decrease |
Positive |
|
307 |
| Acyclovir |
|
|
|
|
|
decrease |
Positive |
|
307 |
| Ganciclovir |
|
|
|
|
|
decrease |
Positive |
|
307 |
| Zalcitabine |
|
|
|
|
|
decrease |
Positive |
|
307 |
| Linezolid |
16 ± 2 μM |
|
|
Isolated rat heart mitochondria |
Mitochondrial protein synthesis (MPS) assay with [35S]methionine |
|
Positive |
IC50 |
282 |
| eperezolid |
9.5 ± 1.5 μM |
|
|
Isolated rat heart mitochondria |
Mitochondrial protein synthesis (MPS) assay with [35S]methionine |
|
Positive |
IC50 |
282 |
| eperezolid |
4.2 ± 0.4 μM |
|
rat |
Isolated liver mitochondria |
Mitochondrial protein synthesis assay (The incorporation of [35S]methionine into mitochondrial protein was determined by a filter paper disk assay ) |
|
Positive |
IC50 |
281 |
| Chloramphenicol |
9.8 ± 0.5 μM |
|
rat |
liver mitochondria |
Mitochondrial protein synthesis assay (The incorporation of [35S]methionine into mitochondrial protein was determined by a filter paper disk assay ) |
|
Positive |
IC50 |
281 |
| tetracyclines |
2.1 ± 0.5 μM |
|
rat |
liver mitochondria |
Mitochondrial protein synthesis assay (The incorporation of [35S]methionine into mitochondrial protein was determined by a filter paper disk assay ) |
|
Positive |
IC50 |
281 |
| Linezolid |
12.8 ± 2.8 μM |
|
rat |
liver mitochondria |
Mitochondrial protein synthesis assay (The incorporation of [35S]methionine into mitochondrial protein was determined by a filter paper disk assay ) |
|
Positive |
IC50 |
281 |
| Linezolid |
|
|
|
|
haplo-insufficiency profiling (HIP), a well-validated chemical genomics platform developed in the yeast S. Cerevisiae. |
inhibitor |
Positive |
|
288 |
| doxycycline |
|
|
|
143B osteosarcoma cells |
|
inhibitor |
Positive |
|
285 |
| Chloramphenicol |
|
|
|
|
haplo-insufficiency profiling (HIP), a well-validated chemical genomics platform developed in the yeast S. Cerevisiae. |
inhibitor |
Positive |
|
288 |
| Linezolid |
|
|
|
|
|
|
Positive |
|
197 |
| tigecycline |
|
|
|
|
haplo-insufficiency profiling (HIP), a well-validated chemical genomics platform developed in the yeast S. Cerevisiae. |
inhibitor |
Positive |
|
288 |
| tigecycline |
2.5-10μM |
48hr |
|
TEX, OCI-AML2, and two AML patients' cells |
weatern blot (protein levels of Cox-1, Cox-2, Cox-4, Grp78, XIAP, Actin, and tubulin) |
inhibitor |
Positive |
|
288 |
