Overexpression test

Intracellular single-chain mAbs are supposed to prevent membrane localization of the receptors. Antireceptor mAbs conjugated to radionucleides, or to prodrugs, are tested as well, and DNA vaccines may induce an active immune response against RTK overexpressing tumors. 

Bcl-2 is one of the many factors that control apoptosis, and overexpression of Bcl-2 has been observed in many different cancers. A homology model of Bcl-2 was derived from the NMR 3D structure of the Bcl-XL complex with a Bak BH3 peptide. This model served to search the NCI 3D database of 206,876 organic compounds for potential Bcl-2 inhibitors, which bind to the Bak BH3 binding site of Bcl-2. Full conformational flexibility of the ligands was taken into account in the program DOCK. Thirty-five potential inhibitors were tested, and seven of them had IC50 values from 1.6 to W.OpM. One of... 

An important validation of the mice that overexpress human mutant 3APP as a platform for testing therapeutics targeting 3-peptide deposition has been provided by the Elan company, using their PDAPP mouse [146]. Immunization of the mice, either at an early age or after plaques had formed, resulted in clearance of immunoreactive plaques and peptide from the subjects brains. Although the elucidation of the mechanism explaining... 

MIC > 64 ig/ml) against other bacterial species tested. MIC values were elevated in a Murl overexpressing strain but unaffected by overexpressing H. pylori efflux systems [88]. 

Figure 4. Therapeutic strategies to counteract CBP loss of function. CBP loss of function leads to a decrease in histone acetylation levels as well as a decrease in CBP-dependent transcription. Two main approaches can be tested to reverse diis process either resetting HAT functionality or resetting global acetylation levels widi die use of HDAC inhibitors. Whereas both strategies would increase histone acetylation levels, HDAC inhibition would act on a broad range of genes, while CBP activation (overexpression or by a pharmacological approach) would specifically target bodi CBP-dependent histone acetylation and transcription. The structure of some of the HDACi that have been tested in different models, such as small fatty acids and hydroxamic acids, are represented in the boxes...

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