Angiogenesis, blocking

Human explants induced angiogenesis in rat cornea. Blocked by IL-8 antibodies. 

Brooks PC Stromblad S, Klemke R, et al. Antiintegrin alpha v Beta 3 blocks human breast cancer growth and angiogenesis in human skin. J Clin Investig 1995 96(4) 1815-1822. 

In addition, very recent work indicates that COX-2 may play a vital role in the regulation of angiogenesis associated with neoplastic tumor cells, hence COX-2 inhibitors may block the growth of blood vessels into developing tumors (56). Thus, according to epidemiological, clinical, and experimental data, COX-2 appears to be intimately related to the development and growth of some types of cancer, especially of colorectal cancer. 

Mechanism of Action-. A selective vascular endothelial growth factor (VEGF) antagonize that selectively binds and activates receptors located on the surface of vascular endothelial cells. Therapeutic Effect Blocks angiogenesis and vascular permeability and inflammation which contribute to the progression of the neovascular (wet) form of age-related macular degeneration (AMD). 

Borrelidin 1 has attracted attention because it inhibits angiogenesis, and so potentially blocks tumor growth, with an IC of 0.8 nM. Retrosynthetic analysis of 1 led the investigators to the prospective intermediates 2 and 3. To assemble these two fragments, they interatively deployed the elegant enantio- and diastereoselective intermolecular reductive ester aldol condensation that they had recently developed. This transformation is exemplified by the homologation of 4 to 6 catalyzed by the enantiomerically-pure Ir complex 5. 

As well as apoptosis, the p53 tumor suppressor gene causes DNA repair, blocks angiogenesis, and causes cell cycle arrest. As with oncogenes, tumor suppressor genes also have effects on cell cycle control. 

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