Glutamic acids, antitumor activities

Being the first poly(glutamic acid) conjugate tested in clinical trials, paclitaxel conjugate of poly(glutamic acid) (CT-2103) was observed to have superior antitumor activity to free paclitaxel. In preclinical studies, it was evidenced that the whole conjugate extravasated to the tumor site and the drug was released extracellularly in... 

Rosowski, A., Eorsch, R. A., Freisheim, J. H., Moran, R. G., Wick, M. Methotrexate analogues. 19. Replacement of the glutamate side chain in classical antifolates by L-homocysteic acid and L-cysteic acid effect on enzyme inhibition and antitumor activity. J. Med. Chem. 1984,27, 600-604. 

Regarding the pharmacological effects of theanine, previous reports have indicated a reduction in blood pressure in spontaneously hypertensive rats, a relief from convulsions induced by caffeine, and an influence on the brain levels of norepinephrine, serotonin, 5-hydroxyindoleacetic acid, and dopamine. Moreover, oral intake of theanine results in the generation of a-electric waves in the occipital and parietal regions of the human brain Theanine-induced inhibition of glutamate transporter enhances the activity of an antitumor agent. It increased doxorubicin (DOX)-induced antitumor activity, and confirmed that this action contributed to the increase in the DOX concentration in a tumor with inhibition of the DOX efflux from tumor cells. ... 

Retinoic acid inhibits estrogen sulfotransferase, glutamate dehyrogenase, metaplasia shows antitumor activity. (The sufflx metaplasia means develc ment.)... 

Wallace. 1999. Antitumor activity ofPoly(L-glutamic acid)-Paclitaxel on syngeneic and xenografted tumours, Clin Cancer Res 5 891-897. 

Bhatt, R. L., de Vries, E,Tulinsky, J, Bellamy, G., Baker, B., Singer, J. W. and Klein, P. (2003) Synthesis and in vivo antitumor activity of poly(L-glutamic acid) conjugates of 20(S)-camptothecin. J Med Chem, 46,190-193. 

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