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1¡¢Irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. Irinotecan is a derivative of camptothecin. Irinotecan inhibits the action of topoisomerase I. Irinotecan prevents religation of the DNA strand by binding to topoisomerase I-DNA complex, and causes double-strand DNA breakage and cell death. 2¡¢Decitabine is indicated for treatment of patients with myelodysplastic syndrome (MDS). It is a chemical analogue of cytidine, a nucleoside present in DNA and RNA. Cells in the presence of Decitabine incorporate it into DNA during replication and RNA during transcription. The incorporation of Decitabine into DNA or RNA inhibits methyltransferase thereby causing demethylation in that sequence. This adversely affects the way that cell regulatory proteins are able to bind to the DNA/RNA substrate. 3¡¢Pimecrolimus is a chemical that is used to treat atopic dermatitis (eczema). Atopic dermatitis is a skin condition characterized by redness, itching, scaling and inflammation of the skin. The cause of atopic dermatitis is not known; however, scientists believe that it may be due to activation of the immune system by various environmental or emotional triggers. Scientists do not know exactly how pimecrolimus reduces the manifestations of atopic dermatitis, but pimecrolimus reduces the action of T-cells and mast cells which are part of the immune system and contribute to responses of the immune system. Pimecrolimus prevents the activation of T-cells by blocking the effects of chemicals (cytokines) released by the body that stimulate T-cells. Pimecrolimus also reduces the ability of mast cells to release chemicals that promote inflammation. 4¡¢Temsirolimus is an inhibitor of mTOR (mammalian target of rapamycin). Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor. 5¡¢Everolimus is a derivative of Rapamycin (sirolimus), and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor. It is currently used as an immunosuppressant to prevent rejection of organ transplants. In a similar fashion to other mTOR inhibitors Everolimus' effect is solely on the mTORC1 protein and not on the mTORC2 protein. |
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2Â¥2010-05-25 23:15:11
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ÎÒÖ»ÊÇÀ´Ñ§Ï°µÄ£¬Â¥Ö÷ºöÂÔÎÒ°É antineoplastic¿¹Ö×ÁöµÄ colorectal cancer´ó³¦°© camptothecinϲÊ÷¼î topoisomeraseÍØÆËÒ칹ø religationÖØÐÂÁ¬½Ó recombinantÖØ×é DNA strand DNAÁ´ myelodysplastic syndrome (MDS)¹ÇËèÔöÉúÒì³£×ÛºÏÕ÷£¬ÔÃû°×Ѫ²¡Ç°ÆÚpreleukemia cytidine°ûà×ठnucleosideºËÜÕ incorporateºÏ²¢¡¢²ô½ø replication¸´ÖÆ transcriptionת¼ methyltransferase¼×»ù×ªÒÆÃ¸ adversely affects²»ÀûÓ°Ïì regulatoryµ÷½Ú atopic dermatitisÒìλÐÔÆ¤·ôÑ× eczemaʪÕî Ì«ÍíÁË ¶¼ÊÇЩҩƷ¼ò½é |
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aloin(½ð±Ò+95):лл 2010-05-26 10:23:19
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