Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines

Purpose: Farnesyltransferase (FTase) is a zinc-dependent enzyme that adds a farnesyl group to the Ras proteins. L778, 123 is a potent peptidomimetic imidazole-containing FTase inhibitor. Methods: L778123 was synthesized according to known methods and evaluated alone and in combination with doxorubic...

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Main Authors: Ali Abdollahi (Author), Davoud Asgari (Author), Simin Sharifi (Author), Soodabeh Davaran (Author), Saeed Ghasemi (Author), Javid Shahbazi Mojarrad (Author)
Format: Book
Published: Tabriz University of Medical Sciences, 2013-02-01T00:00:00Z.
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100 1 0 |a Ali Abdollahi  |e author 
700 1 0 |a Davoud Asgari  |e author 
700 1 0 |a Simin Sharifi  |e author 
700 1 0 |a Soodabeh Davaran  |e author 
700 1 0 |a Saeed Ghasemi  |e author 
700 1 0 |a Javid Shahbazi Mojarrad  |e author 
245 0 0 |a Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines 
260 |b Tabriz University of Medical Sciences,   |c 2013-02-01T00:00:00Z. 
500 |a 10.5681/apb.2013.012 
500 |a 2228-5881 
500 |a 2251-7308 
520 |a Purpose: Farnesyltransferase (FTase) is a zinc-dependent enzyme that adds a farnesyl group to the Ras proteins. L778, 123 is a potent peptidomimetic imidazole-containing FTase inhibitor. Methods: L778123 was synthesized according to known methods and evaluated alone and in combination with doxorubicin against A549 (adenocarcinomic human alveolar basal epithelial cells) and HT29 (human colonic adenocarcinoma) cell lines by MTT assay. Results: L778123 showed weak cytotoxic activity with IC50 of 100 and 125 for A549 and HT-29 cell lines, respectively. The combination of doxorubicin and L778123 can decrease IC50 of doxorubicin in both cell lines significantly. Conclusion: It can be concluded that L778, 123 can be a good agent for combination therapy. 
546 |a EN 
690 |a Farnesyltransferase inhibitor 
690 |a MTT assay 
690 |a Combination therapy 
690 |a L-778123 
690 |a Therapeutics. Pharmacology 
690 |a RM1-950 
655 7 |a article  |2 local 
786 0 |n Advanced Pharmaceutical Bulletin, Vol 3, Iss 1, Pp 73-77 (2013) 
787 0 |n http://journals.tbzmed.ac.ir/PDF/APB/Manuscript/APB-3-73.pdf 
787 0 |n https://doaj.org/toc/2228-5881 
787 0 |n https://doaj.org/toc/2251-7308 
856 4 1 |u https://doaj.org/article/8bb975bed40f489980a527d8799a1ca1  |z Connect to this object online.