نتایج جستجو برای: 0.77 and 1.16

تعداد نتایج: 16829454  

2012
John L. Chunta Kerry S. Vistisen Zeinab Yazdi Rod D. Braun

OBJECTIVE Since tumor radiation response is oxygen-dependent, radiosensitivity can be enhanced by increasing tumor oxygenation. Theoretically, inhibiting cellular oxygen consumption is the most efficient way to increase oxygen levels. The cationic, rhodacyanine dye-analog MKT-077 inhibits mitochondrial respiration and could be an effective metabolic inhibitor. However, the relationship between ...

Journal: :Cancer research 1996
K Koya Y Li H Wang T Ukai N Tatsuta M Kawakami Shishido L B Chen

MKT-077 (formerly known as FJ-776) is a newly synthesized, highly water-soluble ( > 200 mg/ml) rhodacyanine dye that exhibits significant antitumor activity in a variety of model systems. In culture, MKT-077 inhibits the growth of five human cancer cell lines (colon carcinoma CX-1, breast carcinoma MCF-7, pancreatic carcinoma (CRL 1420, bladder transitional cell carcinoma EJ, and melanoma LOX) ...

Journal: :Cancer research 1996
J S Modica-Napolitano K Koya E Weisberg B T Brunelli Y Li L B Chen

We investigated the mitochondrial toxicity of the lipophilic cation, MKT-077, and the role of mitochondria in selective malignant cell killing by this compound by examining the effect of MKT-077 on mitochondrial structure and function in treated cells and in isolated organelles. Results of this study demonstrate changes in mitochondrial ultrastructure that are induced by MKT-077 treatment in ca...

Journal: :Cancer research 2002
Renu Wadhwa Lorel Colgin Tomoko Yaguchi Kazunari Taira Roger R Reddel Sunil C Kaul

MKT-077, a cationic rhodacyanine dye analogue, causes selective toxicity to cancer cells. Its cellular targets elucidated thus far include oncogenic Ras, F-actin, mortalin (hmot-2)/mthsp70, and telomerase. Here we report that MKT-077 causes growth arrest of cancer cells in culture independent of their Ras, p53, or telomerase status. Telomerase activity is inhibited in vitro by MKT-077 in the te...

2015
Dmytro Starenki Jong-In Park

BACKGROUND Medullary thyroid carcinoma (MTC) is a neuroendocrine tumor mainly caused by mutations in the rearranged during transfection (RET) proto-oncogene. Not all patients with progressive MTC respond to current therapy inhibiting RET, demanding additional therapeutic strategies. We recently demonstrated that disrupting mitochondrial metabolism using a mitochondria-targeted agent or by deple...

Journal: :Cancer research 2000
R Wadhwa T Sugihara A Yoshida H Nomura R R Reddel R Simpson H Maruta S C Kaul

MKT-077, a cationic rhodacyanine dye analogue has been under preclinical cancer therapeutical trials because of its selective toxicity to cancer cells. Its cellular targets and mechanism of action remain poorly understood. Here we report that MKT-077 binds to an hsp70 family member, mortalin (mot-2), and abrogates its interactions with the tumor suppressor protein, p53. In cancer cells, but not...

Journal: :Cancer research 1996
E L Weisberg K Koya J Modica-Napolitano Y Li L B Chen

The effects of in vivo administration of a pharmacologically toxic dose of the lipophilic cationic compound, MKT-077, were investigated in selected vital organs of the rat. MKT-077 (15 mg/kg body weight), administered by bolus i.v. injection every day for 5 days, did not detectably influence rat heart and kidney mitochondrial respiration. Although the same dosage of MKT-077 significantly decrea...

Journal: :Clinical cancer research : an official journal of the American Association for Cancer Research 2000
C D Britten E K Rowinsky S D Baker G R Weiss L Smith J Stephenson M Rothenberg L Smetzer J Cramer W Collins D D Von Hoff S G Eckhardt

This Phase I study was performed to evaluate the tolerability and pharmacokinetic behavior of MKT-077, a water soluble rhodacyanine dye analogue, which partitions into tumor cell mitochondria where it is thought to act as a metabolic poison, leading to G1 arrest and apoptosis. Thirteen patients with advanced solid malignancies were treated with MKT-077 administered as a 30-min i.v. infusion wee...

Journal: :Pediatric Critical Care Medicine 2018

2012
John Koren Yoshinari Miyata Janine Kiray John C. O'Leary Lana Nguyen Jianping Guo Laura J. Blair Xiokai Li Umesh K. Jinwal Jin Q. Cheng Jason E. Gestwicki Chad A. Dickey

MKT-077, a rhodacyanine dye, was shown to produce cancer specific cell death. However, complications prevented the use of this compound beyond clinical trials. Here we describe YM-1, a derivative of MKT-077. We found that YM-1 was more cytotoxic and localized differently than MKT-077. YM-1 demonstrated this cytotoxicity across multiple cancer cell lines. This toxicity was limited to cancer cell...

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