Synthesis of CpM(CO)3-DAB and -PAMAM Dendrimer Conjugates and Preliminary Evaluation of Their Biological Activity

2015 ◽  
Vol 2015 (9) ◽  
pp. 1505-1510 ◽  
Author(s):  
Wanning Hu ◽  
Jan Hoyer ◽  
Ines Neundorf ◽  
Preshendren Govender ◽  
Gregory S. Smith ◽  
...  
Polymers ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 1422 ◽  
Author(s):  
Marcinkowska ◽  
Stanczyk ◽  
Janaszewska ◽  
Gajek ◽  
Ksiezak ◽  
...  

Taxanes are considered fundamental drugs in the treatment of breast cancer, but despite the similarities, docetaxel (doc) and paclitaxel (ptx) work differently. For this reason, it is interesting to identify mechanisms of antitumor activity of PAMAM dendrimer conjugates that carry docetaxel or paclitaxel and monoclonal antibody trastuzumab, specifically targeted to cells which overexpressed HER-2. For this purpose, the impact on the level of reactive oxygen species, the mitochondrial membrane potential, cell cycle distribution and the activity of caspases-3/7, -8 and -9 of PAMAM-doc-trastuzumab and PAMAM-ptx-trastuzumab conjugates was determined and compared with free docetaxel and paclitaxel toward HER-2-positive (SKBR-3) and negative (MCF-7) human breast cancer cell lines. Moreover, apoptosis and necrosis were studied using flow cytometry and confocal microscopy, respectively. Our studies show the complexity of the potential mechanism of cytotoxic action of PAMAM-drug-trastuzumab conjugates that should be sought as a resultant of oxidative stress, mitochondrial activation of the caspase cascade and the HER-2 receptor blockade.


2012 ◽  
Vol 13 (4) ◽  
pp. 982-991 ◽  
Author(s):  
Hong Zong ◽  
Thommey P. Thomas ◽  
Kyung-Hoon Lee ◽  
Ankur M. Desai ◽  
Ming-hsin Li ◽  
...  

2016 ◽  
Vol 14 (46) ◽  
pp. 10787-10798 ◽  
Author(s):  
David Mangan ◽  
Neasa McNabola ◽  
Emily H. Clark ◽  
Isabel Bermudez ◽  
Susan Wonnacott ◽  
...  

A new synthesis of mecamylamine allowed the preparation of analogues to probe biological activity.


2013 ◽  
Vol 10 (2) ◽  
pp. 606-618 ◽  
Author(s):  
Alexandra Vetter ◽  
Kulpreet S. Virdi ◽  
Sigrid Espenlaub ◽  
Wolfgang Rödl ◽  
Ernst Wagner ◽  
...  

Sensors ◽  
2009 ◽  
Vol 9 (8) ◽  
pp. 6346-6361 ◽  
Author(s):  
Hidetoshi Arima ◽  
Keiichi Motoyama

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2017 ◽  
Author(s):  
Roman Komor ◽  
Gabriela Pastuch-Gawolek ◽  
Ewelina Krol ◽  
Wieslaw Szeja

Herein we present the methodology for obtaining glycosyltransferase inhibitors, analogues of natural enzyme substrates of donor-type: UDP-glucose and UDP-galactose. The synthesis concerned glycoconjugates, nucleoside analogues containing an acyclic ribose mimetic linked to a uracil moiety in their structure. The biological activity of the synthesised compounds was determined on the basis of their ability to inhibit the model enzyme action of β-1,4-galactosyltransferase from bovine milk. The obtained results allowed to expand and supplement the existing library of synthetic compounds that are able to regulate the biological activity of enzymes from the GT class.


2016 ◽  
Vol 2016 (34) ◽  
pp. 5667-5677
Author(s):  
Koichi Narita ◽  
Yuya Katoh ◽  
Ken-ichi Ojima ◽  
Singo Dan ◽  
Takao Yamori ◽  
...  

2010 ◽  
Vol 21 (2) ◽  
pp. 372-384 ◽  
Author(s):  
Dilip K. Tosh ◽  
Lena S. Yoo ◽  
Moshe Chinn ◽  
Kunlun Hong ◽  
S. Michael Kilbey ◽  
...  

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