By a News Reporter-Staff News Editor at Biotech Week -- A new study on Oncology is now available. According to news originating from Hong Kong, People's Republic of China, by NewsRx correspondents, research stated, "Small-molecule inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) have currently drawn much attention as promising chemotherapeutic drug candidates, and there is a need to develop more potent PARP inhibitors with improved bioavailability. Here we report a strategy to improve the cytotoxicity of PARP inhibitors by conjugation with organometallic ruthenium(II)-arene compounds."
Our news journalists obtained a quote from the research from the Hong Kong University of Science and Technology, "We also report a systematic study to reveal the mechanism of action of these ruthenium-PARP inhibitor conjugates. The complexes have been synthesized and characterized spectroscopically. The improved antiproliferative activity from the as-prepared complexes in four human cancer cell lines has indicated their potential for further development as antitumor drugs. Cellular uptake study reveals that the most active complex 3 easily entered into cells. Target validation assays show that the complexes inhibited PARP-1 slightly better than the original PARP inhibitors, that complex 3 strongly bound to DNA and inhibited transcription, and that this complex arrested the cell cycle at the G(0)/G(1) stage."
According to the news editors, the research concluded: "This type of information could shed light on the design of the next generation of more active ruthenium-PARP inhibitor conjugates."
For more information on this research see: Multi-targeted organometallic ruthenium(II)-arene anticancer complexes bearing inhibitors of poly(ADP-ribose) polymerase-1: A strategy to improve cytotoxicity. Journal of Inorganic Biochemistry, 2014;131():47-55. Journal of Inorganic Biochemistry can be contacted at: Elsevier Science Inc, 360 Park Ave South, New York, NY 10010-1710, USA. (Elsevier - www.elsevier.com; Journal of Inorganic Biochemistry - www.elsevier.com/wps/product/cws_home/505772)
The news correspondents report that additional information may be obtained from Z.G. Wang, Hong Kong University of Science & Technology, Dept. of Chem, Kowloon, Hong Kong, People's Republic of China. Additional authors for this research include H. Qian, S.M. Yiu, J.W. Sun and G.Y. Zhu (see also Oncology).
Keywords for this news article include: Asia, Therapy, Oncology, Hong Kong, Ruthenium, Nanotechnology, Transition Elements, Glycosyltransferases, Emerging Technologies, Enzymes and Coenzymes, ADP Ribose Transferases, Organometallic Organosol, People's Republic of China, Poly(ADP-ribose) Polymerases
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