Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.

作者: Hans E. Purkey , Kirk Robarge , Jinhua Chen , Zhongguo Chen , Laura B. Corson

DOI: 10.1021/ACSMEDCHEMLETT.6B00190

关键词:

摘要: … LDHA inhibition for the treatment of cancer. A recent report from our laboratories identified the lactate dehydrogenase … breast cancer tumors. (9) Given this linkage, we sought a pan-LDH …

参考文章(23)
Han Xie, Jun-ichi Hanai, Jian-Guo Ren, Lev Kats, Kerri Burgess, Parul Bhargava, Sabina Signoretti, Julia Billiard, Kevin J. Duffy, Aaron Grant, Xiaoen Wang, Pawel K. Lorkiewicz, Sabrina Schatzman, Michael Bousamra, Andrew N. Lane, Richard M. Higashi, Teresa W.M. Fan, Pier Paolo Pandolfi, Vikas P. Sukhatme, Pankaj Seth, Targeting lactate dehydrogenase-A inhibits tumorigenesis and tumor progression in mouse models of lung cancer and impacts tumor initiating cells Cell Metabolism. ,vol. 19, pp. 795- 809 ,(2014) , 10.1016/J.CMET.2014.03.003
M I Koukourakis, A Giatromanolaki, M Panteliadou, S E Pouliliou, P S Chondrou, S Mavropoulou, E Sivridis, Lactate dehydrogenase 5 isoenzyme overexpression defines resistance of prostate cancer to radiotherapy. British Journal of Cancer. ,vol. 110, pp. 2217- 2223 ,(2014) , 10.1038/BJC.2014.158
Mark McClellan, Joshua Benner, Richard Schilsky, David Epstein, Ray Woosley, Stephen Friend, David Sidransky, Cindy Geoghegan, David Kessler, An accelerated pathway for targeted cancer therapies Nature Reviews Drug Discovery. ,vol. 10, pp. 79- 80 ,(2011) , 10.1038/NRD3360
Anne Le, Charles R. Cooper, Arvin M. Gouw, Ramani Dinavahi, Anirban Maitra, Lorraine M. Deck, Robert E. Royer, David L. Vander Jagt, Gregg L. Semenza, Chi V. Dang, Inhibition of lactate dehydrogenase A induces oxidative stress and inhibits tumor progression Proceedings of the National Academy of Sciences of the United States of America. ,vol. 107, pp. 2037- 2042 ,(2010) , 10.1073/PNAS.0914433107
Jennifer D. Irvine, Lori Takahashi, Karen Lockhart, Jonathan Cheong, John W. Tolan, H.E. Selick, J.Russell Grove, MDCK (Madin-Darby canine kidney) cells : a tool for membrane permeability screening Journal of Pharmaceutical Sciences. ,vol. 88, pp. 28- 33 ,(1999) , 10.1021/JS9803205
Benjamin P. Fauber, Peter S. Dragovich, Jinhua Chen, Laura B. Corson, Charles Z. Ding, Charles Eigenbrot, Sharada Labadie, Shiva Malek, David Peterson, Hans E. Purkey, Kirk Robarge, Steve Sideris, Mark Ultsch, BinQing Wei, Ivana Yen, Qin Yue, Aihe Zhou, Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase. Bioorganic & Medicinal Chemistry Letters. ,vol. 24, pp. 5683- 5687 ,(2014) , 10.1016/J.BMCL.2014.10.067
Anna Kohlmann, Stephan G. Zech, Feng Li, Tianjun Zhou, Rachel M. Squillace, Lois Commodore, Matthew T. Greenfield, Xiaohui Lu, David P. Miller, Wei-Sheng Huang, Jiwei Qi, R. Mathew Thomas, Yihan Wang, Sen Zhang, Rory Dodd, Shuangying Liu, Rongsong Xu, Yongjin Xu, Juan J. Miret, Victor Rivera, Tim Clackson, William C. Shakespeare, Xiaotian Zhu, David C. Dalgarno, Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors. Journal of Medicinal Chemistry. ,vol. 56, pp. 1023- 1040 ,(2013) , 10.1021/JM3014844
O. Warburg, On the origin of cancer cells. Science. ,vol. 123, pp. 309- 314 ,(1956) , 10.1126/SCIENCE.123.3191.309