@article{567e0336277b4fa4a95628b9cf39ac06,
title = "Drugging the 'undruggable' cancer targets",
abstract = "The term 'undruggable' was coined to describe proteins that could not be targeted pharmacologically. However, progress is being made to 'drug' many of these targets, and therefore more appropriate terms might be 'difficult to drug' or 'yet to be drugged'. Many desirable targets in cancer fall into this category, including the RAS and MYC oncogenes, and pharmacologically targeting these intractable proteins is now a key challenge in cancer research that requires innovation and the development of new technologies. In this Viewpoint article, we asked four scientists working in this field for their opinions on the most crucial advances, as well as the challenges and what the future holds for this important area of research.",
author = "Dang, {Chi V.} and Reddy, {E. Premkumar} and Shokat, {Kevan M.} and Laura Soucek",
note = "Funding Information: K.M.S. would like to thank J. Taunton for pointing out the example of GBT440. L.S. acknowledges funding from the European Research Council (CoG Grant #617473), the Instituto de Salud Carlos III (FIS Grant #PI13/01705 and #PI16/01224), the BBVA Foundation and the FERO Foundation. Funding Information: Chi V. Dang is Professor at The Wistar Institute, Philadelphia, Pennsylvania, USA and Scientific Director of the Ludwig Institute for Cancer Research. He has made contributions to the understanding of the role of MYC in cancer, particularly its role as a transcription factor and its target genes that reprogramme cancer metabolism. E. Premkumar Reddy is a professor at the Icahn School of Medicine at Mount Sinai, New York, USA. His early work showed that point mutations in RAS genes result in their oncogenic activation. In recent years, he has focused on the development of small-molecule inhibitors targeted against oncogenes and cell cycle regulators for cancer therapy. Kevan M. Shokat received his B.A. in chemistry from Reed College, Portland, Oregon, USA, in 1986; his Ph.D. in organic chemistry at the University of California Berkeley, USA, with Peter Schultz; and completed his postdoctoral work in immunology at Stanford University, California, USA, with Chris Goodnow. He is a pioneer in the use of organic synthesis to develop pharmacological agents as molecularly targeted therapies for cancer, immune dysfunction such as asthma and neurodegenerative disorders such as Parkinson disease. His laboratory has developed first-in-class inhibitors of protein kinases such as mTOR, lipid kinases such as PI3K and most recently the oncogene KRAS. Laura Soucek graduated in 1996 in biological sciences from University La Sapienza in Rome, Italy. She obtained her Ph.D. in genetics and molecular biology at the National Research Center, in Rome. In 2001 she joined Gerard Evan{\textquoteright}s laboratory at the University of California San Francisco, USA, initially as a postdoctoral fellow and later, in 2006, as an assistant researcher. There she published in some of the most prestigious international journals. Since early 2011, she has headed the Mouse Models of Cancer Therapies group at the Vall d{\textquoteright}Hebron Institute of Oncology (VHIO), in Barcelona, Spain. She received prestigious awards and grants from the American Association for Cancer Research, the Miguel Servet Program, the FERO Foundation, the Association for International Cancer Research, the European Research Council, FIS and BBVA. In October 2014 she was appointed Instituci{\'o} Catalana de Recerca I Estudis Avan{\c c}ats (ICREA) Research Professor. In December 2014 she founded a spin-off company, Peptomyc S.L. In April 2015, she became Associate Professor at the Universitat Aut{\`o}noma de Barcelona. Publisher Copyright: {\textcopyright} 2017 Macmillan Publishers Limited, part of Springer Nature.",
year = "2017",
month = jul,
day = "25",
doi = "10.1038/nrc.2017.36",
language = "English",
volume = "17",
pages = "502--508",
journal = "Nature Reviews Cancer",
issn = "1474-175X",
publisher = "Nature Publishing Group",
number = "8",
}