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Current Opinion in Pharmacology, ISSN 1471-4892, 08/2010, Volume 10, Issue 4, p. 391
The predictive value of non-clinical cancer pharmacology models has been poor with many drugs failing in the clinic that previously demonstrated anti-tumor... 
Care and treatment | Analysis | Pharmacology | Cancer
Journal Article
Nature, ISSN 0028-0836, 07/2016, Volume 535, Issue 7610, pp. 148 - 152
The non-receptor protein tyrosine phosphatase SHP2, encoded by PTPN11, has an important role in signal transduction downstream of growth factor receptor... 
TARGET | POTENT | PTPN11 | PROTOONCOGENE | MULTIDISCIPLINARY SCIENCES | Protein Tyrosine Phosphatase, Non-Receptor Type 11 - metabolism | Humans | Extracellular Signal-Regulated MAP Kinases - metabolism | Oncogene Protein p21(ras) - metabolism | Pyrimidines - chemistry | Piperidines - pharmacology | Inhibitory Concentration 50 | Female | Allosteric Regulation - drug effects | Piperidines - chemistry | Reproducibility of Results | Protein Tyrosine Phosphatase, Non-Receptor Type 11 - antagonists & inhibitors | Models, Molecular | Neoplasms - enzymology | Protein Tyrosine Phosphatase, Non-Receptor Type 11 - chemistry | Pyrimidines - pharmacology | Receptor Protein-Tyrosine Kinases - metabolism | Neoplasms - drug therapy | Xenograft Model Antitumor Assays | Animals | MAP Kinase Signaling System - drug effects | Mice, Nude | Piperidines - therapeutic use | Pyrimidines - therapeutic use | Protein Stability - drug effects | Cell Line, Tumor | Cell Proliferation - drug effects | Mice | Protein Kinase Inhibitors - pharmacology | Protein Tyrosine Phosphatase, Non-Receptor Type 11 - genetics | Neoplasms - pathology | Protein Structure, Tertiary - drug effects | Phosphatases | Observations | Health aspects | Phosphotransferases | Protein-protein interactions | Signal transduction | Cell growth | Peptides | Kinases | Phosphatase | Drug dosages | Cancer | BASIC BIOLOGICAL SCIENCES
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2018, Volume 61, Issue 7, pp. 2837 - 2864
In breast cancer, estrogen receptor alpha (ERα) positive cancer accounts for approximately 74% of all diagnoses, and in these settings, it is a primary driver... 
TRIAL | AROMATASE INHIBITOR | CHEMISTRY, MEDICINAL | ACID | EFFICACY | FULVESTRANT | MODULATORS | TAMOXIFEN RESISTANCE | ALPHA | POSTMENOPAUSAL WOMEN
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2016, Volume 59, Issue 17, pp. 7773 - 7782
Journal Article
by Townsend, Elizabeth C and Murakami, Mark A and Murakami, Masato and Christodoulou, Alexandra and Christie, Amanda L and Köster, Johannes and DeSouza, Tiffany A and Morgan, Elizabeth A and Kallgren, Scott P and Liu, Huiyun and Wu, Shuo-Chieh and Plana, Olivia and Montero, Joan and Stevenson, Kristen E and Rao, Prakash and Vadhi, Raga and Andreeff, Michael and Armand, Philippe and Ballen, Karen K and Barzaghi-Rinaudo, Patrizia and Cahill, Sarah and Clark, Rachael A and Cooke, Vesselina G and Davids, Matthew S and DeAngelo, Daniel J and Dorfman, David M and Eaton, Hilary and Ebert, Benjamin L and Etchin, Julia and Firestone, Brant and Fisher, David C and Freedman, Arnold S and Galinsky, Ilene A and Gao, Hui and Garcia, Jacqueline S and Garnache-Ottou, Francine and Graubert, Timothy A and Gutierrez, Alejandro and Halilovic, Ensar and Harris, Marian H and Herbert, Zachary T and Horwitz, Steven M and Inghirami, Giorgio and Intlekofer, Andrew M and Ito, Moriko and Izraeli, Shai and Jacobsen, Eric D and Jacobson, Caron A and Jeay, Sébastien and Jeremias, Irmela and Kelliher, Michelle A and Koch, Raphael and Konopleva, Marina and Kopp, Nadja and Kornblau, Steven M and Kung, Andrew L and Kupper, Thomas S and LeBoeuf, Nicole R and LaCasce, Ann S and Lees, Emma and Li, Loretta S and Look, A. Thomas and Muschen, Markus and Neuberg, Donna and Ng, Samuel Y and Odejide, Oreofe O and Orkin, Stuart H and Paquette, Rachel R and Place, Andrew E and Roderick, Justine E and Ryan, Jeremy A and Sallan, Stephen E and Shoji, Brent and Silverman, Lewis B and Soiffer, Robert J and Steensma, David P and Stegmaier, Kimberly and Stone, Richard M and Tamburini, Jerome and Thorner, Aaron R and van Hummelen, Paul and Wadleigh, Martha and Wiesmann, Marion and Weng, Andrew P and Wuerthner, Jens U and Williams, David A and Wollison, Bruce M and Lane, Andrew A and Letai, Anthony and Bertagnolli, Monica M and Ritz, Jerome and Brown, Myles and Long, Henry and Aster, Jon C and Shipp, Margaret A and Griffin, James D and Weinstock, David M
Cancer Cell, ISSN 1535-6108, 04/2016, Volume 29, Issue 4, pp. 574 - 586
Journal Article
Oncogene, ISSN 0950-9232, 11/2016, Volume 35, Issue 47, pp. 6077 - 6086
Journal Article
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 02/2019, Volume 62, Issue 4, pp. 1781 - 1792
SHP2 is a nonreceptor protein tyrosine phosphatase within the mitogen-activated protein kinase (MAPK) pathway controlling cell growth, differentiation, and... 
CHEMISTRY, MEDICINAL | PTPN11 | TYROSINE-PHOSPHATASE SHP2
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 02/2019, Volume 62, Issue 4, pp. 1793 - 1802
Protein tyrosine phosphatase SHP2 is an oncoprotein associated with cancer as well as a potential immune modulator because of its role in the programmed cell... 
ALLOSTERIC-INHIBITION | CHEMISTRY, MEDICINAL | PTPN11 | TYROSINE-PHOSPHATASE SHP2 | MUTATIONS | IDENTIFICATION | DISCOVERY
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 10/2017, Volume 8, Issue 10, pp. 1116 - 1121
Inhibition of mutant IDH1 is being evaluated clinically as a promising treatment option for various cancers with hotspot mutation at Arg132. Having identified... 
Mutant IDH1 | clinical candidate | inhibition of 2-HG production | in vivo anticancer activity | brain penetration | ISOCITRATE DEHYDROGENASE 1 | SELECTIVE-INHIBITION | CHEMISTRY, MEDICINAL | SMALL-MOLECULE | ACUTE MYELOID-LEUKEMIA | OPPORTUNITIES | HYPOXIA | Mutant IDHI | METABOLISM | MUTATIONS
Journal Article
by Townsend, Elizabeth C and Murakami, Mark A and Murakami, Masato and Christodoulou, Alexandra and Christie, Amanda L and Köster, Johannes and DeSouza, Tiffany A and Morgan, Elizabeth A and Kallgren, Scott P and Liu, Huiyun and Wu, Shuo-Chieh and Plana, Olivia and Montero, Joan and Stevenson, Kristen E and Rao, Prakash and Vadhi, Raga and Andreeff, Michael and Armand, Philippe and Ballen, Karen K and Barzaghi-Rinaudo, Patrizia and Cahill, Sarah and Clark, Rachael A and Cooke, Vesselina G and Davids, Matthew S and DeAngelo, Daniel J and Dorfman, David M and Eaton, Hilary and Ebert, Benjamin L and Etchin, Julia and Firestone, Brant and Fisher, David C and Freedman, Arnold S and Galinsky, Ilene A and Gao, Hui and Garcia, Jacqueline S and Garnache-Ottou, Francine and Graubert, Timothy A and Gutierrez, Alejandro and Halilovic, Ensar and Harris, Marian H and Herbert, Zachary T and Horwitz, Steven M and Inghirami, Giorgio and Intlekofer, Andrew M and Ito, Moriko and Izraeli, Shai and Jacobsen, Eric D and Jacobson, Caron A and Jeay, Sébastien and Jeremias, Irmela and Kelliher, Michelle A and Koch, Raphael and Konopleva, Marina and Kopp, Nadja and Kornblau, Steven M and Kung, Andrew L and Kupper, Thomas S and LeBoeuf, Nicole R and LaCasce, Ann S and Lees, Emma and Li, Loretta S and Look, A. Thomas and Muschen, Markus and Neuberg, Donna and Ng, Samuel Y and Odejide, Oreofe O and Orkin, Stuart H and Paquette, Rachel R and Place, Andrew E and Roderick, Justine E and Ryan, Jeremy A and Sallan, Stephen E and Shoji, Brent and Silverman, Lewis B and Soiffer, Robert J and Steensma, David P and Stegmaier, Kimberly and Stone, Richard M and Tamburini, Jerome and Thorner, Aaron R and van Hummelen, Paul and Wadleigh, Martha and Wiesmann, Marion and Weng, Andrew P and Wuerthner, Jens U and Williams, David A and Wollison, Bruce M and Lane, Andrew A and Letai, Anthony and Bertagnolli, Monica M and Ritz, Jerome and Brown, Myles and Long, Henry and Aster, Jon C and Shipp, Margaret A and Griffin, James D and Weinstock, David M
Cancer Cell, ISSN 1535-6108, 07/2016, Volume 30, Issue 1, pp. 183 - 183
Journal Article
by Townsend, Elizabeth C and Murakami, Mark A and Christodoulou, Alexandra and Christie, Amanda L and Köster, Johannes and DeSouza, Tiffany A and Morgan, Elizabeth A and Kallgren, Scott P and Liu, Huiyun and Wu, Shuo-Chieh and Plana, Olivia and Montero, Joan and Stevenson, Kristen E and Rao, Prakash and Vadhi, Raga and Andreeff, Michael and Armand, Philippe and Ballen, Karen K and Barzaghi-Rinaudo, Patrizia and Cahill, Sarah and Clark, Rachael A and Cooke, Vesselina G and Davids, Matthew S and DeAngelo, Daniel J and Dorfman, David M and Eaton, Hilary and Ebert, Benjamin L and Etchin, Julia and Firestone, Brant and Fisher, David C and Freedman, Arnold S and Galinsky, Ilene A and Gao, Hui and Garcia, Jacqueline S and Garnache-Ottou, Francine and Graubert, Timothy A and Gutierrez, Alejandro and Halilovic, Ensar and Harris, Marian H and Herbert, Zachary T and Horwitz, Steven M and Inghirami, Giorgio and Intlekofer, Andrew M and Ito, Moriko and Izraeli, Shai and Jacobsen, Eric D and Jacobson, Caron A and Jeay, Sébastien and Jeremias, Irmela and Kelliher, Michelle A and Koch, Raphael and Konopleva, Marina and Kopp, Nadja and Kornblau, Steven M and Kung, Andrew L and Kupper, Thomas S and LeBoeuf, Nicole R and LaCasce, Ann S and Lees, Emma and Li, Loretta S and Look, A. Thomas and Murakami, Masato and Muschen, Markus and Neuberg, Donna and Ng, Samuel Y and Odejide, Oreofe O and Orkin, Stuart H and Paquette, Rachel R and Place, Andrew E and Roderick, Justine E and Ryan, Jeremy A and Sallan, Stephen E and Shoji, Brent and Silverman, Lewis B and Soiffer, Robert J and Steensma, David P and Stegmaier, Kimberly and Stone, Richard M and Tamburini, Jerome and Thorner, Aaron R and van Hummelen, Paul and Wadleigh, Martha and Wiesmann, Marion and Weng, Andrew P and Wuerthner, Jens U and Williams, David A and Wollison, Bruce M and Lane, Andrew A and Letai, Anthony and Bertagnolli, Monica M and Ritz, Jerome and Brown, Myles and Long, Henry and Aster, Jon C and Shipp, Margaret A and Griffin, James D and Weinstock, David M
Cancer Cell, ISSN 1535-6108, 07/2016, Volume 30, Issue 1, p. 183
(Cancer Cell 29, 574–586; April 11, 2016) In the originally published version of this article, coauthor Andrew M. Intlekofer was listed incorrectly as Andrew... 
Journal Article