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Page 1
Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.
Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB. Blake JF, et al. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2635-9. doi: 10.1016/j.bmcl.2014.04.068. Epub 2014 Apr 29. Bioorg Med Chem Lett. 2014. PMID: 24813737
Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.
Ren L, Grina J, Moreno D, Blake JF, Gaudino JJ, Garrey R, Metcalf AT, Burkard M, Martinson M, Rasor K, Chen H, Dean B, Gould SE, Pacheco P, Shahidi-Latham S, Yin J, West K, Wang W, Moffat JG, Schwarz JB. Ren L, et al. J Med Chem. 2015 Feb 26;58(4):1976-91. doi: 10.1021/jm501921k. Epub 2015 Feb 11. J Med Chem. 2015. PMID: 25603482
Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.
Blake JF, Burkard M, Chan J, Chen H, Chou KJ, Diaz D, Dudley DA, Gaudino JJ, Gould SE, Grina J, Hunsaker T, Liu L, Martinson M, Moreno D, Mueller L, Orr C, Pacheco P, Qin A, Rasor K, Ren L, Robarge K, Shahidi-Latham S, Stults J, Sullivan F, Wang W, Yin J, Zhou A, Belvin M, Merchant M, Moffat J, Schwarz JB. Blake JF, et al. J Med Chem. 2016 Jun 23;59(12):5650-60. doi: 10.1021/acs.jmedchem.6b00389. Epub 2016 Jun 7. J Med Chem. 2016. PMID: 27227380
Combined MEK and ERK inhibition overcomes therapy-mediated pathway reactivation in RAS mutant tumors.
Merchant M, Moffat J, Schaefer G, Chan J, Wang X, Orr C, Cheng J, Hunsaker T, Shao L, Wang SJ, Wagle MC, Lin E, Haverty PM, Shahidi-Latham S, Ngu H, Solon M, Eastham-Anderson J, Koeppen H, Huang SA, Schwarz J, Belvin M, Kirouac D, Junttila MR. Merchant M, et al. Among authors: shahidi latham s. PLoS One. 2017 Oct 5;12(10):e0185862. doi: 10.1371/journal.pone.0185862. eCollection 2017. PLoS One. 2017. PMID: 28982154 Free PMC article.
Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma.
Salphati L, Alicke B, Heffron TP, Shahidi-Latham S, Nishimura M, Cao T, Carano RA, Cheong J, Greve J, Koeppen H, Lau S, Lee LB, Nannini-Pepe M, Pang J, Plise EG, Quiason C, Rangell L, Zhang X, Gould SE, Phillips HS, Olivero AG. Salphati L, et al. Drug Metab Dispos. 2016 Dec;44(12):1881-1889. doi: 10.1124/dmd.116.071423. Epub 2016 Sep 16. Drug Metab Dispos. 2016. PMID: 27638506
Lung-restricted inhibition of Janus kinase 1 is effective in rodent models of asthma.
Dengler HS, Wu X, Peng I, Rinderknecht CH, Kwon Y, Suto E, Kohli PB, Liimatta M, Barrett K, Lloyd J, Cain G, Briggs M, Addo S, Salmon G, Ubhayakar S, Deshmukh G, Shahidi-Latham SK, Quiason-Huynh CM, Jackman J, Liu J, Ray NC, Goodacre SC, Johnson A, McKenzie BS, Lee WP, Zak M, Kenny JR, Ghilardi N. Dengler HS, et al. Among authors: shahidi latham sk. Sci Transl Med. 2018 Nov 21;10(468):eaao2151. doi: 10.1126/scitranslmed.aao2151. Sci Transl Med. 2018. PMID: 30463918
Correction: Combined MEK and ERK inhibition overcomes therapy-mediated pathway reactivation in RAS mutant tumors.
Merchant M, Moffat J, Schaefer G, Chan J, Wang X, Orr C, Cheng J, Hunsaker T, Shao L, Wang SJ, Wagle MC, Lin E, Haverty PM, Shahidi-Latham S, Ngu H, Solon M, Eastham-Anderson J, Koeppen H, Huang SA, Schwarz J, Belvin M, Kirouac D, Junttila MR. Merchant M, et al. Among authors: shahidi latham s. PLoS One. 2018 Jan 25;13(1):e0192059. doi: 10.1371/journal.pone.0192059. eCollection 2018. PLoS One. 2018. PMID: 29370292 Free PMC article.
22 results