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AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity.
Chresta CM, Davies BR, Hickson I, Harding T, Cosulich S, Critchlow SE, Vincent JP, Ellston R, Jones D, Sini P, James D, Howard Z, Dudley P, Hughes G, Smith L, Maguire S, Hummersone M, Malagu K, Menear K, Jenkins R, Jacobsen M, Smith GC, Guichard S, Pass M. Chresta CM, et al. Among authors: critchlow se. Cancer Res. 2010 Jan 1;70(1):288-98. doi: 10.1158/0008-5472.CAN-09-1751. Epub 2009 Dec 22. Cancer Res. 2010. PMID: 20028854
Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.
Kettle JG, Ballard P, Bardelle C, Cockerill M, Colclough N, Critchlow SE, Debreczeni J, Fairley G, Fillery S, Graham MA, Goodwin L, Guichard S, Hudson K, Ward RA, Whittaker D. Kettle JG, et al. Among authors: critchlow se. J Med Chem. 2015 Mar 26;58(6):2834-44. doi: 10.1021/acs.jmedchem.5b00098. Epub 2015 Mar 12. J Med Chem. 2015. PMID: 25738750
Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3.
Boyd S, Brookfield JL, Critchlow SE, Cumming IA, Curtis NJ, Debreczeni J, Degorce SL, Donald C, Evans NJ, Groombridge S, Hopcroft P, Jones NP, Kettle JG, Lamont S, Lewis HJ, MacFaull P, McLoughlin SB, Rigoreau LJ, Smith JM, St-Gallay S, Stock JK, Turnbull AP, Wheatley ER, Winter J, Wingfield J. Boyd S, et al. Among authors: critchlow se. J Med Chem. 2015 Apr 23;58(8):3611-25. doi: 10.1021/acs.jmedchem.5b00352. Epub 2015 Apr 13. J Med Chem. 2015. PMID: 25849762
Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
Finlay MRV, Anderton M, Bailey A, Boyd S, Brookfield J, Cairnduff C, Charles M, Cheasty A, Critchlow SE, Culshaw J, Ekwuru T, Hollingsworth I, Jones N, Leroux F, Littleson M, McCarron H, McKelvie J, Mooney L, Nissink JWM, Perkins D, Powell S, Quesada MJ, Raubo P, Sabin V, Smith J, Smith PD, Stark A, Ting A, Wang P, Wilson Z, Winter-Holt JJ, Wood JM, Wrigley GL, Yu G, Zhang P. Finlay MRV, et al. Among authors: critchlow se. J Med Chem. 2019 Jul 25;62(14):6540-6560. doi: 10.1021/acs.jmedchem.9b00260. Epub 2019 Jul 16. J Med Chem. 2019. PMID: 31199640
A High-Throughput Screening Triage Workflow to Authenticate a Novel Series of PFKFB3 Inhibitors.
St-Gallay SA, Bennett N, Critchlow SE, Curtis N, Davies G, Debreczeni J, Evans N, Hardern I, Holdgate G, Jones NP, Leach L, Maman S, McLoughlin S, Preston M, Rigoreau L, Thomas A, Turnbull AP, Walker G, Walsh J, Ward RA, Wheatley E, Winter-Holt J. St-Gallay SA, et al. Among authors: critchlow se. SLAS Discov. 2018 Jan;23(1):11-22. doi: 10.1177/2472555217732289. Epub 2017 Sep 25. SLAS Discov. 2018. PMID: 28945981 Free article.
Combined Inhibition of PI3Kβ and mTOR Inhibits Growth of PTEN-null Tumors.
Lynch JT, Polanska UM, Hancox U, Delpuech O, Maynard J, Trigwell C, Eberlein C, Lenaghan C, Polanski R, Avivar-Valderas A, Cumberbatch M, Klinowska T, Critchlow SE, Cruzalegui F, Barry ST. Lynch JT, et al. Among authors: critchlow se. Mol Cancer Ther. 2018 Nov;17(11):2309-2319. doi: 10.1158/1535-7163.MCT-18-0183. Epub 2018 Aug 10. Mol Cancer Ther. 2018. PMID: 30097489
AZD3514: a small molecule that modulates androgen receptor signaling and function in vitro and in vivo.
Loddick SA, Ross SJ, Thomason AG, Robinson DM, Walker GE, Dunkley TP, Brave SR, Broadbent N, Stratton NC, Trueman D, Mouchet E, Shaheen FS, Jacobs VN, Cumberbatch M, Wilson J, Jones RD, Bradbury RH, Rabow A, Gaughan L, Womack C, Barry ST, Robson CN, Critchlow SE, Wedge SR, Brooks AN. Loddick SA, et al. Among authors: critchlow se. Mol Cancer Ther. 2013 Sep;12(9):1715-27. doi: 10.1158/1535-7163.MCT-12-1174. Epub 2013 Jul 16. Mol Cancer Ther. 2013. PMID: 23861347 Free PMC article.
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Johannes JW, Balazs A, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey K, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner C, Leo E, Liu L, Madin A, Martin S, McWilliams L, O'Connor MJ, Orme JP, Pachl F, Packer MJ, Pei X, Pike A, Schimpl M, She H, Staniszewska AD, Talbot V, Underwood E, Varnes JG, Xue L, Yao T, Zhang K, Zhang AX, Zheng X. Johannes JW, et al. Among authors: critchlow se. J Med Chem. 2021 Oct 14;64(19):14498-14512. doi: 10.1021/acs.jmedchem.1c01012. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34570508
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