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Structural basis of AMPK regulation by small molecule activators.
Xiao B, Sanders MJ, Carmena D, Bright NJ, Haire LF, Underwood E, Patel BR, Heath RB, Walker PA, Hallen S, Giordanetto F, Martin SR, Carling D, Gamblin SJ. Xiao B, et al. Among authors: underwood e. Nat Commun. 2013;4:3017. doi: 10.1038/ncomms4017. Nat Commun. 2013. PMID: 24352254 Free PMC article.
Structure of mammalian AMPK and its regulation by ADP.
Xiao B, Sanders MJ, Underwood E, Heath R, Mayer FV, Carmena D, Jing C, Walker PA, Eccleston JF, Haire LF, Saiu P, Howell SA, Aasland R, Martin SR, Carling D, Gamblin SJ. Xiao B, et al. Among authors: underwood e. Nature. 2011 Apr 14;472(7342):230-3. doi: 10.1038/nature09932. Epub 2011 Mar 13. Nature. 2011. PMID: 21399626 Free PMC article.
ADP regulates SNF1, the Saccharomyces cerevisiae homolog of AMP-activated protein kinase.
Mayer FV, Heath R, Underwood E, Sanders MJ, Carmena D, McCartney RR, Leiper FC, Xiao B, Jing C, Walker PA, Haire LF, Ogrodowicz R, Martin SR, Schmidt MC, Gamblin SJ, Carling D. Mayer FV, et al. Among authors: underwood e. Cell Metab. 2011 Nov 2;14(5):707-14. doi: 10.1016/j.cmet.2011.09.009. Epub 2011 Oct 20. Cell Metab. 2011. PMID: 22019086 Free PMC article.
Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy.
Nissink JWM, Bazzaz S, Blackett C, Clark MA, Collingwood O, Disch JS, Gikunju D, Goldberg K, Guilinger JP, Hardaker E, Hennessy EJ, Jetson R, Keefe AD, McCoull W, McMurray L, Olszewski A, Overman R, Pflug A, Preston M, Rawlins PB, Rivers E, Schimpl M, Smith P, Truman C, Underwood E, Warwicker J, Winter-Holt J, Woodcock S, Zhang Y. Nissink JWM, et al. Among authors: underwood e. J Med Chem. 2021 Mar 25;64(6):3165-3184. doi: 10.1021/acs.jmedchem.0c01904. Epub 2021 Mar 8. J Med Chem. 2021. PMID: 33683117
Fragment-Based Design of a Potent MAT2a Inhibitor and in Vivo Evaluation in an MTAP Null Xenograft Model.
De Fusco C, Schimpl M, Börjesson U, Cheung T, Collie I, Evans L, Narasimhan P, Stubbs C, Vazquez-Chantada M, Wagner DJ, Grondine M, Sanders MG, Tentarelli S, Underwood E, Argyrou A, Smith JM, Lynch JT, Chiarparin E, Robb G, Bagal SK, Scott JS. De Fusco C, et al. Among authors: underwood e. J Med Chem. 2021 May 27;64(10):6814-6826. doi: 10.1021/acs.jmedchem.1c00067. Epub 2021 Apr 26. J Med Chem. 2021. PMID: 33900758 Free 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: underwood e. 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
242 results