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Kyle R Brimacombe
Kyle R Brimacombe
Unknown affiliation
Verified email at mail.nih.gov
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Cited by
Year
Remdesivir: a review of its discovery and development leading to emergency use authorization for treatment of COVID-19
RT Eastman, JS Roth, KR Brimacombe, A Simeonov, M Shen, S Patnaik, ...
ACS central Science 6 (5), 672-683, 2020
9052020
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis
D Anastasiou, Y Yu, WJ Israelsen, JK Jiang, MB Boxer, BS Hong, ...
Nature chemical biology 8 (10), 839-847, 2012
7682012
A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate
ME Pacold, KR Brimacombe, SH Chan, JM Rohde, CA Lewis, ...
Nature chemical biology 12 (6), 452-458, 2016
4642016
Small molecule inhibitor of NRF2 selectively intervenes therapeutic resistance in KEAP1-deficient NSCLC tumors
A Singh, S Venkannagari, KH Oh, YQ Zhang, JM Rohde, L Liu, ...
ACS chemical biology 11 (11), 3214-3225, 2016
4352016
Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo
FJ Najm, M Madhavan, A Zaremba, E Shick, RT Karl, DC Factor, TE Miller, ...
Nature 522 (7555), 216-220, 2015
4082015
Effective transvascular delivery of nanoparticles across the blood-brain tumor barrier into malignant glioma cells
H Sarin, AS Kanevsky, H Wu, KR Brimacombe, SH Fung, AA Sousa, ...
Journal of translational medicine 6, 1-15, 2008
3002008
Synthesis and structure–activity evaluation of isatin-β-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein
MD Hall, KR Brimacombe, MS Varonka, KM Pluchino, JK Monda, J Li, ...
Journal of medicinal chemistry 54 (16), 5878-5889, 2011
1242011
Discovery and optimization of potent, cell-active pyrazole-based inhibitors of lactate dehydrogenase (LDH)
G Rai, KR Brimacombe, BT Mott, DJ Urban, X Hu, SM Yang, TD Lee, ...
Journal of medicinal chemistry 60 (22), 9184-9204, 2017
1052017
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays
DJ Urban, NJ Martinez, MI Davis, KR Brimacombe, DM Cheff, TD Lee, ...
Scientific reports 7 (1), 12758, 2017
802017
ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model
J Jiang, MJ Walsh, KR Brimacombe, D Anastasiou, Y Yu, WJ Israelsen, ...
Probe Reports from the NIH Molecular Libraries Program [Internet], 2013
762013
An OpenData portal to share COVID-19 drug repurposing data in real time
KR Brimacombe, T Zhao, RT Eastman, X Hu, K Wang, M Backus, ...
BioRxiv, 2020
742020
2-Oxo-N-aryl-1, 2, 3, 4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase
MJ Walsh, KR Brimacombe, H Veith, JM Bougie, T Daniel, W Leister, ...
Bioorganic & medicinal chemistry letters 21 (21), 6322-6327, 2011
712011
Assay guidance manual [Internet]
S Markossian, A Grossman, K Brimacombe, M Arkin, D Auld, C Austin, ...
Eli Lilly & Company and the National Center for Advancing Translational Sciences, 2004
632004
Discovery of NCT-501, a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1)
SM Yang, A Yasgar, B Miller, M Lal-Nag, K Brimacombe, X Hu, H Sun, ...
Journal of medicinal chemistry 58 (15), 5967-5978, 2015
602015
Inhibition of glutathione peroxidase mediates the collateral sensitivity of multidrug-resistant cells to tiopronin
MD Hall, TS Marshall, ADT Kwit, LMM Jenkins, AE Dulcey, JP Madigan, ...
Journal of Biological Chemistry 289 (31), 21473-21489, 2014
602014
A high-content imaging-based screening pipeline for the systematic identification of anti-progeroid compounds
N Kubben, KR Brimacombe, M Donegan, Z Li, T Misteli
Methods 96, 46-58, 2016
572016
A dual-fluorescence high-throughput cell line system for probing multidrug resistance
KR Brimacombe, MD Hall, DS Auld, J Inglese, CP Austin, MM Gottesman, ...
Assay and drug development technologies 7 (3), 233-249, 2009
572009
Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PET
P Kannan, KR Brimacombe, WC Kreisl, JS Liow, SS Zoghbi, S Telu, ...
Proceedings of the National Academy of Sciences 108 (6), 2593-2598, 2011
562011
High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2
NP Coussens, SC Kales, MJ Henderson, OW Lee, KY Horiuchi, Y Wang, ...
Journal of Biological Chemistry 293 (35), 13750-13765, 2018
502018
N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrier
P Kannan, KR Brimacombe, SS Zoghbi, JS Liow, C Morse, AK Taku, ...
Drug Metabolism and Disposition 38 (6), 917-922, 2010
502010
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