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Items: 35

1.

Quantitative high-throughput screening using an organotypic model identifies compounds that inhibit ovarian cancer metastasis.

Kenny HA, Lal-Nag M, Shen M, Kara B, Nahotko DA, Wroblewski K, Fazal S, Chen S, Chiang CY, Chen YJ, Brimacombe KR, Marugan J, Ferrer M, Lengyel E.

Mol Cancer Ther. 2019 Sep 27. pii: molcanther.0052.2019. doi: 10.1158/1535-7163.MCT-19-0052. [Epub ahead of print]

PMID:
31562255
2.

A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.

Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD.

Mol Pharmacol. 2019 Nov;96(5):629-640. doi: 10.1124/mol.119.115964. Epub 2019 Sep 12.

3.

Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.

Kearney SE, Zahoránszky-Kőhalmi G, Brimacombe KR, Henderson MJ, Lynch C, Zhao T, Wan KK, Itkin Z, Dillon C, Shen M, Cheff DM, Lee TD, Bougie D, Cheng K, Coussens NP, Dorjsuren D, Eastman RT, Huang R, Iannotti MJ, Karavadhi S, Klumpp-Thomas C, Roth JS, Sakamuru S, Sun W, Titus SA, Yasgar A, Zhang YQ, Zhao J, Andrade RB, Brown MK, Burns NZ, Cha JK, Mevers EE, Clardy J, Clement JA, Crooks PA, Cuny GD, Ganor J, Moreno J, Morrill LA, Picazo E, Susick RB, Garg NK, Goess BC, Grossman RB, Hughes CC, Johnston JN, Joullie MM, Kinghorn AD, Kingston DGI, Krische MJ, Kwon O, Maimone TJ, Majumdar S, Maloney KN, Mohamed E, Murphy BT, Nagorny P, Olson DE, Overman LE, Brown LE, Snyder JK, Porco JA Jr, Rivas F, Ross SA, Sarpong R, Sharma I, Shaw JT, Xu Z, Shen B, Shi W, Stephenson CRJ, Verano AL, Tan DS, Tang Y, Taylor RE, Thomson RJ, Vosburg DA, Wu J, Wuest WM, Zakarian A, Zhang Y, Ren T, Zuo Z, Inglese J, Michael S, Simeonov A, Zheng W, Shinn P, Jadhav A, Boxer MB, Hall MD, Xia M, Guha R, Rohde JM.

ACS Cent Sci. 2018 Dec 26;4(12):1727-1741. doi: 10.1021/acscentsci.8b00747. Epub 2018 Dec 5.

4.

High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2.

Coussens NP, Kales SC, Henderson MJ, Lee OW, Horiuchi KY, Wang Y, Chen Q, Kuznetsova E, Wu J, Chakka S, Cheff DM, Cheng KC, Shinn P, Brimacombe KR, Shen M, Simeonov A, Lal-Nag M, Ma H, Jadhav A, Hall MD.

J Biol Chem. 2018 Aug 31;293(35):13750-13765. doi: 10.1074/jbc.RA118.004274. Epub 2018 Jun 26.

5.

Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors.

Rohde JM, Brimacombe KR, Liu L, Pacold ME, Yasgar A, Cheff DM, Lee TD, Rai G, Baljinnyam B, Li Z, Simeonov A, Hall MD, Shen M, Sabatini DM, Boxer MB.

Bioorg Med Chem. 2018 May 1;26(8):1727-1739. doi: 10.1016/j.bmc.2018.02.016. Epub 2018 Feb 27.

6.

PKM2 activation sensitizes cancer cells to growth inhibition by 2-deoxy-D-glucose.

Tee SS, Park JM, Hurd RE, Brimacombe KR, Boxer MB, Massoud TF, Rutt BK, Spielman DM.

Oncotarget. 2017 Jul 26;8(53):90959-90968. doi: 10.18632/oncotarget.19630. eCollection 2017 Oct 31.

7.

Genome Editing Using Engineered Nucleases and Their Use in Genomic Screening.

Costa JR, Bejcek BE, McGee JE, Fogel AI, Brimacombe KR, Ketteler R.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin CP, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Coussens NP, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Hoare SRJ, Inglese J, Iversen PW, Kahl SD, Kales SC, Kirshner S, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Saradjian P, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2017 Nov 20.

8.

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).

Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ.

J Med Chem. 2017 Nov 22;60(22):9184-9204. doi: 10.1021/acs.jmedchem.7b00941. Epub 2017 Nov 9.

9.

Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays.

Urban DJ, Martinez NJ, Davis MI, Brimacombe KR, Cheff DM, Lee TD, Henderson MJ, Titus SA, Pragani R, Rohde JM, Liu L, Fang Y, Karavadhi S, Shah P, Lee OW, Wang A, McIver A, Zheng H, Wang X, Xu X, Jadhav A, Simeonov A, Shen M, Boxer MB, Hall MD.

Sci Rep. 2017 Oct 6;7(1):12758. doi: 10.1038/s41598-017-12630-x.

10.

Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors.

Singh A, Venkannagari S, Oh KH, Zhang YQ, Rohde JM, Liu L, Nimmagadda S, Sudini K, Brimacombe KR, Gajghate S, Ma J, Wang A, Xu X, Shahane SA, Xia M, Woo J, Mensah GA, Wang Z, Ferrer M, Gabrielson E, Li Z, Rastinejad F, Shen M, Boxer MB, Biswal S.

ACS Chem Biol. 2016 Nov 18;11(11):3214-3225. Epub 2016 Oct 17.

11.

Corrigendum: A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate.

Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu MR, Shaul YD, Liu CM, Zhou M, Koh MJ, Chung H, Davidson SM, Luengo A, Wang AQ, Xu X, Yasgar A, Liu L, Rai G, Westover KD, Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM.

Nat Chem Biol. 2016 Jul 19;12(8):656. doi: 10.1038/nchembio0816-656. No abstract available.

PMID:
27434767
12.

A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate.

Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu-Remaileh M, Shaul YD, Liu CM, Zhou M, Koh MJ, Chung H, Davidson SM, Luengo A, Wang AQ, Xu X, Yasgar A, Liu L, Rai G, Westover KD, Vander Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM.

Nat Chem Biol. 2016 Jun;12(6):452-8. doi: 10.1038/nchembio.2070. Epub 2016 Apr 25. Erratum in: Nat Chem Biol. 2016 Jul 19;12 (8):656.

13.

A high-content imaging-based screening pipeline for the systematic identification of anti-progeroid compounds.

Kubben N, Brimacombe KR, Donegan M, Li Z, Misteli T.

Methods. 2016 Mar 1;96:46-58. doi: 10.1016/j.ymeth.2015.08.024. Epub 2015 Sep 1.

14.

Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo.

Najm FJ, Madhavan M, Zaremba A, Shick E, Karl RT, Factor DC, Miller TE, Nevin ZS, Kantor C, Sargent A, Quick KL, Schlatzer DM, Tang H, Papoian R, Brimacombe KR, Shen M, Boxer MB, Jadhav A, Robinson AP, Podojil JR, Miller SD, Miller RH, Tesar PJ.

Nature. 2015 Jun 11;522(7555):216-20. doi: 10.1038/nature14335. Epub 2015 Apr 20.

15.

Discovery of two small molecule inhibitors, ML387 and ML388, of human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase.

Duveau DY, Yasgar A, Hu X, Kouznetsova J, Brimacombe KR, Kerns EH, Mathews L, Zhang X, Sun H, Ferrer M, Jadhav A, Simeonov A, Thomas CJ, Maloney DJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Dec 15 [updated 2015 Feb 11].

16.

Structure activity relationships of human galactokinase inhibitors.

Liu L, Tang M, Walsh MJ, Brimacombe KR, Pragani R, Tanega C, Rohde JM, Baker HL, Fernandez E, Blackman B, Bougie JM, Leister WH, Auld DS, Shen M, Lai K, Boxer MB.

Bioorg Med Chem Lett. 2015 Feb 1;25(3):721-7. doi: 10.1016/j.bmcl.2014.11.061. Epub 2014 Dec 13.

PMID:
25553891
17.

Inhibition of glutathione peroxidase mediates the collateral sensitivity of multidrug-resistant cells to tiopronin.

Hall MD, Marshall TS, Kwit AD, Miller Jenkins LM, Dulcey AE, Madigan JP, Pluchino KM, Goldsborough AS, Brimacombe KR, Griffiths GL, Gottesman MM.

J Biol Chem. 2014 Aug 1;289(31):21473-89. doi: 10.1074/jbc.M114.581702. Epub 2014 Jun 14.

18.

Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase.

Brimacombe KR, Walsh MJ, Liu L, Vásquez-Valdivieso MG, Morgan HP, McNae I, Fothergill-Gilmore LA, Michels PA, Auld DS, Simeonov A, Walkinshaw MD, Shen M, Boxer MB.

ACS Med Chem Lett. 2013 Oct 30;5(1):12-7. doi: 10.1021/ml400259d. eCollection 2014 Jan 9.

19.

Research resource: modulators of glucocorticoid receptor activity identified by a new high-throughput screening assay.

Blackford JA Jr, Brimacombe KR, Dougherty EJ, Pradhan M, Shen M, Li Z, Auld DS, Chow CC, Austin CP, Simons SS Jr.

Mol Endocrinol. 2014 Jul;28(7):1194-206. doi: 10.1210/me.2014-1069. Epub 2014 May 21.

20.

Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors.

Duveau DY, Yasgar A, Wang Y, Hu X, Kouznetsova J, Brimacombe KR, Jadhav A, Simeonov A, Thomas CJ, Maloney DJ.

Bioorg Med Chem Lett. 2014 Jan 15;24(2):630-5. doi: 10.1016/j.bmcl.2013.11.081. Epub 2013 Dec 4.

21.

Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.

Patnaik S, Marugan JJ, Liu K, Zheng W, Southall N, Dehdashti SJ, Thorsell A, Heilig M, Bell L, Zook M, Eskay B, Brimacombe KR, Austin CP.

J Med Chem. 2013 Nov 27;56(22):9045-56. doi: 10.1021/jm400904m. Epub 2013 Nov 11.

22.

Identification of Selective Inhibitors of Phosphofructokinase as Lead Compounds Against Trypanosomiasis.

Walsh MJ, Brimacombe KR, Vásquez-Valdivieso MG, Auld DS, Simeonov A, Morgan HP, Fothergill-Gilmore LA, Michels PAM, Walkinshaw MD, Shen M, Boxer MB.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Oct 18 [updated 2013 Feb 25].

23.

ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model.

Jiang J, Walsh MJ, Brimacombe KR, Anastasiou D, Yu Y, Israelsen WJ, Hong BS, Tempel W, Dimov S, Veith H, Yang H, Kung C, Yen KE, Dang L, Salituro F, Auld DS, Park HW, Vander Heiden MG, Thomas CJ, Shen M, Boxer MB.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Mar 16 [updated 2013 May 8].

24.

ML285 affects reactive oxygen species’ inhibition of pyruvate kinase M2.

Brimacombe KR, Anastasiou D, Hong BS, Tempel W, Dimov S, Veith H, Auld DS, Vander Heiden MG, Thomas CJ, Park HW, Shen M, Cantley LC, Boxer MB.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Aug 3 [updated 2013 May 8].

25.

Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.

Anastasiou D, Yu Y, Israelsen WJ, Jiang JK, Boxer MB, Hong BS, Tempel W, Dimov S, Shen M, Jha A, Yang H, Mattaini KR, Metallo CM, Fiske BP, Courtney KD, Malstrom S, Khan TM, Kung C, Skoumbourdis AP, Veith H, Southall N, Walsh MJ, Brimacombe KR, Leister W, Lunt SY, Johnson ZR, Yen KE, Kunii K, Davidson SM, Christofk HR, Austin CP, Inglese J, Harris MH, Asara JM, Stephanopoulos G, Salituro FG, Jin S, Dang L, Auld DS, Park HW, Cantley LC, Thomas CJ, Vander Heiden MG.

Nat Chem Biol. 2012 Oct;8(10):839-47. Erratum in: Nat Chem Biol. 2012 Dec;8(12):1008.

26.

2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.

Walsh MJ, Brimacombe KR, Veith H, Bougie JM, Daniel T, Leister W, Cantley LC, Israelsen WJ, Vander Heiden MG, Shen M, Auld DS, Thomas CJ, Boxer MB.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6322-7. doi: 10.1016/j.bmcl.2011.08.114. Epub 2011 Sep 14.

27.

Synthesis and structure-activity evaluation of isatin-β-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein.

Hall MD, Brimacombe KR, Varonka MS, Pluchino KM, Monda JK, Li J, Walsh MJ, Boxer MB, Warren TH, Fales HM, Gottesman MM.

J Med Chem. 2011 Aug 25;54(16):5878-89. doi: 10.1021/jm2006047. Epub 2011 Aug 1.

28.

Collateral sensitivity of multidrug-resistant cells to the orphan drug tiopronin.

Goldsborough AS, Handley MD, Dulcey AE, Pluchino KM, Kannan P, Brimacombe KR, Hall MD, Griffiths G, Gottesman MM.

J Med Chem. 2011 Jul 28;54(14):4987-97. doi: 10.1021/jm2001663. Epub 2011 Jun 24.

29.

Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PET.

Kannan P, Brimacombe KR, Kreisl WC, Liow JS, Zoghbi SS, Telu S, Zhang Y, Pike VW, Halldin C, Gottesman MM, Innis RB, Hall MD.

Proc Natl Acad Sci U S A. 2011 Feb 8;108(6):2593-8. doi: 10.1073/pnas.1014641108. Epub 2011 Jan 24.

30.

N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrier.

Kannan P, Brimacombe KR, Zoghbi SS, Liow JS, Morse C, Taku AK, Pike VW, Halldin C, Innis RB, Gottesman MM, Hall MD.

Drug Metab Dispos. 2010 Jun;38(6):917-22. doi: 10.1124/dmd.109.031161. Epub 2010 Mar 8.

31.

Muscleblind-like 1 is a negative regulator of TGF-beta-dependent epithelial-mesenchymal transition of atrioventricular canal endocardial cells.

Vajda NA, Brimacombe KR, LeMasters KE, Ladd AN.

Dev Dyn. 2009 Dec;238(12):3266-72. doi: 10.1002/dvdy.22155.

32.

A dual-fluorescence high-throughput cell line system for probing multidrug resistance.

Brimacombe KR, Hall MD, Auld DS, Inglese J, Austin CP, Gottesman MM, Fung KL.

Assay Drug Dev Technol. 2009 Jun;7(3):233-49. doi: 10.1089/adt.2008.165.

33.

Effective transvascular delivery of nanoparticles across the blood-brain tumor barrier into malignant glioma cells.

Sarin H, Kanevsky AS, Wu H, Brimacombe KR, Fung SH, Sousa AA, Auh S, Wilson CM, Sharma K, Aronova MA, Leapman RD, Griffiths GL, Hall MD.

J Transl Med. 2008 Dec 18;6:80. doi: 10.1186/1479-5876-6-80.

34.

CELF-mediated alternative splicing is required for cardiac function during early, but not later, postnatal life.

Terenzi F, Brimacombe KR, Penn MS, Ladd AN.

J Mol Cell Cardiol. 2009 Mar;46(3):395-404. doi: 10.1016/j.yjmcc.2008.10.030. Epub 2008 Nov 24.

PMID:
19073192
35.

Cloning and embryonic expression patterns of the chicken CELF family.

Brimacombe KR, Ladd AN.

Dev Dyn. 2007 Aug;236(8):2216-24.

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