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Items: 1 to 50 of 200

1.

Generation of High-Throughput Three-Dimensional Tumor Spheroids for Drug Screening.

Griner LM, Gampa K, Do T, Nguyen H, Farley D, Hogan CJ, Auld DS, Silver SJ.

J Vis Exp. 2018 Sep 5;(139). doi: 10.3791/57476.

PMID:
30247463
2.

Interferences with Luciferase Reporter Enzymes.

Auld DS, Inglese J.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin C, 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, 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-.
2016 Jul 1 [updated 2018 Jul 1].

3.

Receptor Binding Assays for HTS and Drug Discovery.

Auld DS, Farmen MW, Kahl SD, Kriauciunas A, McKnight KL, Montrose C, Weidner JR.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin C, 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, 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-.
2012 May 1 [updated 2018 Jul 1].

4.

A Scalable Pipeline for High-Throughput Flow Cytometry.

Wilson AC, Moutsatsos IK, Yu G, Pineda JJ, Feng Y, Auld DS.

SLAS Discov. 2018 Aug;23(7):708-718. doi: 10.1177/2472555218774770. Epub 2018 May 16.

PMID:
29768981
5.

Characterization and Use of TurboLuc Luciferase as a Reporter for High-Throughput Assays.

Auld DS, Narahari J, Ho PI, Casalena D, Nguyen V, Cirbaite E, Hughes D, Daly J, Webb B.

Biochemistry. 2018 Aug 7;57(31):4700-4706. doi: 10.1021/acs.biochem.8b00290. Epub 2018 Apr 20.

PMID:
29641191
6.

Assay Interference by Aggregation.

Auld DS, Inglese J, Dahlin JL.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin C, 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, 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-. No abstract available.
2017 Jul 26.

7.

Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models.

Davis MI, Pragani R, Fox JT, Shen M, Parmar K, Gaudiano EF, Liu L, Tanega C, McGee L, Hall MD, McKnight C, Shinn P, Nelson H, Chattopadhyay D, D'Andrea AD, Auld DS, DeLucas LJ, Li Z, Boxer MB, Simeonov A.

J Biol Chem. 2016 Nov 18;291(47):24628-24640. Epub 2016 Sep 28.

8.

Matrix-Based Activity Pattern Classification as a Novel Method for the Characterization of Enzyme Inhibitors Derived from High-Throughput Screening.

Auld DS, Jimenez M, Yue K, Busby S, Chen YC, Bowes S, Wendel G, Smith T, Zhang JH.

J Biomol Screen. 2016 Dec;21(10):1075-1089. doi: 10.1177/1087057116667255. Epub 2016 Sep 27.

PMID:
27601436
10.

Examining Ligand-Based Stabilization of Proteins in Cells with MEK1 Kinase Inhibitors.

Auld DS, Davis CA, Jimenez M, Knight S, Orme JP.

Assay Drug Dev Technol. 2015 Jun;13(5):266-76. doi: 10.1089/adt.2014.614. Epub 2015 Jun 24.

PMID:
26107610
11.

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
12.

Variomics screen identifies the re-entrant loop of the calcium-activated chloride channel ANO1 that facilitates channel activation.

Bill A, Popa MO, van Diepen MT, Gutierrez A, Lilley S, Velkova M, Acheson K, Choudhury H, Renaud NA, Auld DS, Gosling M, Groot-Kormelink PJ, Gaither LA.

J Biol Chem. 2015 Jan 9;290(2):889-903. doi: 10.1074/jbc.M114.618140. Epub 2014 Nov 25.

13.

Composition and applications of focus libraries to phenotypic assays.

Wassermann AM, Camargo LM, Auld DS.

Front Pharmacol. 2014 Jul 24;5:164. doi: 10.3389/fphar.2014.00164. eCollection 2014. Review.

14.

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.

15.

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.

16.

Biochemical, cellular, and biophysical characterization of a potent inhibitor of mutant isocitrate dehydrogenase IDH1.

Davis MI, Gross S, Shen M, Straley KS, Pragani R, Lea WA, Popovici-Muller J, DeLaBarre B, Artin E, Thorne N, Auld DS, Li Z, Dang L, Boxer MB, Simeonov A.

J Biol Chem. 2014 May 16;289(20):13717-25. doi: 10.1074/jbc.M113.511030. Epub 2014 Mar 25.

17.

Application of Titration-Based Screening for the Rapid Pilot Testing of High-Throughput Assays.

Zhang JH, Kang ZB, Ardayfio O, Ho PI, Smith T, Wallace I, Bowes S, Hill WA, Auld DS.

J Biomol Screen. 2014 Jun;19(5):651-60. doi: 10.1177/1087057113512151. Epub 2013 Nov 18.

PMID:
24246376
18.

Identification of therapeutic candidates for chronic lymphocytic leukemia from a library of approved drugs.

Shen M, Zhang Y, Saba N, Austin CP, Wiestner A, Auld DS.

PLoS One. 2013 Sep 20;8(9):e75252. doi: 10.1371/journal.pone.0075252. eCollection 2013.

19.

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].

20.

Identification of selective inhibitors of cdc2-like kinases 1 and 4 (Clk1, Clk4).

Coombs TC, Tanega C, Shen M, Neuenswander B, Porubsky P, Wang JL, Misteli T, Auld DS, Schoenen F, Thomas CJ, Aubé J.

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

21.

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].

22.

Modulators of Lipid Storage.

Boxer MB, Shen M, Zhang Y, Liu L, Auld DS, Beller M.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Dec 15 [updated 2013 May 3].

23.

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].

24.

Kinetic characterization of ebselen, chelerythrine and apomorphine as glutaminase inhibitors.

Thomas AG, Rojas C, Tanega C, Shen M, Simeonov A, Boxer MB, Auld DS, Ferraris DV, Tsukamoto T, Slusher BS.

Biochem Biophys Res Commun. 2013 Aug 23;438(2):243-8. doi: 10.1016/j.bbrc.2013.06.110. Epub 2013 Jul 10.

25.

Physicochemical characterization of a thermostable alcohol dehydrogenase from Pyrobaculum aerophilum.

Vitale A, Thorne N, Lovell S, Battaile KP, Hu X, Shen M, D'Auria S, Auld DS.

PLoS One. 2013 Jun 5;8(6):e63828. doi: 10.1371/journal.pone.0063828. Print 2013.

26.

Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.

Coombs TC, Tanega C, Shen M, Wang JL, Auld DS, Gerritz SW, Schoenen FJ, Thomas CJ, Aubé J.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3654-61. doi: 10.1016/j.bmcl.2013.02.096. Epub 2013 Mar 30.

27.

Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays.

Dranchak P, MacArthur R, Guha R, Zuercher WJ, Drewry DH, Auld DS, Inglese J.

PLoS One. 2013;8(3):e57888. doi: 10.1371/journal.pone.0057888. Epub 2013 Mar 7.

28.

Reporter enzyme inhibitor study to aid assembly of orthogonal reporter gene assays.

Ho PI, Yue K, Pandey P, Breault L, Harbinski F, McBride AJ, Webb B, Narahari J, Karassina N, Wood KV, Hill A, Auld DS.

ACS Chem Biol. 2013 May 17;8(5):1009-17. doi: 10.1021/cb3007264. Epub 2013 Mar 26.

PMID:
23485150
29.

Bioluminescent assays for cytochrome P450 enzymes.

Auld DS, Veith H, Cali JJ.

Methods Mol Biol. 2013;987:1-9. doi: 10.1007/978-1-62703-321-3_1.

PMID:
23475663
30.

A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation.

Davis MI, Sasaki AT, Shen M, Emerling BM, Thorne N, Michael S, Pragani R, Boxer M, Sumita K, Takeuchi K, Auld DS, Li Z, Cantley LC, Simeonov A.

PLoS One. 2013;8(1):e54127. doi: 10.1371/journal.pone.0054127. Epub 2013 Jan 10.

31.

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.

32.

Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter.

Thorne N, Shen M, Lea WA, Simeonov A, Lovell S, Auld DS, Inglese J.

Chem Biol. 2012 Aug 24;19(8):1060-72. doi: 10.1016/j.chembiol.2012.07.015.

33.

A new family of covalent inhibitors block nucleotide binding to the active site of pyruvate kinase.

Morgan HP, Walsh MJ, Blackburn EA, Wear MA, Boxer MB, Shen M, Veith H, McNae IW, Nowicki MW, Michels PA, Auld DS, Fothergill-Gilmore LA, Walkinshaw MD.

Biochem J. 2012 Nov 15;448(1):67-72. doi: 10.1042/BJ20121014.

34.

Comparison of compound administration methods in biochemical assays: effects on apparent compound potency using either assay-ready compound plates or pin tool-delivered compounds.

Smith T, Ho PI, Yue K, Itkin Z, MacDougall D, Paolucci M, Hill A, Auld DS.

J Biomol Screen. 2013 Jan;18(1):14-25. doi: 10.1177/1087057112455434. Epub 2012 Aug 17.

PMID:
22904199
35.

Titration-based screening for evaluation of natural product extracts: identification of an aspulvinone family of luciferase inhibitors.

Cruz PG, Auld DS, Schultz PJ, Lovell S, Battaile KP, MacArthur R, Shen M, Tamayo-Castillo G, Inglese J, Sherman DH.

Chem Biol. 2011 Nov 23;18(11):1442-52. doi: 10.1016/j.chembiol.2011.08.011.

36.

Inhibition of pyruvate kinase M2 by reactive oxygen species contributes to cellular antioxidant responses.

Anastasiou D, Poulogiannis G, Asara JM, Boxer MB, Jiang JK, Shen M, Bellinger G, Sasaki AT, Locasale JW, Auld DS, Thomas CJ, Vander Heiden MG, Cantley LC.

Science. 2011 Dec 2;334(6060):1278-83. doi: 10.1126/science.1211485. Epub 2011 Nov 3.

37.

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.

38.

Identification of a novel allosteric binding site in the CXCR2 chemokine receptor.

de Kruijf P, Lim HD, Roumen L, Renjaän VA, Zhao J, Webb ML, Auld DS, Wijkmans JC, Zaman GJ, Smit MJ, de Graaf C, Leurs R.

Mol Pharmacol. 2011 Dec;80(6):1108-18. doi: 10.1124/mol.111.073825. Epub 2011 Sep 23.

PMID:
21948388
39.

A small molecule inhibitor of Caspase 1.

Boxer MB, Shen M, Auld DS, Wells JA, Thomas CJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 25 [updated 2011 Mar 3].

40.

Toward Improved Therapy for Classic Galactosemia.

Boxer MB, Shen M, Tanega C, Tang M, Lai K, Auld DS.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Mar 18 [updated 2011 Mar 3].

41.

An inhibitor of the Cdc2-like kinase 4 (Clk4).

Rosenthal AS, Tanega C, Shen M, Mott BT, Bougie JM, Nguyen DT, Misteli T, Auld DS, Maloney DJ, Thomas CJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Mar 29 [updated 2011 Mar 3].

42.

The trypanocidal drug suramin and other trypan blue mimetics are inhibitors of pyruvate kinases and bind to the adenosine site.

Morgan HP, McNae IW, Nowicki MW, Zhong W, Michels PA, Auld DS, Fothergill-Gilmore LA, Walkinshaw MD.

J Biol Chem. 2011 Sep 9;286(36):31232-40. doi: 10.1074/jbc.M110.212613. Epub 2011 Jul 5.

43.

Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.

Napier SE, Letourneau JJ, Ansari N, Auld DS, Baker J, Best S, Campbell-Wan L, Chan R, Craighead M, Desai H, Ho KK, MacSweeney C, Milne R, Richard Morphy J, Neagu I, Ohlmeyer MH, Pick J, Presland J, Riviello C, Zanetakos HA, Zhao J, Webb ML.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3813-7. doi: 10.1016/j.bmcl.2011.04.022. Epub 2011 Apr 13.

PMID:
21596563
44.

Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).

Rosenthal AS, Tanega C, Shen M, Mott BT, Bougie JM, Nguyen DT, Misteli T, Auld DS, Maloney DJ, Thomas CJ.

Bioorg Med Chem Lett. 2011 May 15;21(10):3152-8. doi: 10.1016/j.bmcl.2011.02.114. Epub 2011 Mar 4.

45.

Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.

Napier SE, Letourneau JJ, Ansari N, Auld DS, Baker J, Best S, Campbell-Wan L, Chan JH, Craighead M, Desai H, Goan KA, Ho KK, Hulskotte EG, MacSweeney CP, Milne R, Morphy JR, Neagu I, Ohlmeyer MH, Peeters AW, Presland J, Riviello C, Ruigt GS, Thomson FJ, Zanetakos HA, Zhao J, Webb ML.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1871-5. doi: 10.1016/j.bmcl.2010.12.081. Epub 2010 Dec 21.

PMID:
21353540
46.

Identification of clinically used drugs that activate pregnane X receptors.

Shukla SJ, Sakamuru S, Huang R, Moeller TA, Shinn P, Vanleer D, Auld DS, Austin CP, Xia M.

Drug Metab Dispos. 2011 Jan;39(1):151-9. doi: 10.1124/dmd.110.035105. Epub 2010 Oct 21. Erratum in: Drug Metab Dispos. 2011 Feb;39(2):351.

47.

Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists.

Letourneau JJ, Riviello CM, Li H, Cole AG, Ho KK, Zanetakos HA, Desai H, Zhao J, Auld DS, Napier SE, Thomson FJ, Goan KA, Morphy JR, Ohlmeyer MH, Webb ML.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5394-7. doi: 10.1016/j.bmcl.2010.07.118. Epub 2010 Aug 1.

PMID:
20719508
48.

Illuminating insights into firefly luciferase and other bioluminescent reporters used in chemical biology.

Thorne N, Inglese J, Auld DS.

Chem Biol. 2010 Jun 25;17(6):646-57. doi: 10.1016/j.chembiol.2010.05.012. Review.

49.

Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase.

Jiang JK, Boxer MB, Vander Heiden MG, Shen M, Skoumbourdis AP, Southall N, Veith H, Leister W, Austin CP, Park HW, Inglese J, Cantley LC, Auld DS, Thomas CJ.

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3387-93. doi: 10.1016/j.bmcl.2010.04.015. Epub 2010 Apr 11.

50.

Apparent activity in high-throughput screening: origins of compound-dependent assay interference.

Thorne N, Auld DS, Inglese J.

Curr Opin Chem Biol. 2010 Jun;14(3):315-24. doi: 10.1016/j.cbpa.2010.03.020. Epub 2010 Apr 22. Review.

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