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Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift.

Dart ML, Machleidt T, Jost E, Schwinn MK, Robers MB, Shi C, Kirkland TA, Killoran MP, Wilkinson JM, Hartnett JR, Zimmerman K, Wood KV.

ACS Med Chem Lett. 2018 Apr 16;9(6):546-551. doi: 10.1021/acsmedchemlett.8b00081. eCollection 2018 Jun 14.


Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia.

Wagner FF, Benajiba L, Campbell AJ, Weïwer M, Sacher JR, Gale JP, Ross L, Puissant A, Alexe G, Conway A, Back M, Pikman Y, Galinsky I, DeAngelo DJ, Stone RM, Kaya T, Shi X, Robers MB, Machleidt T, Wilkinson J, Hermine O, Kung A, Stein AJ, Lakshminarasimhan D, Hemann MT, Scolnick E, Zhang YL, Pan JQ, Stegmaier K, Holson EB.

Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460. doi: 10.1126/scitranslmed.aam8460.


Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.

Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Hartnett JR, Ingold MR, Zimmerman K, Machleidt T, Kirkland TA, Huwiler KG, Ohana RF, Slater M, Otto P, Cong M, Wells CI, Berger BT, Hanke T, Glas C, Ding K, Drewry DH, Huber KVM, Willson TM, Knapp S, Müller S, Meisenheimer PL, Fan F, Wood KV, Robers MB.

Cell Chem Biol. 2018 Feb 15;25(2):206-214.e11. doi: 10.1016/j.chembiol.2017.10.010. Epub 2017 Nov 22.


Coelenterazine analogues emit red-shifted bioluminescence with NanoLuc.

Shakhmin A, Hall MP, Machleidt T, Walker JR, Wood KV, Kirkland TA.

Org Biomol Chem. 2017 Oct 18;15(40):8559-8567. doi: 10.1039/c7ob01985h.


CRISPR-Mediated Tagging of Endogenous Proteins with a Luminescent Peptide.

Schwinn MK, Machleidt T, Zimmerman K, Eggers CT, Dixon AS, Hurst R, Hall MP, Encell LP, Binkowski BF, Wood KV.

ACS Chem Biol. 2018 Feb 16;13(2):467-474. doi: 10.1021/acschembio.7b00549. Epub 2017 Sep 21.


Cell-based, bioluminescent assay for monitoring the interaction between PCSK9 and the LDL receptor.

Duellman SJ, Machleidt T, Cali JJ, Vidugiriene J.

J Lipid Res. 2017 Aug;58(8):1722-1729. doi: 10.1194/jlr.D074658. Epub 2017 Jun 13.


Real-time analysis of the binding of fluorescent VEGF165a to VEGFR2 in living cells: Effect of receptor tyrosine kinase inhibitors and fate of internalized agonist-receptor complexes.

Kilpatrick LE, Friedman-Ohana R, Alcobia DC, Riching K, Peach CJ, Wheal AJ, Briddon SJ, Robers MB, Zimmerman K, Machleidt T, Wood KV, Woolard J, Hill SJ.

Biochem Pharmacol. 2017 Jul 15;136:62-75. doi: 10.1016/j.bcp.2017.04.006. Epub 2017 Apr 7.


Highly Potent Cell-Permeable and Impermeable NanoLuc Luciferase Inhibitors.

Walker JR, Hall MP, Zimprich CA, Robers MB, Duellman SJ, Machleidt T, Rodriguez J, Zhou W.

ACS Chem Biol. 2017 Apr 21;12(4):1028-1037. doi: 10.1021/acschembio.6b01129. Epub 2017 Feb 22.


Three Efficient Methods for Preparation of Coelenterazine Analogues.

Shakhmin A, Hall MP, Walker JR, Machleidt T, Binkowski BF, Wood KV, Kirkland TA.

Chemistry. 2016 Jul 18;22(30):10369-75. doi: 10.1002/chem.201601111. Epub 2016 Jun 15.


Target engagement and drug residence time can be observed in living cells with BRET.

Robers MB, Dart ML, Woodroofe CC, Zimprich CA, Kirkland TA, Machleidt T, Kupcho KR, Levin S, Hartnett JR, Zimmerman K, Niles AL, Ohana RF, Daniels DL, Slater M, Wood MG, Cong M, Cheng YQ, Wood KV.

Nat Commun. 2015 Dec 3;6:10091. doi: 10.1038/ncomms10091.


NanoLuc Complementation Reporter Optimized for Accurate Measurement of Protein Interactions in Cells.

Dixon AS, Schwinn MK, Hall MP, Zimmerman K, Otto P, Lubben TH, Butler BL, Binkowski BF, Machleidt T, Kirkland TA, Wood MG, Eggers CT, Encell LP, Wood KV.

ACS Chem Biol. 2016 Feb 19;11(2):400-8. doi: 10.1021/acschembio.5b00753. Epub 2015 Dec 10.


A luminescent assay for real-time measurements of receptor endocytosis in living cells.

Robers MB, Binkowski BF, Cong M, Zimprich C, Corona C, McDougall M, Otto G, Eggers CT, Hartnett J, Machleidt T, Fan F, Wood KV.

Anal Biochem. 2015 Nov 15;489:1-8. doi: 10.1016/j.ab.2015.08.005. Epub 2015 Aug 13.


Application of BRET to monitor ligand binding to GPCRs.

Stoddart LA, Johnstone EKM, Wheal AJ, Goulding J, Robers MB, Machleidt T, Wood KV, Hill SJ, Pfleger KDG.

Nat Methods. 2015 Jul;12(7):661-663. doi: 10.1038/nmeth.3398. Epub 2015 Jun 1.


NanoBRET--A Novel BRET Platform for the Analysis of Protein-Protein Interactions.

Machleidt T, Woodroofe CC, Schwinn MK, Méndez J, Robers MB, Zimmerman K, Otto P, Daniels DL, Kirkland TA, Wood KV.

ACS Chem Biol. 2015 Aug 21;10(8):1797-804. doi: 10.1021/acschembio.5b00143. Epub 2015 Jun 9.


Identification of known drugs targeting the endoplasmic reticulum stress response.

Bi K, Nishihara K, Machleidt T, Hermanson S, Wang J, Sakamuru S, Huang R, Xia M.

Anal Bioanal Chem. 2015 Jul;407(18):5343-51. doi: 10.1007/s00216-015-8694-2. Epub 2015 Apr 30.


Engineered luciferase reporter from a deep sea shrimp utilizing a novel imidazopyrazinone substrate.

Hall MP, Unch J, Binkowski BF, Valley MP, Butler BL, Wood MG, Otto P, Zimmerman K, Vidugiris G, Machleidt T, Robers MB, Benink HA, Eggers CT, Slater MR, Meisenheimer PL, Klaubert DH, Fan F, Encell LP, Wood KV.

ACS Chem Biol. 2012 Nov 16;7(11):1848-57. doi: 10.1021/cb3002478. Epub 2012 Aug 30.


Discovery of potent and selective covalent inhibitors of JNK.

Zhang T, Inesta-Vaquera F, Niepel M, Zhang J, Ficarro SB, Machleidt T, Xie T, Marto JA, Kim N, Sim T, Laughlin JD, Park H, LoGrasso PV, Patricelli M, Nomanbhoy TK, Sorger PK, Alessi DR, Gray NS.

Chem Biol. 2012 Jan 27;19(1):140-54. doi: 10.1016/j.chembiol.2011.11.010.


TR-FRET cellular assays for interrogating posttranslational modifications of histone H3.

Machleidt T, Robers MB, Hermanson SB, Dudek JM, Bi K.

J Biomol Screen. 2011 Dec;16(10):1236-46. doi: 10.1177/1087057111422943. Epub 2011 Oct 4.


Design and characterization of a potent and selective dual ATP- and substrate-competitive subnanomolar bidentate c-Jun N-terminal kinase (JNK) inhibitor.

Stebbins JL, De SK, Pavlickova P, Chen V, Machleidt T, Chen LH, Kuntzen C, Kitada S, Karin M, Pellecchia M.

J Med Chem. 2011 Sep 22;54(18):6206-14. doi: 10.1021/jm200479c. Epub 2011 Aug 23.


Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase.

De SK, Barile E, Chen V, Stebbins JL, Cellitti JF, Machleidt T, Carlson CB, Yang L, Dahl R, Pellecchia M.

Bioorg Med Chem. 2011 Apr 15;19(8):2582-8. doi: 10.1016/j.bmc.2011.03.017. Epub 2011 Mar 12.


Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.

De SK, Chen V, Stebbins JL, Chen LH, Cellitti JF, Machleidt T, Barile E, Riel-Mehan M, Dahl R, Yang L, Emdadi A, Murphy R, Pellecchia M.

Bioorg Med Chem. 2010 Jan 15;18(2):590-6. doi: 10.1016/j.bmc.2009.12.013. Epub 2009 Dec 11.


Generation of site-specific retargeting platform cell lines for drug discovery using phiC31 and R4 integrases.

Lieu PT, Machleidt T, Thyagarajan B, Fontes A, Frey E, Fuerstenau-Sharp M, Thompson DV, Swamilingiah GM, Derebail SS, Piper D, Chesnut JD.

J Biomol Screen. 2009 Dec;14(10):1207-15. doi: 10.1177/1087057109348941.


Characterization of serotonin 5-hydroxytryptamine-1A receptor activation using a phospho-extracellular-signal regulated kinase 2 sensor.

Huwiler KG, Machleidt T, Chase L, Hanson B, Robers MB.

Anal Biochem. 2009 Oct 1;393(1):95-104. doi: 10.1016/j.ab.2009.06.018. Epub 2009 Jun 17.


Multiplexing of pathway-specific beta-lactamase reporter gene assays by optical coding with Qtracker nanocrystals.

Machleidt T, Whitney P, Bi K.

J Biomol Screen. 2009 Aug;14(7):845-52. doi: 10.1177/1087057109335742. Epub 2009 Jun 5.


Discovery of 2-(5-nitrothiazol-2-ylthio)benzo[d]thiazoles as novel c-Jun N-terminal kinase inhibitors.

De SK, Chen LH, Stebbins JL, Machleidt T, Riel-Mehan M, Dahl R, Chen V, Yuan H, Barile E, Emdadi A, Murphy R, Pellecchia M.

Bioorg Med Chem. 2009 Apr 1;17(7):2712-7. doi: 10.1016/j.bmc.2009.02.046. Epub 2009 Feb 26.


Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase.

De SK, Stebbins JL, Chen LH, Riel-Mehan M, Machleidt T, Dahl R, Yuan H, Emdadi A, Barile E, Chen V, Murphy R, Pellecchia M.

J Med Chem. 2009 Apr 9;52(7):1943-52. doi: 10.1021/jm801503n.


Development of LanthaScreen cellular assays for key components within the PI3K/AKT/mTOR pathway.

Carlson CB, Robers MB, Vogel KW, Machleidt T.

J Biomol Screen. 2009 Feb;14(2):121-32. doi: 10.1177/1087057108328132. Epub 2009 Feb 4.


Identification of a new JNK inhibitor targeting the JNK-JIP interaction site.

Stebbins JL, De SK, Machleidt T, Becattini B, Vazquez J, Kuntzen C, Chen LH, Cellitti JF, Riel-Mehan M, Emdadi A, Solinas G, Karin M, Pellecchia M.

Proc Natl Acad Sci U S A. 2008 Oct 28;105(43):16809-13. doi: 10.1073/pnas.0805677105. Epub 2008 Oct 15.


Fluorescent labeling of proteins in living cells using the FKBP12 (F36V) tag.

Robers M, Pinson P, Leong L, Batchelor RH, Gee KR, Machleidt T.

Cytometry A. 2009 Mar;75(3):207-24. doi: 10.1002/cyto.a.20649.


Cellular LanthaScreen and beta-lactamase reporter assays for high-throughput screening of JAK2 inhibitors.

Robers MB, Machleidt T, Carlson CB, Bi K.

Assay Drug Dev Technol. 2008 Aug;6(4):519-29. doi: 10.1089/adt.2008.144.


HTS assays using a disease-relevant cell model for interrogating the MAP kinase pathway initiated by multiple receptors.

Wilkinson JM, Machleidt T, Echeverria VM, Vandenheuvel-Kramer K, Honer J, Zhong Z, Bi K.

Assay Drug Dev Technol. 2008 Jun;6(3):351-9. doi: 10.1089/adt.2007.117.


High-throughput cellular assays for regulated posttranslational modifications.

Robers MB, Horton RA, Bercher MR, Vogel KW, Machleidt T.

Anal Biochem. 2008 Jan 15;372(2):189-97. Epub 2007 Sep 14.


Analysis of nanocrystalline films on rough substrates.

Cimalla V, Machleidt T, Spiess L, Gubisch M, Hotovy I, Romanus H, Ambacher O.

Ultramicroscopy. 2007 Oct;107(10-11):989-94. Epub 2007 May 17.


Using defined structures on very thin foils for characterizing AFM tips.

Machleidt T, Franke KH, Romanus H, Cimalla V, Niebelschütz M, Spiess L, Ambacher O.

Ultramicroscopy. 2007 Oct;107(10-11):1086-90. Epub 2007 May 22.


Protein labeling with FlAsH and ReAsH.

Machleidt T, Robers M, Hanson GT.

Methods Mol Biol. 2007;356:209-20.


Granulysin-derived peptides demonstrate antimicrobial and anti-inflammatory effects against Propionibacterium acnes.

McInturff JE, Wang SJ, Machleidt T, Lin TR, Oren A, Hertz CJ, Krutzik SR, Hart S, Zeh K, Anderson DH, Gallo RL, Modlin RL, Kim J.

J Invest Dermatol. 2005 Aug;125(2):256-63.


Dual control of caveolar membrane traffic by microtubules and the actin cytoskeleton.

Mundy DI, Machleidt T, Ying YS, Anderson RG, Bloom GS.

J Cell Sci. 2002 Nov 15;115(Pt 22):4327-39.


Protein phosphatase 2A associates with and regulates atypical PKC and the epithelial tight junction complex.

Nunbhakdi-Craig V, Machleidt T, Ogris E, Bellotto D, White CL 3rd, Sontag E.

J Cell Biol. 2002 Sep 2;158(5):967-78. Epub 2002 Aug 26.


Human endothelial cell activation and mediator release in response to Listeria monocytogenes virulence factors.

Rose F, Zeller SA, Chakraborty T, Domann E, Machleidt T, Kronke M, Seeger W, Grimminger F, Sibelius U.

Infect Immun. 2001 Feb;69(2):897-905.


Multiple domains in caveolin-1 control its intracellular traffic.

Machleidt T, Li WP, Liu P, Anderson RG.

J Cell Biol. 2000 Jan 10;148(1):17-28.


Identification of caveolin-1 in lipoprotein particles secreted by exocrine cells.

Liu P, Li WP, Machleidt T, Anderson RG.

Nat Cell Biol. 1999 Oct;1(6):369-75.


Inhibition of receptor internalization by monodansylcadaverine selectively blocks p55 tumor necrosis factor receptor death domain signaling.

Schütze S, Machleidt T, Adam D, Schwandner R, Wiegmann K, Kruse ML, Heinrich M, Wickel M, Krönke M.

J Biol Chem. 1999 Apr 9;274(15):10203-12.


Purified truncated recombinant HLA-B7 molecules abrogate cell function in alloreactive cytotoxic T lymphocytes by apoptosis induction.

Hansen B, Janssen E, Machleidt T, Krönke M, Zavazava N.

Transplantation. 1998 Dec 27;66(12):1818-22.


Caspase 7-induced cleavage of kinectin in apoptotic cells.

Machleidt T, Geller P, Schwandner R, Scherer G, Krönke M.

FEBS Lett. 1998 Sep 25;436(1):51-4.


Function of the p55 tumor necrosis factor receptor "death domain" mediated by phosphatidylcholine-specific phospholipase C.

Machleidt T, Krämer B, Adam D, Neumann B, Schütze S, Wiegmann K, Krönke M.

J Exp Med. 1996 Aug 1;184(2):725-33.


Crucial role of 55-kilodalton TNF receptor in TNF-induced adhesion molecule expression and leukocyte organ infiltration.

Neumann B, Machleidt T, Lifka A, Pfeffer K, Vestweber D, Mak TW, Holzmann B, Krönke M.

J Immunol. 1996 Feb 15;156(4):1587-93.


TNF-induced activation of NF-kappa B.

Schütze S, Wiegmann K, Machleidt T, Krönke M.

Immunobiology. 1995 Jul;193(2-4):193-203. Review.


CD28 signals through acidic sphingomyelinase.

Boucher LM, Wiegmann K, Fütterer A, Pfeffer K, Machleidt T, Schütze S, Mak TW, Krönke M.

J Exp Med. 1995 Jun 1;181(6):2059-68.


Superantigen-induced transcriptional activation of the human TNF gene promoter in T cells.

Krämer B, Machleidt T, Wiegmann K, Krönke M.

J Inflamm. 1995;45(3):183-92.


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