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Items: 31

1.

Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.

Shen S, Hadley M, Ustinova K, Pavlicek J, Knox T, Noonepalle S, Tavares MT, Zimprich CA, Zhang G, Robers MB, Bařinka C, Kozikowski AP, Villagra A.

J Med Chem. 2019 Sep 26;62(18):8557-8577. doi: 10.1021/acs.jmedchem.9b00946. Epub 2019 Sep 4.

PMID:
31414801
2.

Utilizing a Simple Method for Stoichiometric Protein Labeling to Quantify Antibody Blockade.

Friedman Ohana R, Hurst R, Rosenblatt M, Levin S, Machleidt T, Kirkland TA, Encell LP, Robers MB, Wood KV.

Sci Rep. 2019 May 7;9(1):7046. doi: 10.1038/s41598-019-43469-z.

3.

Complex Formation between VEGFR2 and the β2-Adrenoceptor.

Kilpatrick LE, Alcobia DC, White CW, Peach CJ, Glenn JR, Zimmerman K, Kondrashov A, Pfleger KDG, Ohana RF, Robers MB, Wood KV, Sloan EK, Woolard J, Hill SJ.

Cell Chem Biol. 2019 Jun 20;26(6):830-841.e9. doi: 10.1016/j.chembiol.2019.02.014. Epub 2019 Apr 4.

4.

Quantitative, Real-Time Measurements of Intracellular Target Engagement Using Energy Transfer.

Robers MB, Vasta JD, Corona CR, Ohana RF, Hurst R, Jhala MA, Comess KM, Wood KV.

Methods Mol Biol. 2019;1888:45-71. doi: 10.1007/978-1-4939-8891-4_3.

PMID:
30519940
5.

Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and Learning Impairments in a Mouse Model of Fragile X Syndrome.

Kozikowski AP, Shen S, Pardo M, Tavares MT, Szarics D, Benoy V, Zimprich CA, Kutil Z, Zhang G, Bařinka C, Robers MB, Van Den Bosch L, Eubanks JH, Jope RS.

ACS Chem Neurosci. 2019 Mar 20;10(3):1679-1695. doi: 10.1021/acschemneuro.8b00600. Epub 2018 Dec 14.

PMID:
30511829
6.

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.

Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs AP, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB, Vasta JD, Thezenas ML, Bonham S, Kessler B, Bennett J, Fedorov O, Raynaud F, Donovan A, Blagg J, Bavetsias V, Oppermann U, Bountra C, Kawamura A, Brennan PE.

Angew Chem Int Ed Engl. 2019 Jan 8;58(2):515-519. doi: 10.1002/anie.201810179. Epub 2018 Dec 7.

7.

Binding Kinetics Survey of the Drugged Kinome.

Georgi V, Schiele F, Berger BT, Steffen A, Marin Zapata PA, Briem H, Menz S, Preusse C, Vasta JD, Robers MB, Brands M, Knapp S, Fernández-Montalván A.

J Am Chem Soc. 2018 Nov 21;140(46):15774-15782. doi: 10.1021/jacs.8b08048. Epub 2018 Nov 6.

PMID:
30362749
8.

Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action.

Riching KM, Mahan S, Corona CR, McDougall M, Vasta JD, Robers MB, Urh M, Daniels DL.

ACS Chem Biol. 2018 Sep 21;13(9):2758-2770. doi: 10.1021/acschembio.8b00692. Epub 2018 Aug 30.

9.

Real-Time Ligand Binding of Fluorescent VEGF-A Isoforms that Discriminate between VEGFR2 and NRP1 in Living Cells.

Peach CJ, Kilpatrick LE, Friedman-Ohana R, Zimmerman K, Robers MB, Wood KV, Woolard J, Hill SJ.

Cell Chem Biol. 2018 Oct 18;25(10):1208-1218.e5. doi: 10.1016/j.chembiol.2018.06.012. Epub 2018 Jul 26.

10.

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.

11.

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.

12.

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.

13.

Histone deacetylase inhibitor thailandepsin-A activates Notch signaling and suppresses neuroendocrine cancer cell growth in vivo.

Jang S, Janssen A, Aburjania Z, Robers MB, Harrison A, Dammalapati A, Cheng YQ, Chen H, Jaskula-Sztul R.

Oncotarget. 2017 Aug 7;8(41):70828-70840. doi: 10.18632/oncotarget.19993. eCollection 2017 Sep 19.

14.

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.

15.

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.

PMID:
28195704
16.

Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket.

Forster M, Chaikuad A, Bauer SM, Holstein J, Robers MB, Corona CR, Gehringer M, Pfaffenrot E, Ghoreschi K, Knapp S, Laufer SA.

Cell Chem Biol. 2016 Nov 17;23(11):1335-1340. doi: 10.1016/j.chembiol.2016.10.008. Epub 2016 Nov 10.

17.

Potent and selective bivalent inhibitors of BET bromodomains.

Waring MJ, Chen H, Rabow AA, Walker G, Bobby R, Boiko S, Bradbury RH, Callis R, Clark E, Dale I, Daniels DL, Dulak A, Flavell L, Holdgate G, Jowitt TA, Kikhney A, McAlister M, Méndez J, Ogg D, Patel J, Petteruti P, Robb GR, Robers MB, Saif S, Stratton N, Svergun DI, Wang W, Whittaker D, Wilson DM, Yao Y.

Nat Chem Biol. 2016 Dec;12(12):1097-1104. doi: 10.1038/nchembio.2210. Epub 2016 Oct 24.

PMID:
27775716
18.

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.

19.

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.

PMID:
26278171
20.

Deciphering the Cellular Targets of Bioactive Compounds Using a Chloroalkane Capture Tag.

Ohana RF, Kirkland TA, Woodroofe CC, Levin S, Uyeda HT, Otto P, Hurst R, Robers MB, Zimmerman K, Encell LP, Wood KV.

ACS Chem Biol. 2015 Oct 16;10(10):2316-24. doi: 10.1021/acschembio.5b00351. Epub 2015 Aug 6.

21.

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.

22.

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.

23.

Tumor-suppressor role of Notch3 in medullary thyroid carcinoma revealed by genetic and pharmacological induction.

Jaskula-Sztul R, Eide J, Tesfazghi S, Dammalapati A, Harrison AD, Yu XM, Scheinebeck C, Winston-McPherson G, Kupcho KR, Robers MB, Hundal AK, Tang W, Chen H.

Mol Cancer Ther. 2015 Feb;14(2):499-512. doi: 10.1158/1535-7163.MCT-14-0073. Epub 2014 Dec 15.

24.

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.

25.

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.

PMID:
21972037
26.

Measurement of the cellular deacetylase activity of SIRT1 on p53 via LanthaScreen® technology.

Robers MB, Loh C, Carlson CB, Yang H, Frey EA, Hermanson SB, Bi K.

Mol Biosyst. 2011 Jan;7(1):59-66. doi: 10.1039/c0mb00026d. Epub 2010 Oct 8.

PMID:
20931131
27.

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.

PMID:
19539597
28.

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.

PMID:
19196698
29.

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.

PMID:
18694336
30.

Pharmacological characterization of purified recombinant mTOR FRB-kinase domain using fluorescence-based assays.

Reichling LJ, Lebakken CS, Riddle SM, Vedvik KL, Robers MB, Kopp LM, Bruinsma R, Vogel KW.

J Biomol Screen. 2008 Mar;13(3):238-44. doi: 10.1177/1087057108314609.

PMID:
18354135
31.

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.

PMID:
17961489

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