The Spatiotemporal Regulation of the Keap1/Nrf2 Pathway (Joint with University College London)

2022

Detection of thermal shift in cellular Keap1 by protein-protein interaction inhibitors using immunoblot- and fluorescence microplate-based assays

Dayalan Naidu, S., Dikovskaya, D., Moore, T. W. & Dinkova-Kostova, A. (Lead / Corresponding author), 17 Jun 2022, In: STAR Protocols. 3, 2, 17 p., 101265.

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8 Citations (Scopus)

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Phenyl Bis-Sulfonamide Keap1-Nrf2 Protein-Protein Interaction Inhibitors with an Alternative Binding Mode

Georgakopoulos, N., Talapatra, S., Dikovskaya, D., Dayalan Naidu, S., Higgins, M., Gatliff, J., Ayhan, A., Nikoloudaki, R., Schaap, M., Valko, K., Javid, F., Dinkova-Kostova, A. T., Kozielski, F. & Wells, G. (Lead / Corresponding author), 26 May 2022, In: Journal of Medicinal Chemistry. 65, 10, p. 7380-7398 19 p.

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18 Citations (Scopus)

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The isoquinoline PRL-295 increases the thermostability of Keap1 and disrupts its interaction with Nrf2

Dayalan Naidu, S., Suzuki, T., Dikovskaya, D., Knatko, E. V., Higgins, M., Sato, M., Novak, M., Villegas, J. A., Moore, T. W., Yamamoto, M. & Dinkova-Kostova, A. (Lead / Corresponding author), 21 Jan 2022, In: iScience. 25, 1, 19 p., 103703.

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18 Citations (Scopus)

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2021

Novel iodinated quinazolinones bearing sulfonamide as new scaffold targeting radiation induced oxidative stress

Soliman, A. M. (Lead / Corresponding author), Mekkawy, M. H., Karam, H. M., Higgins, M., Dinkova-kostova, A. T. & Ghorab, M. M. (Lead / Corresponding author), 15 Jun 2021, In: Bioorganic & Medicinal Chemistry Letters. 42, 9 p., 128002.

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9 Citations (Scopus)

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2020

Measuring Changes in Keap1‐Nrf2 Protein Complex Conformation in Individual Cells by FLIM‐FRET

Dikovskaya, D. (Lead / Corresponding author) & Dinkova-Kostova, A., Sept 2020, In: Current Protocols in Toxicology. 85, 1, 34 p., e96.

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2 Citations (Scopus)

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Nrf2 is activated by disruption of mitochondrial thiol homeostasis but not by enhanced mitochondrial superoxide production

Cvetko, F., Caldwell, S. T., Higgins, M., Suzuki, T., Yamamoto, M., Prag, H. A., Hartley, R. C., Dinkova-Kostova, A. & Murphy, M. P. (Lead / Corresponding author), 20 Dec 2020, In: Journal of Biological Chemistry. 296, 14 p., 100169.

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32 Citations (Scopus)

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Sulfoxythiocarbamate S-4 inhibits HSP90 in human cutaneous squamous cell carcinoma cells

Zhang, Y., VanHecke, G. C., Ahn, Y.-H., Proby, C. M. & Dinkova-Kostova, A. T. (Lead / Corresponding author), 15 Dec 2020, In: European Journal of Pharmacology. 889, 9 p., 173609.

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4 Citations (Scopus)

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2019

Investigation into the use of histone deacetylase inhibitor MS-275 as a topical agent for the prevention and treatment of cutaneous squamous cell carcinoma in an SKH-1 hairless mouse model

Kalin, J. H. (Lead / Corresponding author), Eroglu, A., Liu, H., Holtzclaw, W. D., Leigh, I., Proby, C. M., Fahey, J. W., Cole, P. A. & Dinkova-Kostova, A. T. (Lead / Corresponding author), 13 Mar 2019, In: PLoS ONE. 14, 3, 13 p., e0213095.

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16 Citations (Scopus)

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Measuring the Interaction of Transcription Factor Nrf2 with Its Negative Regulator Keap1 in Single Live Cells by an Improved FRET/FLIM Analysis

Dikovskaya, D. (Lead / Corresponding author), Appleton, P., Bento-Pereira, C. & Dinkova-Kostova, A. (Lead / Corresponding author), 18 Mar 2019, In: Chemical Research in Toxicology. 32, 3, p. 500-512 13 p.

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8 Citations (Scopus)

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2018

C151 in KEAP1 is the main cysteine sensor for the cyanoenone class of NRF2 activators, irrespective of molecular size or shape

Dayalan Naidu, S., Muramatsu, A., Saito, R., Asami, S., Honda, T., Hosoya, T., Itoh, K., Yamamoto, M., Suzuki, T. & Dinkova-Kostova, A. (Lead / Corresponding author), 23 May 2018, In: Scientific Reports. 8, 1, p. 1-12 12 p., 8037.

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70 Citations (Scopus)

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Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1

Mills, E. L., Ryan, D. G., Prag, H. A., Dikovskaya, D., Menon, D., Zaslona, Z., Jedrychowski, M. P., Costa, A. S. H., Higgins, M., Hams, E., Szpyt, J., Runtsch, M. C., King, M. S., McGouran, J. F., Fischer, R., Kessler, B. M., McGettrick, A. F., Hughes, M. M., Carroll, R. G. & Booty, L. M. & 15 others, Knatko, E. V., Meakin, P. J., Ashford, M. L. J., Modis, L. K., Brunori, G., Sévin, D. C., Fallon, P. G., Caldwell, S. T., Kunji, E. R. S., Chouchani, E. T., Frezza, C., Dinkova-Kostova, A. T., Hartley, R. C., Murphy, M. P. & O'Neill, L. A. (Lead / Corresponding author), 5 Apr 2018, In: Nature. 556, 7699, p. 113-117 5 p.

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1338 Citations (Scopus)

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KEAP₁ inhibition is neuroprotective and suppresses the development of epilepsy

Shekh-Ahmad, T., Eckel, R., Dayalan Naidu, S., Higgins, M., Yamamoto, M., Dinkova-Kostova, A., Kovac, S., Abramov, A. Y. (Lead / Corresponding author) & Walker, M. C. (Lead / Corresponding author), May 2018, In: Brain. 141, 5, p. 1390-1403 14 p.

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110 Citations (Scopus)

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2017

Activation of Nrf2 signaling augments Vesicular Stomatitis Virus Oncolysis via Autophagy-Driven Suppression of Antiviral Immunity

Olagnier, D. (Lead / Corresponding author), Lababidi, R. R., Bel Hadj, S., Sze, A., Liu, Y., Dayalan Naidu, S., Ferrari, M., Jiang, Y., Chiang, C., Beljanski, V., Goulet, M.-L., Knatko, E. V., Dinkova-Kostova, A. T., Hiscott, J. (Lead / Corresponding author) & Lin, R. (Lead / Corresponding author), 2 Aug 2017, In: Molecular Therapy. 25, 8, p. 1900-1916 17 p.

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71 Citations (Scopus)

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Epigenetic Control of NRF2-Directed Cellular Antioxidant Status in Dictating Life-Death Decisions

Hayes, J. D. (Lead / Corresponding author) & Dinkova-Kostova, A. T., 5 Oct 2017, In: Molecular Cell. 68, 1, p. 5-7 3 p.

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23 Citations (Scopus)

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KEAP1-modifying small molecule reveals muted NRF2 signaling responses in neural stem cells from Huntington's disease patients

Quinti, L., Dayalan Naidu, S., Träge, U., Chen, X., Kegel-Gleason, K., Lleres, D., Connolly, C., Chopra, V., Low, C., Moniot, S., Sapp, E., Tousley, A. R., Vodicka, P., Van Kanegan, M. J., Kaltenbach, L. S., Crawford, L. A., Fuszard, M., Higgins, M., Miller, J. R. C. & Farmer, R. E. & 19 others, Potluri, V., Samajdar, S., Meisel, L., Zhang, N., Snyder, A., Stein, R., Hersch, S. M., Ellerby, L. M., Weerapana, E., Schwarzschild, M. A., Steegborn, C., Leavitt, B. R., Degterev, A., Tabrizi, S. J., Lo, D. C., DiFiglia, M., Thompson, L. M., Dinkova-Kostova, A. & Kazantsev, A. G. (Lead / Corresponding author), 6 Jun 2017, In: Proceedings of the National Academy of Sciences of the United States of America. 114, 23, p. e4676-e4685 10 p.

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113 Citations (Scopus)

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Oncogene-Stimulated Congestion at the KEAP1 Stress Signaling Hub Allows Bypass of NRF2 and Induction of NRF2-Target Genes that Promote Tumor Survival

Hayes, J. D. & Dinkova-Kostova, A. T. (Lead / Corresponding author), Nov 2017, In: Cancer Cell. 32, 5, p. 539-541 3 p.

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25 Citations (Scopus)

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Transcription factors NRF2 and HSF1 have opposing functions in autophagy

Dayalan Naidu, S., Dikovskaya, D., Gaurilcikaite, E., Knatko, E., Healy, Z. R., Mohan, H., Koh, G., Laurell, A., Ball, G., Olagnier, D., de la Vega, L., Ganley, I., Talalay, P. & Dinkova-Kostova, A. (Lead / Corresponding author), 8 Sept 2017, In: Scientific Reports. 7, p. 1-12 12 p., 11023.

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35 Citations (Scopus)

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2016

Nrf2 activation in the treatment of neurodegenerative diseases: A focus on its role in mitochondrial bioenergetics and function

Esteras, N. (Lead / Corresponding author), Dinkova-Kostova, A. T. & Abramov, A. Y. (Lead / Corresponding author), May 2016, In: Biological Chemistry. 397, 5, p. 383-400 18 p.

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141 Citations (Scopus)

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SIRT2- and NRF2-Targeting Thiazole-Containing Compound with Therapeutic Activity in Huntington's Disease Models

Quinti, L., Casale, M., Moniot, S., Pais, T. F., Van Kanegan, M. J., Kaltenbach, L. S., Pallos, J., Lim, R. G., Naidu, S. D., Runne, H., Meisel, L., Rauf, N. A., Leyfer, D., Maxwell, M. M., Saiah, E., Landers, J. E., Luthi-Carter, R., Abagyan, R., Dinkova-Kostova, A. T. & Steegborn, C. & 4 others, Marsh, J. L., Lo, D. C., Thompson, L. M. & Kazantsev, A. G., 21 Jul 2016, In: Cell Chemical Biology. 23, 7, p. 849-861 13 p.

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78 Citations (Scopus)

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2015

Design, synthesis, and evaluation of triazole derivatives that induce Nrf2 dependent gene products and inhibit the Keap1-Nrf2 protein-protein interaction

Bertrand, H. C., Schaap, M., Baird, L., Georgakopoulos, N. D., Fowkes, A., Thiollier, C., Kachi, H., Dinkova-Kostova, A. T. & Wells, G. (Lead / Corresponding author), 24 Sept 2015, In: Journal of Medicinal Chemistry. 58, 18, p. 7186-7194 9 p.

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105 Citations (Scopus)

Mechanisms of activation of the transcription factor Nrf2 by redox stressors, nutrient cues, and energy status and the pathways through which it attenuates degenerative disease

Tebay, L. E., Robertson, H., Durant, S. T., Vitale, S. R., Penning, T. M., Dinkova-Kostova, A. T. & Hayes, J. D. (Lead / Corresponding author), Nov 2015, In: Free Radical Biology and Medicine. 88, Part B, p. 108-146 39 p.

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724 Citations (Scopus)

New monocyclic, bicyclic, and tricyclic ethynylcyanodienones as activators of the Keap1/Nrf2/ARE pathway and inhibitors of inducible nitric oxide synthase

Li, W., Zheng, S., Higgins, M., Morra, R. P., Mendis, A. T., Chien, C.-W., Ojima, I., Mierke, D. F., Dinkova-Kostova, A. T. & Honda, T. (Lead / Corresponding author), 11 Jun 2015, In: Journal of Medicinal Chemistry. 58, 11, p. 4738-4748 11 p.

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28 Citations (Scopus)

The emerging role of Nrf2 in mitochondrial function

Dinkova-Kostova, A. T. (Lead / Corresponding author) & Abramov, A. Y. (Lead / Corresponding author), Nov 2015, In: Free Radical Biology and Medicine. 88, Part B, p. 179-188 10 p.

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795 Citations (Scopus)

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The spatiotemporal regulation of the Keap1-Nrf2 pathway and its importance in cellular bioenergetics

Dinkova-Kostova, A. T. (Lead / Corresponding author), Baird, L., Holmström, K. M., Meyer, C. J. & Abramov, A. Y. (Lead / Corresponding author), Aug 2015, In: Biochemical Society Transactions. 43, 4, p. 602-610 9 p.

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77 Citations (Scopus)

Transcription factors Hsf1 and Nrf2 engage in crosstalk for cytoprotection

Dayalan Naidu, S., Kostov, R. V. & Dinkova-Kostova, A. T. (Lead / Corresponding author), Jan 2015, In: Trends in Pharmacological Sciences. 36, 1, p. 6-14 9 p.

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119 Citations (Scopus)

The Spatiotemporal Regulation of the Keap1/Nrf2 Pathway (Joint with University College London)

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