Stressing out with electrophiles.

Stanton C, Nutsch K, Bollong MJ.Nat Chem Biol. 2024 Oct 24. doi: 10.1038/s41589-024-01749-4.

PMID: 39448843 

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Identification of Tunable, Environmentally Responsive Fluorogenic Dyes by High-Throughput Screening.

You S, Nguyen T, Li-Ma C, Bollong MJ.

ACS Chem Biol. 2024 Sep 9. doi: 10.1021/acschembio.4c00373. 

PMID: 39250827

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HPPE Activates NRF2 Signaling by Liberating Heavy Metal Stores.

Freeman R, Bollong M.

Chembiochem. 2024 Sep 6:e202400529. doi: 10.1002/cbic.202400529. 

PMID: 39240245

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Metabolically activated proteostasis regulators that protect against erastin-induced ferroptosis.

Kline GM, Madrazo N, Cole CM, Pannikkat M, Bollong MJ, Rosarda JD, Kelly JW, Wiseman RL.RSC Chem Biol. 2024 Jul 17;5(9):866-876. doi: 10.1039/d4cb00027g

PMID: 39211477 

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The glycolytic metabolite methylglyoxal covalently inactivates the NLRP3 inflammasome.

Stanton C, Buasakdi C, Sun J, Levitan I, Bora P, Kutseikin S, Wiseman RL, Bollong MJ.

Cell Rep. 2024 Aug 27;43(9):114688. doi: 10.1016/j.celrep.2024.114688.

PMID: 39196782

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Pharmacological expansion of type 2 alveolar epithelial cells promotes regenerative lower airway repair.

Shao S, Zhang N, Specht GP, You S, Song L, Fu Q, Huang D, You H, Shu J, Domissy A, Li S, Nguyen-Tran V, Joseph SB, Chatterjee AK, Chen JJ, Schultz PG, Bollong MJ.

Proc Natl Acad Sci U S A. 2024 Apr 16;121(16):e2400077121. doi: 10.1073/pnas.2400077121. 

PMID: 38598345

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Covalent Targeting As a Common Mechanism for Inhibiting NLRP3 Inflammasome Assembly.

Stanton C, Sun J, Nutsch K, Rosarda JD, Nguyen T, Li-Ma C, Njomen E, Melillo B, Kutseikin S, Saez E, Cravatt BF, Teijaro JR, Wiseman RL, Bollong MJ.

ACS Chem Biol. 2024 Jan 10. doi: 10.1021/acschembio.3c00330.

PMID: 38198472

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Pharmacological inhibition of CLK2 activates YAP by promoting alternative splicing of AMOTL2.

Bulos ML, Grzelak EM, Li-Ma C, Chen E, Hull M, Johnson KA, Bollong MJ.

Elife. 2023 Dec 21;12:RP88508. doi: 10.7554/eLife.88508.

PMID: 38126343 

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A covalent inhibitor of the YAP-TEAD transcriptional complex identified by high-throughput screening.

Nutsch K, Song L, Chen E, Hull M, Chatterjee AK, Chen JJ, Bollong MJ.

RSC Chem Biol. 2023 Aug 29;4(11):894-905. doi: 10.1039/d3cb00044c. eCollection 2023 Nov 1.

PMID: 37920398 

 

A high throughput screen for pharmacological inhibitors of the carbohydrate response element.

You S, Bollong MJ.

Sci Data. 2023 Oct 4;10(1):676. doi: 10.1038/s41597-023-02596-z.

PMID: 37794069 

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Succinylation of a KEAP1 sensor lysine promotes NRF2 activation.

Ibrahim L, Stanton C, Nutsch K, Nguyen T, Li-Ma C, Ko Y, Lander GC, Wiseman RL, Bollong MJ.

Cell Chem Biol. 2023 Aug 11:S2451-9456(23)00243-X. doi: 10.1016/j.chembiol.2023.07.014. Online ahead of print.

PMID: 37619563

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Pharmacological YAP activation promotes regenerative repair of cutaneous wounds.

Grzelak EM, Elshan NGRD, Shao S, Bulos ML, Joseph SB, Chatterjee AK, Chen JJ, Nguyên-Trân V, Schultz PG, Bollong MJ.

Proc Natl Acad Sci U S A. 2023 Jul 11;120(28):e2305085120. doi: 10.1073/pnas.2305085120. Epub 2023 Jul 3.

PMID: 37399395

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S-lactoyl modification of KEAP1 by a reactive glycolytic metabolite activates NRF2 signaling.

Ko Y, Hong M, Lee S, Kumar M, Ibrahim L, Nutsch K, Stanton C, Sondermann P, Sandoval B, Bulos ML, Iaconelli J, Chatterjee AK, Wiseman RL, Schultz PG, Bollong MJ.

Proc Natl Acad Sci U S A. 2023 May 16;120(20):e2300763120. doi: 10.1073/pnas.2300763120.

PMID: 37155889

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Optimization of 3-aminotetrahydrothiophene 1,1-dioxides with improved potency and efficacy as non-electrophilic antioxidant response element (ARE) activators.

Jo J, Kim J, Ibrahim L, Kumar M, Iaconelli J, So Tran C, Ryong Moon H, Jung Y, Luke Wiseman R, Lairson LL, Chatterjee AK, Bollong MJ, Yun H.

Bioorg Med Chem Lett. 2023 Apr 26:129306. doi: 10.1016/j.bmcl.2023.129306. 

PMID: 37116763

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Circadian disruption enhances HSF1 signaling and tumorigenesis in Kras-driven lung cancer.

Pariollaud M, Ibrahim LH, Irizarry E, Mello RM, Chan AB, Altman BJ, Shaw RJ, Bollong MJ, Wiseman RL, Lamia KA.

Sci Adv. 2022 Sep 30;8(39):eabo1123. doi: 10.1126/sciadv.abo1123. 2022 Sep 28.

PMID: 36170373 

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Metabolically Activated Proteostasis Regulators Protect against Glutamate Toxicity by Activating NRF2.

Rosarda JD, Baron KR, Nutsch K, Kline GM, Stanton C, Kelly JW, Bollong MJ, Wiseman RL.ACS Chem Biol. 2021 Nov 19. doi: 10.1021/acschembio.1c00810. 

PMID: 34797633

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CRY2 missense mutations suppress P53 and enhance cell growth.

Chan AB, Parico GCG, Fribourgh JL, Ibrahim LH, Bollong MJ, Partch CL, Lamia KA.Proc Natl Acad Sci U S A. 2021 Jul 6;118(27):e2101416118. doi: 10.1073/pnas.2101416118.

PMID: 34183418

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YAP-dependent proliferation by a small molecule targeting annexin A2.

Shalhout SZ, Yang PY, Grzelak EM, Nutsch K, Shao S, Zambaldo C, Iaconelli J, Ibrahim L, Stanton C, Chadwick SR, Chen E, DeRan M, Li S, Hull M, Wu X, Chatterjee AK, Shen W, Camargo FD, Schultz PG, Bollong MJ.

Nat Chem Biol. 2021 Mar 15. doi: 10.1038/s41589-021-00755-0.

PMID: 33723431

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A short ORF-encoded transcriptional regulator.

Koh M, Ahmad I, Ko Y, Zhang Y, Martinez TF, Diedrich JK, Chu Q, Moresco JJ, Erb MA, Saghatelian A, Schultz PG, Bollong MJ.

Proc Natl Acad Sci U S A. 2021 Jan 26;118(4):e2021943118. doi: 10.1073/pnas.2021943118.

PMID: 33468658

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Defining the Functional Targets of Cap'n'collar Transcription Factors NRF1, NRF2, and NRF3.

Ibrahim L, Mesgarzadeh J, Xu I, Powers ET, Wiseman RL, Bollong MJ.

Antioxidants (Basel). 2020 Oct 21;9(10). pii: E1025. doi: 10.3390/antiox9101025.

PMID: 33096892

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2-Sulfonyl pyridines as tunable, cysteine-reactive electrophiles.

Zambaldo C, Vinogradova EV, Qi X, Iaconelli J, Suciu RM, Koh M, Senkane K, Chadwick SR, Sanchez BB, Chen JS, Chatterjee AK, Liu P, Schultz PG, Cravatt BF, Bollong MJ.

J Am Chem Soc. 2020 Apr 17. doi: 10.1021/jacs.0c02721.

PMID:32302104

 

Small molecule stimulators of NRF1 transcriptional activity.

Iaconelli J, Ibrahim L, Chen E, Hull M, Schultz PG, Bollong MJ.

Chembiochem. 2019 Oct 9. doi: 10.1002/cbic.201900487. 

PMID:31596542

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A cell type-selective apoptosis-inducing small molecule for the treatment of brain cancer.

Lucki NC, Villa GR, Vergani N, Bollong MJ, Beyer BA, Lee JW, Anglin JL, Spangenberg SH, Chin EN, Sharma A, Johnson K, Sander PN, Gordon P, Skirboll SL, Wurdak H, Schultz PG, Mischel PS, Lairson LL. Proc Natl Acad Sci U S A. 2019 Mar 26;116(13):6435-6440

PMID:30846550

 

Deconvoluting Stress-Responsive Proteostasis Signaling Pathways for Pharmacologic Activation Using Targeted RNA Sequencing.

Grandjean JMD, Plate L, Morimoto RI, Bollong MJ, Powers ET, Wiseman RL. ACS Chem Biol. 2019 Mar 13.

PMID:30821953

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A metabolite-derived protein modification integrates glycolysis with KEAP1-NRF2 signaling.*

Bollong MJ, Lee G, Coukos JS, Yun H, Zambaldo C, Chang JW, Chin EN, Ahmad I, Chatterjee AK, Lairson LL, Schultz PG, Moellering RE. Nature. 2018 Oct;562(7728):600-604. doi: 10.1038/s41586-018-0622-0. Epub 2018 Oct 15.

PMID: 30323285

*F1000 recommended

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A vimentin binding small molecule leads to mitotic disruption in mesenchymal cancers.

Bollong MJ, Pietilä M, Pearson AD, Sarkar TR, Ahmad I, Soundararajan R, Lyssiotis CA, Mani SA, Schultz PG, Lairson LL.

Proc Natl Acad Sci U S A. 2017 Nov 14;114(46):E9903-E9912. doi: 10.1073/pnas.1716009114. Epub 2017 Oct 30.

PMID:29087350

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Small molecule-mediated inhibition of myofibroblast transdifferentiation for the treatment of fibrosis.*

Bollong MJ, Yang B, Vergani N, Beyer BA, Chin EN, Zambaldo C, Wang D, Chatterjee AK, Lairson LL, Schultz PG.

Proc Natl Acad Sci U S A. 2017 May 2;114(18):4679-4684. doi: 10.1073/pnas.1702750114. Epub 2017 Apr 17.

PMID:28416697

*F1000 recommended

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Targeted Delivery of an Anti-inflammatory PDE4 Inhibitor to Immune Cells via an Antibody-drug Conjugate.

Yu S, Pearson AD, Lim RK, Rodgers DT, Li S, Parker HB, Weglarz M, Hampton EN, Bollong MJ, Shen J, Zambaldo C, Wang D, Woods AK, Wright TM, Schultz PG, Kazane SA, Young TS, Tremblay MS.

Mol Ther. 2016 Dec;24(12):2078-2089. doi: 10.1038/mt.2016.175. Epub 2016 Oct 12.

PMID:27731313

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A Small Molecule Inhibits Deregulated NRF2 Transcriptional Activity in Cancer.

Bollong MJ, Yun H, Sherwood L, Woods AK, Lairson LL, Schultz PG.

ACS Chem Biol. 2015 Oct 16;10(10):2193-8. doi: 10.1021/acschembio.5b00448. Epub 2015 Aug 17.

PMID:26270491

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Efficient viral delivery system for unnatural amino acid mutagenesis in mammalian cells.

Chatterjee A, Xiao H, Bollong M, Ai HW, Schultz PG.

Proc Natl Acad Sci U S A. 2013 Jul 16;110(29):11803-8. doi: 10.1073/pnas.1309584110. Epub 2013 Jul 1.

PMID:23818609

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Pan-Src family kinase inhibitors replace Sox2 during the direct reprogramming of somatic cells.

Staerk J, Lyssiotis CA, Medeiro LA, Bollong M, Foreman RK, Zhu S, Garcia M, Gao Q, Bouchez LC, Lairson LL, Charette BD, Supekova L, Janes J, Brinker A, Cho CY, Jaenisch R, Schultz PG.

Angew Chem Int Ed Engl. 2011 Jun 14;50(25):5734-6. doi: 10.1002/anie.201101042. Epub 2011 May 5. No abstract available.

PMID:21547985

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Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4.

Lyssiotis CA, Foreman RK, Staerk J, Garcia M, Mathur D, Markoulaki S, Hanna J, Lairson LL, Charette BD, Bouchez LC, Bollong M, Kunick C, Brinker A, Cho CY, Schultz PG, Jaenisch R.

Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7. doi: 10.1073/pnas.0903860106. Epub 2009 May 15.

PMID:19447925

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