{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,13]],"date-time":"2026-03-13T00:17:31Z","timestamp":1773361051605,"version":"3.50.1"},"reference-count":58,"publisher":"Oxford University Press (OUP)","issue":"16","license":[{"start":{"date-parts":[[2022,8,30]],"date-time":"2022-08-30T00:00:00Z","timestamp":1661817600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by-nc\/4.0\/"}],"funder":[{"DOI":"10.13039\/100000002","name":"NIH","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100000002","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000026","name":"NIDA","doi-asserted-by":"publisher","award":["R01DA040621"],"award-info":[{"award-number":["R01DA040621"]}],"id":[{"id":"10.13039\/100000026","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000026","name":"NIDA","doi-asserted-by":"publisher","award":["P01DA047233"],"award-info":[{"award-number":["P01DA047233"]}],"id":[{"id":"10.13039\/100000026","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Sealy Center for Structural Biology and Molecular Biophysics"},{"DOI":"10.13039\/100004917","name":"Cancer Prevention Research Institute of Texas","doi-asserted-by":"publisher","award":["RP190682"],"award-info":[{"award-number":["RP190682"]}],"id":[{"id":"10.13039\/100004917","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100004917","name":"Cancer Prevention Research Institute of Texas","doi-asserted-by":"publisher","award":["RP150578"],"award-info":[{"award-number":["RP150578"]}],"id":[{"id":"10.13039\/100004917","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Stuart & Suzanne Steele MGH Research Scholars Program"},{"name":"UTMB Center for Addiction Research","award":["NIDA T32 DA 07287"],"award-info":[{"award-number":["NIDA T32 DA 07287"]}]},{"name":"John D. Stobo, M.D. Distinguished Chair Endowment Fund"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2022,9,9]]},"abstract":"<jats:title>Abstract<\/jats:title>\n               <jats:p>The AP1 transcription factor \u0394FOSB, a splice variant of FOSB, accumulates in the brain in response to chronic insults such as exposure to drugs of abuse, depression, Alzheimer's disease\u00a0and tardive dyskinesias, and mediates subsequent long-term neuroadaptations. \u0394FOSB forms heterodimers with other AP1 transcription factors, e.g. JUND, that bind DNA under control of a putative cysteine-based redox switch. Here, we reveal the structural basis of the redox switch by determining a key missing crystal structure in a trio, the \u0394FOSB\/JUND bZIP domains in the reduced, DNA-free form. Screening a cysteine-focused library containing 3200 thiol-reactive compounds, we identify specific compounds that target the redox switch, validate their activity biochemically and in cell-based assays, and show that they are well tolerated in different cell lines despite their general potential to bind to cysteines covalently. A crystal structure of the \u0394FOSB\/JUND bZIP domains in complex with a redox-switch-targeting compound reveals a deep compound-binding pocket near the DNA-binding site. We demonstrate that \u0394FOSB, and potentially other, related AP1 transcription factors, can be targeted specifically and discriminately by exploiting unique structural features such as the redox switch and the binding partner to modulate biological function despite these proteins previously being thought to be undruggable.<\/jats:p>","DOI":"10.1093\/nar\/gkac710","type":"journal-article","created":{"date-parts":[[2022,8,30]],"date-time":"2022-08-30T08:58:33Z","timestamp":1661849913000},"page":"9548-9567","source":"Crossref","is-referenced-by-count":15,"title":["Chemically targeting the redox switch in AP1 transcription factor \u0394FOSB"],"prefix":"10.1093","volume":"50","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-6727-1521","authenticated-orcid":false,"given":"Ashwani","family":"Kumar","sequence":"first","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, TX 77555, USA"},{"name":"Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Galina","family":"Aglyamova","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, TX 77555, USA"},{"name":"Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yun\u00a0Young","family":"Yim","sequence":"additional","affiliation":[{"name":"Nash Family Department of Neuroscience and the Friedman Brain Institute, Icahn School of Medicine at Mount Sinai , New\u00a0York, NY 10029, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Aaron O","family":"Bailey","sequence":"additional","affiliation":[{"name":"Department of Biochemistry and Molecular Biology, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Haley\u00a0M","family":"Lynch","sequence":"additional","affiliation":[{"name":"Department of Physiology, Michigan State University , East Lansing, MI 48824, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Reid\u00a0T","family":"Powell","sequence":"additional","affiliation":[{"name":"HTS Screening Core, Texas A&M University School of Medicine, Institute of Biosciences and Technology, Center for Translational Cancer Research , Houston, TX 77030, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Nghi\u00a0D","family":"Nguyen","sequence":"additional","affiliation":[{"name":"HTS Screening Core, Texas A&M University School of Medicine, Institute of Biosciences and Technology, Center for Translational Cancer Research , Houston, TX 77030, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Zachary","family":"Rosenthal","sequence":"additional","affiliation":[{"name":"Chemical Neurobiology Laboratory, Center for Genomic Medicine, Massachusetts General Hospital, Departments of Psychiatry & Neurology, Harvard Medical School , Boston, MA\u00a002114, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Wen-Ning","family":"Zhao","sequence":"additional","affiliation":[{"name":"Chemical Neurobiology Laboratory, Center for Genomic Medicine, Massachusetts General Hospital, Departments of Psychiatry & Neurology, Harvard Medical School , Boston, MA\u00a002114, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yi","family":"Li","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jianping","family":"Chen","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shanghua","family":"Fan","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, TX 77555, USA"},{"name":"Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hubert","family":"Lee","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, TX 77555, USA"},{"name":"Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"William\u00a0K","family":"Russell","sequence":"additional","affiliation":[{"name":"Department of Biochemistry and Molecular Biology, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Clifford","family":"Stephan","sequence":"additional","affiliation":[{"name":"HTS Screening Core, Texas A&M University School of Medicine, Institute of Biosciences and Technology, Center for Translational Cancer Research , Houston, TX 77030, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Alfred\u00a0J","family":"Robison","sequence":"additional","affiliation":[{"name":"Department of Physiology, Michigan State University , East Lansing, MI 48824, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Stephen\u00a0J","family":"Haggarty","sequence":"additional","affiliation":[{"name":"Chemical Neurobiology Laboratory, Center for Genomic Medicine, Massachusetts General Hospital, Departments of Psychiatry & Neurology, Harvard Medical School , Boston, MA\u00a002114, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Eric\u00a0J","family":"Nestler","sequence":"additional","affiliation":[{"name":"Nash Family Department of Neuroscience and the Friedman Brain Institute, Icahn School of Medicine at Mount Sinai , New\u00a0York, NY 10029, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2811-1090","authenticated-orcid":false,"given":"Jia","family":"Zhou","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, TX 77555, USA"},{"name":"Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6040-1362","authenticated-orcid":false,"given":"Mischa","family":"Machius","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, TX 77555, USA"},{"name":"Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7372-0530","authenticated-orcid":false,"given":"Gabby","family":"Rudenko","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, TX 77555, USA"},{"name":"Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch , Galveston, TX 77555, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"286","published-online":{"date-parts":[[2022,8,30]]},"reference":[{"key":"2022090900042637000_B1","doi-asserted-by":"crossref","first-page":"623","DOI":"10.1038\/nrn3111","article-title":"Transcriptional and epigenetic mechanisms of addiction","volume":"12","author":"Robison","year":"2011","journal-title":"Nat. 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Neurosci"},{"key":"2022090900042637000_B10","doi-asserted-by":"crossref","first-page":"745","DOI":"10.1038\/nn.2551","article-title":"DeltaFosB in brain reward circuits mediates resilience to stress and antidepressant responses","volume":"13","author":"Vialou","year":"2010","journal-title":"Nat. Neurosci."},{"key":"2022090900042637000_B11","doi-asserted-by":"crossref","first-page":"5913","DOI":"10.1523\/JNEUROSCI.0296-18.2018","article-title":"Cell-Type-Specific role of DeltaFosB in nucleus accumbens in modulating intermale aggression","volume":"38","author":"Aleyasin","year":"2018","journal-title":"J. Neurosci."},{"key":"2022090900042637000_B12","doi-asserted-by":"crossref","first-page":"562154","DOI":"10.3389\/fnsys.2020.562154","article-title":"Differential expression of DeltaFosB in reward processing regions between binge eating prone and resistant female rats","volume":"14","author":"Quansah\u00a0Amissah","year":"2020","journal-title":"Front. Syst. Neurosci."},{"key":"2022090900042637000_B13","doi-asserted-by":"crossref","first-page":"18664","DOI":"10.1073\/pnas.1907810116","article-title":"Role of striatal \u0394FosB in l-Dopa-induced dyskinesias of parkinsonian nonhuman primates","volume":"116","author":"Beck","year":"2019","journal-title":"Proc. Natl. Acad. Sci. U.S.A."},{"key":"2022090900042637000_B14","doi-asserted-by":"crossref","first-page":"13773","DOI":"10.1523\/JNEUROSCI.2083-15.2015","article-title":"Experience-Dependent induction of hippocampal \u0394FosB controls learning","volume":"35","author":"Eagle","year":"2015","journal-title":"J. Neurosci."},{"key":"2022090900042637000_B15","first-page":"237","article-title":"Reduction of cocaine-induced locomotor effects by enriched environment is associated with cell-specific accumulation of DeltaFosB in striatal and cortical subregions","volume":"20","author":"Lafragette","year":"2017","journal-title":"Int. J. Neuropsychopharmacol."},{"key":"2022090900042637000_B16","doi-asserted-by":"crossref","first-page":"77","DOI":"10.1016\/j.neulet.2018.11.036","article-title":"Reduced DeltaFosB expression in the rat nucleus accumbens has causal role in the neuropathic pain phenotype","volume":"702","author":"Pollema-Mays","year":"2019","journal-title":"Neurosci. Lett."},{"key":"2022090900042637000_B17","doi-asserted-by":"crossref","first-page":"10","DOI":"10.1016\/S0006-8993(98)01191-3","article-title":"DeltaFosB: a molecular mediator of long-term neural and behavioral plasticity","volume":"835","author":"Nestler","year":"1999","journal-title":"Brain Res."},{"key":"2022090900042637000_B18","doi-asserted-by":"crossref","first-page":"296","DOI":"10.1021\/acschemneuro.1c00723","article-title":"DeltaFOSB: a potentially druggable master orchestrator of activity-dependent gene expression","volume":"13","author":"Robison","year":"2022","journal-title":"ACS Chem. Neurosci."},{"key":"2022090900042637000_B19","doi-asserted-by":"crossref","first-page":"760","DOI":"10.1038\/s41434-021-00249-7","article-title":"Striatal DeltaFosB gene suppression inhibits the development of abnormal involuntary movements induced by L-Dopa in rats","volume":"28","author":"Beck","year":"2021","journal-title":"Gene Ther."},{"key":"2022090900042637000_B20","doi-asserted-by":"crossref","first-page":"369","DOI":"10.1016\/j.neuroscience.2008.10.059","article-title":"Phosphorylation of DeltaFosB mediates its stability in vivo","volume":"158","author":"Ulery-Reynolds","year":"2009","journal-title":"Neuroscience"},{"key":"2022090900042637000_B21","doi-asserted-by":"crossref","first-page":"3009","DOI":"10.1111\/j.1460-9568.2007.05575.x","article-title":"Proteasome-dependent and -independent mechanisms for FosB destabilization: identification of FosB degron domains and implications for DeltaFosB stability","volume":"25","author":"Carle","year":"2007","journal-title":"Eur. J. 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