Publications

2 0 2 3

DW71177: A novel [1,2,4]triazolo[4,3-a]quinoxaline-based potent and BD1-Selective BET inhibitor for the treatment of acute myeloid leukemia

Imran Ali, Hyung Jin Cha, Byungho Lim, Chong Hak Chae, Jihyun Youm, Whui Jung Park, Sang Ho Lee, Jung Hwan Kim, Docgyun Jeong, Jae Kyung Lim, Yun-Ha Hwang, Jae-Seok Roe, Jae-Sung Woo, Kwangho Lee, Gildon Choi

European Journal of Medicinal Chemistry. 2023 Dec 11. doi: https://doi.org/10.1016/j.ejmech.2023.116052

Streamlined DNA-encoded small molecule library screening and validation for the discovery of novel chemotypes targeting BET proteins

Seoyeon Jeong, Hwa-Ryeon Kim, June-Ha Shin, Insung Na, Joonseong Lee, Kyung Hyun Yoo, Min-Hee Son, In-Hyun Lee, Jae-Seok Roe

Molecular Therapy Nucleic Acids. April 24, 2023. DOI:https://doi.org/10.1016/j.omtn.2023.04.023

A pipeline to characterize p53 effectors by integrative cistrome and transcriptome analysis in genetically-defined organoid model

June-Ha Shin, Hwa-Ryeon Kim, Jae-Seok Roe

Genes & Diseases. 2023 Apr 7;11(2):512-515. doi: 10.1016/j.gendis.2023.03.009. eCollection 2024 Mar.

Reprogramming anchorage dependency by adherent-to-suspension transition promotes metastatic dissemination

Huh HD, Sub Y, Oh J, Kim YE, Lee JY, Kim HR, Lee S, Lee H, Pak S, Amos SE, Vahala D, Park JH, Shin JE, Park SY, Kim HS, Roh YH, Lee HW, Guan KL, Choi YS, Jeong J, Choi J, Roe JS, Gee HY, Park HW.

Molecular Cancer. 2023 Mar 30;22(1):63. doi: 10.1186/s12943-023-01753-7.


A TEAD2-driven endothelial-like program shapes basal-like differentiation and metastasis of pancreatic cancer

Hye-Been Yoo, Jin Woo Moon, Hwa-Ryeon Kim, Hee Seung Lee, Koji Miyabayashi, Chan Hee Park, Sabrina Ge, Amy Zhang, Yoo Keung Tae, Yujin Sub, Hyun-Woo Park, Heon Yung Gee, Faiyaz Notta, David A. Tuveson, Seungmin Bang, Mi-Young Kim, Jae-Seok Roe.

Gastroenterology. March 10, 2023. DOI:https://doi.org/10.1053/j.gastro.2023.02.049


2 0 2 2

LCK-Mediated RIPK3 Activation Controls Double-Positive Thymocyte Proliferation and Restrains Thymic Lymphoma by Regulating the PP2A-ERK Axis.

Hwang SM, Ha YJ, Koo GB, Noh HJ, Lee AY, Kim BJ, Hong SM, Morgan MJ, Eyun SI, Lee D, Roe JS, Lee Y, Kim YS.

Adv Sci (Weinh). 2022 Nov;9(32):e2204522. doi: 10.1002/advs.202204522. Epub 2022 Sep 25.


2 0 2 1

RIPK3 activation induces TRIM28 derepression in cancer cells and enhances the anti-tumor microenvironment.

Park HH, Kim HR, Park SY, Hwang SM, Hong SM, Park S, Kang HC, Morgan MJ, Cha JH, Lee D, Roe JS, Kim YS.

Mol Cancer. 2021 Aug 21;20(1):107. doi: 10.1186/s12943-021-01399-3.


Core promoter activity contributes to chromatin-based regulation of internal cryptic promoters.

Lee BB, Woo H, Lee MK, Youn S, Lee S, Roe JS, Lee SY, Kim T.

Nucleic Acids Res. 2021 Aug 20;49(14):8097-8109. doi: 10.1093/nar/gkab639.


GALNT3 suppresses lung cancer by inhibiting myeloid-derived suppressor cell infiltration and angiogenesis in a TNFR and c-MET pathway-dependent manner.

Park MS, Yang AY, Lee JE, Kim SK, Roe JS, Park MS, Oh MJ, An HJ, Kim MY.

Cancer Lett. 2021 Aug 17;521:294-307. doi: 10.1016/j.canlet.2021.08.015. Online ahead of print.


Phosphorylation of OGFOD1 by Cell Cycle-Dependent Kinase 7/9 Enhances the Transcriptional Activity of RNA Polymerase II in Breast Cancer Cells.

Lee HT, Lee IH, Kim JH, Lee S, Kwak S, Suh MY, Hwang IY, Kang BG, Cha SS, Lee BI, Lee SE, Choi J, Roe JS, Cho EJ, Youn HD.

Cancers (Basel). 2021 Jul 8;13(14):3418. doi: 10.3390/cancers13143418.


Epigenetic Upregulation of MAGE-A Isoforms Promotes Breast Cancer Cell Aggressiveness.

Oh C, Kim HR, Oh S, Ko JY, Kim Y, Kang K, Yang Y, Kim J, Park JH, Roe JS, Yoo KH.

Cancers (Basel). 2021 Jun 25;13(13):3176. doi: 10.3390/cancers13133176.


EVI1 activates tumor-promoting transcriptional enhancers in pancreatic cancer.

Kim HR, Yim J, Yoo HB, Lee SE, Oh S, Jung S, Hwang CI, Shin DM, Kim T, Yoo KH, Kim YS, Lee HW, Roe JS.

NAR Cancer. 2021 Jun 17;3(2):zcab023. doi: 10.1093/narcan/zcab023. eCollection 2021 Jun.


Mitochondrial dysfunction induced by callyspongiolide promotes autophagy-dependent cell death.

Lee S, Jeong Y, Roe JS, Huh H, Paik SH, Song J.

BMB Rep. 2021 Apr;54(4):227-232. doi: 10.5483/BMBRep.2021.54.4.037.


2 0 2 0

Identification of MYC as an antinecroptotic protein that stifles RIPK1-RIPK3 complex formation.

Seong D, Jeong M, Seo J, Lee JY, Hwang CH, Shin HC, Shin JY, Nam YW, Jo JY, Lee H, Kim HJ, Kim HR, Oh JH, Ha SJ, Kim SJ, Roe JS, Kim W, Cheong JW, Bae KH, Lee SC, Oberst A, Vandenabeele P, Shin DH, Lee EW, Song J.

Proc Natl Acad Sci U S A. 2020 Aug 18;117(33):19982-19993. doi: 10.1073/pnas.2000979117. Epub 2020 Aug 4.


Divergence of the PIERCE1 expression between mice and humans as a p53 target gene.

Kim HJ, Lee SE, Na H, Roe JS, Roh JI, Lee HW.

PLoS One. 2020 Aug 3;15(8):e0236881. doi: 10.1371/journal.pone.0236881. eCollection 2020.


Glutathione dynamics determine the therapeutic efficacy of mesenchymal stem cells for graft-versus-host disease via CREB1-NRF2 pathway.

Lim J, Heo J, Ju H, Shin JW, Kim Y, Lee S, Yu HY, Ryu CM, Yun H, Song S, Hong KS, Chung HM, Kim HR, Roe JS, Choi K, Kim IG, Jeong EM, Shin DM.

Sci Adv. 2020 Apr 15;6(16):eaba1334. doi: 10.1126/sciadv.aba1334. eCollection 2020 Apr.


Deubiquitylation and stabilization of Notch1 intracellular domain by ubiquitin-specific protease 8 enhance tumorigenesis in breast cancer.

Shin S, Kim K, Kim HR, Ylaya K, Do SI, Hewitt SM, Park HS, Roe JS, Chung JY, Song J.

Cell Death Differ. 2020 Apr;27(4):1341-1354. doi: 10.1038/s41418-019-0419-1. Epub 2019 Sep 17.


Non-thermal atmospheric pressure plasma induces epigenetic modifications that activate the expression of various cytokines and growth factors in human mesoderm-derived stem cells.

Park J, Suh D, Tang T, Lee HJ, Roe JS, Kim GC, Han S, Song K.

Free Radic Biol Med. 2020 Feb 20;148:108-122. doi: 10.1016/j.freeradbiomed.2019.12.035. Epub 2019 Dec 26.


Ascorbic Acid 2-Glucoside Stably Promotes the Primitiveness of Embryonic and Mesenchymal Stem Cells Through Ten-Eleven Translocation- and cAMP-Responsive Element-Binding Protein-1-Dependent Mechanisms.

Lee S, Lim J, Lee JH, Ju H, Heo J, Kim Y, Kim S, Yu HY, Ryu CM, Lee SY, Han JM, Oh YM, Lee H, Jang H, Yoon TJ, Ahn HS, Kim K, Kim HR, Roe JS, Chung HM, Son J, Kim JS, Shin DM.

Antioxid Redox Signal. 2020 Jan 1;32(1):35-59. doi: 10.1089/ars.2019.7743.


2 0 1 9

Oncogenic KRAS Sensitizes Lung Adenocarcinoma to GSK-J4-Induced Metabolic and Oxidative Stress.

Hong BJ, Park WY, Kim HR, Moon JW, Lee HY, Park JH, Kim SK, Oh Y, Roe JS, Kim MY.

Cancer Res. 2019 Nov 15;79(22):5849-5859. doi: 10.1158/0008-5472.CAN-18-3511. Epub 2019 Sep 10.


Epigenetic regulation of mammalian Hedgehog signaling to the stroma determines the molecular subtype of bladder cancer.

Kim S, Kim Y, Kong J, Kim E, Choi JH, Yuk HD, Lee H, Kim HR, Lee KH, Kang M, Roe JS, Moon KC, Kim S, Ku JH, Shin K.

Elife. 2019 Apr 30;8:e43024. doi: 10.7554/eLife.43024.


2 0 1 8

The SS18-SSX Oncoprotein Hijacks KDM2B-PRC1.1 to Drive Synovial Sarcoma.

Banito A, Li X, Laporte AN, Roe JS, Sanchez-Vega F, Huang CH, Dancsok AR, Hatzi K, Chen CC, Tschaharganeh DF, Chandwani R, Tasdemir N, Jones KB, Capecchi MR, Vakoc CR, Schultz N, Ladanyi M, Nielsen TO, Lowe SW.

Cancer Cell. 2018 Aug 13;34(2):346-348. doi: 10.1016/j.ccell.2018.07.006.


The SS18-SSX Oncoprotein Hijacks KDM2B-PRC1.1 to Drive Synovial Sarcoma.

Banito A, Li X, Laporte AN, Roe JS, Sanchez-Vega F, Huang CH, Dancsok AR, Hatzi K, Chen CC, Tschaharganeh DF, Chandwani R, Tasdemir N, Jones KB, Capecchi MR, Vakoc CR, Schultz N, Ladanyi M, Nielsen TO, Lowe SW.

Cancer Cell. 2018 Mar 12;33(3):527-541.e8. doi: 10.1016/j.ccell.2018.01.018. Epub 2018 Mar 1.


2 0 1 7

Harnessing BET Inhibitor Sensitivity Reveals AMIGO2 as a Melanoma Survival Gene.

Fontanals-Cirera B, Hasson D, Vardabasso C, Di Micco R, Agrawal P, Chowdhury A, Gantz M, de Pablos-Aragoneses A, Morgenstern A, Wu P, Filipescu D, Valle-Garcia D, Darvishian F, Roe JS, Davies MA, Vakoc CR, Hernando E, Bernstein E.

Mol Cell. 2017 Nov 16;68(4):731-744.e9. doi: 10.1016/j.molcel.2017.11.004.


Enhancer Reprogramming Promotes Pancreatic Cancer Metastasis.

Roe JS, Hwang CI, Somerville TDD, Milazzo JP, Lee EJ, Da Silva B, Maiorino L, Tiriac H, Young CM, Miyabayashi K, Filippini D, Creighton B, Burkhart RA, Buscaglia JM, Kim EJ, Grem JL, Lazenby AJ, Grunkemeyer JA, Hollingsworth MA, Grandgenett PM, Egeblad M, Park Y, Tuveson DA, Vakoc CR.

Cell. 2017 Aug 24;170(5):875-888.e20. doi: 10.1016/j.cell.2017.07.007. Epub 2017 Jul 27.


2 0 0 6 ~ 2 0 1 6

Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition.

Hohmann AF, Martin LJ, Minder JL, Roe JS, Shi J, Steurer S, Bader G, McConnell D, Pearson M, Gerstberger T, Gottschamel T, Thompson D, Suzuki Y, Koegl M, Vakoc CR.

Nat Chem Biol. 2016 Sep;12(9):672-9. doi: 10.1038/nchembio.2115. Epub 2016 Jul 4.


BRD4 Connects Enhancer Remodeling to Senescence Immune Surveillance.

Tasdemir N, Banito A, Roe JS, Alonso-Curbelo D, Camiolo M, Tschaharganeh DF, Huang CH, Aksoy O, Bolden JE, Chen CC, Fennell M, Thapar V, Chicas A, Vakoc CR, Lowe SW.

Cancer Discov. 2016 Jun;6(6):612-29. doi: 10.1158/2159-8290.CD-16-0217. Epub 2016 Apr 20.


BET Bromodomain Inhibition Releases the Mediator Complex from Select cis-Regulatory Elements.

Bhagwat AS, Roe JS, Mok BYL, Hohmann AF, Shi J, Vakoc CR.

Cell Rep. 2016 Apr 19;15(3):519-530. doi: 10.1016/j.celrep.2016.03.054. Epub 2016 Apr 7.


The Essential Transcriptional Function of BRD4 in Acute Myeloid Leukemia.

Roe JS, Vakoc CR.

Cold Spring Harb Symp Quant Biol. 2016;81:61-66. doi: 10.1101/sqb.2016.81.031039. Epub 2017 Feb 7.


NSD3-Short Is an Adaptor Protein that Couples BRD4 to the CHD8 Chromatin Remodeler.

Shen C, Ipsaro JJ, Shi J, Milazzo JP, Wang E, Roe JS, Suzuki Y, Pappin DJ, Joshua-Tor L, Vakoc CR.

Mol Cell. 2015 Dec 17;60(6):847-59. doi: 10.1016/j.molcel.2015.10.033. Epub 2015 Nov 25.


Transcriptional plasticity promotes primary and acquired resistance to BET inhibition.

Rathert P, Roth M, Neumann T, Muerdter F, Roe JS, Muhar M, Deswal S, Cerny-Reiterer S, Peter B, Jude J, Hoffmann T, Boryń ŁM, Axelsson E, Schweifer N, Tontsch-Grunt U, Dow LE, Gianni D, Pearson M, Valent P, Stark A, Kraut N, Vakoc CR, Zuber J.

Nature. 2015 Sep 24;525(7570):543-547. doi: 10.1038/nature14898. Epub 2015 Sep 14.


OGFOD1 is required for breast cancer cell proliferation and is associated with poor prognosis in breast cancer.

Kim JH, Lee SM, Lee JH, Chun S, Kang BH, Kwak S, Roe JS, Kim TW, Kim H, Kim WH, Cho EJ, Youn HD.

Oncotarget. 2015 Aug 14;6(23):19528-41. doi: 10.18632/oncotarget.3683.


BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia.

Roe JS, Mercan F, Rivera K, Pappin DJ, Vakoc CR.

Mol Cell. 2015 Jun 18;58(6):1028-39. doi: 10.1016/j.molcel.2015.04.011. Epub 2015 May 14.


The transcriptional cofactor TRIM33 prevents apoptosis in B lymphoblastic leukemia by deactivating a single enhancer.

Wang E, Kawaoka S, Roe JS, Shi J, Hohmann AF, Xu Y, Bhagwat AS, Suzuki Y, Kinney JB, Vakoc CR.

Elife. 2015 Apr 28;4:e06377. doi: 10.7554/eLife.06377.


TGF-β/Smad signaling through DOCK4 facilitates lung adenocarcinoma metastasis.

Yu JR, Tai Y, Jin Y, Hammell MC, Wilkinson JE, Roe JS, Vakoc CR, Van Aelst L.

Genes Dev. 2015 Feb 1;29(3):250-61. doi: 10.1101/gad.248963.114.


C/EBPα: critical at the origin of leukemic transformation.

Roe JS, Vakoc CR.

J Exp Med. 2014 Jan 13;211(1):1-4. doi: 10.1084/jem.20132530. Epub 2014 Jan 6.


Role of SWI/SNF in acute leukemia maintenance and enhancer-mediated Myc regulation.

Shi J, Whyte WA, Zepeda-Mendoza CJ, Milazzo JP, Shen C, Roe JS, Minder JL, Mercan F, Wang E, Eckersley-Maslin MA, Campbell AE, Kawaoka S, Shareef S, Zhu Z, Kendall J, Muhar M, Haslinger C, Yu M, Roeder RG, Wigler MH, Blobel GA, Zuber J, Spector DL, Young RA, Vakoc CR.

Genes Dev. 2013 Dec 15;27(24):2648-62. doi: 10.1101/gad.232710.113. Epub 2013 Nov 27.


p53 regulates glucose metabolism by miR-34a.

Kim HR, Roe JS, Lee JE, Cho EJ, Youn HD.

Biochem Biophys Res Commun. 2013 Jul 26;437(2):225-31. doi: 10.1016/j.bbrc.2013.06.043. Epub 2013 Jun 22.


Oncogene interference through targeting of chromatin regulators.

Roe JS, Vakoc CR.

Cell Cycle. 2013 May 15;12(10):1475-6. doi: 10.4161/cc.24748. Epub 2013 Apr 22.


Phosphorylation and ubiquitination-dependent degradation of CABIN1 releases p53 for transactivation upon genotoxic stress.

Choi SY, Jang H, Roe JS, Kim ST, Cho EJ, Youn HD.

Nucleic Acids Res. 2013 Feb 1;41(4):2180-90. doi: 10.1093/nar/gks1319. Epub 2013 Jan 8.


A p53-inducible microRNA-34a downregulates Ras signaling by targeting IMPDH.

Kim HR, Roe JS, Lee JE, Hwang IY, Cho EJ, Youn HD.

Biochem Biophys Res Commun. 2012 Feb 24;418(4):682-8. doi: 10.1016/j.bbrc.2012.01.077. Epub 2012 Jan 24.


pVHL-mediated transcriptional repression of c-Myc by recruitment of histone deacetylases.

Hwang IY, Roe JS, Seol JH, Kim HR, Cho EJ, Youn HD.

Mol Cells. 2012 Feb;33(2):195-201. doi: 10.1007/s10059-012-2268-3.


Phosphorylation of von Hippel-Lindau protein by checkpoint kinase 2 regulates p53 transactivation.

Roe JS, Kim HR, Hwang IY, Ha NC, Kim ST, Cho EJ, Youn HD.

Cell Cycle. 2011 Nov 15;10(22):3920-8. doi: 10.4161/cc.10.22.18096. Epub 2011 Nov 15.


von Hippel-Lindau protein promotes Skp2 destabilization on DNA damage.

Roe JS, Kim HR, Hwang IY, Cho EJ, Youn HD.

Oncogene. 2011 Jul 14;30(28):3127-38. doi: 10.1038/onc.2011.40. Epub 2011 Feb 28.


The positive regulation of p53 by the tumor suppressor VHL.

Roe JS, Youn HD.

Cell Cycle. 2006 Sep;5(18):2054-6. doi: 10.4161/cc.5.18.3247. Epub 2006 Sep 15.


p53 stabilization and transactivation by a von Hippel-Lindau protein.

Roe JS, Kim H, Lee SM, Kim ST, Cho EJ, Youn HD.

Mol Cell. 2006 May 5;22(3):395-405. doi: 10.1016/j.molcel.2006.04.006.