Selected Publications

Zhou, M.-M., & Cole, P.A. (2024) Targeting Lysine Acetylation Readers and Writers. Nature Reviews Drug Discovery, published online (11/21/2024). PMID: 39572658.

Cheung, K.L., Zhao, L., Sharma, R., Ghosh, A.A, Appiah, M., Sun, Y.F., Jaganathan, A., Hu, Y., LeJeune, A., Xu, F., Han, X., Wang, X., Zhang, F., Ren, C.Y., Walsh, M.J., Xiong, H.B., Tsankov, Al., & Zhou, M.-M. (2024) Class IIa HDAC4 and HDAC7 Cooperatively Regulate Gene Transcription in Th17 Cell Differentiation. PNAS, 121(18): e2312111121. PMID: 38657041.

Liu, N., Konuma, K., Sharma, R., Wang, D., Zhao, N., Cao, L.L., Ju, Y., Liu, D., Wang, Shui, Bosch, A., Sun, Y.F., Zhang, S., Ji, D.L., Nagatoishi, S., Suzuki, N., Kikuchi, M., Wakamori, M., Zhao, C.C., Ren, C.Y., Zhou, T.J.C., Xu. Y.Y., Meslamani, J., Fu, S.B., Umehara, T., Tsumoto, K., Akashi, S., Zeng, L., Roeder, R.G., Walsh, M.J., Zhang, Q., & Zhou, M.-M. (2023) Histone H3 Lysine 27 Crotonylation Mediates Gene Transcriptional Repression in Chromatin. Mol. Cell, 83(13): 2206-2221. PMID:37311463

Zhao, L., Wang, Y., Ma, N., Jaganathan, A., Sun, Y., Ma, N., Li, N., Han, X., Sun, X., Yi, H., Fu, S., Han, F., Li, X., Xiao, K., Li, X., Walsh, M.J., Zeng, L., Zhou, M.-M., & Cheung, K.L. (2023) BRD4-PRC2 represses transcription of T-helper 2-specific negative regulators during T-cell differentiation. EMBO J. 42(6): e111473. PMID: 36690674.

Yu, D., Liang, Y., Kim, C., Jaganathan, A., Ji, D., Han, X., Yang, X., Jia, Y., Gu, R., Wang, C., Zhang, Q., Cheung, K.L., Zhou, M.-M., & Zeng, L. (2023) Structural Mechanism of BRD4-NUT and p300 Bipartite Interactions in Propagating Aberrant Gene Transcription in Chromatin in NUT Carcinoma. Nature Commun., 14(1):378. PMID: 36690674, PMCID: PMC9870903.

Cheung, K.L., Jaganathan, A., Hu, Y., Xu, F.H., LeJeune A., Sharma, R., Caescu, C.I., Meslamani, J., Vincek, A., Zhang, F., Lee, K., Nilesh, Z., Qayum, A.A., Ren, C.Y., Kaplan, M.H., He, C.J., Xiong, H.B., & Zhou, M.-M. (2022) HIPK2 Directs Cell Type Specific Regulation of STAT3 Transcriptional Activity in Th17 Cell Differentiation. PNAS, 119(14), e2117112119. Epub 2022 March 28. PMID: 35344430.

Gajjela, B.K., & Zhou, M.-M. (2022) Calming the Cytokine Storm of COVID-19 Through Inhibition of JAK2/STAT3 Signaling. Drug Discovery Today, 27(2):390-400. PMID: 34743903, PMCID: PMC8553370.

Du, Y., Yan, Y., Xie, S., Huang, H., Wang, X., Ng, R.K., Zhou, M.-M., & Qian, C.M. (2021) Structural Mechanism of Bivalent Histone H3K4me3K9me3 Recognition by the Spindlin1/C11orf84 Complex in rRNA Transcription Activation. Nature Commun., 12(1):949. PMID: 33574238; PMCID: PMC7878818.

Wang M, Li A, Sekiya M, Beckmann ND, Quan X, Schrode N, Fernando MB, Yu A, Zhu L, Cao J, Lyu L, Horgusluoglu E, Wang Q, Guo L, Wang YS, Neff R, Song WM, Wang E, Shen Q, Zhou X, Ming C, Ho SM, Vatansever S, Kaniskan HÜ, Jin J, Zhou, M.-M., Ando K, Ho L, Slesinger PA, Yue Z, Zhu J, Katsel P, Gandy S, Ehrlich ME, Fossati V, Noggle S, Cai D, Haroutunian V, Iijima KM, Schadt E, Brennand KJ, Zhang B. (2021) Transformative Network Modeling of Multi-omics Data Reveals Details Circuits, Key Regulators, and Potential Therapeutics for Alzheimer’s Disease. Neuron, 109(2):257-272.e14. PMID: 33238137.

Martinez-Ortiz, W., & Zhou, M.-M. (2020) Could PROTACs Protect Us from COVID-19? Drug Discovery Today, 25 (11): 1894-6. PMID: 32889063.

Han, X.Y., Yu, D., Gu, R.R., Jia, Y.J., Wang, Q., Yang, X.L., Yu, M.M., Babault, N., Zhao, C.C., Yi, H.F., Zhang, Q., Zhou, M.-M., & Zeng, L. (2020) Roles of BRD4 Short Isoform in Phase Separation and Active Gene Transcription. Nature Struct. & Mol. Biol., 27(4):333-341. PMID: 32203489.

Zaware, N., & Zhou, M.-M. (2019) Bromodomain Biology and Drug Discovery. Nature Struct. & Mol. Biol., 26(10): 870-879. PMID: 31582847.

Han, F.H., & Zhou, M.-M. (2019) Small Molecules with Big Promise for Curing Demyelinating Diseases. Cell Chem. Biol., 26(4): 468-470. PMID: 31002801

Liu, J.Y., Duan, Z.B., Guo, W.J., Zeng, L., Wu, Y.D., Chen, Y., Wang, Y.F., Lin, Y.W., Zhang, Q., Deng, J., Stewart, R.L., Wang, C., Lin, P.C., Ghaffari, S., Evers, B.M., Liu, S., Zhou, M.-M., Zhou, B.H., & Shi, J. (2018) Targeting the BRD4/FOXO3a/CDK6 Axis Sensitizes AKT Inhibition in Luminal Breast Cancer. Nature Comm.,9(1): 5200. PMID: 30518851.

Ren, C.Y., Zhang, G., Han, F.B., Fu, S.B., Cao, Y.D., Zhang, F., Zhang, Q., Meslamani, J., Xu, Y.Y., Ji, D.L., Cao, L.L., Zhou, Q., Ceung, K.L., Sharma, R., Babault, N., Yi, Z.Z., Zhang, W.J., Walsh, M.J., Zeng, L., & Zhou, M.-M. (2018) Spatially Constrained Tandem Bromodomain Inhibition Bolsters a Sustained Repression of BRD4 Transcriptional Activity for TNBC Cell Growth. PNAS, 115(31):7949-7954. PMID: 30012592. PMCID: PMC6077712.

Konuma, T., Yu, D., Zhao, C., Ju, Y., Sharma, R., Ren, C., Zhang, Q., Zhou, M.-M., & Zeng, L. (2017) Structural Mechanism of the Oxygenase JMJD6 Recognition by the Extraterminal (ET) Domain of BRD4. Scientific Reports. 7(1): 16272. PMID: 29176719, PMCID: PMC5701133.

Zaware, N., & Zhou, M.-M. (2017) Chemical Modulators for Epigenome Reader Domains as Emerging Epigenetic Therapies for Cancer and Inflammation. Curr. Opin. Chem. Biol., 39:116-125. PMID: 28689146, PMCID: PMC5581715. 

Conrad, R.J., Fozouni, P., Thomas, S., Sy, H., Zhang, Q., Zhou, M.-M., Ott, M. (2017) The Short Isoform of BRD4 Promotes HIV-1 Latency by Engaging Repressive SWI/SNF Chromatin-Remodeling Complexes. Mol. Cell, 67(6): 1001-1012. PMID: 28844864, PMCID: PMC5610089. 

Cheung, K.L., Lu, G.M., Sharma, R., Vincek, A.S., Zhang, R.H., Plotnikov, A.N., Zhang, F., Zhang, Q., Ju, Y., Hu, Y., Zhao, L., Han, X., Meslamani, J., Xu, F., Jaganathan, A., Shen, T., Zhu, H., Rusinova, E., Zeng, L., Zhou, J.C., Yang, J.C., Peng, L., Ohlmeyer, M., Walsh, M.J., Zhang, D.Y., Xiong, H.B., & Zhou, M.-M. (2017) Selective BET Bromodomain Inhibition Blocks Th17 Cell Differentiation and Ameliorates Colitis in Mice. PNAS. 114(11): 2952-2957. PMID: 28265070. 

Cheung, K.L., Zhang, F.,  Jaganathan, A., Sharma, R., Zhang, Q., Konuma, T., Shen, T., Lee, J.-Y., Ren, C.Y., Chen, C.-H., Lu, G., Olson, M.R., Zhang, W., Kaplan, M.H., Littman, D.R., Walsh, M.J., Xiong, H., Zeng, L., & Zhou, M.-M. (2017) Distinct Roles of Brd2 and Brd4 in Potentiating the Transcriptional Program for Th17 Cell Differentiation. Mol. Cell, 65(6): 1068-1080. PMID: 28262505, PMCID: PMC5357147. 

Martin-Martinez, M., Perez-Gordillo, F.L., De la Rosa, D.A., Rodriguez, Y., Gerona-Navarro, G., Gonzalez-Muniz, R., & Zhou, M.-M. (2017) Modulating Mineralocorticoid Receptor with Non-steroid Antagonists: New Opportunities for the Development of Potent and Selective Ligands without Off-target Side-effects. J. Med. Chem. 60(7): 2629-2650. PMID: 28051871. 

Meslamani, J., Smith, S.G., Sanchez, R., & Zhou, M.-M. (2016) Structural Features and Inhibitors of Bromodomains. Drug Discov. Today Technol. 19:3-15. PMID: 27769355.

Ren, C., Smith, S.G., Yap, K., Li, S., Li, J., Mezei, M., Rodriguez, Y., Vincek, A., Agulo, F., Walsh, M.J., & Zhou, M.-M. (2016) Structure-Guided Discovery of Selective Antagonists for the Chromodomain of Polycomb Repressive Protein CBX7. ACS Med. Chem. Letts. 7(6):601-5. PMID: 27326334.

Zhang, G., Smith, S.G., & Zhou, M.-M. (2015) Discovery of Chemical Inhibitors of Human Bromodomains. Chemical Reviews. 115(21):11625-68. Epub 2015 Oct 23. PMID: 26492937.

Stratikopoulos, E.E., Dendy, M., Szabolcs, M., Khaykin, A.J., Lefebvre, C., Zhou, M.-M., & Parsons, R. (2015) Kinase and BET Inhibitors Together Clamp Inhibition of PI3K Signaling and Overcome Resistance to Therapy. Cancer Cell, 27(6), 837-851. PMID: 26058079.

Ren, C.Y., Morohashi, K., Plotnikov, A.N., Jakoncic, J., Smith, S.G., Li, J., Zeng, L., Rodrigues, Y., Stojanoff, V., Walsh, M.J., & Zhou, M.-M. (2015) Small-Molecule Modulators of Methyl-Lysine Binding for the CBX7 Chromodomain. Chemistry & Biology 22(2): 161-168. PMID: 25660273. PMCID: PMC4336573.

Gacias-Monserrat, M., Gerona-Navarro, G., Plotnikov, A.N., Zhang, G.T., Zeng, L., Kaur, J., Moy, G., Rusinova, E., Rodríguez-Fernández, Y., Matikainen, Joshua, J., Vincek, A., Joshua, J., Casaccia, P., & Zhou, M.-M. (2014) Selective Chemical Modification of Gene Transcription Favors Oligodendrocyte Lineage Progression. Chemistry & Biology, 21(7): 841-54. PMID: 24954007. PMCID: PMC4104156.

Smith, S.G., Sanchez, R., & Zhou, M.-M. (2014) Privileged Diazepine Compounds and Their Emergence as Bromodomain Inhibitors. Chemistry & Biology, 21(5):573-583. PMID: 24746559. PMCID: PMC4035449.

Shi, J., Wang, Y., Zeng, L., Wu, Y., Deng, J., Zhang, Q., Dong, C., Li, J., Rusinova, E., Zhang, G., Wang, C., Zhu, H., Evers, B.M., Zhou, M.-M., & Zhou, B.P. (2014) Disrupting the Interaction of BRD4 with Diacetylated Twist Suppresses Tumorigenesis in Basal-like Breast Cancer. Cancer Cell, 25(2):210-225. PMID: 24525235. PMCID: PMC4004960.

Zhang, G., Plotnikov, A.N., Rusinova, E., Shen, T., Morohashi, K., Joshua, J., Zeng, L., Mujtaba, S., Ohlmeyer, M., & Zhou, M.-M. (2013) Structure-Guided Design of Potent  Diazobenzene Inhibitors for the BET Bromodomains. Journal of Med. Chem., 56(22):9251-64. PMID: 24144283. PMCID: PMC3894848.

Yang, J., Zhang, R., Lu, G., Shen, Y., Zhu, C., Cui, M., Wang,W., Arnaboldi, P., Peng, L., Tang, M., Gupta, M., Qi, C.-F., Jayaraman, P., Zhu, H., Jiang, B., Chen, S.H., He, J.C., Ting, A.T., Zhou, M.-M., Kuchroo, V.K., Morse III, H.C., Ozato, K., Sikora, A.G., & Xiong, H. (2013) T cell-derived inducible nitric oxide synthase switches off  T_H17 cell differentiation. Journal of Experimental Med. 210(7):1447-1462. PMID: 23797094. PMCID: PMC3698516.

Zhang, G., Sanchez, R., & Zhou, M.-M. (2012) Scaling the Druggability Landscape of Human Bromodomains, a New Class of Drug Targets. Journal of Med. Chem., 55, 7342-7345. PMID: 22928775. PMCID: PMC3454531.

Zhang, G., Liu, R., Zhong, Y., Plotnikov, A.N., Zhang, W., Zeng, L., Rusinova, E., Gerona-Nevarro, G., Moshkina, N., Joshua, J., Chuang, P.Y., Ohlmeyer, M., He, J.C., & Zhou, M.-M. (2012) Down-Regulation of NF-kB Transcriptional Activation in HIV-Associated Kidney Disease by BRD4 Inhibition. Journal of Biol. Chem. 287(34): 28840-51. PMID: 22645123. PMCID: PMC3436579. Cover image.

Wu, H., Moshkina, N., Min, J., Zeng, H., Joshua, J., Zhou, M.-M., & Plotnikov, A.N. (2012) New Mechanistic Insights into Substrate Specificity and Catalysis of Human Histone acetyltransferase 1 from the HAT1-Acetyl CoA-Histone H4 Ternary Complex Structure. Proc. Natl. Acad. Sci. USA. 109(23):8925-30. PMID: 22615379. PMCID: PMC3384170.

Li, J.J., Wei, H., & Zhou, M.-M. (2011) Structure-guided design of a methyl donor cofactor that controls a viral histone lysine 27 methyltransferase. Journal of Med. Chem. 54(21):7734-8. PMID: 21958314. PMCID: PMC3326379.

Borah, J.C., Mujtaba, S., Karakikes, I., Zeng, L., Muller, M., Zhang, W., Gerona-Navarro, G., Hajjar, R.J., & Zhou, M.-M. (2011) A Small Molecule Binding to the Co-Activator CREB-Binding Protein Blocks Apoptosis in Ischemic Cardiomyocytes. Chemistry & Biology 18(4):531-41. PMID: 2153899. PMCID: PMC3103858.

Gerona-Navarro, G., Rodríguez-Fernández, Y., Mutjaba, S., Frasca, A., Patel, J., Plotniov, A.N., Osman, R. & Zhou, M.-M. (2011) Rational Design of Cyclic Peptide Modulators of the Transcriptional Coactivator CBP: A New Class of p53 Inhibitors. Journal of Am. Chem. Soc., 133(7): 2040-2043. PMID: 21271695. PMCID: PMC3047509.

Wei, H., & Zhou, M.-M. (2010) Dimerization of a Viral SET Protein Endows its Function. Proc. Natl. Acad. Sci. USA, 107(43): 18433-8. PMID: 20937900.

Zeng, L., Zhang, Q., Li, SiDe, Plotnikov, A.N., Walsh, M.J., & Zhou, M.-M. (2010) Mechanism and Regulation of Acetylated Histone Binding of the Tandem PHD Finger of DPF3b. Nature, 466(7303): 258-62. PMID: 20613843. PMCID: PMC2901902.

Yap, K.L., Li, S., Munoz-Cabello, A.M., Raguz, S., Zeng, L., Mujtaba, S., Gil, J., Walsh, W.J., & Zhou, M.-M. (2010) Molecular Interplay of the Non-coding RNA ANRIL and Methylated Histone H3 Lysine 27 by Polycomb CBX7 in Transcriptional Silencing of INK4a. Mol. Cell, 38(5): 662-674. PMID: 20541999. PMCID: PMC2886305.

Barradas, M., Anderton, E, Acosta, J. C., Li, S., Banito, A., Rodriguez-Niedenführ, M., Banck, M., Zhou, M.-M., Peters, G., Walsh, M. J., & Gil, J. (2009) Histone demethylase JMJD3 contributes to the epigenetic control of INK4a/ARF by oncogenic RAS. Genes & Dev. 23(10): 1177-1182. PMID: 19451218. PMCID: PMC2685533.

Mujtaba, S., Manzur, K.L., Gurnon, J.R., Kang, M., Van Etten. J.L. & Zhou, M.-M. (2008) Epigenetic Transcription Repression of Cellular Genes by a Viral SET Protein. Nature Cell Biology, 10, 1114-1122. PMID: 18711358. PMCID: 2898185.

Zeng, L., Yap, K.L., Ivanov, A.V, Wang, X., Mujtaba, S., Plotnikova, O., Rauscher, F.J., & Zhou, M.-M. (2008) Structural Insights into the Functional Cooperativity of the Tandem PHD Finger-Bromodomain of Human KAP1 in Sumoylation-Dependence Gene Silencing. Nature Struct. & Mol. Biol. 15(6), 626-633. PMID: 18488044. PMCID: PMC3331790.

Ivanov, A.V., Peng, H., Yurchenko, V., Yap, K.L., Negorev, D.G., Schultz, D.C., Psulkowsky, E., Fredericks, W.J., White, D.E., Maul, G.G., Sadofsky, M.J., Zhou, M.-M., & Rauscher, F.J. (2007) PHD Domain-Mediated E3 Ligase Activity Directs Intramolecular Sumoylation of an Adjacent Bromodomain which is Required for Gene Silencing. Mol. Cell, 28(5), 823-37. PMID: 18082607. PMCID: PMC

Sampath, S., Marazzi, I., Yap, K.L., Sampath, S., Krutchinskly, A., Mecklenbräuker, I., Vlale, A., Rudensky, E., Zhou, M.-M., Chait, B., & Tarakhovsky, A. (2007) Methylation of a Histone Mimic within the Histone Methyltransferase G9a Regulates Protein Complex Assembly. Mol. Cell, 27(4), 596-608. PMID: 17707231

Pan, C., Mezei, M., Mujtaba,S., Muller, M., Zeng, L., Li, J.M., Wang, Z.Y., & Zhou, M.-M. (2007) Structure-Guided Optimization of Small Molecules Selectively Inhibiting Human Immunodeficiency Virus 1 Tat Association with the Human Coactivator p300/CREB Binding Protein-Associated Factor. Journal of Med. Chem., 50, 2285-2288. PMID: 17444627. 

Seet, B.T., Dikic, I., Zhou, M.-M., & Pawson, T (2006) Reading Protein Modifications with Interaction Domains. Nature Reviews Mol. Cell Biol., 7(7):473-483. PMID: 16829979.

Sachchidanand, Resnick-Silverman, L., Yan, S., Mutjaba, S., Liu, W.-J., Zeng, L., Manfredi, L., & Zhou, M.-M.(2006) Target Structure-Based Discovery of Small Molecules that Block Human p53 and CREB Binding Protein (CBP) Association. Chemistry & Biology, 13, 81-90. PMID: 16426974.

Qian, C., Zhang, Q., Li, S., Zeng, L., Walsh, M.J., & Zhou, M.-M. (2005) Structure and Chromosomal DNA Binding of the SWIRM Domain. Nature Struct. & Mol. Biol., 12, 1078-1085. PMID: 16299514.

Zeng, L., Li, J., Muller, M., Yan, S., Mujtaba, S., Pan, C., Wang, Z., & Zhou, M.-M. (2005) Selective Small Molecules Blocking HIV-1 Tat and Coactivator PCAF Association. Journal of Am. Chem. Soc., 127(8), 2376-2377. PMID: 15724976.

Mujtaba, S., He, Y., Zeng, L., Yan, S., Plotnikova, O., Sachchidanand, Sanchez, R., Zeleznik-Le, N., Ronai, Z., Zhou, M.-M. (2004) Structural Mechanism of the Bromodomain of the Coactivator CBP in p53 Transcriptional Activation. Mol. Cell, 13(2), 251-263. PMID: 14759370.

Yan, K.S., Yan, S., Farooq, A., Han, A., Zeng, L., & Zhou, M.-M. (2003) Structure and Conserved RNA Binding of the PAZ Domain. Nature, 426(6965), 469-474. PMID: 14615802.

Manzur, K., Farooq, A., Zeng, L., Plotnikova, O., Koch, A. W., Sachchidanand, & Zhou, M.-M. (2003) A Dimeric Viral SET Domain Methyltransferase Specific to Lys27 of Histone H3. Nature Struct. Biol., 10, 187-196. PMID: 12567185.

Dorr, A., Kiermer, V., Pedal, A., Rackwitz, H.-R., Henklein, P., Schubert, U., Zhou, M.-M., Verdin, E. & Ott, M. (2002) Transcriptional synergy between at and PCAF is dependent on the binding of acetylated Tat to the PCAF bromodomain. EMBO J., 21, 2715-23. PMID: 12032084.

Farooq, A., Chaturvedi, G., Mutjaba, S., Plotnikova, O., Zeng, L., Dhalluin, C., Ashton, R., & Zhou, M.-M.(2001) Solution Structure of ERK2 Binding Domain of MAPK Phosphatase MKP-3: Structural Insights into MKP-3 Activation by ERK2. Molecular Cell, 7, 387-399. PMID: 11239467.

Dhalluin, C., Yan, K., Plotnikova, O., Lee, K.W., Zeng, L., Kuti, M., Mutjaba, S., Goldfarb, M.P., & Zhou, M.-M.(2000) Structural Basis of SNT PTB Domain Interactions with Distinct Neurotrophic Receptors. Molecular Cell,6, 921-29. PMID: 11090629.

Dhalluin, C., Carlson, J.,Zeng, L., He, C., Aggarwal, A.K., & Zhou, M.-M. (1999) Structure and Ligand of a Histone Acetyltransferase Bromodomain. Nature, 399(6735):491-496. 1999 Jun 3. PMID: 10365964.

Zhou, M.-M., Huang, B., Olejniczak, E.T., Meadows, R.P., Shuker, S.B., Miyazak, M., Trub, T., Shoelson, S.E., & Fesik, S.W. (1996) Structural Basis of IL-4 Receptor Phosphopeptide Recognition by the IRS-1 PTB Domain. Nature Struct. Biol., 3, 388-393. PMID: 8599766.

Zhou, M.-M., Ravichandran, K.S., Olejniczak, E.T., Petros, A.P., Meadows, R.P., Sattler, M., Harlan, J.E., Wade, W., Burakoff, S.J., & Fesik, S.W. (1995) Structure and Ligand Recognition of the Phosphotyrosine Binding Domain of Shc. Nature, 378(6557):584-592. PMID: 8524391.

Zhou, M.-M., Meadows, R.P., Logan, T.M., Yoon, H.P., Wade, W., Ravichandran, K.S., Burakoff, S.J., & Fesik, S.W. (1995) Solution Structure of the Shc SH2 domain Complexed with a Tyrosine phosphorylated Peptide from the T-cell Receptor. Proc. Natl. Acad. Sci. USA, 92, 7784-88. PMID: 7544002.