Selected Publications

2017

Cheung KL, Lu G, Sharma R, Vincek A, Zhang R, Plotnikov AN, 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, Yang J, Peng L, Ohlmeyer M, Walsh MJ, Zhang DY, Xiong H, Zhou MM. BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice. Proc Natl Acad Sci U S A. 2017 Mar 14;114(11):2952-2957. doi: 10.1073/pnas.1615601114. PMID: 28265070

Cheung KL, Zhang F, Jaganathan A, Sharma R, Zhang Q, Konuma T, Shen T, Lee JY, Ren C, Chen CH, Lu G, Olson MR, Zhang W, Kaplan MH, Littman DR, Walsh MJ, Xiong H, Zeng L, Zhou MM. Distinct Roles of Brd2 and Brd4 in Potentiating the Transcriptional Program for Th17 Cell Differentiation. Mol Cell. 2017 Mar 16;65(6):1068-1080.doi: 10.1016/j.molcel.2016.12.022. Epub 2017 Mar 3. PMID: 28262505

Martín-Martínez M, Pérez-Gordillo FL, Álvarez de la Rosa D, Rodríguez Y, Gerona-Navarro G, González-Muñiz R, Zhou MM. Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects.  J Med Chem. 2017 Jan 24. doi: 10.1021/acs.jmedchem.6b01065. PMID: 28051871

2016

Li J, Rodriguez Y, Cheng C, Zeng L, Wong EY, Xu CY, Zhou MM, Xu PX. EYA1’s Conformation Specificity in Dephosphorylating Phosphothreonine in Myc and Its Activity on Myc Stabilization in Breast Cancer. Mol Cell Biol. 2016 Dec 19;37(1). pii: e00499-16. Print 2017 Jan 1. PMID: 27795300

Meslamani J, Smith SG, Sanchez R, Zhou MM. Structural features and inhibitors of bromodomains. Drug Discov Today Technol. 2016 Mar;19:3-15. doi: 10.1016/j.ddtec.2016.09.001. Review. PMID: 27769355

Zhang Q, Zeng L, Zhao C, Ju Y, Konuma T, Zhou MM. (2016) Structural Insights into Histone Crotonyl-Lysine Recognition by the AF9 YEATS Domain. Structure, Aug 5, S0969-2126. PMID: 27545619

Zhang Q, Zeng L, Shen C, Ju Y, Konuma T, Zhao C, Vakoc CR, Zhou MM (2016) Structural Mechanism of Transcriptional Regulator NSD3 Recognition by the ET Domain of BRD4. Structure, Jul 6;24(7):1201-8. PMID: 27291650

Ren C, Smith SG, Yap KL, Li S, Li J, Mezei M, Vincek AS, Aguilo F, Walsh MJ, and Zhou MM (2016) Structure-Guided Discovery of Selective Antagonists for the Chromodomain of Polycomb Repressive Protein CBX7. ACS Med. Chem. Lett., 2016, 7 (6), 601–605. PMID: 27326334

2015-

Zhang G, Smith SG, Zhou MM. (2015) Discovery of Chemical Inhibitors of Human Bromodomains. Chem Rev. 2015 Nov 11;115(21):11625-68. PMID: 26492937

Bansal N, Petrie K, Christova R, Chung CY, Leibovitch BA, Howell L, Gil V, Sbirkov Y, Lee E, Wexler J, Ariztia EV, Sharma R, Zhu J, Bernstein E, Zhou MM, Zelent A, Farias E, Waxman S. (2015) Targeting the SIN3A-PF1 interaction inhibits epithelial to mesenchymal transition and maintenance of a stem cell phenotype in triple negative breast cancer. Oncotarget. 2015 Oct 27;6(33):34087-105. PMID: 26460951

Kwon YJ, Petrie K, Leibovitch BA, Zeng L, Mezei M, Howell L, Gil V, Christova R, Bansal N, Yang S, Sharma R, Ariztia EV, Frankum J, Brough R, Sbirkov Y, Ashworth A, Lord CJ, Zelent A, Farias E, Zhou MM, Waxman S. (2015). Selective Inhibition of SIN3 Corepressor with Avermectins as a Novel Therapeutic Strategy in Triple-Negative Breast Cancer. Mol Cancer Ther. 2015 Aug;14(8):1824-36. PMID: 26078298

Stratikopoulos EE, Dendy M, Szabolcs M, Khaykin AJ, Lefebvre C, Zhou MM, Parsons R. (2015). Kinase and BET Inhibitors Together Clamp Inhibition of PI3K Signaling and Overcome Resistance to Therapy. Cancer Cell. 2015 Jun 8;27(6):837-51. doi: 10.1016/j.ccell.2015.05.006. PMID: 26058079

Ren C, Morohashi K, Plotnikov AN, Jakoncic J, Smith SG, Li J, Zeng L, Rodriguez Y, Stojanoff V, Walsh M, Zhou MM. (2015). Small-Molecule Modulators of Methyl-Lysine Binding for the CBX7 Chromodomain. Chem Biol. 2015 Feb 5. pii: S1074-5521. PMID: 25660273

Di Micco R, Fontanals-Cirera B, Low V, Ntziachristos P, Yuen SK, Lovell CD, Dolgalev I, Yonekubo Y, Zhang G, Rusinova E, Gerona-Navarro G, Camero M, Ohlmeyer M, Aifantis I, Zhou MM,Tsirigos A, Hernando E. (2014). Control of embryonic stem cell identity by BRD4-dependent transcriptional elongation of super-enhancer-associated pluripotency genes. Cell Rep. 2014 014 Oct 9;9(1):234-47. PMID: 25263550

Marmorstein R, Zhou MM. (2014) Writers and readers of histone acetylation: structure, mechanism, and inhibition. Cold Spring Harb Perspect Biol. 2014 Jul 1;6(7):a018762. PMID: 24984779

Gacias M, Gerona-Navarro G, Plotnikov AN, Zhang G, Zeng L, Kaur J, Moy G, Rusinova E, Rodriguez Y, Matikainen B, Vincek A, Joshua J, Casaccia P, Zhou MM. (2014) Selective chemical modulation of gene transcription favors oligodendrocyte lineage progression.
Chem Biol. 2014 Jul 17;21(7):841-54. PMID: 24954007

Smith SG, Sanchez R, Zhou MM. (2014) Privileged Diazepine Compounds and Their Emergence as Bromodomain Inhibitors. Chem Biol. 2014 May 22;21(5):573-583. PMID: 24746559

Zeng L, Kuti M, Mujtaba S, Zhou MM. (2014) Structural insights into FRS2α PTB domain recognition by neurotrophin receptor TrkB. Proteins. 2014 Jan 27. PMID: 24470253

Liu R., Zhong Y., Li X., Chen H., Jim B., Zhou M-M., Chuang PY., He JC. (2014) Role of Transcription Factor Acetylation in Diabetic Kidney Disease. Diabetes. 2014 Mar 7. PMID: 24608443

Meslamani, J., Smith, S.G., Sanchez, R., & Zhou, M.-M. (2014) ChEpiMod: A Knowledgebase for Chemical Modulators of Epigenome Reader Domains. Bioinformatics, in press. Epub 2014 Jan 27. PMID: 24470572.

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: 210-225. PMID: 24525235.

Plotnikov, A.N., Yang, S., Zhou, T.J., Rusinov, E., Frasca, A., & Zhou, M.-M. (2014) Structural Insights into Acetylated-Histone H4 Recognition by the Bromodomain-PHD Tandem Module of Human Transcriptional Co-activator CBP. Structure, 22(2): 353-360. PMID: 24361270.

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 Medicinal Chemistry, 56(22):9251-64. PMID: 24144283. PMCID: PMC3894848.

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.

Zhang G, Sanchez R, Zhou MM (2012) Scaling the druggability landscape of human bromodomains, a new class of drug targets.  J. Med. Chem. 55(17):7342-5.

Zhang G, Liu R, Zhong Y, Plotnikov AN, Zhang W, Zeng L, Rusinova E, Gerona-Nevarro G, Moshkina N, Joshua J, Chuang PY, Ohlmeyer M, He JC, Zhou MM (2012) Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition. J. Biol. Chem. 287(34):28840-51.

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.

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. Molecular Cell 38(5): 662-674.

Sanchez, R., & Zhou, M.-M. (2009) The Role of Human Bromodomains in Chromatin Biology and Gene Transcription. Current Opinion in Drug Discovery and Development 12(5): 659-65.

Chakravarty, S., Zeng, L., & Zhou, M.-M. (2009) Structure and Site-Specific Recognition of Histone H3 Lysine 4 by the PHD Finger of Human AIRE. Structure 7(5):670-9.

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

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 Structural & Molecular Biology 15, 626-633.

Zeng, L., Zhang, Q., Gerona-Navarro, G., Moshkina, N., & Zhou, M.-M. (2008) Structural Basis of Site-Specific Histone Recognition by the Bromodomains of Human Coactivators PCAF and CBP/p300. Structure 16, 643-652.

Ivanov, A.V., Peng, H., Yuchenko, 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. Molecular Cell 28(5), 823-837.

Sampath, S., Marazzi, I., Yap, K.L., Sampath, S., Krutchinskly, A., Mecklenbrauker, 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. Molecular Cell 27(4), 596-608.

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 Selectivity Inhibiting Human Immunodeficiency Virus 1 Tat Association with the Human Coactivator p300/CREB Binding Protein-Associated Facor. Journal of Medicinal Chemistry 50, 2285-2288.

Seet, B.T., Dikic, I., Zhou, M.-M., & Pawson, T (2006) Reading Protein Modifications with Interaction Domains. Nature Reviews Molecular Cell Biology 7, 473-483.

Qian, C., Wang, X., Manzur, K., Sachchidanand, Farooq, A., Zeng, L., Wang, R. & Zhou, M.-M. (2006) Structural Insights of the Specificity and Catalysis of a Viral Histone H3 Lysine-27 Methyltransferase. J. Mol. Biol. 359, 86-96.

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; featured by Nature Reviews in Drug Discovery in March 2006.

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 Structural & Molecular Biology 12, 1078-1085.

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, 2376-2377.

Mujtaba, M., 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. Molecular Cell, 13, 251-263.

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, 469-474.

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 Structural Biology 10, 187-196.

Mujtaba, S., He, Y. Zeng, L., Farooq, A., Carlson, J., Ott, M., Verdin, E., & Zhou, M.-M. (2002) Structural Basis of HIV-1 Tat Recognition by P/CAF Bromodomain, Molecular Cell 9, 575-586.

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 6, 921-929.

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, 921-929.

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, 491-496.

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 Structural Biology 3, 388-393.

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, 584-592.