Â鶹ӳ»­

24. Zhang X, Blumenthal RM, Cheng X. (2024) . Epigenomes 8(2): 23. doi: 10.3390/epigenomes8020023 [2024 June 19]

23. Zhang X, Xia F, Zhang X, Blumenthal RM, Cheng X. (2023) . J Mol Biol. doi: 10.1016/j.jmb.2023.168343 [Epub 2023 Nov 2]

22. Yang J, Horton JR, Liu B, Corces VG, Blumenthal RM, Zhang X, Cheng X. (2023) . Nucleic Acids Res. 51(16): 8447-8462. doi: 10.1093/nar/gkad594. [Epub 2023 July 13]

21. Kaur G, Ren R, Hammel M, Horton JR, Yang J, Cao Y, He C, Lan F, Lan X, Blobel GA, Blumenthal RM, Zhang X, Cheng X. (2023)  Nucleic Acids Res. :gkac1274. doi: 10.1093/nar/gkac1274. [Epub 2023 Jan 20]

20. Ren R, Horton JR, Chen Q, Yang J, Liu B, Huang Y, Blumenthal RM, Zhang X, Cheng X. (2023) . J Biol Chem. 299(2): 102885. doi: 10.1016/j.jbc.2023.102885. [Epub 2023 Jan 7]

19. Huang P, Peslak SA, Ren R, Khandros E, Qin K, Keller CA, Giardine B, Bell HW, Lan X, Sharma M, Horton JR, Abdulmalik O, Chou ST, Shi J, Crossley M, Hardison RC, Cheng X, Blobel GA. (2022) . Nat Genet. 54(9): 1417-1426. doi: 10.1038/s41588-022-01152-6. [Epub 2022 Aug 8]

18. Yang Y, Ren R, Ly LC, Horton JR, Li F, Quinlan KGR, Crossley M, Shi Y, Cheng X. (2021) Structural basis for human ZBTB7A action at the fetal globin promoter. Cell Rep. 36(13): 109759. doi: 10.1016/j.celrep.2021.109759 [Epub 2021 Sep 28]

17. Lan X, Ren R, Feng R, Ly LC, Lan Y, Zhang Z, Aboreden N, Qin K, Horton JR, Grevet JD, Mayuranathan T, Abdulmalik O, Keller CA, Giardine B, Hardison RC, Crossley M, Weiss MJ, Cheng X, Shi J, Blobel GA (2021) ZNF410 uniquely activates the NuRD component CHD4 to silence fetal hemoglobin expression. Mol Cell 81(2): 239-254 [Epub 2020 Dec 9]

16. Yang J, Zhang X, Blumenthal RM, Cheng X (2020) Detection of DNA modifications by sequence-specific transcription factors. J Mol Biol. 432: 1661-1673. [Epub 2019 Oct 15]

15. Ren R, Hardikar S, Horton JR, Lu Y, Zeng Y, Singh AK, Lin K, Coletta LD, Shen J, Lin Kong CS, Hashimoto H, Zhang X, Chen T, Cheng X (2019). Structural basis of specific DNA binding by the transcription factor ZBTB24. Nucleic Acids Res. 47(16): 8388-8398. doi: 10.1093/nar/gkz557. [Epub 2019 June 21]

14. Ren R, Horton JR, Zhang X, Blumenthal RM, Cheng X (2018) Detecting and interpreting DNA methylation marks. Curr Opin Struct Biol. 53: 88-99

13. Patel A, Yang P, Tinkham M, Pradhan M, Sun MA, Wang Y, Hoang D, Wolf G, Horton JR, Zhang X, Macfarlan T, Cheng X (2018) DNA Conformation Induces Adaptable Binding by Tandem Zinc Finger Proteins. Cell 173(1): 221-233 [Epub 2018 Mar 15]

12. Wang D, Horton JR, Zheng Y, Blumenthal RM, Zhang X, Cheng X (2018) Role for first zinc finger of WT1 in DNA sequence specificity: Denys-Drash syndrome-associated WT1 mutant in ZF1 enhances affinity for a subset of WT1 binding sites. Nucleic Acids Res. 46(8): 3864-3877 [Epub 2017 Dec 27]

11. Patel A, Zhang X, Blumenthal RM, Cheng X (2017) Structural basis of human PRDM9 allele C specific recognition of its cognate DNA sequence. J Biol Chem. 292(39): 15994-16002 [Epub 2017 Aug 11]

10. Hashimoto H, Wang D, Horton JR, Zhang X, Corces VG, Cheng X (2017) Structural Basis for the Versatile and Methylation-Dependent Binding of CTCF to DNA. Mol Cell 66(5): 711-720 [Epub 2017 May 18]

9. Hashimoto H, Wang D, Steves AN, Jin P, Blumenthal RM, Zhang X, Cheng X (2016) Distinctive Klf4 mutants determine preference for DNA methylation status. Nucleic Acids Res. 44(21): 10177-10185 [Epub 2016 Sep 4]

8. Hashimoto H, Zhang X, Zheng Y, Wilson GG, Cheng X (2016) Denys-Drash syndrome associated WT1 glutamine 369 mutants have altered sequence-preferences and altered responses to epigenetic modifications. Nucleic Acids Res. 44(21): 10165-10176 [Epub 2016 Sep 4]

7. Patel A, Hashimoto H, Zhang X, Cheng X (2016) Characterization of How DNA Modifications Affect DNA Binding by C2H2 Zinc Finger Proteins. Methods in Enzymology 573: 387-401 [Epub 2016 Feb 16]

6. Patel A, Horton JR, Wilson GG, Zhang X, Cheng X (2016) Structural basis for human PRDM9 action at recombination hot spots. Genes Dev. 30(3): 257-65. [Epub 2016 Feb 1]

5. Hashimoto H, Olanrewaju YO, Zheng Y, Wilson GG, Zhang X, Cheng X (2014) Wilms tumor protein recognizes 5-carboxylcytosine within a specific DNA sequence. Genes Dev. 28(20): 2304-13 [Epub 2014 Sept 25]

4. Liu Y, Olanrewaju YO, Zheng Y, Hashimoto H, Blumenthal RM, Zhang X, Cheng X (2014) Structural basis for Klf4 recognition of methylated DNA. Nucleic Acids Res. 42(8): 4859-67 [Epub 2014 Feb 11]

3. Liu Y, Olanrewaju YO, Zhang X, Cheng X (2013) DNA recognition of 5-carboxylcytosine by a Zfp57 mutant at atomic resolution of 0.97 angstrom. Biochemistry 52: 9301-7 [Epub 2013 Nov 15]

2. Liu Y, Zhang X, Blumenthal RM, Cheng X (2013) A common mode of recognition for methylated CpG. Trends Biochem Sci. 38: 177-183 [Epub 2013 Jan 22]

1. Liu Y, Toh H, Sasaki H, Zhang X, Cheng X (2012) An atomic model of Zfp57 recognition of CpG methylation within a specific DNA sequence. Genes Dev. 26, 2374-9 [Epub 2012 Oct 11]

Base flipping involves rotation of backbone bonds in double-stranded deoxyribonucleic acid (DNA) to expose an out-of-stack base, which can then be a substrate for an enzyme-catalyzed chemical reaction or for a specific protein binding interaction. The phenomenon was first observed for a DNA methyltransferase in 1994 (reference 1), and is now widespread for enzymes or proteins that require access to unpaired, mismatched, damaged or modified bases or even undamaged and unmodified bases for specific functions.

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6. Horton JR, Woodcock CB, Opot SB, Reich NO, Zhang X, Cheng X (2019) The cell cycle-regulated DNA adenine methyltransferase CcrM opens a bubble at its DNA recognition site. Nat Commun. 10(1): 4600. doi: 10.1038/s41467-019-12498-7. [Epub Oct 10]

7. Zeng Y, Ren R, Kaur G, Hardikar S, Ying Z, Babcock L, Gupta E, Zhang X, Chen T, Cheng X. (2020) The inactive Dnmt3b3 isoform preferentially enhances Dnmt3b-mediated DNA methylation. Genes Dev. 34: 1546-1558 doi: 10.1101/gad.341925.120 [Epub Oct 1]

8. Zhou J, Horton JR, Blumenthal RM, Zhang X, Cheng X. (2021) Clostridioides difficile specific DNA adenine methyltransferase CamA squeezes and flips adenine out of DNA helix. Nat Commun. 12(1): 3436. doi: 10.1038/s41467-021-23693-w. [Epub Jun 8]

S-adenosyl-l-methionine (AdoMet or SAM) is the second most commonly used enzyme cofactor after ATP. The AdoMet-dependent methyltransferases act on a wide variety of target molecules, including DNA, RNA, proteins, polysaccharides, lipids, and a range of small molecules involved in metabolism. We determined the first structure of a DNA methyltransferase (1993), the first structure of protein arginine methyltransferase (2000), the first structure of a protein (histone) lysine methyltransferase (2002) and its complex with histone peptide substrate (2003). In addition, we determined structures of PvuII, a DNA cytosine-N4 methyltransferase (1997), DNMT2 - a tRNA cytosine methyltransferase (2001), HNMT - a small molecule (histamine) methyltransferase (2001), HemK - a protein glutamine methyltransferase (2004), Dot1p - a histone H3 lysine79 methyltransferase (2004), and SETD6 - a non-histone lysine methyltransferase (2011).

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12. Wilkinson AE, Diep J, Dai S, Liu S, Ooi YS, Song D, Li TM, Horton JR, Zhang X, Liu C, Trivedi DV, Ruppel KM, Vilches-Moure JG, Casey KM, Mak J, Cowan T, Elias JE, Nagamine CM, Spudich JA, Cheng X*, Carette JE*, Gozani O* (2019) SETD3 is an actin histidine methyltransferase that prevents primary dystocia. *Co-corresponding authors. Nature 565(7739): 372-376 [Epub Dec 10, 2018] see comment by P. Lappalainen: Protein modification fine-tunes the cell's force producers. Nature 565(7739): 297-298 (2019) and has been recommended in F1000Prime as being of special significance in its field by F1000 Faculty Member Pekka Lappalainen.

13. Dai S, Horton JR, Woodcock CB, Wilkinson AW, Zhang X, Gozani O, Cheng X (2019) Structural basis for the target specificity of actin histidine methyltransferase SETD3. Nat Commun. 10(1): 3541. doi: 10.1038/s41467-019-11554-6 [Epub Aug 6]

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In addition to cytosine C5 modification (5mC) in DNA and RNA, the exocyclic amino group of adenine in DNA and RNA is also methylated, resulting in N6-methyl-adenine (N6mA).

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7. Woodcock CB, Yu D, Zhang X, Cheng X (2019) Human HemK2/KMT9/N6AMT1 is an active protein methyltransferase, but does not act on DNA in vitro, in the presence of Trm112. Cell Discovery 5: 50. doi: 10.1038/s41421-019-0119-5 [Epub Sept 10]

8. Woodcock CB, Yu D, Hajian T, Li J, Huang Y, Dai N, Correa IR Jr, Wu T, Vedadi M, Zhang X, Cheng X (2019) Human MettL3¨CMettL14 complex is a sequence-specific DNA adenine methyltransferase active on single-strand and unpaired DNA in vitro. Cell Discov. 5: 63. doi: 10.1038/s41421-019-0136-4 [Epub Dec 24]

9. Woodcock CB, Horton JR, Zhang X, Blumenthal RM, Cheng X. (2020) Beta Class Amino Methyltransferases From Bacteria to Humans: Evolution and Structural Consequence. Nucleic Acids Res. 48(18): 10034-10044 doi: 10.1093/nar/gkaa446 [Epub May 26]

10. Woodcock CB, Horton JR, Zhou J, Bedford MT, Blumenthal RM, Zhang X, Cheng X. (2020) Biochemical and structural basis for YTH domain of human YTHDC1 binding to methylated adenine in DNA. Nucleic Acids Res. 48(18): 10329-10341 doi: 10.1093/nar/gkaa604 [Epub July 14]  

11. Zhang X, Blumenthal RM, Cheng X. (2021) A role for N6-methyladenine in DNA damage repair. Trends in Biochemical Sciences 46(3): 175-183 https://doi.org/10.1016/j.tibs.2020.09.007 [Epub Oct 16, 2020]

12. Yu D, Horton JR, Yang J, Hajian T, Vedadi M, Sagum CA, Bedford MT, Blumenthal RM, Zhang X, Cheng X. (2021) Human MettL3-MettL14 RNA adenine methyltransferase complex is active on double-stranded DNA containing lesions. Nucleic Acids Res. doi: 10.1093/nar/gkab460 [Epub Jun 4]

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14. Yu D, Dai N, Wolf EJ, Corr¨ºa IR Jr, Zhou J, Wu T, Blumenthal RM, Zhang X, Cheng X. (2022) Enzymatic characterization of mRNA cap adenosine-N6 methyltransferase PCIF1 activity on uncapped RNAs. J Biol Chem. 298(4): 101751. doi: 10.1016/j.jbc.2022.101751 [Epub Feb 18]

15. Yu D, Zhou J, Chen Q, Wu T, Blumenthal RM, Zhang X, Cheng X. (2022) Enzymatic Characterization of In Vitro Activity of RNA Methyltransferase PCIF1 on DNA. Biochemistry  doi: 10.1021/acs.biochem.2c00134. [Epub May 23]

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Chromatin regulates transcriptional processes through postsynthetic modifications of both of its components: DNA and histones. Much remains to be learned about how the combination of these modifications (or lack thereof) facilitates or silences transcription. One broad theme has emerged that a web of interactions tightly coordinates the modification of a segment of DNA and its associated histones, affecting local chromatin structure and determining the functional states. We are the first to illustrate the mechanistic insights of anti-correlation of histone H3 lysine 4 (H3K4) methylation and DNA methylation (2007), coordinated methylations of H3K9 and DNA (2011), and a methyl-and-phospho switch in DNMT1 (2011).

1. Tamaru H, Zhang X, McMillen D, Singh P, Nakayama J, Grewal SI, Allis CD, Cheng X, Selker EU (2003) . Nature Genetics, 34, 75-79

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In principle, epigenetic modifications alter the interaction with DNA binding proteins by strengthening, weakening, or abolishing the interaction altogether. This, in turn, can modulate gene expression and control cellular metabolism and is believed to be one of the principal mechanisms underlying epigenetic processes such as differentiation, development, aging, and disease. We have identified and determined structures of reader domains recognizing histone and DNA modifications (or lack thereof).

1. C. Qiu, K. Sawada, X. Zhang, X. Cheng (2002) . Nature Struct. Biol. 9, 217-224

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4. Liu Y, Zhang X, Blumenthal RM, Cheng X (2013) . Trends Biochem Sci. 38, 177-183

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8. Patel A, Horton JR, Wilson GG, Zhang X, Cheng X (2016) . Genes Dev. 30(3): 257-265

9. Hashimoto H, Wang D, Steves AN, Jin P, Blumenthal RM, Zhang X, Cheng X (2016) . Nucleic Acids Res. 44(21): 10177-10185

10. Wang D, Hashimoto H, Zhang X, Barwick BG, Lonial S, Boise LH, Vertino PM, Cheng X (2017) . Nucleic Acids Res. 45(5): 2396-2407

11. Hong S, Wang D, Horton JR, Zhang X, Speck SH, Blumenthal RM, Cheng X (2017) . Nucleic Acids Res. 45(5): 2503-2515  

12. Hashimoto H, Wang D, Horton JR, Zhang X, Corces VG, Cheng X (2017) . Mol. Cell 66(5): 711-720

13. Yang J, Horton JR, Wang D, Ren R, Li J, Sun D, Huang Y, Zhang X, Blumenthal RM, Cheng X (2019) Structural basis for effects of CpA modifications on C/EBPb binding of DNA. Nucleic Acids Res. 47(4): 1774-1785 [Epub Dec 19, 2018]

14. Yang J, Horton JR, Li J, Huang Y, Zhang X, Blumenthal RM, Cheng X (2019) Structural basis for preferential binding of human TCF4 to DNA containing 5-carboxylcytosine. Nucleic Acids Res. 47(16): 8375-8387. doi: 10.1093/nar/gkz381 [Epub May 13]

15. Woodcock CB, Horton JR, Zhou J, Bedford MT, Blumenthal RM, Zhang X, Cheng X. (2020) Biochemical and structural basis for YTH domain of human YTHDC1 binding to methylated adenine in DNA. Nucleic Acids Res. 48(18): 10329-10341 doi: 10.1093/nar/gkaa604 [Epub July 14]

16. Yang J, Horton JR, Akdemir KC, Li J, Huang Y, Kumar J, Blumenthal RM, Zhang X, Cheng X. (2021) Preferential CEBP binding to T:G mismatches and increased C-to-T human somatic mutations. Nucleic Acids Res. 49(9): 5084-5094. doi: 10.1093/nar/gkab276 [Epub Apr 20]

17. Ichino L, Boone BA, Strauskulage L, Harris CJ, Kaur G, Gladstone MA, Tan M, Feng S, Jami-Alahmadi Y, Duttke SH, Wohlschlegel JA, Cheng X, Redding S, Jacobsen SE. (2021) MBD5 and MBD6 couple DNA methylation to gene silencing through the J-domain protein SILENZIO. Science doi: 10.1126/science.abg6130. [Epub Jun 3]

18. Yang J, Gupta E, Horton JR, Blumenthal RM, Zhang X, Cheng X. (2022) Differential ETS1 binding to T:G mismatches within a CpG dinucleotide contributes to C-to-T somatic mutation rate of the IDH2 hotspot at codon Arg140. DNA Repair (Amst). 113: 103306. doi: 10.1016/j.dnarep.2022.103306. [Epub Feb 26]

19. Hardikar S, Ren R, Ying Z, Zhou J, Horton JR, Bramble MD, Liu B, Lu Y, Liu B, Coletta LD, Shen J, Dan J, Zhang X, Cheng X, Chen T. (2024) . Sci Adv. 10(34): eadr0036. doi: 10.1126/sciadv.adr0036. [Epub 2024 Aug 23]

We illustrated the mechanistic insight of anti-correlation of H3K4 and H3K9 methylation by PHF8 (2010). The crosstalk between different modifications also applies to non-histone proteins such as ER¦Á (2008) and NF-¦ÊB (2011).

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2. Collins RE, Northrop JP, Horton JR, Lee DY, Zhang X, Stallcup MR, Cheng X (2008) . Nature Struct. Mol. Biol. 15, 245-50

3. Subramanian K, Jia D, Kapoor-Vazirani P, Powell DR, Collins RE, Sharma D, Peng J, Cheng X, Vertino PM (2008) . Mol. Cell 30, 336-347

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6. Levy D, Kuo, AJ, Chang Y, Schaefer U, Kitson C, Cheung P, Espejo A, Zee BM, Liu CL, Tangsombatvisit S, Tennen RI, Kuo AY, Tanjing S, Cheung R, Chua KF, Utz PJ, Shi X, Prinjha RK, Lee K, Garcia BA, Bedford MT, Tarakhovsky A, Cheng X, Gozani O (2011) . Nat Immunol. 12, 29-36

7. Mahgoub M, Paiano J, Bruno M, Wu W, Pathuri S, Zhang X, Ralls S, Cheng X, Nussenzweig A, Macfarlan TS. (2020) Dual Histone Methyl Reader ZCWPW1 Facilitates Repair of Meiotic Double Strand Breaks in Male Mice. Elife 9: e53360. doi: 10.7554/eLife.53360 [Epub Apr 30] [bioRxiv: https://doi.org/10.1101/821603. Posted October 29, 2019] [see Insight by Mathilde Blot and Bernard de Massy]

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8. Yang J, Gupta E, Horton JR, Blumenthal RM, Zhang X, Cheng X. (2022) Differential ETS1 binding to T:G mismatches within a CpG dinucleotide contributes to C-to-T somatic mutation rate of the IDH2 hotspot at codon Arg140. DNA Repair (Amst). 113: 103306. doi: 10.1016/j.dnarep.2022.103306. [Epub Feb 26]

Histone lysine methylation is often compromised in cancers, and the corresponding enzymes (methyltransferases and demethylases) have since become important therapeutic targets, particularly in human cancers where these enzymes are frequently mutated and/or misregulated.

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3. Chang Y, Ganesh T, Horton JR, Spannhoff A, Liu J, Sun A, Zhang X, Bedford MT, Shinkai Y, Snyder JP, Cheng X (2010) . J Mol Biol. 400, 1-7

4. Zhao J, Du Y, Horton JR, Upadhyay AK, Lou B, Bai Y, Zhang X, Du L, Li M, Wang B, Zhang L, Barbieri JT, Khuri FR, Cheng X, Fu H (2011) . Proc Natl Acad Sci U S A. 108, 16212-6

5. Upadhyay AK, Rotili D, Han JW, Hu R, Chang Y, Labella D, Zhang X, Yoon YS, Mai A, Cheng X (2012) . J. Mol. Biol. 416, 319-327

6. Valente S, Liu Y, Schnekenburger M, Zwergel C, Cosconati S, Gros C, Tardugno M, Labella D, Florean C, Minden S, Hashimoto H, Chang Y, Zhang X, Kirsch G, Novellino E, Arimondo PB, Miele E, Ferretti E, Gulino A, Diederich M, Cheng X, Mai A (2014) . J. Med. Chem. 57, 701-13

7. Rotili D, Tarantino D, Marrocco B, Gros C, Masson V, Poughon V, Ausseil F, Chang Y, Labella D, Cosconati S, Di Maro S, Novellino E, Schnekenburger M, Grandjenette C, Bouvy C, Diederich M, Cheng X, Arimondo PB, Mai A. (2014) . PLoS One 9(5):e96941  

8. Horton JR, Engstrom A, Zoeller EL, Liu X, Shanks JR, Zhang X, Johns MA, Vertino PM, Fu H, Cheng X. (2016) . J. Biol. Chem. 291(6): 2631-46

9. Horton JR, Liu X, Gale M, Wu L, Shanks JR, Zhang X, Webber PJ, Bell JS, Kales SC, Mott BT, Rai G, Jansen DJ, Henderson MJ, Urban DJ, Hall MD, Simeonov A, Maloney DJ, Johns MA, Fu H, Jadhav A, Vertino PM, Yan Q, Cheng X (2016) . Cell Chem. Biol. 23(7): 769-81

10. Horton JR, Liu X, Wu L, Zhang K, Shanks J, Zhang X, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Pohida K, Fang Y, Hu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Yan Q, Cheng X (2018) Insights into the action of inhibitor enantiomers against histone lysine demethylase 5A. J Med Chem. 61(7): 3193-3208 [Epub Mar 14]

11. Wu L, Cao J, Cai WL, Lang SM, Horton JR, Jansen DJ, Liu ZZ, Chen JF, Zhang M, Mott BT, Pohida K, Rai G, Kales SC, Henderson MJ, Hu X, Jadhav A, Maloney DJ, Simeonov A, Zhu S, Iwasaki A, Hall MD, Cheng X, Shadel GS, Yan Q (2018) KDM5 histone demethylases repress immune response via suppression of STING. PLoS Biol. 16(8): e2006134. eCollection 2018 Aug.

12. Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Cyr M, Pohida K, Hu X, Shah P, Xu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Cheng X (2018) Structure-based engineering of irreversible inhibitors against histone lysine demethylase KDM5A. J Med Chem. 61(23): 10588¨C10601 [Epub Nov 3]

13. Milite C, Feoli A, Horton JR, Rescigno D, Cipriano A, Pisapia V, Viviano M, Pepe G, Amendola G, Novellino E, Cosconati S, Cheng X, Castellano S, Sbardella G. (2019) Discovery of a novel chemotype of histone lysine methyltransferase EHMT1/2 (GLP/G9a) inhibitors: rational design, synthesis, biological evaluation and co-crystal structure. J Med Chem. 62(5): 2666-2689 [Epub Feb 12]

14. Chen D, Meng Y, Yu D, Noinaj N, Cheng X, Huang R (2021) . ACS Chem Biol. 16(7):1234-1242. doi: 10.1021/acschembio.1c00279 [Epub Jun 30] [Posted April 13, 2021]

15. Zhou J, Horton JR, Yu D, Ren R, Blumenthal RM, Zhang X, Cheng X. (2021) Repurposing epigenetic inhibitors to target the Clostridioides difficile- specific DNA adenine methyltransferase and sporulation regulator CamA. Epigenetics doi: 10.1080/15592294.2021.1976910. [Epub Sep 15]

16. Pappalardi MB, Keenan K, Cockerill M, Kellner WA, Stowell A, Sherk C, Wong K, Pathuri S, Briand J, Steidel M, Chapman P, Groy A, Wiseman AK, McHugh CF, Campobasso N, Graves AP, Fairweather E, Werner T, Raoof A, Butlin RJ, Rueda L, Horton JR, Fosbenner DT, Zhang C, Handler JL, Muliaditan M, Mebrahtu M, Jaworski JP, McNulty DE, Burt C, Eberl HC, Taylor AN, Ho T, Merrihew S, Foley SW, Rutkowska A, Li M, Romeril SP, Goldberg K, Zhang X, Kershaw CS, Bantscheff M, Jurewicz AJ, Minthorn E, Grandi P, Patel M, Benowitz AB, Mohammad HP, Gilmartin AG, Prinjha RK, Ogilvie D, Carpenter C, Heerding D, Baylin SB, Jones PA, Cheng X, King BW, Luengo JI, Jordan AM, Waddell I, Kruger RG, McCabe MT (2021) Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nature Cancer 2(10): 1002-1017. https://doi.org/10.1038/s43018-021-00249-x [Epub Sep 27 2021] (see in brief - A safe and effective DNA hypomethylating agent)

17. Horton JR, Pathuri S, Wong K, Ren R, Rueda L, Fosbenner DT, Heerding DA, McCabe MT, Pappalardi MB, Zhang X, King BW, Cheng X. (2022) Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors. Structure. 30(6):793-802.e5. doi: 10.1016/j.str.2022.03.009. [Epub April 7]

18. Zhou J, Horton JR, Menna M, Fiorentino F, Ren R, Yu D, Hajian T, Vedadi M, Mazzoccanti G, Ciogli A, Weinhold E, H¨¹ben M, Blumenthal RM, Zhang X, Mai A, Rotili D, Cheng X. (2023) . J Med Chem. 66(1): 934-950. doi: 10.1021/acs.jmedchem.2c01789. [Epub 2022 Dec 29]

19. Zhou J, Deng Y, Iyamu ID, Horton JR, Yu D, Hajian T, Vedadi M, Rotili D, Mai A, Blumenthal RM, Zhang X, Huang R, Cheng X. (2023) . ACS Chem Biol. 18(4): 734-745. doi: 10.1021/acschembio.3c00035. [Epub 2023 Feb 22].

20. Chen Q, Liu B, Zeng Y, Hwang JW, Dai N, Corr¨ºa IR Jr, Estecio MR, Zhang X, Santos MA, Chen T, Cheng X. (2023) . NAR Cancer. 5(2): zcad022. doi: 10.1093/narcan/zcad022. [Epub 2023 May 17]