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For: Kong X, Chen L, Jiao L, Jiang X, Lian F, Lu J, Zhu K, Du D, Liu J, Ding H, Zhang N, Shen J, Zheng M, Chen K, Liu X, Jiang H, Luo C. Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2. J Med Chem 2014;57:9512-21. [PMID: 25369470 DOI: 10.1021/jm501230c] [Citation(s) in RCA: 76] [Impact Index Per Article: 6.9] [Reference Citation Analysis] [What about the content of this article? (0)] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/17/2022]
Number Cited by Other Article(s)
1
Cao D, Liu G, Wang Y, Xia X. Repurposing astemizole to kill multidrug-resistant bacteria isolated in general surgery. Microb Pathog 2025;200:107369. [PMID: 39929397 DOI: 10.1016/j.micpath.2025.107369] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 10/25/2024] [Revised: 01/31/2025] [Accepted: 02/07/2025] [Indexed: 02/13/2025]
2
Cheng S, Li J, Song YQ, Jing S, Lan YX, Wang L, Chan DSH, Wong CY, Sheng C, Wang W, Wang HMD, Leung CH. A Bioactive Benzimidazole-Cyclometalated Iridium(III) Complex as an Epigenetic Regulator through Effectively Interrupting the EED-EZH2 Interaction. SMALL (WEINHEIM AN DER BERGSTRASSE, GERMANY) 2025;21:e2405771. [PMID: 39967436 DOI: 10.1002/smll.202405771] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Subscribe] [Scholar Register] [Received: 07/11/2024] [Revised: 01/24/2025] [Indexed: 02/20/2025]
3
Ji Y, Chen Z, Cai J. Roles and mechanisms of histone methylation in vascular aging and related diseases. Clin Epigenetics 2025;17:35. [PMID: 39988699 PMCID: PMC11849368 DOI: 10.1186/s13148-025-01842-y] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/20/2024] [Accepted: 02/14/2025] [Indexed: 02/25/2025]  Open
4
Perumal N, Gopalakrishnan P, Burkovetskaya M, Doss D, Dukkipati SS, Kanchan RK, Mahapatra S. Nuclear factor I/B: Duality in action in cancer pathophysiology. Cancer Lett 2025;609:217349. [PMID: 39581218 DOI: 10.1016/j.canlet.2024.217349] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/07/2024] [Revised: 11/15/2024] [Accepted: 11/21/2024] [Indexed: 11/26/2024]
5
Wagih N, Abdel-Rahman IM, El-Koussi NA, El-Din A Abuo-Rahma G. Anticancer benzimidazole derivatives as inhibitors of epigenetic targets: a review article. RSC Adv 2025;15:966-1010. [PMID: 39807197 PMCID: PMC11726184 DOI: 10.1039/d4ra05014b] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/11/2024] [Accepted: 12/11/2024] [Indexed: 01/16/2025]  Open
6
Wozniak M, Czyz M. Exploring oncogenic roles and clinical significance of EZH2: focus on non-canonical activities. Ther Adv Med Oncol 2025;17:17588359241306026. [PMID: 39776536 PMCID: PMC11705335 DOI: 10.1177/17588359241306026] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/20/2024] [Accepted: 11/21/2024] [Indexed: 01/11/2025]  Open
7
Chang Y, Guo H, Li X, Zong L, Wei J, Li Z, Luo C, Yang X, Fang H, Kong X, Hou X. Development of a First-in-Class DNMT1/HDAC Inhibitor with Improved Therapeutic Potential and Potentiated Antitumor Immunity. J Med Chem 2024;67:16480-16504. [PMID: 39264152 DOI: 10.1021/acs.jmedchem.4c01310] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 09/13/2024]
8
Bao Q, Kumar A, Wu D, Zhou J. Targeting EED as a key PRC2 complex mediator toward novel epigenetic therapeutics. Drug Discov Today 2024;29:103986. [PMID: 38642703 PMCID: PMC11416859 DOI: 10.1016/j.drudis.2024.103986] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/23/2024] [Revised: 04/06/2024] [Accepted: 04/15/2024] [Indexed: 04/22/2024]
9
Huang X, Chen Y, Xiao Q, Shang X, Liu Y. Chemical inhibitors targeting histone methylation readers. Pharmacol Ther 2024;256:108614. [PMID: 38401773 DOI: 10.1016/j.pharmthera.2024.108614] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/19/2023] [Revised: 02/01/2024] [Accepted: 02/15/2024] [Indexed: 02/26/2024]
10
Guo Y, Cheng R, Wang Y, Gonzalez ME, Zhang H, Liu Y, Kleer CG, Xue L. Regulation of EZH2 protein stability: new mechanisms, roles in tumorigenesis, and roads to the clinic. EBioMedicine 2024;100:104972. [PMID: 38244292 PMCID: PMC10835131 DOI: 10.1016/j.ebiom.2024.104972] [Citation(s) in RCA: 7] [Impact Index Per Article: 7.0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 10/05/2023] [Revised: 12/13/2023] [Accepted: 01/04/2024] [Indexed: 01/22/2024]  Open
11
Wang D, Guo Q, Wu Z, Li M, He B, Du Y, Zhang K, Tao Y. Molecular mechanism of antihistamines recognition and regulation of the histamine H1 receptor. Nat Commun 2024;15:84. [PMID: 38167898 PMCID: PMC10762250 DOI: 10.1038/s41467-023-44477-4] [Citation(s) in RCA: 11] [Impact Index Per Article: 11.0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/02/2023] [Accepted: 12/14/2023] [Indexed: 01/05/2024]  Open
12
Chandnani N, Gupta I, Thakkar V, Sarkar K. Epigenetic regulation of enhancer of zeste homolog 2 (EZH2) -Yin Yang 1 (YY1) axis in cancer. Pathol Res Pract 2023;251:154885. [PMID: 37862922 DOI: 10.1016/j.prp.2023.154885] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 08/26/2023] [Revised: 10/08/2023] [Accepted: 10/09/2023] [Indexed: 10/22/2023]
13
Giuliano S, Montemagno C, Domdom MA, Teisseire M, Brest P, Klionsky DJ, Hofman P, Pagès G, Mograbi B. Should evidence of an autolysosomal de-acidification defect in Alzheimer and Parkinson diseases call for caution in prescribing chronic PPI and DMARD? Autophagy 2023;19:2800-2806. [PMID: 37482676 PMCID: PMC10472882 DOI: 10.1080/15548627.2023.2214960] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/14/2022] [Revised: 04/18/2023] [Accepted: 05/08/2023] [Indexed: 07/25/2023]  Open
14
Campbell WA, El-Hodiri HM, Torres D, Hawthorn EC, Kelly LE, Volkov L, Akanonu D, Fischer AJ. Chromatin access regulates the formation of Müller glia-derived progenitor cells in the retina. Glia 2023;71:1729-1754. [PMID: 36971459 PMCID: PMC11335016 DOI: 10.1002/glia.24366] [Citation(s) in RCA: 10] [Impact Index Per Article: 5.0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/07/2022] [Revised: 03/06/2023] [Accepted: 03/12/2023] [Indexed: 03/29/2023]
15
Liu Y, Yang Q. The roles of EZH2 in cancer and its inhibitors. Med Oncol 2023;40:167. [PMID: 37148376 PMCID: PMC10162908 DOI: 10.1007/s12032-023-02025-6] [Citation(s) in RCA: 47] [Impact Index Per Article: 23.5] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/26/2023] [Accepted: 04/10/2023] [Indexed: 05/08/2023]
16
Ghate NB, Kim S, Shin Y, Kim J, Doche M, Valena S, Situ A, Kim S, Rhie SK, Lenz HJ, Ulmer TS, Mumenthaler SM, An W. Phosphorylation and stabilization of EZH2 by DCAF1/VprBP trigger aberrant gene silencing in colon cancer. Nat Commun 2023;14:2140. [PMID: 37069142 PMCID: PMC10110550 DOI: 10.1038/s41467-023-37883-1] [Citation(s) in RCA: 4] [Impact Index Per Article: 2.0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/08/2022] [Accepted: 04/04/2023] [Indexed: 04/19/2023]  Open
17
Hanot M, Raby L, Völkel P, Le Bourhis X, Angrand PO. The Contribution of the Zebrafish Model to the Understanding of Polycomb Repression in Vertebrates. Int J Mol Sci 2023;24:ijms24032322. [PMID: 36768643 PMCID: PMC9916924 DOI: 10.3390/ijms24032322] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/29/2022] [Revised: 01/20/2023] [Accepted: 01/21/2023] [Indexed: 01/26/2023]  Open
18
Multiomics characteristics and immunotherapeutic potential of EZH2 in pan-cancer. Biosci Rep 2023;43:232355. [PMID: 36545914 PMCID: PMC9842950 DOI: 10.1042/bsr20222230] [Citation(s) in RCA: 5] [Impact Index Per Article: 2.5] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/03/2022] [Revised: 11/29/2022] [Accepted: 12/13/2022] [Indexed: 12/24/2022]  Open
19
Guo Y, Yu Y, Wang GG. Polycomb Repressive Complex 2 in Oncology. Cancer Treat Res 2023;190:273-320. [PMID: 38113005 DOI: 10.1007/978-3-031-45654-1_9] [Citation(s) in RCA: 2] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/21/2023]
20
Mészáros B, Csoti A, Szanto TG, Telek A, Kovács K, Toth A, Volkó J, Panyi G. The hEag1 K+ Channel Inhibitor Astemizole Stimulates Ca2+ Deposition in SaOS-2 and MG-63 Osteosarcoma Cultures. Int J Mol Sci 2022;23:ijms231810533. [PMID: 36142445 PMCID: PMC9504018 DOI: 10.3390/ijms231810533] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/02/2022] [Revised: 08/27/2022] [Accepted: 09/06/2022] [Indexed: 11/29/2022]  Open
21
Critical Roles of Polycomb Repressive Complexes in Transcription and Cancer. Int J Mol Sci 2022;23:ijms23179574. [PMID: 36076977 PMCID: PMC9455514 DOI: 10.3390/ijms23179574] [Citation(s) in RCA: 6] [Impact Index Per Article: 2.0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/24/2022] [Revised: 08/16/2022] [Accepted: 08/18/2022] [Indexed: 11/17/2022]  Open
22
Xu L, Zhang J, Sun J, Hou K, Yang C, Guo Y, Liu X, Kalvakolanu DV, Zhang L, Guo B. Epigenetic regulation of cancer stem cells: Shedding light on the refractory/relapsed cancers. Biochem Pharmacol 2022;202:115110. [PMID: 35640714 DOI: 10.1016/j.bcp.2022.115110] [Citation(s) in RCA: 2] [Impact Index Per Article: 0.7] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/31/2022] [Revised: 05/23/2022] [Accepted: 05/24/2022] [Indexed: 02/05/2023]
23
Van den Eynde C, Held K, Ciprietti M, De Clercq K, Kerselaers S, Marchand A, Chaltin P, Voets T, Vriens J. Loratadine, an antihistaminic drug, suppresses the proliferation of endometrial stromal cells by inhibition of TRPV2. Eur J Pharmacol 2022;928:175086. [PMID: 35714693 DOI: 10.1016/j.ejphar.2022.175086] [Citation(s) in RCA: 5] [Impact Index Per Article: 1.7] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/24/2021] [Revised: 06/01/2022] [Accepted: 06/01/2022] [Indexed: 11/03/2022]
24
Wang B, Zhou MJ, Zhou QL. Visible-Light-Induced α,γ-C(sp3)-H Difunctionalization of Piperidines. Org Lett 2022;24:2894-2898. [PMID: 35416677 DOI: 10.1021/acs.orglett.2c00831] [Citation(s) in RCA: 2] [Impact Index Per Article: 0.7] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/16/2022]
25
Recent progress on small molecules targeting epigenetic complexes. Curr Opin Chem Biol 2022;67:102130. [DOI: 10.1016/j.cbpa.2022.102130] [Citation(s) in RCA: 3] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/27/2021] [Revised: 01/13/2022] [Accepted: 01/26/2022] [Indexed: 12/16/2022]
26
Zeng J, Zhang J, Sun Y, Wang J, Ren C, Banerjee S, Ouyang L, Wang Y. Targeting EZH2 for cancer therapy: From current progress to novel strategies. Eur J Med Chem 2022;238:114419. [DOI: 10.1016/j.ejmech.2022.114419] [Citation(s) in RCA: 4] [Impact Index Per Article: 1.3] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/03/2022] [Revised: 04/19/2022] [Accepted: 04/26/2022] [Indexed: 12/14/2022]
27
Identification of SET/EED dual binders as innovative PRC2 inhibitors. Future Med Chem 2022;14:609-621. [DOI: 10.4155/fmc-2022-0010] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/17/2022]  Open
28
Link between the EZH2 noncanonical pathway and microtubule organization center polarization during early T lymphopoiesis. Sci Rep 2022;12:3655. [PMID: 35256668 PMCID: PMC8901749 DOI: 10.1038/s41598-022-07684-5] [Citation(s) in RCA: 1] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/03/2021] [Accepted: 02/22/2022] [Indexed: 12/11/2022]  Open
29
Mirzaei S, Gholami MH, Hushmandi K, Hashemi F, Zabolian A, Canadas I, Zarrabi A, Nabavi N, Aref AR, Crea F, Wang Y, Ashrafizadeh M, Kumar AP. The long and short non-coding RNAs modulating EZH2 signaling in cancer. J Hematol Oncol 2022;15:18. [PMID: 35236381 PMCID: PMC8892735 DOI: 10.1186/s13045-022-01235-1] [Citation(s) in RCA: 122] [Impact Index Per Article: 40.7] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/03/2021] [Accepted: 02/09/2022] [Indexed: 02/08/2023]  Open
30
Zhang Q, Yang H, Feng Q, Cao J, Zhang Y, Li L, Yu L. Focus on the classical and non-classical functions of EZH2: Guide the development of inhibitors and degraders. Pharmacol Res 2022;178:106159. [DOI: 10.1016/j.phrs.2022.106159] [Citation(s) in RCA: 1] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 12/26/2021] [Revised: 02/28/2022] [Accepted: 03/03/2022] [Indexed: 12/16/2022]
31
Levy S, Somasundaram L, Raj IX, Ic-Mex D, Phal A, Schmidt S, Ng WI, Mar D, Decarreau J, Moss N, Alghadeer A, Honkanen H, Sarthy J, Vitanza N, Hawkins RD, Mathieu J, Wang Y, Baker D, Bomsztyk K, Ruohola-Baker H. dCas9 fusion to computer-designed PRC2 inhibitor reveals functional TATA box in distal promoter region. Cell Rep 2022;38:110457. [PMID: 35235780 PMCID: PMC8984963 DOI: 10.1016/j.celrep.2022.110457] [Citation(s) in RCA: 16] [Impact Index Per Article: 5.3] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/30/2020] [Revised: 11/23/2021] [Accepted: 02/08/2022] [Indexed: 11/18/2022]  Open
32
Zhao Y, Guan YY, Zhao F, Yu T, Zhang SJ, Zhang YZ, Duan YC, Zhou XL. Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs. Eur J Med Chem 2022;231:114144. [DOI: 10.1016/j.ejmech.2022.114144] [Citation(s) in RCA: 1] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/13/2021] [Revised: 12/27/2021] [Accepted: 01/17/2022] [Indexed: 11/26/2022]
33
Liu KL, Zhu K, Zhang H. An overview of the development of EED inhibitors to disable the PRC2 function. RSC Med Chem 2022;13:39-53. [PMID: 35224495 PMCID: PMC8792826 DOI: 10.1039/d1md00274k] [Citation(s) in RCA: 14] [Impact Index Per Article: 4.7] [Reference Citation Analysis] [Abstract] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/15/2021] [Accepted: 10/21/2021] [Indexed: 10/24/2023]  Open
34
Conery AR, Rocnik JL, Trojer P. Small molecule targeting of chromatin writers in cancer. Nat Chem Biol 2021;18:124-133. [PMID: 34952934 DOI: 10.1038/s41589-021-00920-5] [Citation(s) in RCA: 14] [Impact Index Per Article: 3.5] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/13/2020] [Accepted: 10/13/2021] [Indexed: 01/10/2023]
35
Wang S, C Ordonez-Rubiano S, Dhiman A, Jiao G, Strohmier BP, Krusemark CJ, Dykhuizen EC. Polycomb group proteins in cancer: multifaceted functions and strategies for modulation. NAR Cancer 2021;3:zcab039. [PMID: 34617019 PMCID: PMC8489530 DOI: 10.1093/narcan/zcab039] [Citation(s) in RCA: 10] [Impact Index Per Article: 2.5] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/09/2021] [Revised: 08/24/2021] [Accepted: 09/10/2021] [Indexed: 12/12/2022]  Open
36
Zoroddu S, Marchesi I, Bagella L. PRC2: an epigenetic multiprotein complex with a key role in the development of rhabdomyosarcoma carcinogenesis. Clin Epigenetics 2021;13:156. [PMID: 34372908 PMCID: PMC8351429 DOI: 10.1186/s13148-021-01147-w] [Citation(s) in RCA: 10] [Impact Index Per Article: 2.5] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/09/2021] [Accepted: 08/02/2021] [Indexed: 02/02/2023]  Open
37
Tomassi S, Romanelli A, Zwergel C, Valente S, Mai A. Polycomb Repressive Complex 2 Modulation through the Development of EZH2-EED Interaction Inhibitors and EED Binders. J Med Chem 2021;64:11774-11797. [PMID: 34351144 PMCID: PMC8404197 DOI: 10.1021/acs.jmedchem.1c00226] [Citation(s) in RCA: 33] [Impact Index Per Article: 8.3] [Reference Citation Analysis] [Abstract] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/31/2022]
38
Du D, Xu D, Zhu L, Stazi G, Zwergel C, Liu Y, Luo Z, Li Y, Zhang Y, Zhu K, Ding Y, Liu J, Fan S, Zhao K, Zhang N, Kong X, Jiang H, Chen K, Zhao K, Valente S, Min J, Duan W, Luo C. Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction. J Med Chem 2021;64:8194-8207. [PMID: 34077206 DOI: 10.1021/acs.jmedchem.0c02261] [Citation(s) in RCA: 22] [Impact Index Per Article: 5.5] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/13/2022]
39
Li X, Gera L, Zhang S, Chen Y, Lou L, Wilson LM, Xie ZR, Sautto G, Liu D, Danaher A, Mamouni K, Yang Y, Du Y, Fu H, Kucuk O, Osunkoya AO, Zhou J, Wu D. Pharmacological inhibition of noncanonical EED-EZH2 signaling overcomes chemoresistance in prostate cancer. Theranostics 2021;11:6873-6890. [PMID: 34093859 PMCID: PMC8171087 DOI: 10.7150/thno.49235] [Citation(s) in RCA: 20] [Impact Index Per Article: 5.0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/08/2020] [Accepted: 04/22/2021] [Indexed: 12/25/2022]  Open
40
Davidovich C, Zhang Q. Allosteric regulation of histone lysine methyltransferases: from context-specific regulation to selective drugs. Biochem Soc Trans 2021;49:591-607. [PMID: 33769454 PMCID: PMC8106495 DOI: 10.1042/bst20200238] [Citation(s) in RCA: 3] [Impact Index Per Article: 0.8] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/19/2021] [Revised: 03/02/2021] [Accepted: 03/03/2021] [Indexed: 02/06/2023]
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Identification of novel EED-EZH2 PPI inhibitors using an in silico fragment mapping method. J Comput Aided Mol Des 2021;35:601-611. [PMID: 33635506 DOI: 10.1007/s10822-021-00378-6] [Citation(s) in RCA: 4] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Key Words] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/01/2020] [Accepted: 02/11/2021] [Indexed: 12/27/2022]
42
Martin MC, Zeng G, Yu J, Schiltz GE. Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer. J Med Chem 2020;63:15344-15370. [PMID: 33283516 DOI: 10.1021/acs.jmedchem.0c01344] [Citation(s) in RCA: 33] [Impact Index Per Article: 6.6] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/19/2022]
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Martin CJ, Moorehead RA. Polycomb repressor complex 2 function in breast cancer (Review). Int J Oncol 2020;57:1085-1094. [PMID: 33491744 PMCID: PMC7549536 DOI: 10.3892/ijo.2020.5122] [Citation(s) in RCA: 7] [Impact Index Per Article: 1.4] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/10/2020] [Accepted: 09/07/2020] [Indexed: 11/24/2022]  Open
44
Li Q, Liu KY, Liu Q, Wang G, Jiang W, Meng Q, Yi Y, Yang Y, Wang R, Zhu S, Li C, Wu L, Zhao D, Yan L, Zhang L, Kim JS, Zu X, Kozielski AJ, Qian W, Chang JC, Patnaik A, Chen K, Cao Q. Antihistamine Drug Ebastine Inhibits Cancer Growth by Targeting Polycomb Group Protein EZH2. Mol Cancer Ther 2020;19:2023-2033. [PMID: 32855270 PMCID: PMC7541747 DOI: 10.1158/1535-7163.mct-20-0250] [Citation(s) in RCA: 13] [Impact Index Per Article: 2.6] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/30/2020] [Revised: 05/21/2020] [Accepted: 08/05/2020] [Indexed: 12/17/2022]
45
Chen Y, Bi X, Zhang F, Sun Z, Xu P, Jiang H, Lu W, Lu T, Ding H, Zhang N, Jiang H, Chen K, Zhou B, Luo C. Design, synthesis, and biological evaluation of tetrahydroquinolin derivatives as potent inhibitors of CBP bromodomain. Bioorg Chem 2020;101:103991. [PMID: 32559581 DOI: 10.1016/j.bioorg.2020.103991] [Citation(s) in RCA: 4] [Impact Index Per Article: 0.8] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/10/2020] [Revised: 05/28/2020] [Accepted: 06/01/2020] [Indexed: 12/23/2022]
46
Duan R, Du W, Guo W. EZH2: a novel target for cancer treatment. J Hematol Oncol 2020;13:104. [PMID: 32723346 PMCID: PMC7385862 DOI: 10.1186/s13045-020-00937-8] [Citation(s) in RCA: 563] [Impact Index Per Article: 112.6] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/03/2020] [Accepted: 07/13/2020] [Indexed: 12/17/2022]  Open
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Chen Y, Jin J. The application of ubiquitin ligases in the PROTAC drug design. Acta Biochim Biophys Sin (Shanghai) 2020;52:776-790. [PMID: 32506133 DOI: 10.1093/abbs/gmaa053] [Citation(s) in RCA: 7] [Impact Index Per Article: 1.4] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/13/2020] [Revised: 06/25/2019] [Accepted: 06/26/2019] [Indexed: 12/13/2022]  Open
48
Zhou Y, Du DH, Wang J, Cai XQ, Deng AX, Nosjean O, Boutin JA, Renard P, Yang DH, Luo C, Wang MW. Identification of catalytic and non-catalytic activity inhibitors against PRC2-EZH2 complex through multiple high-throughput screening campaigns. Chem Biol Drug Des 2020;96:1024-1051. [PMID: 32394628 DOI: 10.1111/cbdd.13702] [Citation(s) in RCA: 5] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/13/2020] [Revised: 04/21/2020] [Accepted: 04/26/2020] [Indexed: 12/19/2022]
49
Cartron PF, Cheray M, Bretaudeau L. Epigenetic protein complexes: the adequate candidates for the use of a new generation of epidrugs in personalized and precision medicine in cancer. Epigenomics 2020;12:171-177. [DOI: 10.2217/epi-2019-0169] [Citation(s) in RCA: 4] [Impact Index Per Article: 0.8] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 02/08/2023]  Open
50
Lu W, Wang J, Li Y, Tao H, Xiong H, Lian F, Gao J, Ma H, Lu T, Zhang D, Ye X, Ding H, Yue L, Zhang Y, Tang H, Zhang N, Yang Y, Jiang H, Chen K, Zhou B, Luo C. Discovery and biological evaluation of vinylsulfonamide derivatives as highly potent, covalent TEAD autopalmitoylation inhibitors. Eur J Med Chem 2019;184:111767. [PMID: 31622854 DOI: 10.1016/j.ejmech.2019.111767] [Citation(s) in RCA: 62] [Impact Index Per Article: 10.3] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/10/2019] [Revised: 09/24/2019] [Accepted: 10/06/2019] [Indexed: 01/09/2023]
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