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Literature DB >> 28414199

Structure of the PRC2 complex and application to drug discovery.

Yi Shi¹, Xiao-Xi Wang¹, You-Wen Zhuang¹, Yi Jiang¹, Karsten Melcher², H Eric Xu^1,2.

Abstract

The polycomb repressive complexes 2 (PRC2) complex catalyzes tri-methylation of histone H3 lysine 27 (H3K27), a repressive chromatin marker associated with gene silencing. Overexpression and mutations of PRC2 are found in a wide variety of cancers, making the catalytic activity of PRC2 an important target of cancer therapy. This review highlights recent structural breakthroughs of the human PRC2 complex bound to the H3K27 peptide and a small molecule inhibitor, which provide critically needed insight into PRC2-targeted drug discovery.

Entities: Chemical Disease Species

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Year: 2017 PMID： 28414199 PMCID： PMC5519257 DOI： 10.1038/aps.2017.7

Source DB: PubMed Journal: Acta Pharmacol Sin ISSN： 1671-4083 Impact factor: 6.150

114 in total

1. Subunit contributions to histone methyltransferase activities of fly and worm polycomb group complexes.

Authors: Carrie S Ketel; Erica F Andersen; Marcus L Vargas; Jinkyo Suh; Susan Strome; Jeffrey A Simon
Journal: Mol Cell Biol Date: 2005-08 Impact factor: 4.272

2. Structural basis of EZH2 recognition by EED.

Authors: Zhifu Han; Xinmiao Xing; Min Hu; Yin Zhang; Peiyuan Liu; Jijie Chai
Journal: Structure Date: 2007-10 Impact factor: 5.006

3. EZH2: a potential new target in T-cell lymphoma?

Authors: Lisa Giulino-Roth
Journal: Leuk Lymphoma Date: 2015-02-14

4. The methyltransferase Ezh2 controls cell adhesion and migration through direct methylation of the extranuclear regulatory protein talin.

Authors: Merry Gunawan; Nandini Venkatesan; Jia Tong Loh; Jong Fu Wong; Heidi Berger; Wen Hao Neo; Liang Yao Jackson Li; Myint Khun La Win; Yin Hoe Yau; Tiannan Guo; Peter Chi Ee See; Sayuri Yamazaki; Keh Chuang Chin; Alexandre R Gingras; Susana Geifman Shochat; Lai Guan Ng; Siu Kwan Sze; Florent Ginhoux; I-hsin Su
Journal: Nat Immunol Date: 2015-03-09 Impact factor: 25.606

5. Isolation of a cDNA encoding a metal response element binding protein using a novel expression cloning procedure: the one hybrid system.

Authors: C Inouye; P Remondelli; M Karin; S Elledge
Journal: DNA Cell Biol Date: 1994-07 Impact factor: 3.311

6. Polycomb PHF19 binds H3K36me3 and recruits PRC2 and demethylase NO66 to embryonic stem cell genes during differentiation.

Authors: Gerard L Brien; Guillermo Gambero; David J O'Connell; Emilia Jerman; Siobhán A Turner; Chris M Egan; Eiseart J Dunne; Maike C Jurgens; Kieran Wynne; Lianhua Piao; Amanda J Lohan; Neil Ferguson; Xiaobing Shi; Krishna M Sinha; Brendan J Loftus; Gerard Cagney; Adrian P Bracken
Journal: Nat Struct Mol Biol Date: 2012-11-18 Impact factor: 15.369

7. Jarid2/Jumonji coordinates control of PRC2 enzymatic activity and target gene occupancy in pluripotent cells.

Authors: Jamy C Peng; Anton Valouev; Tomek Swigut; Junmei Zhang; Yingming Zhao; Arend Sidow; Joanna Wysocka
Journal: Cell Date: 2009-12-24 Impact factor: 41.582

Review 8. Targeting EZH2 in cancer.

Authors: Kimberly H Kim; Charles W M Roberts
Journal: Nat Med Date: 2016-02 Impact factor: 53.440

9. PRC2 binds active promoters and contacts nascent RNAs in embryonic stem cells.

Authors: Syuzo Kaneko; Jinsook Son; Steven S Shen; Danny Reinberg; Roberto Bonasio
Journal: Nat Struct Mol Biol Date: 2013-10-20 Impact factor: 15.369

10. Polycomb repressive complex 2 (PRC2) silences genes responsible for neurodegeneration.

Authors: Melanie von Schimmelmann; Philip A Feinberg; Josefa M Sullivan; Stacy M Ku; Ana Badimon; Mary Kaye Duff; Zichen Wang; Alexander Lachmann; Scott Dewell; Avi Ma'ayan; Ming-Hu Han; Alexander Tarakhovsky; Anne Schaefer
Journal: Nat Neurosci Date: 2016-08-15 Impact factor: 24.884

10 in total

10. suz12 inactivation in p53- and nf1-deficient zebrafish accelerates the onset of malignant peripheral nerve sheath tumors and expands the spectrum of tumor types.

Authors: Felix Oppel; Dong H Ki; Mark W Zimmerman; Kenneth N Ross; Ting Tao; Hui Shi; Shuning He; Jon C Aster; A Thomas Look
Journal: Dis Model Mech Date: 2020-08-27 Impact factor: 5.758

10 in total

Structure of the PRC2 complex and application to drug discovery.

1. Subunit contributions to histone methyltransferase activities of fly and worm polycomb group complexes.

2. Structural basis of EZH2 recognition by EED.

3. EZH2: a potential new target in T-cell lymphoma?

4. The methyltransferase Ezh2 controls cell adhesion and migration through direct methylation of the extranuclear regulatory protein talin.

5. Isolation of a cDNA encoding a metal response element binding protein using a novel expression cloning procedure: the one hybrid system.

6. Polycomb PHF19 binds H3K36me3 and recruits PRC2 and demethylase NO66 to embryonic stem cell genes during differentiation.

7. Jarid2/Jumonji coordinates control of PRC2 enzymatic activity and target gene occupancy in pluripotent cells.

Review 8. Targeting EZH2 in cancer.

9. PRC2 binds active promoters and contacts nascent RNAs in embryonic stem cells.

10. Polycomb repressive complex 2 (PRC2) silences genes responsible for neurodegeneration.

1. New twists on long noncoding RNAs: from mobile elements to motile cancer cells.

2. C10ORF12 modulates PRC2 histone methyltransferase activity and H3K27me3 levels.

3. Telomere dysfunction cooperates with epigenetic alterations to impair murine embryonic stem cell fate commitment.

Review 4. Epigenetic regulation of HIV-1 latency: focus on polycomb group (PcG) proteins.

Review 5. Thiadiazole derivatives as anticancer agents.

Review 6. Polycomb Repressive Complex 2 in Eukaryotes-An Evolutionary Perspective.

Review 7. Diversity of Dysregulated Long Non-Coding RNAs in HBV-Related Hepatocellular Carcinoma.

Review 8. Polycomb Directed Cell Fate Decisions in Development and Cancer.

9. MiR-34 inhibits polycomb repressive complex 2 to modulate chaperone expression and promote healthy brain aging.

10. suz12 inactivation in p53- and nf1-deficient zebrafish accelerates the onset of malignant peripheral nerve sheath tumors and expands the spectrum of tumor types.