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Items: 19

1.

Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).

Kung PP, Bingham P, Brooun A, Collins M, Deng YL, Dinh D, Fan C, Gajiwala KS, Grantner R, Gukasyan HJ, Hu W, Huang B, Kania R, Kephart SE, Krivacic C, Kumpf RA, Khamphavong P, Kraus M, Liu W, Maegley KA, Nguyen L, Ren S, Richter D, Rollins RA, Sach N, Sharma S, Sherrill J, Spangler J, Stewart AE, Sutton S, Uryu S, Verhelle D, Wang H, Wang S, Wythes M, Xin S, Yamazaki S, Zhu H, Zhu J, Zehnder L, Edwards M.

J Med Chem. 2018 Feb 8;61(3):650-665. doi: 10.1021/acs.jmedchem.7b01375. Epub 2017 Dec 27.

PMID:
29211475
2.

Correction to Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.

Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M.

J Med Chem. 2016 Dec 22;59(24):11196. doi: 10.1021/acs.jmedchem.6b01747. Epub 2016 Dec 12. No abstract available.

PMID:
27936698
3.

Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.

Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M.

J Med Chem. 2016 Sep 22;59(18):8306-25. doi: 10.1021/acs.jmedchem.6b00515. Epub 2016 Sep 6. Erratum in: J Med Chem. 2016 Dec 22;59(24):11196.

PMID:
27512831
4.

Epigenetic reprogramming in solid tumors: therapeutic implications of EZH2 gain-of-function mutations.

Barsotti AM, Ryskin M, Rollins RA.

Epigenomics. 2015 Aug;7(5):687-90. doi: 10.2217/epi.15.27. Epub 2015 Aug 28. No abstract available.

PMID:
26317265
5.

Reciprocal regulation of amino acid import and epigenetic state through Lat1 and EZH2.

Dann SG, Ryskin M, Barsotti AM, Golas J, Shi C, Miranda M, Hosselet C, Lemon L, Lucas J, Karnoub M, Wang F, Myers JS, Garza SJ, Follettie MT, Geles KG, Klippel A, Rollins RA, Fantin VR.

EMBO J. 2015 Jul 2;34(13):1773-85. doi: 10.15252/embj.201488166. Epub 2015 May 15.

6.

Methylation Abnormalities in Mammary Carcinoma: The Methylation Suicide Hypothesis.

O'Donnell AH, Edwards JR, Rollins RA, Vander Kraats ND, Su T, Hibshoosh HH, Bestor TH.

J Cancer Ther. 2014 Dec 1;5(14):1311-1324.

7.

Epigenetic reprogramming by tumor-derived EZH2 gain-of-function mutations promotes aggressive 3D cell morphologies and enhances melanoma tumor growth.

Barsotti AM, Ryskin M, Zhong W, Zhang WG, Giannakou A, Loreth C, Diesl V, Follettie M, Golas J, Lee M, Nichols T, Fan C, Li G, Dann S, Fantin VR, Arndt K, Verhelle D, Rollins RA.

Oncotarget. 2015 Feb 20;6(5):2928-38.

8.

Control of mammary tumor differentiation by SKI-606 (bosutinib).

Hebbard L, Cecena G, Golas J, Sawada J, Ellies LG, Charbono A, Williams R, Jimenez RE, Wankell M, Arndt KT, DeJoy SQ, Rollins RA, Diesl V, Follettie M, Chen L, Rosfjord E, Cardiff RD, Komatsu M, Boschelli F, Oshima RG.

Oncogene. 2011 Jan 20;30(3):301-12. doi: 10.1038/onc.2010.412. Epub 2010 Sep 6.

9.

Chromatin and sequence features that define the fine and gross structure of genomic methylation patterns.

Edwards JR, O'Donnell AH, Rollins RA, Peckham HE, Lee C, Milekic MH, Chanrion B, Fu Y, Su T, Hibshoosh H, Gingrich JA, Haghighi F, Nutter R, Bestor TH.

Genome Res. 2010 Jul;20(7):972-80. doi: 10.1101/gr.101535.109. Epub 2010 May 20.

10.

Functional links between Drosophila Nipped-B and cohesin in somatic and meiotic cells.

Gause M, Webber HA, Misulovin Z, Haller G, Rollins RA, Eissenberg JC, Bickel SE, Dorsett D.

Chromosoma. 2008 Feb;117(1):51-66. Epub 2007 Oct 2.

11.

Computational prediction of methylation status in human genomic sequences.

Das R, Dimitrova N, Xuan Z, Rollins RA, Haghighi F, Edwards JR, Ju J, Bestor TH, Zhang MQ.

Proc Natl Acad Sci U S A. 2006 Jul 11;103(28):10713-6. Epub 2006 Jul 3.

12.

Metazoan Scc4 homologs link sister chromatid cohesion to cell and axon migration guidance.

Seitan VC, Banks P, Laval S, Majid NA, Dorsett D, Rana A, Smith J, Bateman A, Krpic S, Hostert A, Rollins RA, Erdjument-Bromage H, Tempst P, Benard CY, Hekimi S, Newbury SF, Strachan T.

PLoS Biol. 2006 Jul;4(8):e242.

13.

Large-scale structure of genomic methylation patterns.

Rollins RA, Haghighi F, Edwards JR, Das R, Zhang MQ, Ju J, Bestor TH.

Genome Res. 2006 Feb;16(2):157-63. Epub 2005 Dec 19.

16.

Mutations in a putative zinc-binding domain inactivate the mitochondrial intermediate peptidase.

Chew A, Rollins RA, Sakati WR, Isaya G.

Biochem Biophys Res Commun. 1996 Sep 24;226(3):822-9.

PMID:
8831696
17.

Mammalian mitochondrial intermediate peptidase: structure/function analysis of a new homologue from Schizophyllum commune and relationship to thimet oligopeptidases.

Isaya G, Sakati WR, Rollins RA, Shen GP, Hanson LC, Ullrich RC, Novotny CP.

Genomics. 1995 Aug 10;28(3):450-61.

PMID:
7490080
19.

Treatment of gynecologic wound complications.

Rollins RA, Corcoran JJ, Gibbs CE.

Obstet Gynecol. 1966 Aug;28(2):268-70. No abstract available.

PMID:
5944843

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