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Glenn S Van Aller

Explore the profile of Glenn S Van Aller including associated specialties, affiliations and a list of published articles. Areas
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Articles 17
Citations 2409
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Recent Articles
1.
Van Aller G, Graves A, Elkins P, Bonnette W, McDevitt P, Zappacosta F, et al.
Structure . 2016 Apr; 24(5):774-781. PMID: 27066749
SMYD3 is a lysine methyltransferase overexpressed in colorectal, breast, prostate, and hepatocellular tumors, and has been implicated as an oncogene in human malignancies. Methylation of MEKK2 by SMYD3 is important...
2.
Mohammad H, Smitheman K, Kamat C, Soong D, Federowicz K, Van Aller G, et al.
Cancer Cell . 2015 Jul; 28(1):57-69. PMID: 26175415
Epigenetic dysregulation has emerged as an important mechanism in cancer. Alterations in epigenetic machinery have become a major focus for targeted therapies. The current report describes the discovery and biological...
3.
Verma S, Tian X, LaFrance L, Duquenne C, Suarez D, Newlander K, et al.
ACS Med Chem Lett . 2014 Jun; 3(12):1091-6. PMID: 24900432
The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays a critical role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. As part...
4.
Knight S, Adams N, Burgess J, Chaudhari A, Darcy M, Donatelli C, et al.
ACS Med Chem Lett . 2014 Jun; 1(1):39-43. PMID: 24900173
Phosphoinositide 3-kinase α (PI3Kα) is a critical regulator of cell growth and transformation, and its signaling pathway is the most commonly mutated pathway in human cancers. The mammalian target of...
5.
Mazur P, Reynoird N, Khatri P, Jansen P, Wilkinson A, Liu S, et al.
Nature . 2014 May; 510(7504):283-7. PMID: 24847881
Deregulation of lysine methylation signalling has emerged as a common aetiological factor in cancer pathogenesis, with inhibitors of several histone lysine methyltransferases (KMTs) being developed as chemotherapeutics. The largely cytoplasmic...
6.
Van Aller G, Pappalardi M, Ott H, Diaz E, Brandt M, Schwartz B, et al.
ACS Chem Biol . 2013 Dec; 9(3):622-9. PMID: 24304166
EZH2/PRC2 catalyzes transcriptionally repressive methylation at lysine 27 of histone H3 and has been associated with numerous cancer types. Point mutations in EZH2 at Tyr641 and Ala677 identified in non-Hodgkin...
7.
Beguelin W, Popovic R, Teater M, Jiang Y, Bunting K, Rosen M, et al.
Cancer Cell . 2013 May; 23(5):677-92. PMID: 23680150
The EZH2 histone methyltransferase is highly expressed in germinal center (GC) B cells and targeted by somatic mutations in B cell lymphomas. Here, we find that EZH2 deletion or pharmacologic...
8.
McCabe M, Ott H, Ganji G, Korenchuk S, Thompson C, Van Aller G, et al.
Nature . 2012 Oct; 492(7427):108-12. PMID: 23051747
In eukaryotes, post-translational modification of histones is critical for regulation of chromatin structure and gene expression. EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2) and is...
9.
Diaz E, Machutta C, Chen S, Jiang Y, Nixon C, Hofmann G, et al.
J Biomol Screen . 2012 Aug; 17(10):1279-92. PMID: 22904200
Histone methyltransferases (HMT) catalyze the methylation of histone tail lysines, resulting in changes in gene transcription. Misregulation of these enzymes has been associated with various forms of cancer, making this...
10.
Axten J, Medina J, Blackledge C, Duquenne C, Grant S, Bobko M, et al.
Bioorg Med Chem Lett . 2012 May; 22(12):4028-32. PMID: 22579486
A new class of PDF inhibitor with potent, broad spectrum antibacterial activity is described. Optimization of blood stability and potency provided compounds with improved pharmacokinetics that were suitable for in...