Mikel P Moyer
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Explore the profile of Mikel P Moyer including associated specialties, affiliations and a list of published articles.
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24
Citations
2893
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Recent Articles
1.
Fedoriw A, Rajapurkar S, OBrien S, Gerhart S, Mitchell L, Adams N, et al.
Cancer Cell
. 2019 Jul;
36(1):100-114.e25.
PMID: 31257072
Type I protein arginine methyltransferases (PRMTs) catalyze asymmetric dimethylation of arginines on proteins. Type I PRMTs and their substrates have been implicated in human cancers, suggesting inhibition of type I...
2.
Drew A, Moradei O, Jacques S, Rioux N, Boriack-Sjodin A, Allain C, et al.
Sci Rep
. 2017 Dec;
7(1):17993.
PMID: 29269946
CARM1 is an arginine methyltransferase with diverse histone and non-histone substrates implicated in the regulation of cellular processes including transcriptional co-activation and RNA processing. CARM1 overexpression has been reported in...
3.
Duncan K, Rioux N, Boriack-Sjodin P, Munchhof M, Reiter L, Majer C, et al.
ACS Med Chem Lett
. 2016 Mar;
7(2):162-6.
PMID: 26985292
The recent publication of a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) provides the scientific community with in vivo-active tool compound EPZ015666 (GSK3235025) to probe the underlying pharmacology...
4.
Kuntz K, Campbell J, Keilhack H, Pollock R, Knutson S, Porter-Scott M, et al.
J Med Chem
. 2016 Jan;
59(4):1556-64.
PMID: 26769278
Posttranslational methylation of histones plays a critical role in gene regulation. Misregulation of histone methylation can lead to oncogenic transformation. Enhancer of Zeste homologue 2 (EZH2) methylates histone 3 at...
5.
Waters N, Smith S, Olhava E, Duncan K, Burton R, ONeill J, et al.
Cancer Chemother Pharmacol
. 2015 Dec;
77(1):43-62.
PMID: 26645404
Purpose: The metabolism and disposition of the first-in-class DOT1L inhibitor, EPZ-5676 (pinometostat), was investigated in rat and dog. Metabolite profiles were compared with those from adult patients in the first-in-man...
6.
Boriack-Sjodin P, Jin L, Jacques S, Drew A, Sneeringer C, Scott M, et al.
ACS Chem Biol
. 2015 Nov;
11(3):763-71.
PMID: 26551522
Coactivator-associated arginine methyltransferase 1 (CARM1) is a protein arginine N-methyltransferase (PRMT) enzyme that has been implicated in a variety of cancers. CARM1 is known to methylate histone H3 and nonhistone...
7.
Rioux N, Duncan K, Lantz R, Miao X, Chan-Penebre E, Moyer M, et al.
Xenobiotica
. 2015 Aug;
46(3):268-77.
PMID: 26294260
1. Metabolite profiling and identification studies were conducted to understand the cross-species differences in the metabolic clearance of EPZ015666, a first-in-class protein arginine methyltransferase-5 (PRMT5) inhibitor, with anti-proliferative effects in...
8.
Mitchell L, Drew A, Ribich S, Rioux N, Swinger K, Jacques S, et al.
ACS Med Chem Lett
. 2015 Jun;
6(6):655-9.
PMID: 26101569
A novel aryl pyrazole series of arginine methyltransferase inhibitors has been identified. Synthesis of analogues within this series yielded the first potent, selective, small molecule PRMT6 inhibitor tool compound, EPZ020411....
9.
Campbell J, Kuntz K, Knutson S, Warholic N, Keilhack H, Wigle T, et al.
ACS Med Chem Lett
. 2015 May;
6(5):491-5.
PMID: 26005520
Inhibitors of the protein methyltransferase Enhancer of Zeste Homolog 2 (EZH2) may have significant therapeutic potential for the treatment of B cell lymphomas and other cancer indications. The ability of...
10.
Chan-Penebre E, Kuplast K, Majer C, Boriack-Sjodin P, Wigle T, Johnston L, et al.
Nat Chem Biol
. 2015 Apr;
11(6):432-7.
PMID: 25915199
Protein arginine methyltransferase-5 (PRMT5) is reported to have a role in diverse cellular processes, including tumorigenesis, and its overexpression is observed in cell lines and primary patient samples derived from...