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
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2893
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Recent Articles
11.
Rioux N, Mitchell L, Tiller P, Plant K, Shaw J, Frost K, et al.
Drug Metab Dispos
. 2015 Apr;
43(7):936-43.
PMID: 25887455
Pharmacokinetic and metabolite identification studies were conducted to understand the clearance pathways of EPZ011652 [(2-aminoethyl)(methyl)({3-[4-(propan-2-yloxy)phenyl]-1H-pyrazol-4-yl}methyl)amine], a potent protein arginine N-methyltransferase inhibitor. Metabolic clearance was the major pathway of EPZ011652 elimination...
12.
Wigle T, Swinger K, Campbell J, Scholle M, Sherrill J, Admirand E, et al.
J Biomol Screen
. 2015 Mar;
20(6):810-20.
PMID: 25755264
Demethylation of histones by lysine demethylases (KDMs) plays a critical role in controlling gene transcription. Aberrant demethylation may play a causal role in diseases such as cancer. Despite the biological...
13.
Knutson S, Warholic N, Johnston L, Klaus C, Wigle T, Iwanowicz D, et al.
PLoS One
. 2014 Dec;
9(12):e111840.
PMID: 25493630
Patients with non-Hodgkin lymphoma (NHL) are treated today with a cocktail of drugs referred to as CHOP (Cyclophosphamide, Hydroxyldaunorubicin, Oncovin, and Prednisone). Subsets of patients with NHL of germinal center...
14.
Swalm B, Knutson S, Warholic N, Jin L, Kuntz K, Keilhack H, et al.
ACS Chem Biol
. 2014 Aug;
9(11):2459-64.
PMID: 25154026
EZH2 and EZH1 are protein methyltransferases (PMTs) responsible for histone H3, lysine 27 (H3K27) methylation. Trimethylation of H3K27 (H3K27me3) is a hallmark of many cancers, including non-Hodgkin lymphoma (NHL). Heterozygous...
15.
Klaus C, Iwanowicz D, Johnston D, Campbell C, Smith J, Moyer M, et al.
J Pharmacol Exp Ther
. 2014 Jul;
350(3):646-56.
PMID: 24993360
EPZ-5676 [(2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol], a small-molecule inhibitor of the protein methyltransferase DOT1L, is currently under clinical investigation for acute leukemias bearing MLL-rearrangements (MLL-r). In this study, we evaluated EPZ-5676 in combination with...
16.
Knutson S, Kawano S, Minoshima Y, Warholic N, Huang K, Xiao Y, et al.
Mol Cancer Ther
. 2014 Feb;
13(4):842-54.
PMID: 24563539
Mutations within the catalytic domain of the histone methyltransferase EZH2 have been identified in subsets of patients with non-Hodgkin lymphoma (NHL). These genetic alterations are hypothesized to confer an oncogenic...
17.
Basavapathruni A, Olhava E, Daigle S, Therkelsen C, Jin L, Boriack-Sjodin P, et al.
Biopharm Drug Dispos
. 2014 Jan;
35(4):237-52.
PMID: 24415392
(2R,3R,4S,5R)-2-(6-Amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol (EPZ-5676) is a novel DOT1L histone methyltransferase inhibitor currently in clinical development for the treatment of MLL-rearranged leukemias. This report describes the preclinical pharmacokinetics and metabolism of EPZ-5676, an...
18.
Daigle S, Olhava E, Therkelsen C, Basavapathruni A, Jin L, Boriack-Sjodin P, et al.
Blood
. 2013 Jun;
122(6):1017-25.
PMID: 23801631
Rearrangements of the MLL gene define a genetically distinct subset of acute leukemias with poor prognosis. Current treatment options are of limited effectiveness; thus, there is a pressing need for...
19.
Swalm B, Hallenbeck K, Majer C, Jin L, Scott M, Moyer M, et al.
Biochem J
. 2013 May;
453(2):241-7.
PMID: 23679895
H3K27 (histone H3 Lys27) methylation is an important epigenetic modification that regulates gene transcription. In humans, EZH (enhancer of zeste homologue) 1 and EZH2 are the only enzymes capable of...
20.
Knutson S, Warholic N, Wigle T, Klaus C, Allain C, Raimondi A, et al.
Proc Natl Acad Sci U S A
. 2013 Apr;
110(19):7922-7.
PMID: 23620515
Inactivation of the switch/sucrose nonfermentable complex component SMARCB1 is extremely prevalent in pediatric malignant rhabdoid tumors (MRTs) or atypical teratoid rhabdoid tumors. This alteration is hypothesized to confer oncogenic dependency...