Detalhe da pesquisa
1.
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Nat Chem Biol
; 11(6): 432-7, 2015 Jun.
Artigo
em Inglês
| MEDLINE | ID: mdl-25915199
2.
Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor.
Xenobiotica
; 46(3): 268-77, 2016.
Artigo
em Inglês
| MEDLINE | ID: mdl-26294260
3.
Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.
Proc Natl Acad Sci U S A
; 110(19): 7922-7, 2013 May 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-23620515
4.
Potent inhibition of DOT1L as treatment of MLL-fusion leukemia.
Blood
; 122(6): 1017-25, 2013 Aug 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-23801631
5.
Structural and Kinetic Characterization of a Novel N-acetylated Aliphatic Amine Metabolite of the PRMT Inhibitor, EPZ011652.
Drug Metab Dispos
; 43(7): 936-43, 2015 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-25887455
6.
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.
Nat Chem Biol
; 8(11): 890-6, 2012 Nov.
Artigo
em Inglês
| MEDLINE | ID: mdl-23023262
7.
Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.
Biopharm Drug Dispos
; 35(4): 237-52, 2014 May.
Artigo
em Inglês
| MEDLINE | ID: mdl-24415392
8.
A microglia clonal inflammatory disorder in Alzheimer's Disease.
bioRxiv
; 2024 Jan 25.
Artigo
em Inglês
| MEDLINE | ID: mdl-38328106
9.
Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies.
ACS Med Chem Lett
; 13(7): 1137-1143, 2022 Jul 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-35859865
10.
Regiospecific and stereoselective syntheses of (+/-) morphine, codeine, and thebaine via a highly stereocontrolled intramolecular 4 + 2 cycloaddition leading to a phenanthrofuran system.
J Am Chem Soc
; 131(32): 11402-6, 2009 Aug 19.
Artigo
em Inglês
| MEDLINE | ID: mdl-19624126
11.
Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss.
Cancer Cell
; 36(1): 100-114.e25, 2019 07 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-31257072
12.
Identification of a peptide inhibitor for the histone methyltransferase WHSC1.
PLoS One
; 13(5): e0197082, 2018.
Artigo
em Inglês
| MEDLINE | ID: mdl-29742153
13.
Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.
PLoS One
; 13(6): e0197372, 2018.
Artigo
em Inglês
| MEDLINE | ID: mdl-29856759
14.
Selective Killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models.
Mol Cancer Ther
; 16(5): 850-860, 2017 05.
Artigo
em Inglês
| MEDLINE | ID: mdl-28292935
15.
Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.
Sci Rep
; 7(1): 17993, 2017 12 21.
Artigo
em Inglês
| MEDLINE | ID: mdl-29269946
16.
Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human.
Cancer Chemother Pharmacol
; 77(1): 43-62, 2016 Jan.
Artigo
em Inglês
| MEDLINE | ID: mdl-26645404
17.
The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
J Med Chem
; 59(4): 1556-64, 2016 Feb 25.
Artigo
em Inglês
| MEDLINE | ID: mdl-26769278
18.
Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.
ACS Med Chem Lett
; 7(2): 162-6, 2016 Feb 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-26985292
19.
Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.
ACS Med Chem Lett
; 7(2): 134-8, 2016 Feb 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-26985287
20.
A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening.
J Biomol Screen
; 20(6): 810-20, 2015 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-25755264