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Items: 47

1.

Sphingosine Kinase 2 Potentiates Amyloid Deposition but Protects against Hippocampal Volume Loss and Demyelination in a Mouse Model of Alzheimer's Disease.

Lei M, Teo JD, Song H, McEwen HP, Yup Lee J, Couttas TA, Duncan T, Chesworth R, Bertz J, Przybyla M, Van Eersel J, Heng B, Guillemin GJ, Ittner LM, Fath T, Garner B, Ittner A, Karl T, Don AS.

J Neurosci. 2019 Nov 27;39(48):9645-9659. doi: 10.1523/JNEUROSCI.0524-19.2019. Epub 2019 Oct 22.

PMID:
31641049
2.

Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss.

Fedoriw A, Rajapurkar SR, O'Brien S, Gerhart SV, Mitchell LH, Adams ND, Rioux N, Lingaraj T, Ribich SA, Pappalardi MB, Shah N, Laraio J, Liu Y, Butticello M, Carpenter CL, Creasy C, Korenchuk S, McCabe MT, McHugh CF, Nagarajan R, Wagner C, Zappacosta F, Annan R, Concha NO, Thomas RA, Hart TK, Smith JJ, Copeland RA, Moyer MP, Campbell J, Stickland K, Mills J, Jacques-O'Hagan S, Allain C, Johnston D, Raimondi A, Porter Scott M, Waters N, Swinger K, Boriack-Sjodin A, Riera T, Shapiro G, Chesworth R, Prinjha RK, Kruger RG, Barbash O, Mohammad HP.

Cancer Cell. 2019 Jul 8;36(1):100-114.e25. doi: 10.1016/j.ccell.2019.05.014. Epub 2019 Jun 27.

PMID:
31257072
3.

First behavioural assessment of a novel Immp2l knockdown mouse model with relevance for Gilles de la Tourette syndrome and Autism spectrum disorder.

Kreilaus F, Chesworth R, Eapen V, Clarke R, Karl T.

Behav Brain Res. 2019 Nov 18;374:112057. doi: 10.1016/j.bbr.2019.112057. Epub 2019 Jun 21.

PMID:
31233820
4.

Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.

Thomenius MJ, Totman J, Harvey D, Mitchell LH, Riera TV, Cosmopoulos K, Grassian AR, Klaus C, Foley M, Admirand EA, Jahic H, Majer C, Wigle T, Jacques SL, Gureasko J, Brach D, Lingaraj T, West K, Smith S, Rioux N, Waters NJ, Tang C, Raimondi A, Munchhof M, Mills JE, Ribich S, Porter Scott M, Kuntz KW, Janzen WP, Moyer M, Smith JJ, Chesworth R, Copeland RA, Boriack-Sjodin PA.

PLoS One. 2018 Jun 1;13(6):e0197372. doi: 10.1371/journal.pone.0197372. eCollection 2018.

5.

Identification of a peptide inhibitor for the histone methyltransferase WHSC1.

Morrison MJ, Boriack-Sjodin PA, Swinger KK, Wigle TJ, Sadalge D, Kuntz KW, Scott MP, Janzen WP, Chesworth R, Duncan KW, Harvey DM, Lampe JW, Mitchell LH, Copeland RA.

PLoS One. 2018 May 9;13(5):e0197082. doi: 10.1371/journal.pone.0197082. eCollection 2018.

7.

Neuregulin 1 Deficiency Modulates Adolescent Stress-Induced Dendritic Spine Loss in a Brain Region-Specific Manner and Increases Complement 4 Expression in the Hippocampus.

Clarke DJ, Chohan TW, Kassem MS, Smith KL, Chesworth R, Karl T, Kuligowski MP, Fok SY, Bennett MR, Arnold JC.

Schizophr Bull. 2019 Mar 7;45(2):339-349. doi: 10.1093/schbul/sby029.

PMID:
29566220
8.

The Endocannabinoid System across Postnatal Development in Transmembrane Domain Neuregulin 1 Mutant Mice.

Chesworth R, Long LE, Weickert CS, Karl T.

Front Psychiatry. 2018 Feb 7;9:11. doi: 10.3389/fpsyt.2018.00011. eCollection 2018.

9.

Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.

Drew AE, Moradei O, Jacques SL, Rioux N, Boriack-Sjodin AP, Allain C, Scott MP, Jin L, Raimondi A, Handler JL, Ott HM, Kruger RG, McCabe MT, Sneeringer C, Riera T, Shapiro G, Waters NJ, Mitchell LH, Duncan KW, Moyer MP, Copeland RA, Smith J, Chesworth R, Ribich SA.

Sci Rep. 2017 Dec 21;7(1):17993. doi: 10.1038/s41598-017-18446-z.

10.

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.

Chan-Penebre E, Armstrong K, Drew A, Grassian AR, Feldman I, Knutson SK, Kuplast-Barr K, Roche M, Campbell J, Ho P, Copeland RA, Chesworth R, Smith JJ, Keilhack H, Ribich SA.

Mol Cancer Ther. 2017 May;16(5):850-860. doi: 10.1158/1535-7163.MCT-16-0678. Epub 2017 Mar 14.

11.

Persistent variations in neuronal DNA methylation following cocaine self-administration and protracted abstinence in mice.

Baker-Andresen D, Zhao Q, Li X, Jupp B, Chesworth R, Lawrence AJ, Bredy T.

Neuroepigenetics. 2015 Oct;4:1-11. Epub 2015 Oct 2.

12.

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.

Duncan KW, Rioux N, Boriack-Sjodin PA, Munchhof MJ, Reiter LA, Majer CR, Jin L, Johnston LD, Chan-Penebre E, Kuplast KG, Porter Scott M, Pollock RM, Waters NJ, Smith JJ, Moyer MP, Copeland RA, Chesworth R.

ACS Med Chem Lett. 2015 Dec 2;7(2):162-6. doi: 10.1021/acsmedchemlett.5b00380. eCollection 2016 Feb 11.

13.

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

Mitchell LH, Boriack-Sjodin PA, Smith S, Thomenius M, Rioux N, Munchhof M, Mills JE, Klaus C, Totman J, Riera TV, Raimondi A, Jacques SL, West K, Foley M, Waters NJ, Kuntz KW, Wigle TJ, Scott MP, Copeland RA, Smith JJ, Chesworth R.

ACS Med Chem Lett. 2015 Aug 27;7(2):134-8. doi: 10.1021/acsmedchemlett.5b00272. eCollection 2016 Feb 11.

14.

The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.

Kuntz KW, Campbell JE, Keilhack H, Pollock RM, Knutson SK, Porter-Scott M, Richon VM, Sneeringer CJ, Wigle TJ, Allain CJ, Majer CR, Moyer MP, Copeland RA, Chesworth R.

J Med Chem. 2016 Feb 25;59(4):1556-64. doi: 10.1021/acs.jmedchem.5b01501. Epub 2016 Jan 27.

PMID:
26769278
15.

Recent developments in the behavioural and pharmacological enhancement of extinction of drug seeking.

Chesworth R, Corbit LH.

Addict Biol. 2017 Jan;22(1):3-43. doi: 10.1111/adb.12337. Epub 2015 Dec 21. Review.

PMID:
26687226
16.

Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human.

Waters NJ, Smith SA, Olhava EJ, Duncan KW, Burton RD, O'Neill J, Rodrigue ME, Pollock RM, Moyer MP, Chesworth R.

Cancer Chemother Pharmacol. 2016 Jan;77(1):43-62. doi: 10.1007/s00280-015-2929-y. Epub 2015 Dec 8.

PMID:
26645404
17.

Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor.

Rioux N, Duncan KW, Lantz RJ, Miao X, Chan-Penebre E, Moyer MP, Munchhof MJ, Copeland RA, Chesworth R, Waters NJ.

Xenobiotica. 2016;46(3):268-77.

PMID:
26294260
18.

Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.

Mitchell LH, Drew AE, Ribich SA, Rioux N, Swinger KK, Jacques SL, Lingaraj T, Boriack-Sjodin PA, Waters NJ, Wigle TJ, Moradei O, Jin L, Riera T, Porter-Scott M, Moyer MP, Smith JJ, Chesworth R, Copeland RA.

ACS Med Chem Lett. 2015 Apr 6;6(6):655-9. doi: 10.1021/acsmedchemlett.5b00071. eCollection 2015 Jun 11.

19.

EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.

Campbell JE, Kuntz KW, Knutson SK, Warholic NM, Keilhack H, Wigle TJ, Raimondi A, Klaus CR, Rioux N, Yokoi A, Kawano S, Minoshima Y, Choi HW, Porter Scott M, Waters NJ, Smith JJ, Chesworth R, Moyer MP, Copeland RA.

ACS Med Chem Lett. 2015 Mar 4;6(5):491-5. doi: 10.1021/acsmedchemlett.5b00037. eCollection 2015 May 14.

20.

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.

Chan-Penebre E, Kuplast KG, Majer CR, Boriack-Sjodin PA, Wigle TJ, Johnston LD, Rioux N, Munchhof MJ, Jin L, Jacques SL, West KA, Lingaraj T, Stickland K, Ribich SA, Raimondi A, Scott MP, Waters NJ, Pollock RM, Smith JJ, Barbash O, Pappalardi M, Ho TF, Nurse K, Oza KP, Gallagher KT, Kruger R, Moyer MP, Copeland RA, Chesworth R, Duncan KW.

Nat Chem Biol. 2015 Jun;11(6):432-7. doi: 10.1038/nchembio.1810. Epub 2015 Apr 27.

PMID:
25915199
21.

Structural and Kinetic Characterization of a Novel N-acetylated Aliphatic Amine Metabolite of the PRMT Inhibitor, EPZ011652.

Rioux N, Mitchell LH, Tiller P, Plant K, Shaw J, Frost K, Ribich S, Moyer MP, Copeland RA, Chesworth R, Waters NJ.

Drug Metab Dispos. 2015 Jul;43(7):936-43. doi: 10.1124/dmd.115.064014. Epub 2015 Apr 17.

PMID:
25887455
22.

A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening.

Wigle TJ, Swinger KK, Campbell JE, Scholle MD, Sherrill J, Admirand EA, Boriack-Sjodin PA, Kuntz KW, Chesworth R, Moyer MP, Scott MP, Copeland RA.

J Biomol Screen. 2015 Jul;20(6):810-20. doi: 10.1177/1087057115575689. Epub 2015 Mar 9.

PMID:
25755264
23.

Adenosine 2A receptors modulate reward behaviours for methamphetamine.

Chesworth R, Brown RM, Kim JH, Ledent C, Lawrence AJ.

Addict Biol. 2016 Mar;21(2):407-21. doi: 10.1111/adb.12225. Epub 2015 Jan 22.

PMID:
25612195
24.

Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma.

Knutson SK, Kawano S, Minoshima Y, Warholic NM, Huang KC, Xiao Y, Kadowaki T, Uesugi M, Kuznetsov G, Kumar N, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Waters NJ, Smith JJ, Porter-Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Uenaka T, Pollock RM, Kuntz KW, Yokoi A, Keilhack H.

Mol Cancer Ther. 2014 Apr;13(4):842-54. doi: 10.1158/1535-7163.MCT-13-0773. Epub 2014 Feb 21.

25.

Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.

Basavapathruni A, Olhava EJ, Daigle SR, Therkelsen CA, Jin L, Boriack-Sjodin PA, Allain CJ, Klaus CR, Raimondi A, Scott MP, Dovletoglou A, Richon VM, Pollock RM, Copeland RA, Moyer MP, Chesworth R, Pearson PG, Waters NJ.

Biopharm Drug Dispos. 2014 May;35(4):237-52. doi: 10.1002/bdd.1889. Epub 2014 Feb 14.

PMID:
24415392
26.

The metabotropic glutamate 5 receptor modulates extinction and reinstatement of methamphetamine-seeking in mice.

Chesworth R, Brown RM, Kim JH, Lawrence AJ.

PLoS One. 2013 Jul 4;8(7):e68371. doi: 10.1371/journal.pone.0068371. Print 2013.

27.

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia.

Daigle SR, Olhava EJ, Therkelsen CA, Basavapathruni A, Jin L, Boriack-Sjodin PA, Allain CJ, Klaus CR, Raimondi A, Scott MP, Waters NJ, Chesworth R, Moyer MP, Copeland RA, Richon VM, Pollock RM.

Blood. 2013 Aug 8;122(6):1017-25. doi: 10.1182/blood-2013-04-497644. Epub 2013 Jun 25.

28.

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.

Knutson SK, Warholic NM, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Porter Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Pollock RM, Kuntz KW, Keilhack H.

Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7. doi: 10.1073/pnas.1303800110. Epub 2013 Apr 25.

29.

Modulation of γ-secretase by EVP-0015962 reduces amyloid deposition and behavioral deficits in Tg2576 mice.

Rogers K, Felsenstein KM, Hrdlicka L, Tu Z, Albayya F, Lee W, Hopp S, Miller MJ, Spaulding D, Yang Z, Hodgdon H, Nolan S, Wen M, Costa D, Blain JF, Freeman E, De Strooper B, Vulsteke V, Scrocchi L, Zetterberg H, Portelius E, Hutter-Paier B, Havas D, Ahlijanian M, Flood D, Leventhal L, Shapiro G, Patzke H, Chesworth R, Koenig G.

Mol Neurodegener. 2012 Dec 18;7:61. doi: 10.1186/1750-1326-7-61.

30.

Role of Abca7 in mouse behaviours relevant to neurodegenerative diseases.

Logge W, Cheng D, Chesworth R, Bhatia S, Garner B, Kim WS, Karl T.

PLoS One. 2012;7(9):e45959. doi: 10.1371/journal.pone.0045959. Epub 2012 Sep 24.

31.

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.

Knutson SK, Wigle TJ, Warholic NM, Sneeringer CJ, Allain CJ, Klaus CR, Sacks JD, Raimondi A, Majer CR, Song J, Scott MP, Jin L, Smith JJ, Olhava EJ, Chesworth R, Moyer MP, Richon VM, Copeland RA, Keilhack H, Pollock RM, Kuntz KW.

Nat Chem Biol. 2012 Nov;8(11):890-6. doi: 10.1038/nchembio.1084. Epub 2012 Sep 30.

PMID:
23023262
32.

Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L.

Basavapathruni A, Jin L, Daigle SR, Majer CR, Therkelsen CA, Wigle TJ, Kuntz KW, Chesworth R, Pollock RM, Scott MP, Moyer MP, Richon VM, Copeland RA, Olhava EJ.

Chem Biol Drug Des. 2012 Dec;80(6):971-80. doi: 10.1111/cbdd.12050. Epub 2012 Oct 9.

PMID:
22978415
33.

Distinct neurobehavioural effects of cannabidiol in transmembrane domain neuregulin 1 mutant mice.

Long LE, Chesworth R, Huang XF, Wong A, Spiro A, McGregor IS, Arnold JC, Karl T.

PLoS One. 2012;7(4):e34129. doi: 10.1371/journal.pone.0034129. Epub 2012 Apr 3.

34.

The response of neuregulin 1 mutant mice to acute restraint stress.

Chesworth R, Yulyaningsih E, Cappas E, Arnold J, Sainsbury A, Karl T.

Neurosci Lett. 2012 Apr 25;515(1):82-6. doi: 10.1016/j.neulet.2012.03.024. Epub 2012 Mar 19.

PMID:
22450046
35.

Transmembrane domain Nrg1 mutant mice show altered susceptibility to the neurobehavioural actions of repeated THC exposure in adolescence.

Long LE, Chesworth R, Huang XF, McGregor IS, Arnold JC, Karl T.

Int J Neuropsychopharmacol. 2013 Feb;16(1):163-75. doi: 10.1017/S1461145711001854. Epub 2012 Jan 9.

PMID:
22226049
36.

EVP-6124, a novel and selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors.

Prickaerts J, van Goethem NP, Chesworth R, Shapiro G, Boess FG, Methfessel C, Reneerkens OA, Flood DG, Hilt D, Gawryl M, Bertrand S, Bertrand D, König G.

Neuropharmacology. 2012 Feb;62(2):1099-110. doi: 10.1016/j.neuropharm.2011.10.024. Epub 2011 Nov 10.

PMID:
22085888
37.

Cognition in female transmembrane domain neuregulin 1 mutant mice.

Chesworth R, Downey L, Logge W, Killcross S, Karl T.

Behav Brain Res. 2012 Jan 1;226(1):218-23. doi: 10.1016/j.bbr.2011.09.019. Epub 2011 Sep 16.

PMID:
21944941
38.

Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.

Daigle SR, Olhava EJ, Therkelsen CA, Majer CR, Sneeringer CJ, Song J, Johnston LD, Scott MP, Smith JJ, Xiao Y, Jin L, Kuntz KW, Chesworth R, Moyer MP, Bernt KM, Tseng JC, Kung AL, Armstrong SA, Copeland RA, Richon VM, Pollock RM.

Cancer Cell. 2011 Jul 12;20(1):53-65. doi: 10.1016/j.ccr.2011.06.009.

39.

Neuronal store-operated calcium entry pathway as a novel therapeutic target for Huntington's disease treatment.

Wu J, Shih HP, Vigont V, Hrdlicka L, Diggins L, Singh C, Mahoney M, Chesworth R, Shapiro G, Zimina O, Chen X, Wu Q, Glushankova L, Ahlijanian M, Koenig G, Mozhayeva GN, Kaznacheyeva E, Bezprozvanny I.

Chem Biol. 2011 Jun 24;18(6):777-93. doi: 10.1016/j.chembiol.2011.04.012.

40.

Do transmembrane domain neuregulin 1 mutant mice exhibit a reliable sensorimotor gating deficit?

Karl T, Burne TH, Van den Buuse M, Chesworth R.

Behav Brain Res. 2011 Oct 1;223(2):336-41. doi: 10.1016/j.bbr.2011.04.051. Epub 2011 May 13.

PMID:
21605597
41.

A follow-up study: acute behavioural effects of Delta(9)-THC in female heterozygous neuregulin 1 transmembrane domain mutant mice.

Long LE, Chesworth R, Arnold JC, Karl T.

Psychopharmacology (Berl). 2010 Aug;211(3):277-89. doi: 10.1007/s00213-010-1896-6. Epub 2010 Jun 23.

PMID:
20571781
42.

Acoustic startle response and sensorimotor gating in a genetic mouse model for the Y1 receptor.

Karl T, Chesworth R, Duffy L, Herzog H.

Neuropeptides. 2010 Jun;44(3):233-9. doi: 10.1016/j.npep.2009.12.008. Epub 2010 Jan 25.

PMID:
20096928
43.

Schizophrenia-relevant behaviours in a genetic mouse model for Y2 deficiency.

Karl T, Chesworth R, Duffy L, Herzog H.

Behav Brain Res. 2010 Mar 5;207(2):434-40. doi: 10.1016/j.bbr.2009.10.029. Epub 2009 Oct 30.

PMID:
19879900
44.

A behavioural comparison of acute and chronic Delta9-tetrahydrocannabinol and cannabidiol in C57BL/6JArc mice.

Long LE, Chesworth R, Huang XF, McGregor IS, Arnold JC, Karl T.

Int J Neuropsychopharmacol. 2010 Aug;13(7):861-76. doi: 10.1017/S1461145709990605. Epub 2009 Sep 29.

PMID:
19785914
45.

Regiospecific and stereoselective syntheses of (+/-) morphine, codeine, and thebaine via a highly stereocontrolled intramolecular 4 + 2 cycloaddition leading to a phenanthrofuran system.

Stork G, Yamashita A, Adams J, Schulte GR, Chesworth R, Miyazaki Y, Farmer JJ.

J Am Chem Soc. 2009 Aug 19;131(32):11402-6. doi: 10.1021/ja9038505.

PMID:
19624126
46.

Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.

Chesworth R, Wessel MD, Heyden L, Mangano FM, Zawistoski M, Gegnas L, Galluzzo D, Lefker B, Cameron KO, Tickner J, Lu B, Castleberry TA, Petersen DN, Brault A, Perry P, Ng O, Owen TA, Pan L, Ke HZ, Brown TA, Thompson DD, DaSilva-Jardine P.

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5562-6. Epub 2005 Oct 10.

PMID:
16219463
47.

Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists.

Chesworth R, Zawistoski MP, Lefker BA, Cameron KO, Day RF, Mangano FM, Rosati RL, Colella S, Petersen DN, Brault A, Lu B, Pan LC, Perry P, Ng O, Castleberry TA, Owen TA, Brown TA, Thompson DD, DaSilva-Jardine P.

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2729-33.

PMID:
15125923

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