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Items: 1 to 50 of 97

1.

Toxicology and Pharmacology of an AAV Vector Expressing Codon-Optimized RPGR in RPGR-Deficient Rd9 Mice.

Song C, Conlon TJ, Deng WT, Coleman KE, Zhu P, Plummer C, Mandapati S, Van Hoosear M, Green KB, Sonnentag P, Sharma AK, Timmers A, Robinson PM, Knop DR, Hauswirth WW, Chulay JD, Shearman MS, Ye GJ.

Hum Gene Ther Clin Dev. 2018 Dec;29(4):188-197. doi: 10.1089/humc.2018.168.

PMID:
30280954
2.

Optimization of Retinal Gene Therapy for X-Linked Retinitis Pigmentosa Due to RPGR Mutations.

Beltran WA, Cideciyan AV, Boye SE, Ye GJ, Iwabe S, Dufour VL, Marinho LF, Swider M, Kosyk MS, Sha J, Boye SL, Peterson JJ, Witherspoon CD, Alexander JJ, Ying GS, Shearman MS, Chulay JD, Hauswirth WW, Gamlin PD, Jacobson SG, Aguirre GD.

Mol Ther. 2017 Aug 2;25(8):1866-1880. doi: 10.1016/j.ymthe.2017.05.004. Epub 2017 May 27.

3.

Safety and Efficacy Evaluation of rAAV2tYF-PR1.7-hCNGA3 Vector Delivered by Subretinal Injection in CNGA3 Mutant Achromatopsia Sheep.

Gootwine E, Ofri R, Banin E, Obolensky A, Averbukh E, Ezra-Elia R, Ross M, Honig H, Rosov A, Yamin E, Ye GJ, Knop DR, Robinson PM, Chulay JD, Shearman MS.

Hum Gene Ther Clin Dev. 2017 Jun;28(2):96-107. doi: 10.1089/humc.2017.028. Epub 2017 May 5.

PMID:
28478700
4.

Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys.

Fischer C, Zultanski SL, Zhou H, Methot JL, Shah S, Hayashi I, Hughes BL, Moxham CM, Bays NW, Smotrov N, Hill AD, Pan BS, Wu Z, Moy LY, Tanga F, Kenific C, Cruz JC, Walker D, Bouthillette M, Nikov GN, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Michener MS, Cook JJ, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3488-94. doi: 10.1016/j.bmcl.2015.07.003. Epub 2015 Jul 9.

PMID:
26212776
5.

Potent benzoazepinone γ-secretase modulators with improved bioavailability.

Methot JL, Fischer C, Li C, Rivkin A, Ahearn SP, Brown WC, Kattar S, Kelley E, Mampreian DM, Schell A, Rosenau A, Zhou H, Ball R, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Moy LY, Kenific CM, Moxham C, Shah S, Nuthall H, Szewczak AA, Hill A, Hughes B, Smotrov N, Munoz B, Miller TA, Shearman MS.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3495-500. doi: 10.1016/j.bmcl.2015.06.032. Epub 2015 Jun 15.

PMID:
26142947
6.

Correction: Pathway-Based Analysis of Genome-Wide siRNA Screens Reveals the Regulatory Landscape of App Processing.

Camargo LM, Zhang XD, Loerch P, Caceres RM, Marine SD, Uva P, Ferrer M, de Rinaldis E, Stone DJ, Majercak J, Ray WJ, Yi-An C, Shearman MS, Mizuguchi K.

PLoS One. 2015 Jun 1;10(6):e0129641. doi: 10.1371/journal.pone.0129641. eCollection 2015. No abstract available.

7.

Pathway-based analysis of genome-wide siRNA screens reveals the regulatory landscape of APP processing.

Camargo LM, Zhang XD, Loerch P, Caceres RM, Marine SD, Uva P, Ferrer M, de Rinaldis E, Stone DJ, Majercak J, Ray WJ, Yi-An C, Shearman MS, Mizuguchi K.

PLoS One. 2015 Feb 27;10(2):e0115369. doi: 10.1371/journal.pone.0115369. eCollection 2015. Erratum in: PLoS One. 2015;10(6):e0129641.

8.

Increased O-GlcNAcylation reduces pathological tau without affecting its normal phosphorylation in a mouse model of tauopathy.

Graham DL, Gray AJ, Joyce JA, Yu D, O'Moore J, Carlson GA, Shearman MS, Dellovade TL, Hering H.

Neuropharmacology. 2014 Apr;79:307-13. doi: 10.1016/j.neuropharm.2013.11.025. Epub 2013 Dec 8.

PMID:
24326295
9.

Triazoloamides as potent γ-secretase modulators with reduced hERG liability.

Fischer C, Zultanski SL, Zhou H, Methot JL, Shah S, Nuthall H, Hughes BL, Smotrov N, Hill A, Szewczak AA, Moxham CM, Bays N, Middleton RE, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2012 May 1;22(9):3140-6. doi: 10.1016/j.bmcl.2012.03.054. Epub 2012 Mar 21.

PMID:
22497762
10.

Triazoles as γ-secretase modulators.

Fischer C, Zultanski SL, Zhou H, Methot JL, Brown WC, Mampreian DM, Schell AJ, Shah S, Nuthall H, Hughes BL, Smotrov N, Kenific CM, Cruz JC, Walker D, Bouthillette M, Nikov GN, Savage DF, Jeliazkova-Mecheva VV, Diaz D, Szewczak AA, Bays N, Middleton RE, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2011 Jul 1;21(13):4083-7. doi: 10.1016/j.bmcl.2011.04.089. Epub 2011 May 4.

PMID:
21616665
11.

Quinazolinones as γ-secretase modulators.

Fischer C, Shah S, Hughes BL, Nikov GN, Crispino JL, Middleton RE, Szewczak AA, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):773-6. doi: 10.1016/j.bmcl.2010.11.111. Epub 2010 Nov 26.

PMID:
21190851
12.

Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound.

Cook JJ, Wildsmith KR, Gilberto DB, Holahan MA, Kinney GG, Mathers PD, Michener MS, Price EA, Shearman MS, Simon AJ, Wang JX, Wu G, Yarasheski KE, Bateman RJ.

J Neurosci. 2010 May 12;30(19):6743-50. doi: 10.1523/JNEUROSCI.1381-10.2010.

13.

Purine derivatives as potent gamma-secretase modulators.

Rivkin A, Ahearn SP, Chichetti SM, Hamblett CL, Garcia Y, Martinez M, Hubbs JL, Reutershan MH, Daniels MH, Siliphaivanh P, Otte KM, Li C, Rosenau A, Surdi LM, Jung J, Hughes BL, Crispino JL, Nikov GN, Middleton RE, Moxham CM, Szewczak AA, Shah S, Moy LY, Kenific CM, Tanga F, Cruz JC, Andrade P, Angagaw MH, Shomer NH, Miller T, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2279-82. doi: 10.1016/j.bmcl.2010.02.008. Epub 2010 Feb 6.

PMID:
20207146
14.

Oral treatment with a gamma-secretase inhibitor improves long-term potentiation in a mouse model of Alzheimer's disease.

Townsend M, Qu Y, Gray A, Wu Z, Seto T, Hutton M, Shearman MS, Middleton RE.

J Pharmacol Exp Ther. 2010 Apr;333(1):110-9. doi: 10.1124/jpet.109.163691. Epub 2010 Jan 7.

PMID:
20056779
15.

Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators.

Rivkin A, Ahearn SP, Chichetti SM, Kim YR, Li C, Rosenau A, Kattar SD, Jung J, Shah S, Hughes BL, Crispino JL, Middleton RE, Szewczak AA, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1269-71. doi: 10.1016/j.bmcl.2009.11.101. Epub 2009 Nov 23.

PMID:
20022243
16.

Glu-333 of nicastrin directly participates in gamma-secretase activity.

Dries DR, Shah S, Han YH, Yu C, Yu S, Shearman MS, Yu G.

J Biol Chem. 2009 Oct 23;284(43):29714-24. doi: 10.1074/jbc.M109.038737. Epub 2009 Sep 3.

17.

Fenton chemistry and oxidative stress mediate the toxicity of the beta-amyloid peptide in a Drosophila model of Alzheimer's disease.

Rival T, Page RM, Chandraratna DS, Sendall TJ, Ryder E, Liu B, Lewis H, Rosahl T, Hider R, Camargo LM, Shearman MS, Crowther DC, Lomas DA.

Eur J Neurosci. 2009 Apr;29(7):1335-47. doi: 10.1111/j.1460-9568.2009.06701.x. Epub 2009 Mar 23.

18.

Novel orally bioavailable gamma-secretase inhibitors with excellent in vivo activity.

Keown LE, Collins I, Cooper LC, Harrison T, Madin A, Mistry J, Reilly M, Shaimi M, Welch CJ, Clarke EE, Lewis HD, Wrigley JD, Best JD, Murray F, Shearman MS.

J Med Chem. 2009 Jun 11;52(11):3441-4. doi: 10.1021/jm900056p.

PMID:
19432431
19.

Apoptosis in T cell acute lymphoblastic leukemia cells after cell cycle arrest induced by pharmacological inhibition of notch signaling.

Lewis HD, Leveridge M, Strack PR, Haldon CD, O'neil J, Kim H, Madin A, Hannam JC, Look AT, Kohl N, Draetta G, Harrison T, Kerby JA, Shearman MS, Beher D.

Chem Biol. 2007 Feb;14(2):209-19.

20.

The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse.

Best JD, Smith DW, Reilly MA, O'Donnell R, Lewis HD, Ellis S, Wilkie N, Rosahl TW, Laroque PA, Boussiquet-Leroux C, Churcher I, Atack JR, Harrison T, Shearman MS.

J Pharmacol Exp Ther. 2007 Feb;320(2):552-8. Epub 2006 Nov 10.

PMID:
17099072
21.

Intra- or intercomplex binding to the gamma-secretase enzyme. A model to differentiate inhibitor classes.

Clarke EE, Churcher I, Ellis S, Wrigley JD, Lewis HD, Harrison T, Shearman MS, Beher D.

J Biol Chem. 2006 Oct 20;281(42):31279-89. Epub 2006 Aug 9.

22.

A comparative assessment of gamma-secretase activity in transgenic and non-transgenic rodent brain.

Goggi JL, Lewis HD, Mok J, Harrison T, Shearman MS, Atack JR, Best JD.

J Neurosci Methods. 2006 Oct 30;157(2):246-52. Epub 2006 Jul 21.

PMID:
16859750
23.

Quantification of Alzheimer pathology in ageing and dementia: age-related accumulation of amyloid-beta(42) peptide in vascular dementia.

Lewis H, Beher D, Cookson N, Oakley A, Piggott M, Morris CM, Jaros E, Perry R, Ince P, Kenny RA, Ballard CG, Shearman MS, Kalaria RN.

Neuropathol Appl Neurobiol. 2006 Apr;32(2):103-18.

PMID:
16599940
24.

The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent.

Stock N, Munoz B, Wrigley JD, Shearman MS, Beher D, Peachey J, Williamson TL, Bain G, Chen W, Jiang X, St-Jacques R, Prasit P.

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2219-23. Epub 2006 Feb 7.

PMID:
16455248
25.

In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat.

Best JD, Jay MT, Otu F, Churcher I, Reilly M, Morentin-Gutierrez P, Pattison C, Harrison T, Shearman MS, Atack JR.

J Pharmacol Exp Ther. 2006 May;317(2):786-90. Epub 2006 Jan 27.

PMID:
16443723
26.

C-terminal PAL motif of presenilin and presenilin homologues required for normal active site conformation.

Wang J, Beher D, Nyborg AC, Shearman MS, Golde TE, Goate A.

J Neurochem. 2006 Jan;96(1):218-27. Epub 2005 Nov 23.

27.

4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.

Churcher I, Beher D, Best JD, Castro JL, Clarke EE, Gentry A, Harrison T, Hitzel L, Kay E, Kerrad S, Lewis HD, Morentin-Gutierrez P, Mortishire-Smith R, Oakley PJ, Reilly M, Shaw DE, Shearman MS, Teall MR, Williams S, Wrigley JD.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):280-4. Epub 2005 Nov 3.

PMID:
16275079
28.

Two domains within the first putative transmembrane domain of presenilin 1 differentially influence presenilinase and gamma-secretase activity.

Brunkan AL, Martinez M, Wang J, Walker ES, Beher D, Shearman MS, Goate AM.

J Neurochem. 2005 Sep;94(5):1315-28. Epub 2005 Jul 7.

29.

Determination of guinea-pig cortical gamma-secretase activity ex vivo following the systemic administration of a gamma-secretase inhibitor.

Grimwood S, Hogg J, Jay MT, Lad AM, Lee V, Murray F, Peachey J, Townend T, Vithlani M, Beher D, Shearman MS, Hutson PH.

Neuropharmacology. 2005 Jun;48(7):1002-11.

PMID:
15857627
30.

Subcellular targeting of DISC1 is dependent on a domain independent from the Nudel binding site.

Brandon NJ, Schurov I, Camargo LM, Handford EJ, Duran-Jimeniz B, Hunt P, Millar JK, Porteous DJ, Shearman MS, Whiting PJ.

Mol Cell Neurosci. 2005 Apr;28(4):613-24.

PMID:
15797709
31.

Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide].

Best JD, Jay MT, Otu F, Ma J, Nadin A, Ellis S, Lewis HD, Pattison C, Reilly M, Harrison T, Shearman MS, Williamson TL, Atack JR.

J Pharmacol Exp Ther. 2005 May;313(2):902-8. Epub 2005 Mar 2.

PMID:
15743924
32.

Functional overexpression of gamma-secretase reveals protease-independent trafficking functions and a critical role of lipids for protease activity.

Wrigley JD, Schurov I, Nunn EJ, Martin AC, Clarke EE, Ellis S, Bonnert TP, Shearman MS, Beher D.

J Biol Chem. 2005 Apr 1;280(13):12523-35. Epub 2004 Dec 21.

33.

A novel series of potent gamma-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core.

Lewis SJ, Smith AL, Neduvelil JG, Stevenson GI, Lindon MJ, Jones AB, Shearman MS, Beher D, Clarke E, Best JD, Peachey JE, Harrison T, Castro JL.

Bioorg Med Chem Lett. 2005 Jan 17;15(2):373-8.

PMID:
15603957
34.

Gamma-secretase complex assembly within the early secretory pathway.

Capell A, Beher D, Prokop S, Steiner H, Kaether C, Shearman MS, Haass C.

J Biol Chem. 2005 Feb 25;280(8):6471-8. Epub 2004 Dec 10.

35.

Fatty acids increase presenilin-1 levels and [gamma]-secretase activity in PSwt-1 cells.

Liu Y, Yang L, Conde-Knape K, Beher D, Shearman MS, Shachter NS.

J Lipid Res. 2004 Dec;45(12):2368-76. Epub 2004 Sep 16.

36.

Conserved residues within the putative active site of gamma-secretase differentially influence enzyme activity and inhibitor binding.

Wrigley JD, Nunn EJ, Nyabi O, Clarke EE, Hunt P, Nadin A, De Strooper B, Shearman MS, Beher D.

J Neurochem. 2004 Sep;90(6):1312-20.

37.

Novel aspects of accumulation dynamics and A beta composition in transgenic models of AD.

Lewis HD, Beher D, Smith D, Hewson L, Cookson N, Reynolds DS, Dawson GR, Jiang M, Van der Ploeg LH, Qian S, Rosahl TW, Kalaria RN, Shearman MS.

Neurobiol Aging. 2004 Oct;25(9):1175-85.

PMID:
15312963
38.

Selected non-steroidal anti-inflammatory drugs and their derivatives target gamma-secretase at a novel site. Evidence for an allosteric mechanism.

Beher D, Clarke EE, Wrigley JD, Martin AC, Nadin A, Churcher I, Shearman MS.

J Biol Chem. 2004 Oct 15;279(42):43419-26. Epub 2004 Aug 10.

39.

Disrupted in Schizophrenia 1 and Nudel form a neurodevelopmentally regulated protein complex: implications for schizophrenia and other major neurological disorders.

Brandon NJ, Handford EJ, Schurov I, Rain JC, Pelling M, Duran-Jimeniz B, Camargo LM, Oliver KR, Beher D, Shearman MS, Whiting PJ.

Mol Cell Neurosci. 2004 Jan;25(1):42-55.

PMID:
14962739
40.

In vitro characterization of the presenilin-dependent gamma-secretase complex using a novel affinity ligand.

Beher D, Fricker M, Nadin A, Clarke EE, Wrigley JD, Li YM, Culvenor JG, Masters CL, Harrison T, Shearman MS.

Biochemistry. 2003 Jul 15;42(27):8133-42.

PMID:
12846562
41.

Catalytic site-directed gamma-secretase complex inhibitors do not discriminate pharmacologically between Notch S3 and beta-APP cleavages.

Lewis HD, Pérez Revuelta BI, Nadin A, Neduvelil JG, Harrison T, Pollack SJ, Shearman MS.

Biochemistry. 2003 Jun 24;42(24):7580-6.

PMID:
12809514
43.

gamma-Secretase cleavage site specificity differs for intracellular and secretory amyloid beta.

Grimm HS, Beher D, Lichtenthaler SF, Shearman MS, Beyreuther K, Hartmann T.

J Biol Chem. 2003 Apr 11;278(15):13077-85. Epub 2003 Jan 29.

44.

gamma-Secretase: characterization and implication for Alzheimer disease therapy.

Xu M, Lai MT, Huang Q, DiMuzio-Mower J, Castro JL, Harrison T, Nadin A, Neduvelil JG, Shearman MS, Shafer JA, Gardell SJ, Li YM.

Neurobiol Aging. 2002 Nov-Dec;23(6):1023-30.

PMID:
12470798
45.

Synthesis and gamma-secretase activity of APP substrate-based hydroxyethylene dipeptide isosteres.

Nadin A, Owens AP, Castro JL, Harrison T, Shearman MS.

Bioorg Med Chem Lett. 2003 Jan 6;13(1):37-41.

PMID:
12467612
46.

Gamma-secretase inhibition.

Beher D, Shearman MS.

Biochem Soc Trans. 2002 Aug;30(4):534-7. Review.

PMID:
12196131
47.

Generation of C-terminally truncated amyloid-beta peptides is dependent on gamma-secretase activity.

Beher D, Wrigley JD, Owens AP, Shearman MS.

J Neurochem. 2002 Aug;82(3):563-75.

48.

Cerebrospinal fluid levels of beta-amyloid(42) in patients with Alzheimer's disease are related to the exon 2 polymorphism of the cathepsin D gene.

Papassotiropoulos A, Lewis HD, Bagli M, Jessen F, Ptok U, Schulte A, Shearman MS, Heun R.

Neuroreport. 2002 Jul 19;13(10):1291-4.

PMID:
12151789
49.

The intramembrane cleavage site of the amyloid precursor protein depends on the length of its transmembrane domain.

Lichtenthaler SF, Beher D, Grimm HS, Wang R, Shearman MS, Masters CL, Beyreuther K.

Proc Natl Acad Sci U S A. 2002 Feb 5;99(3):1365-70. Epub 2002 Jan 22.

50.

The C-terminal fragment of the Alzheimer's disease amyloid protein precursor is degraded by a proteasome-dependent mechanism distinct from gamma-secretase.

Nunan J, Shearman MS, Checler F, Cappai R, Evin G, Beyreuther K, Masters CL, Small DH.

Eur J Biochem. 2001 Oct;268(20):5329-36.

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