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Items: 1 to 20 of 87

1.

Piperidine acetic acid based γ-secretase modulators directly bind to Presenilin-1.

Crump CJ, Fish BA, Castro SV, Chau DM, Gertsik N, Ahn K, Stiff C, Pozdnyakov N, Bales KR, Johnson DS, Li YM.

ACS Chem Neurosci. 2011 Dec 21;2(12):705-710.

2.

γ-Secretase modulator (GSM) photoaffinity probes reveal distinct allosteric binding sites on presenilin.

Pozdnyakov N, Murrey HE, Crump CJ, Pettersson M, Ballard TE, Am Ende CW, Ahn K, Li YM, Bales KR, Johnson DS.

J Biol Chem. 2013 Apr 5;288(14):9710-20. doi: 10.1074/jbc.M112.398602. Epub 2013 Feb 8.

3.

Development and mechanism of γ-secretase modulators for Alzheimer's disease.

Crump CJ, Johnson DS, Li YM.

Biochemistry. 2013 May 14;52(19):3197-216. doi: 10.1021/bi400377p. Epub 2013 May 2. Review.

4.

Novel γ-secretase enzyme modulators directly target presenilin protein.

Ebke A, Luebbers T, Fukumori A, Shirotani K, Haass C, Baumann K, Steiner H.

J Biol Chem. 2011 Oct 28;286(43):37181-6. doi: 10.1074/jbc.C111.276972. Epub 2011 Sep 6.

5.

Beta-amyloid precursor protein mutants respond to gamma-secretase modulators.

Page RM, Gutsmiedl A, Fukumori A, Winkler E, Haass C, Steiner H.

J Biol Chem. 2010 Jun 4;285(23):17798-810. doi: 10.1074/jbc.M110.103283. Epub 2010 Mar 26.

6.

Independent generation of Abeta42 and Abeta38 peptide species by gamma-secretase.

Czirr E, Cottrell BA, Leuchtenberger S, Kukar T, Ladd TB, Esselmann H, Paul S, Schubenel R, Torpey JW, Pietrzik CU, Golde TE, Wiltfang J, Baumann K, Koo EH, Weggen S.

J Biol Chem. 2008 Jun 20;283(25):17049-54. doi: 10.1074/jbc.M802912200. Epub 2008 Apr 21.

7.

γ-Secretase modulator in Alzheimer's disease: shifting the end.

Xia W, Wong ST, Hanlon E, Morin P.

J Alzheimers Dis. 2012;31(4):685-96. doi: 10.3233/JAD-2012-120751. Review.

PMID:
22710916
8.

Presenilin is the molecular target of acidic γ-secretase modulators in living cells.

Jumpertz T, Rennhack A, Ness J, Baches S, Pietrzik CU, Bulic B, Weggen S.

PLoS One. 2012;7(1):e30484. doi: 10.1371/journal.pone.0030484. Epub 2012 Jan 6.

9.

Insensitivity to Abeta42-lowering nonsteroidal anti-inflammatory drugs and gamma-secretase inhibitors is common among aggressive presenilin-1 mutations.

Czirr E, Leuchtenberger S, Dorner-Ciossek C, Schneider A, Jucker M, Koo EH, Pietrzik CU, Baumann K, Weggen S.

J Biol Chem. 2007 Aug 24;282(34):24504-13. Epub 2007 Jun 15.

10.

Presenilin-1 but not amyloid precursor protein mutations present in mouse models of Alzheimer's disease attenuate the response of cultured cells to γ-secretase modulators regardless of their potency and structure.

Hahn S, Brüning T, Ness J, Czirr E, Baches S, Gijsen H, Korth C, Pietrzik CU, Bulic B, Weggen S.

J Neurochem. 2011 Feb;116(3):385-95. doi: 10.1111/j.1471-4159.2010.07118.x. Epub 2010 Dec 13.

11.

Soluble Gamma-secretase Modulators Attenuate Alzheimer's β-amyloid Pathology and Induce Conformational Changes in Presenilin 1.

Raven F, Ward JF, Zoltowska KM, Wan Y, Bylykbashi E, Miller SJ, Shen X, Choi SH, Rynearson KD, Berezovska O, Wagner SL, Tanzi RE, Zhang C.

EBioMedicine. 2017 Oct;24:93-101. doi: 10.1016/j.ebiom.2017.08.028. Epub 2017 Sep 4.

12.

Phenylpiperidine-type γ-secretase modulators target the transmembrane domain 1 of presenilin 1.

Ohki Y, Higo T, Uemura K, Shimada N, Osawa S, Berezovska O, Yokoshima S, Fukuyama T, Tomita T, Iwatsubo T.

EMBO J. 2011 Oct 14;30(23):4815-24. doi: 10.1038/emboj.2011.372.

13.

Substrate-targeting gamma-secretase modulators.

Kukar TL, Ladd TB, Bann MA, Fraering PC, Narlawar R, Maharvi GM, Healy B, Chapman R, Welzel AT, Price RW, Moore B, Rangachari V, Cusack B, Eriksen J, Jansen-West K, Verbeeck C, Yager D, Eckman C, Ye W, Sagi S, Cottrell BA, Torpey J, Rosenberry TL, Fauq A, Wolfe MS, Schmidt B, Walsh DM, Koo EH, Golde TE.

Nature. 2008 Jun 12;453(7197):925-9. doi: 10.1038/nature07055.

14.

Identification of new Presenilin-1 phosphosites: implication for γ-secretase activity and Aβ production.

Matz A, Halamoda-Kenzaoui B, Hamelin R, Mosser S, Alattia JR, Dimitrov M, Moniatte M, Fraering PC.

J Neurochem. 2015 May;133(3):409-21. doi: 10.1111/jnc.12996. Epub 2015 Feb 24.

15.

Activation of γ-Secretase Trimming Activity by Topological Changes of Transmembrane Domain 1 of Presenilin 1.

Cai T, Yonaga M, Tomita T.

J Neurosci. 2017 Dec 13;37(50):12272-12280. doi: 10.1523/JNEUROSCI.1628-17.2017. Epub 2017 Nov 8.

PMID:
29118109
16.

Attenuated Abeta42 responses to low potency gamma-secretase modulators can be overcome for many pathogenic presenilin mutants by second-generation compounds.

Kretner B, Fukumori A, Gutsmiedl A, Page RM, Luebbers T, Galley G, Baumann K, Haass C, Steiner H.

J Biol Chem. 2011 Apr 29;286(17):15240-51. doi: 10.1074/jbc.M110.213587. Epub 2011 Feb 25.

17.

γ-secretase modulators and presenilin 1 mutants act differently on presenilin/γ-secretase function to cleave Aβ42 and Aβ43.

Okochi M, Tagami S, Yanagida K, Takami M, Kodama TS, Mori K, Nakayama T, Ihara Y, Takeda M.

Cell Rep. 2013 Jan 31;3(1):42-51. doi: 10.1016/j.celrep.2012.11.028. Epub 2013 Jan 3.

18.

Photoactivated gamma-secretase inhibitors directed to the active site covalently label presenilin 1.

Li YM, Xu M, Lai MT, Huang Q, Castro JL, DiMuzio-Mower J, Harrison T, Lellis C, Nadin A, Neduvelil JG, Register RB, Sardana MK, Shearman MS, Smith AL, Shi XP, Yin KC, Shafer JA, Gardell SJ.

Nature. 2000 Jun 8;405(6787):689-94.

PMID:
10864326
19.

Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.

Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Evrard E, Efremov I, Kauffman GW, Stepan AF, Stiff CM, Xie L, Bales KR, Hajos-Korcsok E, Murrey HE, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):908-13. doi: 10.1016/j.bmcl.2014.12.059. Epub 2014 Dec 25.

PMID:
25582600
20.

Analyzing Amyloid-β Peptide Modulation Profiles and Binding Sites of γ-Secretase Modulators.

Trambauer J, Fukumori A, Kretner B, Steiner H.

Methods Enzymol. 2017;584:157-183. doi: 10.1016/bs.mie.2016.10.013. Epub 2016 Dec 1.

PMID:
28065262

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