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Items: 50

1.

Restricted Location of PSEN2/γ-Secretase Determines Substrate Specificity and Generates an Intracellular Aβ Pool.

Sannerud R, Esselens C, Ejsmont P, Mattera R, Rochin L, Tharkeshwar AK, De Baets G, De Wever V, Habets R, Baert V, Vermeire W, Michiels C, Groot AJ, Wouters R, Dillen K, Vints K, Baatsen P, Munck S, Derua R, Waelkens E, Basi GS, Mercken M, Vooijs M, Bollen M, Schymkowitz J, Rousseau F, Bonifacino JS, Van Niel G, De Strooper B, Annaert W.

Cell. 2016 Jun 30;166(1):193-208. doi: 10.1016/j.cell.2016.05.020. Epub 2016 Jun 9.

2.

Crystal structure reveals conservation of amyloid-β conformation recognized by 3D6 following humanization to bapineuzumab.

Feinberg H, Saldanha JW, Diep L, Goel A, Widom A, Veldman GM, Weis WI, Schenk D, Basi GS.

Alzheimers Res Ther. 2014 Jun 2;6(3):31. doi: 10.1186/alzrt261. eCollection 2014.

3.

Chronic γ-secretase inhibition reduces amyloid plaque-associated instability of pre- and postsynaptic structures.

Liebscher S, Page RM, Käfer K, Winkler E, Quinn K, Goldbach E, Brigham EF, Quincy D, Basi GS, Schenk DB, Steiner H, Bonhoeffer T, Haass C, Meyer-Luehmann M, Hübener M.

Mol Psychiatry. 2014 Aug;19(8):937-46. doi: 10.1038/mp.2013.122. Epub 2013 Sep 24.

4.

Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.

Probst G, Aubele DL, Bowers S, Dressen D, Garofalo AW, Hom RK, Konradi AW, Marugg JL, Mattson MN, Neitzel ML, Semko CM, Sham HL, Smith J, Sun M, Truong AP, Ye XM, Xu YZ, Dappen MS, Jagodzinski JJ, Keim PS, Peterson B, Latimer LH, Quincy D, Wu J, Goldbach E, Ness DK, Quinn KP, Sauer JM, Wong K, Zhang H, Zmolek W, Brigham EF, Kholodenko D, Hu K, Kwong GT, Lee M, Liao A, Motter RN, Sacayon P, Santiago P, Willits C, Bard F, Bova MP, Hemphill SS, Nguyen L, Ruslim L, Tanaka K, Tanaka P, Wallace W, Yednock TA, Basi GS.

J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20.

PMID:
23713656
5.

Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.

Ye XM, Konradi AW, Sun M, Yuan S, Aubele DL, Dappen M, Dressen D, Garofalo AW, Jagodzinski JJ, Latimer L, Probst GD, Sham HL, Wone D, Xu YZ, Ness D, Brigham E, Kwong GT, Willtis C, Tonn G, Goldbach E, Quinn KP, Zhang HH, Sauer JM, Bova M, Basi GS.

Bioorg Med Chem Lett. 2013 Feb 15;23(4):996-1000. doi: 10.1016/j.bmcl.2012.12.039. Epub 2012 Dec 21.

PMID:
23312944
6.

Treatment strategies targeting amyloid β-protein.

Schenk D, Basi GS, Pangalos MN.

Cold Spring Harb Perspect Med. 2012 Sep 1;2(9):a006387. doi: 10.1101/cshperspect.a006387. Review.

7.

Evidence that enzyme processivity mediates differential Aβ production by PS1 and PS2.

Pintchovski SA, Schenk DB, Basi GS.

Curr Alzheimer Res. 2013 Jan;10(1):4-10.

8.

Accelerating drug discovery for Alzheimer's disease: best practices for preclinical animal studies.

Shineman DW, Basi GS, Bizon JL, Colton CA, Greenberg BD, Hollister BA, Lincecum J, Leblanc GG, Lee LB, Luo F, Morgan D, Morse I, Refolo LM, Riddell DR, Scearce-Levie K, Sweeney P, Yrjänheikki J, Fillit HM.

Alzheimers Res Ther. 2011 Sep 28;3(5):28. doi: 10.1186/alzrt90.

9.

Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors.

Aubele DL, Truong AP, Dressen DB, Probst GD, Bowers S, Mattson MN, Semko CM, Sun M, Garofalo AW, Konradi AW, Sham HL, Zmolek W, Wong K, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Nguyen L, Bova MP, Hemphill SS, Basi G.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5791-4. doi: 10.1016/j.bmcl.2011.08.008. Epub 2011 Aug 9.

PMID:
21885276
10.

Lysine 624 of the amyloid precursor protein (APP) is a critical determinant of amyloid β peptide length: support for a sequential model of γ-secretase intramembrane proteolysis and regulation by the amyloid β precursor protein (APP) juxtamembrane region.

Kukar TL, Ladd TB, Robertson P, Pintchovski SA, Moore B, Bann MA, Ren Z, Jansen-West K, Malphrus K, Eggert S, Maruyama H, Cottrell BA, Das P, Basi GS, Koo EH, Golde TE.

J Biol Chem. 2011 Nov 18;286(46):39804-12. doi: 10.1074/jbc.M111.274696. Epub 2011 Aug 25.

11.

Amino-caprolactam γ-secretase inhibitors showing potential for the treatment of Alzheimer's disease.

Neitzel ML, Aubele DL, Marugg JL, Jagodzinski JJ, Konradi AW, Pleiss MA, Szoke B, Zmolek W, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Bova MP, Hemphill S, Basi G.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3715-20. doi: 10.1016/j.bmcl.2011.04.079. Epub 2011 May 1.

PMID:
21571529
12.

Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.

Basi GS, Hemphill S, Brigham EF, Liao A, Aubele DL, Baker J, Barbour R, Bova M, Chen XH, Dappen MS, Eichenbaum T, Goldbach E, Hawkinson J, Lawler-Herbold R, Hu K, Hui T, Jagodzinski JJ, Keim PS, Kholodenko D, Latimer LH, Lee M, Marugg J, Mattson MN, McCauley S, Miller JL, Motter R, Mutter L, Neitzel ML, Ni H, Nguyen L, Quinn K, Ruslim L, Semko CM, Shapiro P, Smith J, Soriano F, Szoke B, Tanaka K, Tang P, Tucker JA, Ye XM, Yu M, Wu J, Xu YZ, Garofalo AW, Sauer JM, Konradi AW, Ness D, Shopp G, Pleiss MA, Freedman SB, Schenk D.

Alzheimers Res Ther. 2010 Dec 29;2(6):36. doi: 10.1186/alzrt60.

13.

Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II).

Ye XM, Konradi AW, Smith J, Aubele DL, Garofalo AW, Marugg J, Neitzel ML, Semko CM, Sham HL, Sun M, Truong AP, Wu J, Zhang H, Goldbach E, Sauer JM, Brigham EF, Bova M, Basi GS.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3502-6. doi: 10.1016/j.bmcl.2010.04.148. Epub 2010 May 6.

PMID:
20529683
14.

Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.

Ye XM, Konradi AW, Smith J, Xu YZ, Dressen D, Garofalo AW, Marugg J, Sham HL, Truong AP, Jagodzinski J, Pleiss M, Zhang H, Goldbach E, Sauer JM, Brigham E, Bova M, Basi GS.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2195-9. doi: 10.1016/j.bmcl.2010.02.039. Epub 2010 Feb 13.

PMID:
20207136
15.

Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.

Mattson MN, Neitzel ML, Quincy DA, Semko CM, Garofalo AW, Keim PS, Konradi AW, Pleiss MA, Sham HL, Brigham EF, Goldbach EG, Zhang H, Sauer JM, Basi GS.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2148-50. doi: 10.1016/j.bmcl.2010.02.050. Epub 2010 Feb 14.

PMID:
20206516
16.

Structural correlates of antibodies associated with acute reversal of amyloid beta-related behavioral deficits in a mouse model of Alzheimer disease.

Basi GS, Feinberg H, Oshidari F, Anderson J, Barbour R, Baker J, Comery TA, Diep L, Gill D, Johnson-Wood K, Goel A, Grantcharova K, Lee M, Li J, Partridge A, Griswold-Prenner I, Piot N, Walker D, Widom A, Pangalos MN, Seubert P, Jacobsen JS, Schenk D, Weis WI.

J Biol Chem. 2010 Jan 29;285(5):3417-27. doi: 10.1074/jbc.M109.045187. Epub 2009 Nov 18.

17.

N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase.

Bowers S, Probst GD, Truong AP, Hom RK, Konradi AW, Sham HL, Garofalo AW, Wong K, Goldbach E, Quinn KP, Sauer JM, Wallace W, Nguyen L, Hemphill SS, Bova MP, Basi GS.

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6952-6. doi: 10.1016/j.bmcl.2009.10.060. Epub 2009 Oct 30.

PMID:
19879755
18.

Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.

Truong AP, Aubele DL, Probst GD, Neitzel ML, Semko CM, Bowers S, Dressen D, Hom RK, Konradi AW, Sham HL, Garofalo AW, Keim PS, Wu J, Dappen MS, Wong K, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Nguyen L, Hemphill SS, Bova MP, Bard F, Yednock TA, Basi G.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):4920-3. doi: 10.1016/j.bmcl.2009.07.092. Epub 2009 Jul 23. Erratum in: Bioorg Med Chem Lett. 2010 Dec 15;20(24):7553. Bard, Frédérique [added]; Yednock, Ted A [added].

PMID:
19660943
19.

Polo-like kinase 2 (PLK2) phosphorylates alpha-synuclein at serine 129 in central nervous system.

Inglis KJ, Chereau D, Brigham EF, Chiou SS, Schöbel S, Frigon NL, Yu M, Caccavello RJ, Nelson S, Motter R, Wright S, Chian D, Santiago P, Soriano F, Ramos C, Powell K, Goldstein JM, Babcock M, Yednock T, Bard F, Basi GS, Sham H, Chilcote TJ, McConlogue L, Griswold-Prenner I, Anderson JP.

J Biol Chem. 2009 Jan 30;284(5):2598-602. doi: 10.1074/jbc.C800206200. Epub 2008 Nov 12.

20.

Immunotherapy reduces vascular amyloid-beta in PDAPP mice.

Schroeter S, Khan K, Barbour R, Doan M, Chen M, Guido T, Gill D, Basi G, Schenk D, Seubert P, Games D.

J Neurosci. 2008 Jul 2;28(27):6787-93. doi: 10.1523/JNEUROSCI.2377-07.2008.

21.

Antibody capture of soluble Abeta does not reduce cortical Abeta amyloidosis in the PDAPP mouse.

Seubert P, Barbour R, Khan K, Motter R, Tang P, Kholodenko D, Kling K, Schenk D, Johnson-Wood K, Schroeter S, Gill D, Jacobsen JS, Pangalos M, Basi G, Games D.

Neurodegener Dis. 2008;5(2):65-71. doi: 10.1159/000112834. Epub 2008 Jan 4.

PMID:
18182780
22.

Identification of gamma-secretase inhibitor potency determinants on presenilin.

Zhao B, Yu M, Neitzel M, Marugg J, Jagodzinski J, Lee M, Hu K, Schenk D, Yednock T, Basi G.

J Biol Chem. 2008 Feb 1;283(5):2927-38. Epub 2007 Nov 21.

23.

Amyloid beta-protein precursor juxtamembrane domain regulates specificity of gamma-secretase-dependent cleavages.

Ren Z, Schenk D, Basi GS, Shapiro IP.

J Biol Chem. 2007 Nov 30;282(48):35350-60. Epub 2007 Sep 21.

24.

Antagonistic effects of beta-site amyloid precursor protein-cleaving enzymes 1 and 2 on beta-amyloid peptide production in cells.

Basi G, Frigon N, Barbour R, Doan T, Gordon G, McConlogue L, Sinha S, Zeller M.

J Biol Chem. 2003 Aug 22;278(34):31512-20. Epub 2003 Jun 11.

25.

BACE knockout mice are healthy despite lacking the primary beta-secretase activity in brain: implications for Alzheimer's disease therapeutics.

Roberds SL, Anderson J, Basi G, Bienkowski MJ, Branstetter DG, Chen KS, Freedman SB, Frigon NL, Games D, Hu K, Johnson-Wood K, Kappenman KE, Kawabe TT, Kola I, Kuehn R, Lee M, Liu W, Motter R, Nichols NF, Power M, Robertson DW, Schenk D, Schoor M, Shopp GM, Shuck ME, Sinha S, Svensson KA, Tatsuno G, Tintrup H, Wijsman J, Wright S, McConlogue L.

Hum Mol Genet. 2001 Jun 1;10(12):1317-24.

PMID:
11406613
26.

Recent advances in the understanding of the processing of APP to beta amyloid peptide.

Sinha S, Anderson J, John V, McConlogue L, Basi G, Thorsett E, Schenk D.

Ann N Y Acad Sci. 2000;920:206-8. Review. No abstract available.

PMID:
11193151
27.

Purification and cloning of amyloid precursor protein beta-secretase from human brain.

Sinha S, Anderson JP, Barbour R, Basi GS, Caccavello R, Davis D, Doan M, Dovey HF, Frigon N, Hong J, Jacobson-Croak K, Jewett N, Keim P, Knops J, Lieberburg I, Power M, Tan H, Tatsuno G, Tung J, Schenk D, Seubert P, Suomensaari SM, Wang S, Walker D, Zhao J, McConlogue L, John V.

Nature. 1999 Dec 2;402(6761):537-40.

PMID:
10591214
28.

Characterization of caspase processing and activation in HL-60 cell cytosol under cell-free conditions. Nucleotide requirement and inhibitor profile.

Mesner PW Jr, Bible KC, Martins LM, Kottke TJ, Srinivasula SM, Svingen PA, Chilcote TJ, Basi GS, Tung JS, Krajewski S, Reed JC, Alnemri ES, Earnshaw WC, Kaufmann SH.

J Biol Chem. 1999 Aug 6;274(32):22635-45.

29.

Caspase-mediated cleavage of DNA topoisomerase I at unconventional sites during apoptosis.

Samejima K, Svingen PA, Basi GS, Kottke T, Mesner PW Jr, Stewart L, Durrieu F, Poirier GG, Alnemri ES, Champoux JJ, Kaufmann SH, Earnshaw WC.

J Biol Chem. 1999 Feb 12;274(7):4335-40.

30.

Comparison of caspase activation and subcellular localization in HL-60 and K562 cells undergoing etoposide-induced apoptosis.

Martins LM, Mesner PW, Kottke TJ, Basi GS, Sinha S, Tung JS, Svingen PA, Madden BJ, Takahashi A, McCormick DJ, Earnshaw WC, Kaufmann SH.

Blood. 1997 Dec 1;90(11):4283-96.

31.

Comparison of apoptosis in wild-type and Fas-resistant cells: chemotherapy-induced apoptosis is not dependent on Fas/Fas ligand interactions.

Eischen CM, Kottke TJ, Martins LM, Basi GS, Tung JS, Earnshaw WC, Leibson PJ, Kaufmann SH.

Blood. 1997 Aug 1;90(3):935-43.

32.

Activation of multiple interleukin-1beta converting enzyme homologues in cytosol and nuclei of HL-60 cells during etoposide-induced apoptosis.

Martins LM, Kottke T, Mesner PW, Basi GS, Sinha S, Frigon N Jr, Tatar E, Tung JS, Bryant K, Takahashi A, Svingen PA, Madden BJ, McCormick DJ, Earnshaw WC, Kaufmann SH.

J Biol Chem. 1997 Mar 14;272(11):7421-30.

33.
34.

A novel S phase inhibitor in fission yeast.

Woollard A, Basi G, Nurse P.

EMBO J. 1996 Sep 2;15(17):4603-12.

35.
36.

Apoptosis and the cell cycle.

Chiarugi V, Magnelli L, Cinelli M, Basi G.

Cell Mol Biol Res. 1994;40(7-8):603-12. Review.

PMID:
7787878
37.

A three-dimensional model of the Cdc2 protein kinase: localization of cyclin- and Suc1-binding regions and phosphorylation sites.

Marcote MJ, Knighton DR, Basi G, Sowadski JM, Brambilla P, Draetta G, Taylor SS.

Mol Cell Biol. 1993 Aug;13(8):5122-31.

39.

Antibodies to soluble human T cell receptor beta chain recognize multiple epitopes on cell surface TcR.

Basi GS, Riggs MB, Nash K, Singer R.

J Immunol Methods. 1992 Nov 5;155(2):175-91.

PMID:
1385533
40.
41.

Characterization of uptake, degradation and toxicity of antisense ODNs in cancer cells.

Capaccioli S, Quattrone A, Basi G, Schiavone N, Giannini C.

Nucleic Acids Symp Ser. 1991;(24):299. No abstract available.

PMID:
1841356
42.

Transformation by ras oncogene induces nuclear shift of protein kinase C.

Chiarugi V, Magnelli L, Pasquali F, Vannucchi S, Bruni P, Quattrone A, Basi G, Capaccioli S, Ruggiero M.

Biochem Biophys Res Commun. 1990 Dec 14;173(2):528-33.

PMID:
2260965
43.

The old and the new in transformed cell signalling: glycolysis, diacylglycerol and protein kinase C.

Chiarugi V, Basi G, Quattrone A, Micheletti R, Ruggiero M.

Second Messengers Phosphoproteins. 1990;13(1):69-85. Review. No abstract available.

PMID:
2286934
44.

Synthesis of diacylglycerol de novo is responsible for permanent activation and down-regulation of protein kinase C in transformed cells.

Chiarugi V, Bruni P, Pasquali F, Magnelli L, Basi G, Ruggiero M, Farnararo M.

Biochem Biophys Res Commun. 1989 Oct 31;164(2):816-23.

PMID:
2684158
45.
46.
47.

Primary structure and transcriptional regulation of GAP-43, a protein associated with nerve growth.

Basi GS, Jacobson RD, Virág I, Schilling J, Skene JH.

Cell. 1987 Jun 19;49(6):785-91.

PMID:
3581170
48.
49.

Multiple polyadenylation sites in a Drosophila tropomyosin gene are used to generate functional mRNAs.

Boardman M, Basi GS, Storti RV.

Nucleic Acids Res. 1985 Mar 11;13(5):1763-76.

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