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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. Basi GS, et al. Among authors: keim ps. Alzheimers Res Ther. 2010 Dec 29;2(6):36. doi: 10.1186/alzrt60. Alzheimers Res Ther. 2010. PMID: 21190552 Free PMC article.
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. Mattson MN, et al. Among authors: keim ps. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2148-50. doi: 10.1016/j.bmcl.2010.02.050. Epub 2010 Feb 14. Bioorg Med Chem Lett. 2010. PMID: 20206516
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. Truong AP, et al. Among authors: keim ps. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4920-3. doi: 10.1016/j.bmcl.2009.07.092. Epub 2009 Jul 23. Bioorg Med Chem Lett. 2009. PMID: 19660943
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. Probst G, et al. Among authors: keim ps. J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20. J Med Chem. 2013. PMID: 23713656
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. Sinha S, et al. Nature. 1999 Dec 2;402(6761):537-40. doi: 10.1038/990114. Nature. 1999. PMID: 10591214
Phosphorylation of Ser-129 is the dominant pathological modification of alpha-synuclein in familial and sporadic Lewy body disease.
Anderson JP, Walker DE, Goldstein JM, de Laat R, Banducci K, Caccavello RJ, Barbour R, Huang J, Kling K, Lee M, Diep L, Keim PS, Shen X, Chataway T, Schlossmacher MG, Seubert P, Schenk D, Sinha S, Gai WP, Chilcote TJ. Anderson JP, et al. Among authors: keim ps. J Biol Chem. 2006 Oct 6;281(40):29739-52. doi: 10.1074/jbc.M600933200. Epub 2006 Jul 17. J Biol Chem. 2006. PMID: 16847063 Free article.
134 results