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Volumn 20, Issue 3, 2010, Pages 1269-1271

Piperazinyl pyrimidine derivatives as potent γ-secretase modulators

Author keywords

Alzheimer's disease; Secretase modulators

Indexed keywords

GAMMA SECRETASE; NOTCH RECEPTOR; PIPERAZINYL PYRIMIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG; AMYLOID BETA PROTEIN; AMYLOID BETA-PROTEIN (40-42); PEPTIDE FRAGMENT; PIPERAZINE DERIVATIVE; SECRETASE;

EID: 74049093168     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.11.101     Document Type: Article
Times cited : (44)

References (24)
  • 19
    • 20944432999 scopus 로고    scopus 로고
    • 50 measurements for Aβ40 and Aβ42 were determined using electrochemiluminescent detection of peptides secreted by SH-SY5Y cells stably overexpressing the β-APP C-terminal fragment SPA4CT. Consistent with the profiles of γ-secretase modulators, total Aβ peptide levels were constant
    • 50 measurements for Aβ40 and Aβ42 were determined using electrochemiluminescent detection of peptides secreted by SH-SY5Y cells stably overexpressing the β-APP C-terminal fragment SPA4CT. Consistent with the profiles of γ-secretase modulators, total Aβ peptide levels were constant. Best J.D., Jay M.T., Otu F., Ma J., Nadin A., Ellis S., Lewis H.D., Pattison C., Reilly M., Harrison T., Shearman M.S., Williamson T.L., and Atack J.R.J. Pharm. Exp. Ther. 313 (2005) 902
    • (2005) Pharm. Exp. Ther. , vol.313 , pp. 902
    • Best, J.D.1    Jay, M.T.2    Otu, F.3    Ma, J.4    Nadin, A.5    Ellis, S.6    Lewis, H.D.7    Pattison, C.8    Reilly, M.9    Harrison, T.10    Shearman, M.S.11    Williamson, T.L.12    Atack, J.R.J.13
  • 22
    • 69749108869 scopus 로고    scopus 로고
    • Compound 29 was prepared using methods reported by
    • Compound 29 was prepared using methods reported by. Li C., and Rosenau A. Tetrahedron Lett. (2009) 5888
    • (2009) Tetrahedron Lett. , pp. 5888
    • Li, C.1    Rosenau, A.2
  • 23
    • 84925564353 scopus 로고    scopus 로고
    • note
    • Conformational analysis was performed with the implicit Generalized-Born solvent model with 8 kcal/mol energy cutoff. Clustering of conformers based on the atomic RMS dissimilarity was used to generate the 10 most diverse representative conformers. Two of the most diverse conformers for 1 and 2 are shown in Figure 2.
  • 24
    • 14744281422 scopus 로고    scopus 로고
    • HeLa cells were made to co-express nonfunctional halves of luciferase, one fused to NotchΔE and the other to RBP-Jκ. γ-Secretase mediated cleavage of NotchΔE results in release of Notch intracellular domain (NICD)/N-terminal luciferase, which translocates to the nucleus and binds the RBP-Jκ/C-terminal luciferase to form a functional luciferase enzyme. This split-luciferase complementation system is used to detect NICD levels by measuring total luminescence upon addition of luciferin to lysed cells
    • HeLa cells were made to co-express nonfunctional halves of luciferase, one fused to NotchΔE and the other to RBP-Jκ. γ-Secretase mediated cleavage of NotchΔE results in release of Notch intracellular domain (NICD)/N-terminal luciferase, which translocates to the nucleus and binds the RBP-Jκ/C-terminal luciferase to form a functional luciferase enzyme. This split-luciferase complementation system is used to detect NICD levels by measuring total luminescence upon addition of luciferin to lysed cells. Paulmurugan R., and Gambhir S.S. Anal. Chem. 77 (2005) 1295
    • (2005) Anal. Chem. , vol.77 , pp. 1295
    • Paulmurugan, R.1    Gambhir, S.S.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.