메뉴 건너뛰기




Volumn 344, Issue 3, 2013, Pages 686-695

Pharmacodynamics of selective inhibition of γ-secretase by avagacestat

Author keywords

[No Author keywords available]

Indexed keywords

AMYLOID BETA PROTEIN; AMYLOID BETA PROTEIN[1-40]; AMYLOID BETA PROTEIN[1-42]; AMYLOID PRECURSOR PROTEIN; AVAGACESTAT; NOTCH RECEPTOR; TRANSCRIPTION FACTOR HES 1;

EID: 84874426209     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.112.199356     Document Type: Article
Times cited : (59)

References (53)
  • 1
    • 34948850819 scopus 로고    scopus 로고
    • Notch and NFkappaB signaling pathways: Do they collaborate in normal vertebrate brain development and function?
    • Ang HL and Tergaonkar V (2007) Notch and NFkappaB signaling pathways: Do they collaborate in normal vertebrate brain development and function? Bioessays 29: 1039-1047.
    • (2007) Bioessays , vol.29 , pp. 1039-1047
    • Ang, H.L.1    Tergaonkar, V.2
  • 2
    • 19944430290 scopus 로고    scopus 로고
    • Dynamics of beta-amyloid reductions in brain, cerebrospinal fluid, and plasma of beta-amyloid precursor protein transgenic mice treated with a gamma-secretase inhibitor
    • Barten DM, Guss VL, Corsa JA, Loo A, Hansel SB, Zheng M, Munoz B, Srinivasan K, Wang B, and Robertson BJ, et al. (2005) Dynamics of beta-amyloid reductions in brain, cerebrospinal fluid, and plasma of beta-amyloid precursor protein transgenic mice treated with a gamma-secretase inhibitor. J Pharmacol Exp Ther 312: 635-643.
    • (2005) J Pharmacol Exp Ther , vol.312 , pp. 635-643
    • Barten, D.M.1    Guss, V.L.2    Corsa, J.A.3    Loo, A.4    Hansel, S.B.5    Zheng, M.6    Munoz, B.7    Srinivasan, K.8    Wang, B.9    Robertson, B.J.10
  • 6
    • 76449085569 scopus 로고    scopus 로고
    • Gamma-secretases: From cell biology to therapeutic strategies
    • Bergmans BA and De Strooper B (2010) gamma-secretases: From cell biology to therapeutic strategies. Lancet Neurol 9:215-226.
    • (2010) Lancet Neurol , vol.9 , pp. 215-226
    • Bergmans, B.A.1    De Strooper, B.2
  • 7
    • 33846451755 scopus 로고    scopus 로고
    • The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]- 4-(2,5-difluorophenyl)cyclohexyl]-1,11-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, and Boussiquet-Leroux C, et al. (2007) 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. J Pharmacol Exp Ther 320:552-558.
    • (2007) J Pharmacol Exp Ther , vol.320 , pp. 552-558
    • Best, J.D.1    Smith, D.W.2    Reilly, M.A.3    O'Donnell, R.4    Lewis, H.D.5    Ellis, S.6    Wilkie, N.7    Rosahl, T.W.8    Laroque, P.A.9    Boussiquet-Leroux, C.10
  • 13
    • 0027769745 scopus 로고
    • Comparison of four basic models of indirect pharmacodynamic responses
    • Dayneka NL, Garg V, and Jusko WJ (1993) Comparison of four basic models of indirect pharmacodynamic responses. J Pharmacokinet Biopharm 21:457-478.
    • (1993) J Pharmacokinet Biopharm , vol.21 , pp. 457-478
    • Dayneka, N.L.1    Garg, V.2    Jusko, W.J.3
  • 14
    • 10044274045 scopus 로고    scopus 로고
    • Activities of daily living in patients with dementia: Clinical relevance, methods of assessment and effects of treatment
    • Desai AK, Grossberg GT, and Sheth DN (2004) Activities of daily living in patients with dementia: Clinical relevance, methods of assessment and effects of treatment. CNS Drugs 18:853-875.
    • (2004) CNS Drugs , vol.18 , pp. 853-875
    • Desai, A.K.1    Grossberg, G.T.2    Sheth, D.N.3
  • 15
    • 84872320528 scopus 로고    scopus 로고
    • A placebo-controlled, multiple ascending dose study to evaluate the safety, pharmacokinetics and pharmacodynamics of avagacestat (BMS-708163) in healthy young and elderly subjects
    • Dockens R, Wang JS, Castaneda L, Sverdlov O, Huang SP, Slemmon R, Gu H, Wong O, Li H, and Berman RM, et al. (2012) A placebo-controlled, multiple ascending dose study to evaluate the safety, pharmacokinetics and pharmacodynamics of avagacestat (BMS-708163) in healthy young and elderly subjects. Clin Pharmacokinet 51:681-693.
    • (2012) Clin Pharmacokinet , vol.51 , pp. 681-693
    • Dockens, R.1    Wang, J.S.2    Castaneda, L.3    Sverdlov, O.4    Huang, S.P.5    Slemmon, R.6    Gu, H.7    Wong, O.8    Li, H.9    Berman, R.M.10
  • 18
    • 0002954125 scopus 로고
    • Robust estimates, residuals, and outlier detection with multiresponse data
    • Gnanadesikan R and Kettenring JR (1972) Robust estimates, residuals, and outlier detection with multiresponse data. Biometrics 28:81-124.
    • (1972) Biometrics , vol.28 , pp. 81-124
    • Gnanadesikan, R.1    Kettenring, J.R.2
  • 19
    • 77955845945 scopus 로고    scopus 로고
    • Development and validation of sensitive and selective LC-MS/MS methods for the determination of BMS-708163, a gamma-secretase inhibitor, in plasma and cerebrospinal fluid using deprotonated or formate adduct ions as precursor ions
    • Gu H, Deng Y, Wang J, Aubry AF, and Arnold ME (2010) Development and validation of sensitive and selective LC-MS/MS methods for the determination of BMS-708163, a gamma-secretase inhibitor, in plasma and cerebrospinal fluid using deprotonated or formate adduct ions as precursor ions. J Chromatogr B Analyt Technol Biomed Life Sci 878:2319-2326.
    • (2010) J Chromatogr B Analyt Technol Biomed Life Sci , vol.878 , pp. 2319-2326
    • Gu, H.1    Deng, Y.2    Wang, J.3    Aubry, A.F.4    Arnold, M.E.5
  • 20
    • 0037135111 scopus 로고    scopus 로고
    • The amyloid hypothesis of Alzheimer's disease: Progress and problems on the road to therapeutics
    • Hardy J and Selkoe DJ (2002) The amyloid hypothesis of Alzheimer's disease: Progress and problems on the road to therapeutics. Science 297:353-356.
    • (2002) Science , vol.297 , pp. 353-356
    • Hardy, J.1    Selkoe, D.J.2
  • 21
    • 67650407720 scopus 로고    scopus 로고
    • Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease
    • Henley DB, May PC, Dean RA, and Siemers ER (2009) Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease. Expert Opin Pharmacother 10:1657-1664.
    • (2009) Expert Opin Pharmacother , vol.10 , pp. 1657-1664
    • Henley, D.B.1    May, P.C.2    Dean, R.A.3    Siemers, E.R.4
  • 22
    • 33751160615 scopus 로고    scopus 로고
    • Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor 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 (LY411,575) in the CRND8 mouse
    • Hyde LA, McHugh NA, Chen J, Zhang Q, Manfra D, Nomeir AA, Josien H, Bara T, Clader JW, and Zhang L, et al. (2006) Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor 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 (LY411,575) in the CRND8 mouse. J Pharmacol Exp Ther 319: 1133-1143.
    • (2006) J Pharmacol Exp Ther , vol.319 , pp. 1133-1143
    • Hyde, L.A.1    McHugh, N.A.2    Chen, J.3    Zhang, Q.4    Manfra, D.5    Nomeir, A.A.6    Josien, H.7    Bara, T.8    Clader, J.W.9    Zhang, L.10
  • 25
    • 64249172203 scopus 로고    scopus 로고
    • The canonical Notch signaling pathway: Unfolding the activation mechanism
    • Kopan R and Ilagan MX (2009) The canonical Notch signaling pathway: Unfolding the activation mechanism. Cell 137:216-233.
    • (2009) Cell , vol.137 , pp. 216-233
    • Kopan, R.1    Ilagan, M.X.2
  • 28
    • 0038746673 scopus 로고    scopus 로고
    • Catalytic site-directed g-secretase complex inhibitors do not discriminate pharmacologically between Notch S3 and b-APP cleavages
    • Lewis HD, Pérez Revuelta BI, Nadin A, Neduvelil JG, Harrison T, Pollack SJ, and Shearman MS (2003) Catalytic site-directed g-secretase complex inhibitors do not discriminate pharmacologically between Notch S3 and b-APP cleavages. Biochemistry 42:7580-7586.
    • (2003) Biochemistry , vol.42 , pp. 7580-7586
    • Lewis, H.D.1    Pérez Revuelta, B.I.2    Nadin, A.3    Neduvelil, J.G.4    Harrison, T.5    Pollack, S.J.6    Shearman, M.S.7
  • 29
    • 36148993580 scopus 로고    scopus 로고
    • Epidermal growth factor receptor and notch pathways participate in the tumor suppressor function of gamma-secretase
    • Li T, Wen H, Brayton C, Das P, Smithson LA, Fauq A, Fan X, Crain BJ, Price DL, and Golde TE, et al. (2007a) Epidermal growth factor receptor and notch pathways participate in the tumor suppressor function of gamma-secretase. J Biol Chem 282: 32264-32273.
    • (2007) J Biol Chem , vol.282 , pp. 32264-32273
    • Li, T.1    Wen, H.2    Brayton, C.3    Das, P.4    Smithson, L.A.5    Fauq, A.6    Fan, X.7    Crain, B.J.8    Price, D.L.9    Golde, T.E.10
  • 31
    • 0002975203 scopus 로고
    • On the generalised distance in statistics
    • Mahalanobis PC (1936) On the generalised distance in statistics. Proc Nat Inst Sci India 12:49-55.
    • (1936) Proc Nat Inst Sci India , vol.12 , pp. 49-55
    • Mahalanobis, P.C.1
  • 32
    • 70350462583 scopus 로고    scopus 로고
    • Begacestat (GSI-953): A novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease
    • Martone RL, Zhou H, Atchison K, Comery T, Xu JZ, Huang X, Gong X, Jin M, Kreft A, and Harrison B, et al. (2009) Begacestat (GSI-953): A novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. J Pharmacol Exp Ther 331:598-608.
    • (2009) J Pharmacol Exp Ther , vol.331 , pp. 598-608
    • Martone, R.L.1    Zhou, H.2    Atchison, K.3    Comery, T.4    Xu, J.Z.5    Huang, X.6    Gong, X.7    Jin, M.8    Kreft, A.9    Harrison, B.10
  • 33
    • 8444247084 scopus 로고    scopus 로고
    • Modulation of notch processing by gamma-secretase inhibitors causes intestinal goblet cell metaplasia and induction of genes known to specify gut secretory lineage differentiation
    • Milano J, McKay J, Dagenais C, Foster-Brown L, Pognan F, Gadient R, Jacobs RT, Zacco A, Greenberg B, and Ciaccio PJ (2004) Modulation of notch processing by gamma-secretase inhibitors causes intestinal goblet cell metaplasia and induction of genes known to specify gut secretory lineage differentiation. Toxicol Sci 82: 341-358.
    • (2004) Toxicol Sci , vol.82 , pp. 341-358
    • Milano, J.1    McKay, J.2    Dagenais, C.3    Foster-Brown, L.4    Pognan, F.5    Gadient, R.6    Jacobs, R.T.7    Zacco, A.8    Greenberg, B.9    Ciaccio, P.J.10
  • 34
    • 84857020179 scopus 로고    scopus 로고
    • Differential effects between g-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice
    • Mitani Y, Yarimizu J, Saita K, Uchino H, Akashiba H, Shitaka Y, Ni K, and Matsuoka N (2012) Differential effects between g-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice. J Neurosci 32:2037-2050.
    • (2012) J Neurosci , vol.32 , pp. 2037-2050
    • Mitani, Y.1    Yarimizu, J.2    Saita, K.3    Uchino, H.4    Akashiba, H.5    Shitaka, Y.6    Ni, K.7    Matsuoka, N.8
  • 35
    • 40349100482 scopus 로고    scopus 로고
    • Recent progress in the medicinal chemistry of gamma-secretase inhibitors
    • Olson RE and Albright CF (2008) Recent progress in the medicinal chemistry of gamma-secretase inhibitors. Curr Top Med Chem 8:17-33.
    • (2008) Curr Top Med Chem , vol.8 , pp. 17-33
    • Olson, R.E.1    Albright, C.F.2
  • 36
    • 12544258201 scopus 로고    scopus 로고
    • Secretase inhibitors for Alzheimer's disease: Challenges of a promiscuous protease
    • Pollack SJ and Lewis H (2005) Secretase inhibitors for Alzheimer's disease: Challenges of a promiscuous protease. Curr Opin Investig Drugs 6:35-47.
    • (2005) Curr Opin Investig Drugs , vol.6 , pp. 35-47
    • Pollack, S.J.1    Lewis, H.2
  • 37
    • 34250365682 scopus 로고    scopus 로고
    • Discovery of (S) 2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S, Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][12]diazepin-5-yl)propanamide (BMS-433796) a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease
    • Prasad CV, Zheng M, Vig S, Bergstrom C, Smith DW, Gao Q, Yeola S, Polson CT, Corsa JA, and Guss VL, et al. (2007) Discovery of (S)-2-((S)-2-(3,5- difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4, 5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): A gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease. Bioorg Med Chem Lett 17:4006-4011.
    • (2007) Bioorg Med Chem Lett , vol.17 , pp. 4006-4011
    • Prasad, C.V.1    Zheng, M.2    Vig, S.3    Bergstrom, C.4    Smith, D.W.5    Gao, Q.6    Yeola, S.7    Polson, C.T.8    Corsa, J.A.9    Guss, V.L.10
  • 39
  • 40
  • 41
    • 78650810711 scopus 로고    scopus 로고
    • Are g-secretase inhibitors detrimental for Alzheimer's disease patients?
    • Ross JS and Imbimbo BP (2010) Are g-secretase inhibitors detrimental for Alzheimer's disease patients? J Alzheimers Dis 22:401-404.
    • (2010) J Alzheimers Dis , vol.22 , pp. 401-404
    • Ross, J.S.1    Imbimbo, B.P.2
  • 43
    • 39649101710 scopus 로고    scopus 로고
    • Developing preventive therapies for chronic diseases: Lessons learned from Alzheimer's disease
    • Selkoe DJ (2007) Developing preventive therapies for chronic diseases: Lessons learned from Alzheimer's disease. Nutr Rev 65:S239-S243.
    • (2007) Nutr Rev , vol.65
    • Selkoe, D.J.1
  • 44
    • 0030429755 scopus 로고    scopus 로고
    • Characterization of four basic models of indirect pharmacodynamic responses
    • Sharma A and Jusko WJ (1996) Characterization of four basic models of indirect pharmacodynamic responses. J Pharmacokinet Biopharm 24:611-635.
    • (1996) J Pharmacokinet Biopharm , vol.24 , pp. 611-635
    • Sharma, A.1    Jusko, W.J.2
  • 46
    • 57649174625 scopus 로고    scopus 로고
    • Intramembrane proteolysis by g-secretase
    • Steiner H, Fluhrer R, and Haass C (2008) Intramembrane proteolysis by g-secretase. J Biol Chem 283:29627-29631.
    • (2008) J Biol Chem , vol.283 , pp. 29627-29631
    • Steiner, H.1    Fluhrer, R.2    Haass, C.3
  • 47
    • 84863343191 scopus 로고    scopus 로고
    • Multicenter, randomized, double-blind, placebocontrolled, single-ascending dose study of the oral g-secretase inhibitor BMS-708163 (Avagacestat): Tolerability profile, pharmacokinetic parameters, and pharmacodynamic markers
    • Tong G, Wang JS, Sverdlov O, Huang SP, Slemmon R, Croop R, Castaneda L, Gu H, Wong O, and Li H, et al. (2012a) Multicenter, randomized, double-blind, placebocontrolled, single-ascending dose study of the oral g-secretase inhibitor BMS-708163 (Avagacestat): Tolerability profile, pharmacokinetic parameters, and pharmacodynamic markers. Clin Ther 34:654-667.
    • (2012) Clin Ther , vol.34 , pp. 654-667
    • Tong, G.1    Wang, J.S.2    Sverdlov, O.3    Huang, S.P.4    Slemmon, R.5    Croop, R.6    Castaneda, L.7    Gu, H.8    Wong, O.9    Li, H.10
  • 49
    • 5344277556 scopus 로고    scopus 로고
    • Deciphering the molecular basis of memory failure in Alzheimer's disease
    • Walsh DM and Selkoe DJ (2004) Deciphering the molecular basis of memory failure in Alzheimer's disease. Neuron 44:181-193.
    • (2004) Neuron , vol.44 , pp. 181-193
    • Walsh, D.M.1    Selkoe, D.J.2
  • 50
    • 11144355129 scopus 로고    scopus 로고
    • Chronic treatment with the gammasecretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation
    • Wong GT, Manfra D, Poulet FM, Zhang Q, Josien H, Bara T, Engstrom L, Pinzon-Ortiz M, Fine JS, and Lee HJ, et al. (2004) Chronic treatment with the gammasecretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation. J Biol Chem 279:12876-12882.
    • (2004) J Biol Chem , vol.279 , pp. 12876-12882
    • Wong, G.T.1    Manfra, D.2    Poulet, F.M.3    Zhang, Q.4    Josien, H.5    Bara, T.6    Engstrom, L.7    Pinzon-Ortiz, M.8    Fine, J.S.9    Lee, H.J.10
  • 51
    • 64349085139 scopus 로고    scopus 로고
    • Gamma-secretase inhibitors for the treatment of Alzheimer's disease
    • Wu WL and Zhang L (2009) Gamma-secretase inhibitors for the treatment of Alzheimer's disease. Drug Dev Res 70:94-100.
    • (2009) Drug Dev Res , vol.70 , pp. 94-100
    • Wu, W.L.1    Zhang, L.2
  • 53
    • 34547539177 scopus 로고    scopus 로고
    • Presenilin/g-secretasedependent processing of b-amyloid precursor protein regulates EGF receptor expression
    • Zhang YW, Wang R, Liu Q, Zhang H, Liao FF, and Xu H (2007) Presenilin/g-secretasedependent processing of b-amyloid precursor protein regulates EGF receptor expression. Proc Natl Acad Sci USA 104:10613-10618.
    • (2007) Proc Natl Acad Sci USA , vol.104 , pp. 10613-10618
    • Zhang, Y.W.1    Wang, R.2    Liu, Q.3    Zhang, H.4    Liao, F.F.5    Xu, H.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.