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Volumn , Issue , 2012, Pages

γ-secretase modulators: Can we combine potency with safety?

Author keywords

[No Author keywords available]

Indexed keywords

AMYLOID BETA PROTEIN[1-42]; E 2012; E 2212; EVP 0926; GAMMA SECRETASE; GAMMA SECRETASE INHIBITOR; JNJ 40418677; JNJ 42601572; SEMAGACESTAT; TARENFLURBIL; UNCLASSIFIED DRUG;

EID: 84872154160     PISSN: None     EISSN: 20900252     Source Type: Journal    
DOI: 10.1155/2012/295207     Document Type: Article
Times cited : (33)

References (46)
  • 1
    • 84858225391 scopus 로고    scopus 로고
    • 2012 Alzheimer's disease facts and figures
    • Alzheimer's Association, 2012 Alzheimer's disease facts and figures. Alzheimer's and Dementia 2012 8 131 168
    • (2012) Alzheimer's and Dementia , vol.8 , pp. 131-168
    • Association, A.1
  • 2
    • 0037135111 scopus 로고    scopus 로고
    • The amyloid hypothesis of Alzheimer's disease: Progress and problems on the road to therapeutics
    • DOI 10.1126/science.1072994
    • Hardy J., Selkoe D. J., The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics. Science 2002 297 5580 353 356 2-s2.0-0037135111 10.1126/science.1072994 (Pubitemid 34790756)
    • (2002) Science , vol.297 , Issue.5580 , pp. 353-356
    • Hardy, J.1    Selkoe, D.J.2
  • 3
    • 76849086405 scopus 로고    scopus 로고
    • The secretases: Enzymes with therapeutic potential in Alzheimer disease
    • 2-s2.0-76849086405 10.1038/nrneurol.2009.218
    • De Strooper B., Vassar R., Golde T., The secretases: enzymes with therapeutic potential in Alzheimer disease. Nature Reviews Neurology 2010 6 2 99 107 2-s2.0-76849086405 10.1038/nrneurol.2009.218
    • (2010) Nature Reviews Neurology , vol.6 , Issue.2 , pp. 99-107
    • De Strooper, B.1    Vassar, R.2    Golde, T.3
  • 5
    • 70350059834 scopus 로고    scopus 로고
    • Recent advances in the identification of γ -secretase inhibitors to clinically test the A β oligomer hypothesis of Alzheimer's disease
    • 2-s2.0-70350059834 10.1021/jm900188z
    • Kreft A. F., Martone R., Porte A., Recent advances in the identification of γ -secretase inhibitors to clinically test the A β oligomer hypothesis of Alzheimer's disease. Journal of Medicinal Chemistry 2009 52 20 6169 6188 2-s2.0-70350059834 10.1021/jm900188z
    • (2009) Journal of Medicinal Chemistry , vol.52 , Issue.20 , pp. 6169-6188
    • Kreft, A.F.1    Martone, R.2    Porte, A.3
  • 9
    • 68049148021 scopus 로고    scopus 로고
    • Why did tarenflurbil fail in alzheimer's disease?
    • 2-s2.0-68049148021 10.3233/JAD-2009-1092
    • Imbimbo B. P., Why did tarenflurbil fail in alzheimer's disease? Journal of Alzheimer's Disease 2009 17 4 757 760 2-s2.0-68049148021 10.3233/JAD-2009- 1092
    • (2009) Journal of Alzheimer's Disease , vol.17 , Issue.4 , pp. 757-760
    • Imbimbo, B.P.1
  • 10
    • 84872145576 scopus 로고    scopus 로고
    • Aryl compounds and uses in modulating amyloid β
    • 2004110350
    • Cheng S., Comer D. D., Mao L., Balow G. P., Pleynet D., Aryl compounds and uses in modulating amyloid β WO 2004 2004110350
    • (2004) WO
    • Cheng, S.1    Comer, D.D.2    Mao, L.3    Balow, G.P.4    Pleynet, D.5
  • 12
    • 77956187227 scopus 로고    scopus 로고
    • Exploring the chemical space of γ -secretase modulators
    • 2-s2.0-77956187227 10.1016/j.tips.2010.05.007
    • Zettl H., Weggen S., Schneider P., Schneider G., Exploring the chemical space of γ -secretase modulators. Trends in Pharmacological Sciences 2010 31 9 402 410 2-s2.0-77956187227 10.1016/j.tips.2010.05.007
    • (2010) Trends in Pharmacological Sciences , vol.31 , Issue.9 , pp. 402-410
    • Zettl, H.1    Weggen, S.2    Schneider, P.3    Schneider, G.4
  • 13
    • 79851473226 scopus 로고    scopus 로고
    • γ -Secretase modulators as potential disease modifying anti-Alzheimer's drugs
    • 2-s2.0-79851473226 10.1021/jm101168r
    • Oehlrich D., Berthelot D. J. C., Gijsen H. J. M., γ -Secretase modulators as potential disease modifying anti-Alzheimer's drugs. Journal of Medicinal Chemistry 2011 54 3 669 698 2-s2.0-79851473226 10.1021/jm101168r
    • (2011) Journal of Medicinal Chemistry , vol.54 , Issue.3 , pp. 669-698
    • Oehlrich, D.1    Berthelot, D.J.C.2    Gijsen, H.J.M.3
  • 14
    • 1942453243 scopus 로고    scopus 로고
    • Ligand efficiency: A useful metric for lead selection
    • DOI 10.1016/S1359-6446(04)03069-7, PII S1359644604030697
    • Hopkins A. L., Groom C. R., Alex A., Ligand efficiency: a useful metric for lead selection. Drug Discovery Today 2004 9 10 430 431 2-s2.0-1942453243 10.1016/S1359-6446(04)03069-7 (Pubitemid 38510559)
    • (2004) Drug Discovery Today , vol.9 , Issue.10 , pp. 430-431
    • Hopkins, A.L.1    Groom, C.R.2    Alex, A.3
  • 16
    • 79954480259 scopus 로고    scopus 로고
    • Chronic treatment with a novel γ -secretase modulator, JNJ-40418677, inhibits amyloid plaque formation in a mouse model of Alzheimer's disease
    • 2-s2.0-79954480259 10.1111/j.1476-5381.2011.01207.x
    • Van Broeck B., Chen J. M., Tréton G., Desmidt M., Hopf C., Ramsden N., Karran E., Mercken M., Rowley A., Chronic treatment with a novel γ -secretase modulator, JNJ-40418677, inhibits amyloid plaque formation in a mouse model of Alzheimer's disease. British Journal of Pharmacology 2011 163 2 375 389 2-s2.0-79954480259 10.1111/j.1476-5381.2011.01207.x
    • (2011) British Journal of Pharmacology , vol.163 , Issue.2 , pp. 375-389
    • Van Broeck, B.1    Chen, J.M.2    Tréton, G.3    Desmidt, M.4    Hopf, C.5    Ramsden, N.6    Karran, E.7    Mercken, M.8    Rowley, A.9
  • 29
    • 80052974259 scopus 로고    scopus 로고
    • Improving drug candidates by design: A focus on physicochemical properties as a means of improving compound disposition and safety
    • 10.1021/tx200211v
    • Meanwell N. A., Improving drug candidates by design: a focus on physicochemical properties as a means of improving compound disposition and safety. Chemical Research in Toxicology 2011 24 9 1420 1456 10.1021/tx200211v
    • (2011) Chemical Research in Toxicology , vol.24 , Issue.9 , pp. 1420-1456
    • Meanwell, N.A.1
  • 30
    • 84860359784 scopus 로고    scopus 로고
    • Finding the sweet spot: The role of nature and nurture in medicinal chemistry
    • 10.1038/nrd3701
    • Hann M. M., Keseü G. M., Finding the sweet spot: the role of nature and nurture in medicinal chemistry. Nature Reviews Drug Discovery 2012 11 5 355 365 10.1038/nrd3701
    • (2012) Nature Reviews Drug Discovery , vol.11 , Issue.5 , pp. 355-365
    • Hann, M.M.1    Keseü, G.M.2
  • 31
    • 79955613841 scopus 로고    scopus 로고
    • Molecular obesity, potency and other addictions in drug discovery
    • 2-s2.0-79955613841 10.1039/c1md00017a
    • Hann M. M., Molecular obesity, potency and other addictions in drug discovery. Medicinal Chemistry Communications 2011 2 5 349 355 2-s2.0-79955613841 10.1039/c1md00017a
    • (2011) Medicinal Chemistry Communications , vol.2 , Issue.5 , pp. 349-355
    • Hann, M.M.1
  • 32
    • 71049126548 scopus 로고    scopus 로고
    • Escape from flatland: Increasing saturation as an approach to improving clinical success
    • 2-s2.0-71049126548 10.1021/jm901241e
    • Lovering F., Bikker J., Humblet C., Escape from flatland: increasing saturation as an approach to improving clinical success. Journal of Medicinal Chemistry 2009 52 21 6752 6756 2-s2.0-71049126548 10.1021/jm901241e
    • (2009) Journal of Medicinal Chemistry , vol.52 , Issue.21 , pp. 6752-6756
    • Lovering, F.1    Bikker, J.2    Humblet, C.3
  • 33
    • 35748934487 scopus 로고    scopus 로고
    • The influence of drug-like concepts on decision-making in medicinal chemistry
    • DOI 10.1038/nrd2445, PII NRD2445
    • Leeson P. D., Springthorpe B., The influence of drug-like concepts on decision-making in medicinal chemistry. Nature Reviews Drug Discovery 2007 6 11 881 890 2-s2.0-35748934487 10.1038/nrd2445 (Pubitemid 350042396)
    • (2007) Nature Reviews Drug Discovery , vol.6 , Issue.11 , pp. 881-890
    • Leeson, P.D.1    Springthorpe, B.2
  • 34
    • 61649109015 scopus 로고    scopus 로고
    • The influence of lead discovery strategies on the properties of drug candidates
    • 2-s2.0-61649109015 10.1038/nrd2796
    • Keserü G. M., Makara G. M., The influence of lead discovery strategies on the properties of drug candidates. Nature Reviews Drug Discovery 2009 8 3 203 212 2-s2.0-61649109015 10.1038/nrd2796
    • (2009) Nature Reviews Drug Discovery , vol.8 , Issue.3 , pp. 203-212
    • Keserü, G.M.1    Makara, G.M.2
  • 35
    • 84856846240 scopus 로고    scopus 로고
    • Impact of lipophilic efficiency on compound quality
    • 10.1021/jm201388p
    • Tarcsay A., Nyíri K., Keserú G. M., Impact of lipophilic efficiency on compound quality. Journal of Medicinal Chemistry 2012 55 3 1252 1260 10.1021/jm201388p
    • (2012) Journal of Medicinal Chemistry , vol.55 , Issue.3 , pp. 1252-1260
    • Tarcsay, A.1    Nyíri, K.2    Keserú, G.M.3
  • 36
    • 72549105935 scopus 로고    scopus 로고
    • Effect of tarenflurbil on cognitive decline and activities of daily living in patients with mild Alzheimer disease: A randomized controlled trial
    • 2-s2.0-72549105935 10.1001/jama.2009.1866
    • Green R. C., Schneider L. S., Amato D. A., Beelen A. P., Wilcock G., Swabb E. A., Zavitz K. H., Effect of tarenflurbil on cognitive decline and activities of daily living in patients with mild Alzheimer disease: a randomized controlled trial. Journal of the American Medical Association 2009 302 23 2557 2564 2-s2.0-72549105935 10.1001/jama.2009.1866
    • (2009) Journal of the American Medical Association , vol.302 , Issue.23 , pp. 2557-2564
    • Green, R.C.1    Schneider, L.S.2    Amato, D.A.3    Beelen, A.P.4    Wilcock, G.5    Swabb, E.A.6    Zavitz, K.H.7
  • 37
    • 34648813134 scopus 로고    scopus 로고
    • High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery
    • DOI 10.1021/jm070375w
    • Wan H., Rehngren M., Giordanetto F., Bergström F., Tunek A., High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. Journal of Medicinal Chemistry 2007 50 19 4606 4615 2-s2.0-34648813134 10.1021/jm070375w (Pubitemid 47463235)
    • (2007) Journal of Medicinal Chemistry , vol.50 , Issue.19 , pp. 4606-4615
    • Wan, H.1    Rehngren, M.2    Giordanetto, F.3    Bergstrom, F.4    Tunek, A.5
  • 38
    • 80052266213 scopus 로고    scopus 로고
    • The amyloid cascade hypothesis for Alzheimer's disease: An appraisal for the development of therapeutics
    • 10.1038/nrd3505
    • Karran E., Mercken M., Strooper B. D., The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics. Nature Reviews Drug Discovery 2011 10 9 698 712 10.1038/nrd3505
    • (2011) Nature Reviews Drug Discovery , vol.10 , Issue.9 , pp. 698-712
    • Karran, E.1    Mercken, M.2    Strooper, B.D.3
  • 39
    • 84861512510 scopus 로고    scopus 로고
    • Small-molecule BACE1 inhibitors: A patent literature review (2006 - 2011)
    • 10.1517/13543776.2012.681302
    • Probst G., Xu Y.-Z., Small-molecule BACE1 inhibitors: a patent literature review (2006-2011). Expert Opinion on Therapeutic Patents 2012 22 5 511 540 10.1517/13543776.2012.681302
    • (2012) Expert Opinion on Therapeutic Patents , vol.22 , Issue.5 , pp. 511-540
    • Probst, G.1    Xu, Y.-Z.2
  • 41
    • 84855420378 scopus 로고    scopus 로고
    • Presenilin is the molecular target of acidic γ -secretase modulators in living cells
    • e30484 10.1371/journal.pone.0030484
    • Jumpertz T., Rennhack A., Ness J., Baches S., Pietrzik C. U., Bulic B., Weggen S., Presenilin is the molecular target of acidic γ -secretase modulators in living cells. PLoS ONE 2012 7 1 e30484 10.1371/journal.pone. 0030484
    • (2012) PLoS ONE , vol.7 , Issue.1
    • Jumpertz, T.1    Rennhack, A.2    Ness, J.3    Baches, S.4    Pietrzik, C.U.5    Bulic, B.6    Weggen, S.7
  • 46
    • 78049374467 scopus 로고    scopus 로고
    • Novel research horizons for presenilins and γ -secretases in cell biology and disease
    • 2-s2.0-78049374467 10.1146/annurev-cellbio-100109-104117
    • De Strooper B., Annaert W., Novel research horizons for presenilins and γ -secretases in cell biology and disease. Annual Review of Cell and Developmental Biology 2010 26 235 260 2-s2.0-78049374467 10.1146/annurev- cellbio-100109-104117
    • (2010) Annual Review of Cell and Developmental Biology , vol.26 , pp. 235-260
    • De Strooper, B.1    Annaert, W.2


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