Title:
カスパーゼ-2阻害剤およびそれらの生物学的適用
Document Type and Number:
Japanese Patent JP5053836
Kind Code:
B2
Abstract:
The invention relates to selective new caspase-2 inhibitors that recognize caspase-2 and prevent and block its activity based on the following backbone: 2-Quinolinylcarbonyl-L-Valinyl-L-Aspartyl (methyl ester)-L-Valinyl-L-Alanyl-L-Aspartyl (methyl ester) 2,6-difluorophenyl ester SEQ ID NO:1) and derivatives thereof, SEQ ID NO:1 corresponding to formulae Ia or Ib. Application of the inhibitors for preventing and treating diseases involving caspase-2.
Inventors:
Schovie david
Kazimir Richard
Jacoto Etienne
Lubira Dominique
Kazimir Richard
Jacoto Etienne
Lubira Dominique
Application Number:
JP2007509996A
Publication Date:
October 24, 2012
Filing Date:
May 02, 2005
Export Citation:
Assignee:
Theraposis S
International Classes:
A61K38/00; A61P9/10; A61P25/00; A61P43/00; C07K7/00; C07K14/47; C07K14/81
Domestic Patent References:
| JP2004512287A | ||||
| JP61502335A | ||||
| JP9501913A |
Foreign References:
| WO2005080353A1 | ||||
| WO2003047576A1 |
Other References:
JIN,K. et al,Two caspase-2 transcripts are expressed in rat hippocampus after global cerebral ischemia,J Neurochem,2002年,Vol.81, No.1,p.25-35
HENSHALL,D.C. et al,Caspase-2 activation is redundant during seizure-induced neuronal death,J Neurochem,2001年,Vol.77, No.3,p.886-95
KASOF,G.M. et al,The RIP-like kinase, RIP3, induces apoptosis and NF-kappaB nuclear translocation and localizes to mitochondria,FEBS Lett,2000年,Vol.473, No.3,p.285-91
KANAZAWA,T. et al,Bcl-2 blocks apoptosis caused by pierisin-1, a guanine-specific ADP-ribosylating toxin from the cabbage butterfly,Biochem Biophys Res Commun,2002年,Vol.296, No.1,p.20-5
PERCHELLET,E.M. et al,Synthetic 1,4-anthracenedione analogs induce cytochrome c release, caspase-9, -3, and -8 activities, poly(ADP-ribose) polymerase-1 cleavage and internucleosomal DNA fragmentation in HL-60 cells by a mechanism which involves caspase-2 activation but not Fas signaling,Biochem Pharmacol,2004年,Vol.67, No.3,p.523-37
ITO,A. et al,Possible involvement of cytochrome c release and sequential activation of caspases in ceramide-induced apoptosis in SK-N-MC cells,Biochim Biophys Acta,1999年,Vol.1452, No.3,p.263-74
CERUTI,S. et al,A key role for caspase-2 and caspase-3 in the apoptosis induced by 2-chloro-2'-deoxy-adenosine (cladribine) and 2-chloro-adenosine in human astrocytoma cells,Mol Pharmacol,2003年,Vol.63, No.6,p.1437-47
MORIYA,R. et al,Mechanism of nitric oxide-induced apoptosis in human neuroblastoma SH-SY5Y cells,FEBS Lett,2000年,Vol.484, No.3,p.253-60
MASSIEU,L. et al,Effect of Ginkgo biloba (EGb 761) on staurosporine-induced neuronal death and caspase activity in cortical cultured neurons,Brain Res,2004年,Vol.1002, No.1-2,p.76-85
HENSHALL,D.C. et al,Caspase-2 activation is redundant during seizure-induced neuronal death,J Neurochem,2001年,Vol.77, No.3,p.886-95
KASOF,G.M. et al,The RIP-like kinase, RIP3, induces apoptosis and NF-kappaB nuclear translocation and localizes to mitochondria,FEBS Lett,2000年,Vol.473, No.3,p.285-91
KANAZAWA,T. et al,Bcl-2 blocks apoptosis caused by pierisin-1, a guanine-specific ADP-ribosylating toxin from the cabbage butterfly,Biochem Biophys Res Commun,2002年,Vol.296, No.1,p.20-5
PERCHELLET,E.M. et al,Synthetic 1,4-anthracenedione analogs induce cytochrome c release, caspase-9, -3, and -8 activities, poly(ADP-ribose) polymerase-1 cleavage and internucleosomal DNA fragmentation in HL-60 cells by a mechanism which involves caspase-2 activation but not Fas signaling,Biochem Pharmacol,2004年,Vol.67, No.3,p.523-37
ITO,A. et al,Possible involvement of cytochrome c release and sequential activation of caspases in ceramide-induced apoptosis in SK-N-MC cells,Biochim Biophys Acta,1999年,Vol.1452, No.3,p.263-74
CERUTI,S. et al,A key role for caspase-2 and caspase-3 in the apoptosis induced by 2-chloro-2'-deoxy-adenosine (cladribine) and 2-chloro-adenosine in human astrocytoma cells,Mol Pharmacol,2003年,Vol.63, No.6,p.1437-47
MORIYA,R. et al,Mechanism of nitric oxide-induced apoptosis in human neuroblastoma SH-SY5Y cells,FEBS Lett,2000年,Vol.484, No.3,p.253-60
MASSIEU,L. et al,Effect of Ginkgo biloba (EGb 761) on staurosporine-induced neuronal death and caspase activity in cortical cultured neurons,Brain Res,2004年,Vol.1002, No.1-2,p.76-85
Attorney, Agent or Firm:
Norihiko Hibi
Einosuke Kishimoto
Akira Watanabe
Kiyosue Yasuko
Einosuke Kishimoto
Akira Watanabe
Kiyosue Yasuko