Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00434

Target Information
NameInterleukin-1 beta convertase    
Type of targetResearch target    
SynonymsCASP-1    
Caspase-1    
ICE    
IL-1 beta converting enzyme    
IL-1BC    
Interleukin-1 beta converting enzyme    
P45    
DiseaseBrain inflammation[1]
Cerebral ischemia
[ICD9: 459.89   ICD10: I99.8]
[2]
Diabetic retinopathy
[ICD9: 250.5   ICD10: H36, E10.3, E11.3, E13.3]
[3]
Inflammation[4]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.22.36
PathwayAmyotrophic lateral sclerosis (ALS)
UniProt IDP29466
PDB Structure1BMQ; 1IBC; 1ICE; 1RWK; 1RWM; 1RWN; 1RWO; 1RWP.    
FunctionThiol protease that cleaves il-1 beta between an asp and an ala, releasing the mature cytokine which is involved in a variety of inflammatory processes. Specifically inhibited by the cowpox virus crma protein.    
SequenceMADKVLKEKRKLFIRSMGEGTINGLLDELLQTRVLNKEEMEKVKRENATVMDKTRALIDS VIPKGAQACQICITYICEEDSYLAGTLGLSADQTSGNYLNMQDSQGVLSSFPAPQAVQDN PAMPTSSGSEGNVKLCSLEEAQRIWKQKSAEIYPIMDKSSRTRLALIICNEEFDSIPRRT GAEVDITGMTMLLQNLGYSVDVKKNLTASDMTTELEAFAHRPEHKTSDSTFLVFMSHGIR EGICGKKHSEQVPDILQLNAIFNMLNTKNCPSLKDKPKVIIIQACRGDSPGVVWFKDSVG VSGNLSLPTTEEFEDDAIKKAHIEKDFIAFCSSTPDNVSWRHPTMGSVFIGRLIEHMQEY ACSCDVEEIFRKVRFSFEQPDGRAQMPTTERVTLTRCFYLFPGH
Related US Patent6,407,080
6,423,840
6,426,413
6,528,506
6,531,467
6,531,474
6,573,259
6,610,683
Target ValidationClick to Find Target Validation Information.    
InhibitorL-709049[5]
PRALNACASAN[6]
YVAD[1]
Z-VAD-CHO[7]
Z-YVAD-CHO[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Mice deficient in interleukin-1beta converting enzyme resist anorexia induced by central lipopolysaccharide. Am J Physiol. 1999 Nov;277(5 Pt 2):R1435-43. To Reference
Ref 2Attenuation of transient focal cerebral ischemic injury in transgenic mice expressing a mutant ICE inhibitory protein. J Cereb Blood Flow Metab. 1997 Apr;17(4):370-5. To Reference
Ref 3Potential new strategies to prevent the development of diabetic retinopathy. Expert Opin Investig Drugs. 2004 Mar;13(3):189-98. To Reference
Ref 4A novel heterodimeric cysteine protease is required for interleukin-1 beta processing in monocytes. Nature. 1992 Apr 30;356(6372):768-74. To Reference
Ref 5Bioorg Med Chem Lett. 2010 Sep 1;20(17):5184-90. Epub 2010 Jul 8.Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). To Reference
Ref 6Bioorg Med Chem Lett. 2006 Sep 15;16(18):4728-32. Epub 2006 Jul 25.Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors. To Reference
Ref 7Bioorg Med Chem Lett. 2006 Feb;16(3):559-62. Epub 2005 Nov 4.Tethering identifies fragment that yields potent inhibitors of human caspase-1. To Reference



 

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