Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00077

Target Information
NameProtein kinase C, delta type    
Type of targetClinical trial target    
SynonymsNPKC-delta    
Protein Kinase C delta    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Head and neck squamous cell carcinomas
[ICD9: 199   ICD10: C44]
[2]
Melanoma metastasis
[ICD9: 172   ICD10: C43]
[3]
Reperfusion Injury associated with Heart Attacks, or Acute Myocardial Infarction (AMI)[4][5][6]
Drug(s)KAI-9803Phase I/IIReperfusion Injury and Heart Attacks, Acute Myocardial Infarction[4][5][6]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.-
EC 3.4.21.22
PathwayChemokine signaling pathway
Fc epsilon RI signaling pathway
GnRH signaling pathway
Tight junction
Type II diabetes mellitus
Vascular smooth muscle contraction
UniProt IDQ05655
PDB Structure1YRK; 2YUU.    
FunctionThis is calcium-independent, phospholipid-dependent, serine- and threonine-specific enzyme. Pkc is activated by diacylglycerol which in turn phosphorylates a range of cellular proteins. Pkc also serves as the receptor for phorbol esters.    
SequenceMAPFLRIAFNSYELGSLQAEDEANQPFCAVKMKEALSTERGKTLVQKKPTMYPEWKSTFD AHIYEGRVIQIVLMRAAEEPVSEVTVGVSVLAERCKKNNGKAEFWLDLQPQAKVLMSVQY FLEDVDCKQSMRSEDEAKFPTMNRRGAIKQAKIHYIKNHEFIATFFGQPTFCSVCKDFVW GLNKQGYKCRQCNAAIHKKCIDKIIGRCTGTAANSRDTIFQKERFNIDMPHRFKVHNYMS PTFCDHCGSLLWGLVKQGLKCEDCGMNVHHKCREKVANLCGINQKLLAEALNQVTQRASR RSDSASSEPVGIYQGFEKKTGVAGEDMQDNSGTYGKIWEGSSKCNINNFIFHKVLGKGSF GKVLLGELKGRGEYFAIKALKKDVVLIDDDVECTMVEKRVLTLAAENPFLTHLICTFQTK DHLFFVMEFLNGGDLMYHIQDKGRFELYRATFYAAEIMCGLQFLHSKGIIYRDLKLDNVL LDRDGHIKIADFGMCKENIFGESRASTFCGTPDYIAPEILQGLKYTFSVDWWSFGVLLYE MLIGQSPFHGDDEDELFESIRVDTPHYPRWITKESKDILEKLFEREPTKRLGVTGNIKIH PFFKTINWTLLEKRRLEPPFRPKVKSPRDYSNFDQEFLNEKARLSYSDKNLIDSMDQSAF AGFSFVNPKFEHLLED
Target ValidationClick to Find Target Validation Information.    
Inhibitor13-Acetylphorbol[7]
2,3,3-Triphenyl-acrylonitrile[8]
2- (4-Hydroxy-phenyl)-3,3-diphenyl-acrylonitrile[8]
3,3-Bis- (4-hydroxy-phenyl)-2-phenyl-acrylonitrile[8]
3,3-Bis- (4-methoxy-phenyl)-2-phenyl-acrylonitrile[8]
3- (4-Hydroxy-phenyl)-2,3-diphenyl-acrylonitrile[8]
3- (4-Hydroxy-phenyl)-2,3-diphenyl-acrylonitrile[8]
4-HYDROXYTAMOXIFEN[8]
4-[1- (4-hydroxyphenyl)-3-methyl-1-butenyl]phenol[8]
4-cycloheptyliden (4-hydroxyphenyl)methylphenol[8]
4-cyclohexyliden (4-hydroxyphenyl)methylphenol[8]
INDOLACTUM[9]
Indolocarbazole analogue[10]
Indolocarbazole analogue[10]
Indolocarbazole analogue[10]
Indolocarbazole analogue[10]
Indolocarbazole analogue[10]
Indolocarbazole analogue[10]
Indolocarbazole analogue[10]
Ingenol-3-bezoate[11]
KAI-9803[4][5][6]
LY-317644[12]
LY-326449[13]
PROSTRATIN[14]
RO-316233[15]
RO-320432[16]
Ro-32-0557[16]
THYMELEATOXIN[11]
[2,2',   5',2'']Terthiophen-4-yl-methanol[17]
[2,2',   5',2'']Terthiophene-4,5''-dicarbaldehyde[17]
[2,2',   5',2'']Terthiophene-4-carbaldehyde[17]
phorbol 12,13-butyrate[18]
ActivatorAD 198[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Novel extranuclear-targeted anthracyclines override the antiapoptotic functions of Bcl-2 and target protein kinase C pathways to induce apoptosis. Mol Cancer Ther. 2002 May;1(7):469-81. To Reference
Ref 2Antitumor activity of UCN-01 in carcinomas of the head and neck is associated with altered expression of cyclin D3 and p27(KIP1). Clin Cancer Res. 2002 Nov;8(11):3549-60. To Reference
Ref 3nPKCdelta a new therapeutic marker for melanoma metastasis? (Review). Int J Mol Med. 2000 May;5(5):467-71. To Reference
Ref 4PKC delta and epsilon in drug targeting and therapeutics. Recent Pat DNA Gene Seq. 2009;3(2):96-101. To Reference
Ref 5Letter by Metzler et al regarding article, "Intracoronary KAI-9803 as an adjunct to primary coronary intervention for acute ST-segment elevation myocardial infarction". Circulation. 2008 Jul 22;118(4):e80. To Reference
Ref 6Circulation. 2008 Feb 19;117(7):886-96. Epub 2008 Feb 4.Intracoronary KAI-9803 as an adjunct to primary percutaneous coronary intervention for acute ST-segment elevation myocardial infarction. To Reference
Ref 7Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 8J Med Chem. 1992 Feb 7;35(3):573-83.Multivariate analysis by the minimum spanning tree method of the structural determinants of diphenylethylenes and triphenylacrylonitriles implicated in estrogen receptor binding, protein kinase C activity, and MCF7 cell proliferation. To Reference
Ref 9J Med Chem. 2002 Feb 14;45(4):853-60.Structural basis of RasGRP binding to high-affinity PKC ligands. To Reference
Ref 10Bioorg Med Chem Lett. 2002 Jan 21;12(2):147-50.Mixed lineage kinase activity of indolocarbazole analogues. To Reference
Ref 11J Med Chem. 2001 May 24;44(11):1690-701.Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. To Reference
Ref 12Bioorg. Med. Chem. Lett. 5(18):2093-2096 (1995) To Reference
Ref 13J Med Chem. 1996 Jul 5;39(14):2664-71.(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. To Reference
Ref 14J Med Chem. 1992 May 29;35(11):1978-86.A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1. To Reference
Ref 15J Med Chem. 1992 Jan;35(1):177-84.Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. To Reference
Ref 16Bioorg. Med. Chem. Lett. 4(11):1303-1308 (1994) To Reference
Ref 17Bioorg Med Chem Lett. 1999 Aug 2;9(15):2279-82.Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives. To Reference
Ref 18J Med Chem. 2007 Jul 26;50(15):3465-81. Epub 2007 Jun 26.Conformationally constrained analogues of diacylglycerol (DAG). 28. DAG-dioxolanones reveal a new additional interaction site in the C1b domain of PKC delta. To Reference



 

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