Therapeutic Targets Database
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TTD Target ID: TTDC00182

Target Information
NameProtein kinase C, alpha type    
Type of targetClinical trial target    
SynonymsPKC-A    
PKC-alpha    
PKCalpha    
Protein Kinase C alpha    
DiseaseLeukemia, unspecified    [1]
Prostate cancer    [2]
Drug(s)Sotrastaurin acetatePhase IIhttp://clinicaltrials.gov/ct2/show/NCT01064791?term=Sotrastaurin&rank=1[3]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.37
PathwayCalcium signaling pathway
ErbB signaling pathway
Fc epsilon RI signaling pathway
Focal adhesion
Gap junction
Glioma
GnRH signaling pathway
Leukocyte transendothelial migration
Long-term depression
Long-term potentiation
MAPK signaling pathway
Melanogenesis
Natural killer cell mediated cytotoxicity
Non-small cell lung cancer
Pathogenic Escherichia coli infection
Pathogenic Escherichia coli infection
Pathways in cancer
Phosphatidylinositol signaling system
Tight junction
VEGF signaling pathway
Vascular smooth muscle contraction
Vibrio cholerae infection
Wnt signaling pathway
UniProt IDP17252
PDB Structure2ELI.    
FunctionThis is a calcium-activated, 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.    
SequenceMADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGF GKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGS LLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDA KNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRL SVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNME LRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKG TEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYV NGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIA DFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDG EDEDELFQSIMEHNVSYPKSLSKEAVSICKGLMTKHPAKRLGCGPEGERDVREHAFFRRI DWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVN PQFVHPILQSAV
Target ValidationClick to Find Target Validation Information.    
Inhibitor (-)-Cercosporamide[4]
1,2-dioctanoyl-sn-glycerol[5]
2,3,3-Triphenyl-acrylonitrile[6]
2- (4-Hydroxy-phenyl)-3,3-diphenyl-acrylonitrile[6]
3,3-Bis- (4-hydroxy-phenyl)-2-phenyl-acrylonitrile[6]
3,3-Bis- (4-methoxy-phenyl)-2-phenyl-acrylonitrile[6]
3,4-di- (4-methoxyphenyl)-1H-pyrrole-2,5-dione[7]
3,4-diphenyl-1H-pyrrole-2,5-dione[7]
3- (1H-Indol-3-yl)-4-phenylamino-pyrrole-2,5-dione[8]
3- (4-Hydroxy-phenyl)-2,3-diphenyl-acrylonitrile[6]
3- (4-Hydroxy-phenyl)-2,3-diphenyl-acrylonitrile[6]
3- (4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione[7]
3- (indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione[7]
4,5,6,7-tetrabromobenzotriazole[9]
4-[1- (4-hydroxyphenyl)-3-methyl-1-butenyl]phenol[6]
4-cycloheptyliden (4-hydroxyphenyl)methylphenol[6]
4-cyclohexyliden (4-hydroxyphenyl)methylphenol[6]
4-cyclopentyliden (4-hydroxyphenyl)methylphenol[6]
ACETOSIDE[10]
BALANOL[11]
BISINDOLYLMALEIMIDE IX[12]
CALCEOLARIOSIDE A[10]
CALCEOLARIOSIDE B[10]
CI-1040,   PD-18435,   PD-184352[12]
Dequalinium Analogue[13]
Dequalinium Analogue[13]
Dequalinium Analogue[13]
Dequalinium Analogue[13]
FORSYTHIASIDE[10]
Indolocarbazole analogue[14]
Indolocarbazole analogue[14]
Indolocarbazole analogue[14]
Indolocarbazole analogue[14]
Indolocarbazole analogue[14]
Indolocarbazole analogue[14]
Indolocarbazole analogue[14]
KN-62[12]
KT-5720[12]
LEUCOSCEPTOSIDE A[10]
LY-294002[12]
LY-317644[15]
LY-326449[16]
PD-98059[12]
PROSTRATIN[17]
PUNICAFOLIN[18]
Plantainoside D[10]
RO-316233[19]
RO-320432[20]
Ro-32-0557[20]
SB-202190[12]
SB-203580[12]
STAUROSPORINONE[12]
Sotrastaurin acetate[3]
TANNIN[18]
TANNIN[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
TANNIN analogue[18]
U-0126[12]
[2,2',   5',2'']Terthiophen-4-yl-methanol[21]
[2,2',   5',2'']Terthiophene-4,5''-dicarbaldehyde[21]
[2,2',   5',2'']Terthiophene-4-carbaldehyde[21]
diheptan-3-yl 5- (hydroxymethyl)isophthalate[5]
dihexan-3-yl 5- (hydroxymethyl)isophthalate[5]
MultitargetSotrastaurin acetate[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1A functional role for mitochondrial protein kinase Calpha in Bcl2 phosphorylation and suppression of apoptosis. J Biol Chem. 1998 Sep 25;273(39):25436-42. To Reference
Ref 2Protein kinase C-alpha: a novel target for the therapy of androgen-independent prostate cancer? (Review-hypothesis). Oncol Rep. 1998 Mar-Apr;5(2):305-9. To Reference
Ref 3Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63. To Reference
Ref 4Bioorg Med Chem Lett. 2009 Feb 1;19(3):724-6. Epub 2008 Dec 11.(-)-Cercosporamide derivatives as novel antihyperglycemic agents. To Reference
Ref 5J Med Chem. 2009 Jul 9;52(13):3969-81.Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C. To Reference
Ref 6J 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 7J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. To Reference
Ref 8Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4.Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. To Reference
Ref 9J Med Chem. 2004 Dec 2;47(25):6239-47.Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. To Reference
Ref 10J Nat Prod. 1998 Nov;61(11):1410-2.Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity. To Reference
Ref 11Bioorg. Med. Chem. Lett. 5(18):2155-2160 (1995) To Reference
Ref 12Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors. To Reference
Ref 13J Med Chem. 2000 Apr 6;43(7):1413-7.Inhibition of protein kinase C(alpha) by dequalinium analogues: dependence on linker length and geometry. To Reference
Ref 14Bioorg Med Chem Lett. 2002 Jan 21;12(2):147-50.Mixed lineage kinase activity of indolocarbazole analogues. To Reference
Ref 15Bioorg. Med. Chem. Lett. 5(18):2093-2096 (1995) To Reference
Ref 16J 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 17J 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 18Bioorg. Med. Chem. Lett. 2(3):239-244 (1992) To Reference
Ref 19J Med Chem. 1992 Jan;35(1):177-84.Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. To Reference
Ref 20Bioorg. Med. Chem. Lett. 4(11):1303-1308 (1994) To Reference
Ref 21Bioorg 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



 

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