Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00346

Target Information
NameB-Raf proto-oncogene serine/threonine-protein kinase    
Type of targetSuccessful target    
SynonymsB-Raf    
B-raf protein    
BRAF    
BRAF serine/threonine kinase    
BRAF(V599E)    
P94    
V-Raf murine sarcoma viral oncogene homolog B1    
DiseaseMalignant melanoma
[ICD9: 172   ICD10: C43]
[1]
Melanoma
[ICD9: 172   ICD10: C43]
[2]
Pancreatic cancer
[ICD9: 157   ICD10: C25]
[3]
Drug(s)VemurafenibApprovedBRAF-positive unresectable or metastatic melanoma
SorafenibLaunchedAdvanced renal cell carcinoma[4][5][6]
R7204Phase IIIMalignant melanoma[7]
RG7204Phase IIIAdjuvant metastatic melanoma, BRAF mutation positive
RG7421+RG7204Phase IIIMetastatic melanoma BRAF mutation positive
SorafenibPhase IIIHepatocellular carcinoma, NSCLC, melanoma[4][5][6]
Trametinib + dabrafenibPhase IIIMetastatic melanoma, adjuvant therapy
VemurafenibPhase IIIAdjuvant metastatic melanoma, BRAF mutation positive
DabrafenibPhase IINon-small cell lung cancer
PLX4032Phase IIThroid cancer
RG7204Phase IIPapillary thyroid cancer, BRAF mutation positive
SorafenibPhase IIMyelodyspalstic syndrome, AML, head & neck cancer, breast, colon, ovarian, pancreatic cancer[4][5][6]
Trametinib + dabrafenibPhase IIColorectal cancer
VemurafenibPhase IIPapillary thyroid cancer, BRAF mutation positive
GSK2118436Phase I/IIMetastatic melanoma, solid tumors[8]
ARQ 736Phase ILate-stage solid tumors
BMS-908662Phase ICancers[9]
DabrafenibSubmittedMetastatic melanoma
RG7204FiledMetastatic melanoma, BRAF mutation positive
RG7204Phase IMetastatic melanoma, BRAF mutation positive
RG7256Phase IMalignant melanoma
Trametinib + dabrafenibSubmittedMetastatic melanoma
VemurafenibPhase IMetastatic melanoma, BRAF mutation positive
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.37
PathwayAcute myeloid leukemia
Bladder cancer
Chemokine signaling pathway
Chronic myeloid leukemia
Colorectal cancer
Endometrial cancer
ErbB signaling pathway
Focal adhesion
Glioma
Insulin signaling pathway
Long-term depression
Long-term potentiation
MAPK signaling pathway
Melanoma
Natural killer cell mediated cytotoxicity
Non-small cell lung cancer
Pancreatic cancer
Pathways in cancer
Prostate cancer
Regulation of actin cytoskeleton
Renal cell carcinoma
Thyroid cancer
Vascular smooth muscle contraction
mTOR signaling pathway
UniProt IDP15056
PDB Structure1UWH; 1UWJ; 2FB8; 2L05; 3C4C; 3D4Q; 3IDP; 3II5; 3NY5; 3OG7; 3PPJ; 3PPK; 3PRF; 3PRI; 3PSB; 3PSD; 3Q4C; 3Q96; 3SKC; 3TV4; 3TV6; 4DBN; 4E26; 4E4X; 4EHE; 4EHG; 4FK3; 4G9C; 4G9R; 4H58; 4JVG.    
FunctionInvolved in the transduction of mitogenic signals from the cell membrane to the nucleus. May play a role in the postsynaptic responses of hippocampal neuron.    
SequenceMAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEH IEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTV TSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDS LKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRK TFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPI PQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQR DRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSP GPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDV AVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHH LHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATV KSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNIN NRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARS LPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH
Target ValidationClick to Find Target Validation Information.    
InhibitorBMS-908662[9]
GSK2118436[8]
R7204[7]
Sorafenib[4][5][6]
MultitargetSorafenib[4][5][6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Raf proteins and cancer: B-Raf is identified as a mutational target. Biochim Biophys Acta. 2003 Jun 5;1653(1):25-40. To Reference
Ref 2Suppression of BRAF(V599E) in human melanoma abrogates transformation. Cancer Res. 2003 Sep 1;63(17):5198-202. To Reference
Ref 3BRAF and FBXW7 (CDC4, FBW7, AGO, SEL10) mutations in distinct subsets of pancreatic cancer: potential therapeutic targets. Am J Pathol. 2003 Oct;163(4):1255-60. To Reference
Ref 4A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference
Ref 5Pituitary tumors. Curr Treat Options Neurol. 2009 Jul;11(4):287-96. To Reference
Ref 6Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28. To Reference
Ref 7Roche. Product Development Pipeline. July 29 2009. To Reference
Ref 82011 Pipeline of GlaxoSmithKline. To Reference
Ref 92011 Pipeline of Exelixis. To Reference



 

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