Target Information

Target General Infomation
Target ID
T90648
Former ID
TTDR01373
Target Name
mRNA of B-Raf
Gene Name
BRAF
Synonyms
Proto-oncogene B-Raf (mRNA); Serine/threonine-protein kinase B-raf (mRNA); p94 (mRNA); v-Raf murine sarcoma viral oncogene homolog B1 (mRNA); BRAF
Target Type
Clinical Trial
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Parkinson's disease [ICD9: 332; ICD10: G20]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
BioChemical Class
Kinase
Target Validation
T90648
UniProt ID
P15056
EC Number
EC 2.7.11.1
Sequence
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEH
IEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTV
TSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDS
LKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRK
TFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPI
PQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQR
DRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSP
GPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDV
AVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHH
LHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATV
KSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNIN
NRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARS
LPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH
Drugs and Mode of Action
Drug(s) RG7304 Drug Info Phase 1 Solid tumours [548874]
SPN-803 Drug Info Phase 1 Parkinson's disease [548872]
Inhibitor 2-(Benzylamino)-6-(3-acetamidophenyl)pyrazine Drug Info [527954]
2-(Phenylamino)-6-(3-acetamidophenyl)pyrazine Drug Info [527954]
BIIB-024 Drug Info [543525]
compound 2 Drug Info [533265]
L-779450 Drug Info [527836]
PLX-4720 Drug Info [531679]
PLX-ORI3 Drug Info [543525]
Pyrazolo[1,5-a]pyrimidine-3-carboxylate Drug Info [530074]
RG7304 Drug Info [551608]
ZM-336372 Drug Info [529039]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway MAPK signaling pathway
ErbB signaling pathway
Rap1 signaling pathway
cAMP signaling pathway
Chemokine signaling pathway
FoxO signaling pathway
mTOR signaling pathway
Vascular smooth muscle contraction
Focal adhesion
Natural killer cell mediated cytotoxicity
Long-term potentiation
Neurotrophin signaling pathway
Serotonergic synapse
Long-term depression
Regulation of actin cytoskeleton
Insulin signaling pathway
Progesterone-mediated oocyte maturation
Alcoholism
Hepatitis C
Pathways in cancer
Proteoglycans in cancer
Colorectal cancer
Renal cell carcinoma
Pancreatic cancer
Endometrial cancer
Glioma
Prostate cancer
Thyroid cancer
Melanoma
Bladder cancer
Chronic myeloid leukemia
Acute myeloid leukemia
Non-small cell lung cancer
NetPath Pathway IL-7 Signaling Pathway
PANTHER Pathway Angiogenesis
Integrin signalling pathway
Interleukin signaling pathway
PDGF signaling pathway
T cell activation
VEGF signaling pathway
Ras Pathway
CCKR signaling map ST
Pathway Interaction Database CDC42 signaling events
mTOR signaling pathway
Ras signaling in the CD4+ TCR pathway
ErbB1 downstream signaling
PDGFR-beta signaling pathway
Signaling events mediated by VEGFR1 and VEGFR2
Trk receptor signaling mediated by the MAPK pathway
PathWhiz Pathway Intracellular Signalling Through Adenosine Receptor A2a and Adenosine
Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
Reactome Spry regulation of FGF signaling
Frs2-mediated activation
ARMS-mediated activation
CREB phosphorylation through the activation of Ras
RAF activation
MAP2K and MAPK activation
Negative feedback regulation of MAPK pathway
Negative regulation of MAPK pathway
WikiPathways Serotonin Receptor 4/6/7 and NR3C Signaling
Serotonin HTR1 Group and FOS Pathway
Senescence and Autophagy in Cancer
Regulation of Actin Cytoskeleton
EGF/EGFR Signaling Pathway
MAPK Cascade
MAPK Signaling Pathway
Bladder Cancer
Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
Polycystic Kidney Disease Pathway
Corticotropin-releasing hormone
B Cell Receptor Signaling Pathway
Signaling Pathways in Glioblastoma
Integrated Breast Cancer Pathway
Signaling by FGFR
NGF signalling via TRKA from the plasma membrane
Integrin-mediated Cell Adhesion
References
Ref 548872Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029757)
Ref 548874Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029782)
Ref 527836Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81. Epub 2005 Nov 2.The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.
Ref 527954J Med Chem. 2006 Jan 12;49(1):407-16.Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 530074Bioorg Med Chem Lett. 2009 May 15;19(10):2735-8. Epub 2009 Mar 28.Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.
Ref 531679Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51.
Ref 533265Photoactivatable Prodrugs of Antimelanoma Agent Vemurafenib. ACS Chem Biol. 2015 Sep 18;10(9):2099-107.
Ref 543525(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1943).
Ref 549611US patent application no. 5,981,731, Antisense oligonucleotide modulation of B-raf gene expression.
Ref 551608Clinical pipeline report, company report or official report of Roche.

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