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DrugBank target: P15056

DrugBank target: P15056 (BRAF_HUMAN)     

Example drug-target structure: 1uwh

( There are 41 structures corresponding to this UniProt sequence in the PDB. Click the orange, plus icon above for a list. )

Serine/threonine-protein kinase B-raf

Proto-oncogene B-Raf, p94, v-Raf murine sarcoma viral oncogene homolog B1.

Function

Protein kinase involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May play a role in the postsynaptic responses of hippocampal neuron. Phosphorylates MAP2K1, and thereby contributes to the MAP kinase signal transduction pathway..

Enzyme

2.7.11.1   [EC->PDB]   [IntEnz]   [ExPASy]   [KEGG]  

Catalytic activity

ATP + a protein = ADP + a phosphoprotein.

Disease(s)

Note=Defects in BRAF are found in a wide range of cancers.
Colorectal cancer (CRC) [MIM:114500]: A complex disease characterized by malignant lesions arising from the inner wall of the large intestine (the colon) and the rectum. Genetic alterations are often associated with progression from premalignant lesion (adenoma) to invasive adenocarcinoma. Risk factors for cancer of the colon and rectum include colon polyps, long-standing ulcerative colitis, and genetic family history. Note=The disease may be caused by mutations affecting the gene represented in this entry.
Lung cancer (LNCR) [MIM:211980]: A common malignancy affecting tissues of the lung. The most common form of lung cancer is non-small cell lung cancer (NSCLC) that can be divided into 3 major histologic subtypes: squamous cell carcinoma, adenocarcinoma, and large cell lung cancer. NSCLC is often diagnosed at an advanced stage and has a poor prognosis. Note=The gene represented in this entry is involved in disease pathogenesis.
Familial non-Hodgkin lymphoma (NHL) [MIM:605027]: Cancer that starts in cells of the lymph system, which is part of the body's immune system. NHLs can occur at any age and are often marked by enlarged lymph nodes, fever and weight loss. Note=The gene represented in this entry is involved in disease pathogenesis.
Cardiofaciocutaneous syndrome 1 (CFC1) [MIM:115150]: A multiple congenital anomaly disorder characterized by a distinctive facial appearance, heart defects and mental retardation. Heart defects include pulmonic stenosis, atrial septal defects and hypertrophic cardiomyopathy. Some affected individuals present with ectodermal abnormalities such as sparse, friable hair, hyperkeratotic skin lesions and a generalized ichthyosis-like condition. Typical facial features are similar to Noonan syndrome. They include high forehead with bitemporal constriction, hypoplastic supraorbital ridges, downslanting palpebral fissures, a depressed nasal bridge, and posteriorly angulated ears with prominent helices. Note=The disease is caused by mutations affecting the gene represented in this entry.
Noonan syndrome 7 (NS7) [MIM:613706]: A form of Noonan syndrome, a disease characterized by short stature, facial dysmorphic features such as hypertelorism, a downward eyeslant and low-set posteriorly rotated ears, and a high incidence of congenital heart defects and hypertrophic cardiomyopathy. Other features can include a short neck with webbing or redundancy of skin, deafness, motor delay, variable intellectual deficits, multiple skeletal defects, cryptorchidism, and bleeding diathesis. Individuals with Noonan syndrome are at risk of juvenile myelomonocytic leukemia, a myeloproliferative disorder characterized by excessive production of myelomonocytic cells. Note=The disease is caused by mutations affecting the gene represented in this entry.
LEOPARD syndrome 3 (LEOPARD3) [MIM:613707]: A disorder characterized by lentigines, electrocardiographic conduction abnormalities, ocular hypertelorism, pulmonic stenosis, abnormalities of genitalia, retardation of growth, and sensorineural deafness. Note=The disease is caused by mutations affecting the gene represented in this entry.
Note=A chromosomal aberration involving BRAF is found in pilocytic astrocytomas. A tandem duplication of 2 Mb at 7q34 leads to the expression of a KIAA1549-BRAF fusion protein with a constitutive kinase activity and inducing cell transformation.

Schematic diagram of Pfam domains in target sequence plus wiring diagram of PDB structure containing drug molecule

1uwh

Key:    PfamA domain  Secondary structure  Bound drug molecule

Sequence length: 765 a.a.

Approved drugs targeting this protein

The DrugBank database identifies 4 drugs for this target protein:

 

 
Generic name: DB08881 vemurafenib
Formula: C23H18Clf2N3O3S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB08896 regorafenib
Formula: C21H15Clf4N4O3
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB08912 dabrafenib
Formula: C23H20F3N5O2S2
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00398 sorafenib
BAX
Formula: C21H16Clf3N4O3
Structure: There are 6 PDB structures containing this molecule of which 2 are bound to the above target protein.

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