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CRAF is BRAF's sibling in the growth-signal relay; sorafenib and regorafenib were designed against it, and it is the route by which RAS-mutant tumours escape BRAF-only drugs.
RAF1 (CRAF) is one of three RAF kinases that pass the signal from RAS to MEK. Sorafenib was originally developed as a CRAF inhibitor before its VEGF receptor activity explained its clinical effect, and regorafenib shares that profile. CRAF matters clinically because RAS-mutant and BRAF-inhibitor-treated tumours signal through CRAF dimers, the basis for pan-RAF inhibitors now in trials.
In plain words · CRAF is BRAF's sibling in the growth-signal relay; sorafenib and regorafenib were designed against it, and it is the route by which RAS-mutant tumours escape BRAF-only drugs.
CRAF is BRAF's sibling in the growth-signal relay; sorafenib and regorafenib were designed against it, and it is the route by which RAS-mutant tumours escape BRAF-only drugs.
Activated by RAS-GTP at the membrane and by dimerisation; it also has kinase-independent roles in blocking apoptosis.
No product in this corpus aims at CRAF (RAF1) yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Lineage antigen shared with normal granulocytes: HPA finds the gene lineage enriched in that blood lineage, and the 2 medicines aimed at it (Sorafenib, Regorafenib) act on the wild-type protein, so the normal lineage is hit too. HPA RAF1: RNA tissue enhanced (skeletal muscle 163 nTPM); blood lineage lineage enriched (granulocytes 150 nTPM); high antibody staining in 3 normal tissues; highest cancer staining colorectal cancer (1 of 11 high). Distribution: 3 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Hepatocellular carcinoma, Renal cell carcinoma, Colorectal cancer); Open Targets associates it with 4 specific cancer types at or above 0.5 (hepatocellular carcinoma, renal cell carcinoma, colorectal cancer, low grade glioma). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas RAF1 tissue; Human Protein Atlas RAF1 pathology; Open Targets ENSG00000132155 associations
First described 1985. Earliest sequence paper UniProt cites for the protein: Bonner T.I. et al, Mol. Cell. Biol, 1985, "Structure and biological activity of human homologs of the raf/mil oncogene". Source.
Activated by RAS-GTP at the membrane and by dimerisation; it also has kinase-independent roles in blocking apoptosis.
RNA: tissue enhanced (skeletal muscle 163 nTPM), detected in all normal tissues. Blood: lineage enriched (granulocytes 150 nTPM).
Medium: Breast, Colon, Epididymis, Fallopian tube, Gallbladder, Lung, Lymph node, Nasopharynx.
Medium only: breast cancer, cervical cancer, glioma, head and neck cancer.
HPA RAF1 tissue · HPA RAF1 pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Metastatic cancer | all% | Signalling protein present in most cells (CRAF in the RAS-MAPK relay); drugs act on the pathway rather than on a mutation that selects patients, so no prevalence applies. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Query for this target: (TITLE:"CRAF" OR ABSTRACT:"CRAF" OR TITLE:"RAF1" OR ABSTRACT:"RAF1") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about CRAF (RAF1), not a curated reading list.
Shares Regorafenib, Renal cell carcinoma, Hepatocellular carcinoma, Colorectal cancer.
Shares Sorafenib, Hepatocellular carcinoma.
Shares Regorafenib, Hepatocellular carcinoma.
Shares MEK1/2, Regorafenib, Colorectal cancer.
Shares Sorafenib, Hepatocellular carcinoma.
Shares Regorafenib, BRAF, Colorectal cancer.
Shares Regorafenib, Colorectal cancer.
Shares Regorafenib, Colorectal cancer.