CRAF (RAF1)
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
Activated by RAS-GTP at the membrane and by dimerisation; it also has kinase-independent roles in blocking apoptosis.
- 3 · How drugs use it
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.
External identifiers
Biology
Activated by RAS-GTP at the membrane and by dimerisation; it also has kinase-independent roles in blocking apoptosis.
- All tissues
- Drives MAPK signalling in RAS-mutant tumours and in resistance to BRAF inhibitors
Latest papers
topQuery 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.
Similar pages
not linked directly; found by shared links- TargetTIE2 receptor (TEK)
Shares Regorafenib, Renal cell carcinoma, Hepatocellular carcinoma, Colorectal cancer.
- TrialRESORCE
Shares Regorafenib, Hepatocellular carcinoma.
- TrialSARAH and SIRveNIB
Shares Sorafenib, Hepatocellular carcinoma.
- TrialSHARP
Shares Sorafenib, Hepatocellular carcinoma.
- CompanyQuantum Surgical
Shares Renal cell carcinoma, Hepatocellular carcinoma, Colorectal cancer.
- TreatmentGC101 TIL
- Key paperCalle 2003: overweight, obesity and death from cancer in 900,000 US adults
Shares Renal cell carcinoma, Hepatocellular carcinoma, Colorectal cancer.
- TargetAXL