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The first cancer gene ever identified, a kinase that relays growth, adhesion and movement signals. Dasatinib and bosutinib were designed as BCR::ABL1 drugs but also hit SRC-family kinases, part of the reason they work when imatinib has failed.
SRC, discovered through the Rous sarcoma virus, heads a family of non-receptor tyrosine kinases (SRC, LYN, LCK, HCK, FYN, YES1) that sit downstream of growth-factor receptors and integrins. Dasatinib and bosutinib inhibit both BCR::ABL1 and SRC-family kinases and are approved for chronic myeloid leukaemia and, for dasatinib, Philadelphia chromosome-positive acute lymphoblastic leukaemia; LYN signalling contributes to imatinib resistance, so the dual activity matters. Selective SRC inhibitors have not succeeded in solid tumours despite frequent SRC activation, a reminder that activation and dependency are not the same thing.
In plain words · The first cancer gene ever identified, a kinase that relays growth, adhesion and movement signals. Dasatinib and bosutinib were designed as BCR::ABL1 drugs but also hit SRC-family kinases, part of the reason they work when imatinib has failed.
The first cancer gene ever identified, a kinase that relays growth, adhesion and movement signals. Dasatinib and bosutinib were designed as BCR::ABL1 drugs but also hit SRC-family kinases, part of the reason they work when imatinib has failed.
Non-receptor tyrosine kinase family downstream of receptor tyrosine kinases and integrins; dual BCR::ABL1 and SRC-family inhibition by dasatinib and bosutinib.
No product in this corpus aims at SRC family kinases yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Broadly expressed or essential: HPA finds the RNA at low tissue specificity; the 2 medicines aimed at it (Dasatinib, Bosutinib) act on the wild-type protein, so normal tissue is exposed and the therapeutic window comes from the tumour's faster division or its dependence on the protein. HPA SRC: RNA low tissue specificity; blood lineage group enriched (dendritic cells 1 nTPM, monocytes 2 nTPM); high antibody staining in 10 normal tissues; highest cancer staining skin cancer (5 of 10 high). Distribution: 1 cancer family in the corpus carries a prevalence row, label threshold or catalogue link for it (Leukaemia); Open Targets associates it with 4 specific cancer types at or above 0.5 (chronic myeloid leukemia, actinic keratosis, acute lymphoblastic leukemia, medullary thyroid gland carcinoma); the corpus evidence decides and the Open Targets list is quoted for comparison. (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas SRC tissue; Open Targets ENSG00000197122 associations
First described 1985. Earliest sequence paper UniProt cites for the protein: Anderson S.K. et al, Mol. Cell. Biol, 1985, "Human cellular src gene: nucleotide sequence and derived amino acid sequence of the region coding for the carboxy-terminal two-thirds of pp60c-src". Source.
Non-receptor tyrosine kinase family downstream of receptor tyrosine kinases and integrins; dual BCR::ABL1 and SRC-family inhibition by dasatinib and bosutinib.
RNA: low tissue specificity, detected in many normal tissues. Blood: group enriched (dendritic cells 1 nTPM, monocytes 2 nTPM).
Medium: Duodenum, Esophagus, Gallbladder, Kidney, Oral mucosa, Rectum, Stomach, Testis.
Medium only: carcinoid, colorectal cancer, liver cancer, lung cancer.
HPA SRC tissue · HPA SRC 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 (SRC family kinases); 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:"SRC family kinases" OR ABSTRACT:"SRC family kinases" OR TITLE:"SRC" OR ABSTRACT:"SRC") 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 SRC family kinases, not a curated reading list.
Shares Bosutinib, Dasatinib, Chronic myeloid leukaemia (CML).
Shares Bosutinib, Dasatinib, Chronic myeloid leukaemia (CML), Acute lymphoblastic leukaemia.
Shares Bosutinib, Dasatinib, Chronic myeloid leukaemia (CML).
Shares Bosutinib, Dasatinib, Chronic myeloid leukaemia (CML), Acute lymphoblastic leukaemia.
Shares Dasatinib, Chronic myeloid leukaemia (CML).
Shares Bosutinib, Dasatinib, Chronic myeloid leukaemia (CML).
Shares Chronic myeloid leukaemia (CML), Acute lymphoblastic leukaemia.
Shares Chronic myeloid leukaemia (CML), Acute lymphoblastic leukaemia.