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PTK6, also called breast tumour kinase, is over-expressed in most breast cancers and is one of the off-targets of dasatinib; drugs made specifically against it are still experimental.
Protein tyrosine kinase 6, or breast tumour kinase (BRK), is a distant relative of the SRC family that is normally found in differentiating gut and skin epithelium but is over-expressed in the majority of breast cancers and in some colon, prostate and ovarian tumours, where it promotes proliferation, survival and migration through STAT3 and AKT. It appears in ChEMBL as a target because approved multi-kinase inhibitors, dasatinib among them, inhibit it; selective PTK6 inhibitors and degraders are in preclinical development, including for HER2-positive and triple-negative breast cancer.
In plain words · PTK6, also called breast tumour kinase, is over-expressed in most breast cancers and is one of the off-targets of dasatinib; drugs made specifically against it are still experimental.
PTK6, also called breast tumour kinase, is over-expressed in most breast cancers and is one of the off-targets of dasatinib; drugs made specifically against it are still experimental.
An intracellular non-receptor tyrosine kinase lacking a membrane anchor; in tumours it phosphorylates STAT3, paxillin and Sam68 and cooperates with HER2 and EGFR signalling.
No product in this corpus aims at PTK6 (BRK) yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Tumour-associated overexpression: HPA finds the RNA tissue enhanced in normal esophagus, skin 1, vagina, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA PTK6: RNA tissue enhanced (esophagus 104 nTPM, skin 1 51 nTPM, vagina 41 nTPM); high antibody staining in 3 normal tissues; highest cancer staining stomach cancer (1 of 12 high). Distribution: 3 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Breast cancer (all types), Colorectal cancer, Prostate cancer); Open Targets associates it with 1 specific cancer type at or above 0.5 (medullary thyroid gland carcinoma). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas PTK6 tissue; Human Protein Atlas PTK6 pathology; Open Targets ENSG00000101213 associations
First described 1994. Earliest sequence paper UniProt cites for the protein: Mitchell P.J. et al, Oncogene, 1994, "Cloning and characterisation of cDNAs encoding a novel non-receptor tyrosine kinase, brk, expressed in human breast tumours". Source.
An intracellular non-receptor tyrosine kinase lacking a membrane anchor; in tumours it phosphorylates STAT3, paxillin and Sam68 and cooperates with HER2 and EGFR signalling.
RNA: tissue enhanced (esophagus 104 nTPM, skin 1 51 nTPM, vagina 41 nTPM), detected in many normal tissues.
Medium: Appendix, Bronchus, Cerebellum, Cervix, Colon, Duodenum, Epididymis, Esophagus.
Medium only: breast cancer, carcinoid, cervical cancer, colorectal cancer.
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 (PTK6, over-expressed in many breast cancers without a selecting mutation); 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:"PTK6" OR ABSTRACT:"PTK6" OR TITLE:"BRK" OR ABSTRACT:"BRK") 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 PTK6 (BRK), not a curated reading list.
Shares SRC family kinases, Dasatinib.
Shares SRC family kinases, Dasatinib, Colorectal cancer.
Shares SRC family kinases, Dasatinib.
Shares SRC family kinases, Dasatinib, Prostate cancer.
Shares Dasatinib, Colorectal cancer.
Shares Dasatinib, Prostate cancer.