HCK is a SRC-family kinase of white blood cells that dasatinib and bosutinib inhibit; it drives growth in some leukaemias and in Waldenstrom macroglobulinaemia, where ibrutinib also hits it.
Haematopoietic cell kinase (HCK) is a SRC-family tyrosine kinase restricted to myeloid cells and B lymphocytes. It is one of the SRC kinases blocked by dasatinib and bosutinib, and in chronic myeloid leukaemia it associates with BCR-ABL and helps drive STAT5 signalling. In Waldenstrom macroglobulinaemia the MYD88 L265P mutation switches HCK on, and part of the activity of ibrutinib in that disease comes from inhibiting HCK as well as BTK. HCK is also being studied as a target in colorectal cancer, where it is active in tumour-associated macrophages.
In plain words · HCK is a SRC-family kinase of white blood cells that dasatinib and bosutinib inhibit; it drives growth in some leukaemias and in Waldenstrom macroglobulinaemia, where ibrutinib also hits it.
HCK is a SRC-family kinase of white blood cells that dasatinib and bosutinib inhibit; it drives growth in some leukaemias and in Waldenstrom macroglobulinaemia, where ibrutinib also hits it.
A non-receptor tyrosine kinase downstream of Fc, integrin and Toll-like receptors in myeloid cells; it activates STAT5, PI3K and MAPK pathways.
No product in this corpus aims at HCK kinase 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 dendritic cells and granulocytes and monocytes and lymphoid tissue cells: HPA finds the gene tissue enhanced in lymphoid tissue, and the 3 medicines aimed at it (Dasatinib, Bosutinib, Ibrutinib) act on the wild-type protein, so the normal lineage is hit too. HPA HCK: RNA tissue enhanced (lymphoid tissue 107 nTPM); blood lineage group enriched (dendritic cells 336 nTPM, granulocytes 803 nTPM, monocytes 1,255 nTPM); no normal tissue stained high; highest cancer staining endometrial cancer (2 of 11 high). Distribution: 3 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Leukaemia, Lymphoma, Colorectal cancer); Open Targets associates it with 2 specific cancer types at or above 0.5 (chronic myeloid leukemia, acute lymphoblastic leukemia). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas HCK tissue; Human Protein Atlas HCK pathology; Open Targets ENSG00000101336 associations
First described 1987. Earliest sequence paper UniProt cites for the protein: Quintrell et al, Mol. Cell. Biol, 1987, "Identification of a human gene (HCK) that encodes a protein-tyrosine kinase and is expressed in hemopoietic cells". Source.
A non-receptor tyrosine kinase downstream of Fc, integrin and Toll-like receptors in myeloid cells; it activates STAT5, PI3K and MAPK pathways.
RNA: tissue enhanced (lymphoid tissue 107 nTPM), detected in many normal tissues. Blood: group enriched (dendritic cells 336 nTPM, granulocytes 803 nTPM, monocytes 1,255 nTPM).
No normal tissue stained high; medium in Bone marrow, Lung, Testis.
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 (HCK kinase, mainly in white blood cells); 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:"HCK kinase" OR ABSTRACT:"HCK kinase" OR TITLE:"HCK" OR ABSTRACT:"HCK") 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 HCK kinase, not a curated reading list.
Shares SRC family kinases, Dasatinib, Colorectal cancer.
Shares SRC family kinases, Dasatinib.
Shares Bosutinib, Dasatinib, Chronic myeloid leukaemia (CML).
Shares Bosutinib, Dasatinib, Chronic myeloid leukaemia (CML).
Shares Bosutinib, Dasatinib, Chronic myeloid leukaemia (CML).
Shares Dasatinib, Chronic myeloid leukaemia (CML).
Shares SRC family kinases, Dasatinib.
Shares Bosutinib, Dasatinib, Chronic myeloid leukaemia (CML).