SRC family kinases
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
Non-receptor tyrosine kinase family downstream of receptor tyrosine kinases and integrins; dual BCR::ABL1 and SRC-family inhibition by dasatinib and bosutinib.
- 3 · How drugs use it
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.
External identifiers
Biology
Non-receptor tyrosine kinase family downstream of receptor tyrosine kinases and integrins; dual BCR::ABL1 and SRC-family inhibition by dasatinib and bosutinib.
- Chronic myeloid leukaemia and Ph-positive ALL (as a secondary target)
- Activated in many solid tumours without proven dependency
Latest papers
topQuery 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.
Similar pages
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