MPS1 (TTK)
MPS1 arms the checkpoint that holds a dividing cell until its chromosomes are attached. Blocking it lets cancer cells divide carelessly and die; one inhibitor is in phase 1/2 in breast cancer.
Overview
TTK (chromosome 6q14.1) encodes the dual-specificity kinase MPS1, which is involved in mitotic spindle assembly checkpoint signalling, delaying anaphase until chromosomes are bioriented, and in the repair of incorrect kinetochore-microtubule attachments; it phosphorylates MAD1L1 to promote the checkpoint and is present in rapidly proliferating cell lines (UniProt P33981). CFI-402257, a TTK inhibitor, is in phase 1/2 alone, with fulvestrant, and with paclitaxel in HER2-negative breast cancer (NCT05251714, NCT03568422).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · MPS1 arms the checkpoint that holds a dividing cell until its chromosomes are attached. Blocking it lets cancer cells divide carelessly and die; one inhibitor is in phase 1/2 in breast cancer.
- 1 · What it is
MPS1 arms the checkpoint that holds a dividing cell until its chromosomes are attached. Blocking it lets cancer cells divide carelessly and die; one inhibitor is in phase 1/2 in breast cancer.
- 2 · What goes wrong in cancer
The apex kinase of the spindle assembly checkpoint; inhibitors override the checkpoint rather than enforce it.
- 3 · How drugs use it
No product in this corpus aims at MPS1 (TTK) 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
Sources: HGNC HGNC:12401 (approved symbol, name, aliases and cross-references); UniProt P33981 (protein name, function and tissue specificity)
Biology
The apex kinase of the spindle assembly checkpoint; inhibitors override the checkpoint rather than enforce it.
- Rapidly proliferating cells (UniProt P33981)
- Breast cancer trials of CFI-402257
Notes
top- Prevalence not recorded: HGNC and UniProt carry no positivity rates.
Latest papers
topQuery for this target: (TITLE:"MPS1" OR ABSTRACT:"MPS1" OR TITLE:"TTK" OR ABSTRACT:"TTK" OR TITLE:"Mps1" OR ABSTRACT:"Mps1" OR TITLE:"TTK protein kinase" OR ABSTRACT:"TTK protein kinase" OR TITLE:"PYT" OR ABSTRACT:"PYT" OR TITLE:"CT96" OR ABSTRACT:"CT96") 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 MPS1 (TTK), not a curated reading list.
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