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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.
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).
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.
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.
The apex kinase of the spindle assembly checkpoint; inhibitors override the checkpoint rather than enforce 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.
First described 1991. Earliest sequence paper UniProt cites for the protein: Hanks S.K. et al, Methods Enzymol, 1991, "Protein kinase catalytic domain sequence database: identification of conserved features of primary structure and classification of family members". Source.
Sources: HGNC HGNC:12401 (approved symbol, name, aliases and cross-references); UniProt P33981 (protein name, function and tissue specificity)
The apex kinase of the spindle assembly checkpoint; inhibitors override the checkpoint rather than enforce it.
Query 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.
Shares Checkpoint (two meanings) and the tag checkpoint-map.
Shares Checkpoint (two meanings) and the tag checkpoint-map.
Shares Checkpoint (two meanings) and the tag checkpoint-map.
Shares Checkpoint (two meanings) and the tag checkpoint-map.
Shares Checkpoint (two meanings) and the tag checkpoint-map.
Shares Checkpoint (two meanings) and the tag checkpoint-map.
Shares Checkpoint (two meanings) and the tag checkpoint-map.
Shares Checkpoint (two meanings) and the tag checkpoint-map.