FKBP12 (FKBP1A)
FKBP12 is the small protein that rapamycin-type drugs grab first; the drug-FKBP12 pair then clamps onto mTOR and switches off its growth signalling.
Overview
FK506-binding protein 1A (FKBP12) is a peptidyl-prolyl isomerase that acts as the intracellular receptor for rapamycin and its analogues. Everolimus and temsirolimus bind FKBP12, and the complex binds the FRB domain of mTOR, inhibiting mTORC1. The target is therefore listed for every rapalogue approved in kidney cancer, breast cancer, neuroendocrine tumours and tuberous sclerosis.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · FKBP12 is the small protein that rapamycin-type drugs grab first; the drug-FKBP12 pair then clamps onto mTOR and switches off its growth signalling.
- 1 · What it is
FKBP12 is the small protein that rapamycin-type drugs grab first; the drug-FKBP12 pair then clamps onto mTOR and switches off its growth signalling.
- 2 · What goes wrong in cancer
An abundant cytosolic immunophilin that also regulates ryanodine and TGF-beta receptors; drug binding, not its own enzyme activity, is what matters for the mTOR effect.
- 3 · How drugs use it
No product in this corpus aims at FKBP12 (FKBP1A) yet. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
External identifiers
Biology
An abundant cytosolic immunophilin that also regulates ryanodine and TGF-beta receptors; drug binding, not its own enzyme activity, is what matters for the mTOR effect.
- Ubiquitous, cytosolic
- Required for the action of everolimus, temsirolimus and sirolimus
Latest papers
topQuery for this target: (TITLE:"FKBP12" OR ABSTRACT:"FKBP12" OR TITLE:"FKBP1A" OR ABSTRACT:"FKBP1A") 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 FKBP12 (FKBP1A), not a curated reading list.
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