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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.
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.
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.
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.
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.
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.
Broadly expressed or essential: HPA finds the RNA at low tissue specificity; the 2 medicines aimed at it (Everolimus, Temsirolimus) act on the wild-type protein, so normal tissue is exposed and the therapeutic window comes from the tumour's faster division or its dependence on the protein. HPA FKBP1A: RNA low tissue specificity; blood lineage group enriched (dendritic cells 676 nTPM, granulocytes 976 nTPM, monocytes 1,017 nTPM); no normal tissue stained high; highest cancer staining thyroid cancer (2 of 4 high). Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Renal cell carcinoma, Breast cancer (all types)); Open Targets associates it with 7 specific cancer types at or above 0.5 (breast cancer, renal cell carcinoma, tuberous sclerosis, kidney angiomyolipoma, lymphangioleiomyomatosis, hamartoma and more). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas FKBP1A tissue; Open Targets ENSG00000088832 associations
First described 1989. Earliest sequence paper UniProt cites for the protein: Harding M.W. et al, Nature, 1989, "A receptor for the immunosuppressant FK506 is a cis-trans peptidyl-prolyl isomerase". Source.
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.
RNA: low tissue specificity, detected in all normal tissues. Blood: group enriched (dendritic cells 676 nTPM, granulocytes 976 nTPM, monocytes 1,017 nTPM).
No normal tissue stained high.
Medium only: head and neck cancer, ovarian cancer, pancreatic cancer, prostate cancer.
HPA FKBP1A tissue · HPA FKBP1A pathology · HPA protein class: FDA approved drug targets
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% | Housekeeping enzyme present in every dividing cell (rapamycin-binding protein); not a selection marker, which is why these drugs are given by cancer type rather than by test. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Query 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.
Shares Temsirolimus, mTOR, Renal cell carcinoma.
Shares Temsirolimus, Renal cell carcinoma.
Shares Everolimus, Renal cell carcinoma.
Shares Temsirolimus, mTOR.
Shares Everolimus, Renal cell carcinoma.
Shares Temsirolimus, mTOR, Everolimus.
Shares Everolimus, Renal cell carcinoma.