Protein / target
Peptidyl-prolyl cis-trans isomerase FKBP1A
Protein at a glance
Biological role
Type I transforming growth factor beta receptor binding
Strongest disease association
Dermatitis, Atopic
Therapeutic position
Established drug target
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
Keeps in an inactive conformation TGFBR1, the TGF-beta type I serine/threonine kinase receptor, preventing TGF-beta receptor activation in absence of ligand.
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Keeps in an inactive conformation TGFBR1, the TGF-beta type I serine/threonine kinase receptor, preventing TGF-beta receptor activation in absence of ligand. Recruits SMAD7 to ACVR1B which prevents the association of SMAD2 and SMAD3 with the activin receptor complex, thereby blocking the activin signal. May modulate the RYR1 calcium channel activity. PPIases accelerate the folding of proteins. It catalyzes the cis-trans isomerization of proline imidic peptide bonds in oligopeptides
Subcellular location
Domains and Gene Ontology detail (38)Hide
Domains & features
Gene Ontology
- Ccytoplasm
- Ccytoplasmic side of membrane
- Ccytosol
- Cmembrane
- Cryanodine receptor complex
- Csarcoplasmic reticulum
- Csarcoplasmic reticulum membrane
- Cterminal cisterna
- CZ disc
- Factivin receptor binding
- Fcalcium channel regulator activity
- FFK506 binding
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Oncogenic signalling
- ·TGFBR1 LBD Mutants in Cancer
Immune signalling
- ·regulation of immune response
- ·T cell activation
- ·SARS-CoV-1 activates/modulates innate immune responses
Muscle contraction
- ·regulation of cardiac muscle contraction by regulation of the release of sequestered cal…
- ·regulation of skeletal muscle contraction by regulation of release of sequestered calciu…
View underlying pathways (7)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
Broader indication categories (1)Hide
Broad umbrella indications (e.g. “Neoplasms”). Shown here because every medicine also appears under a more specific disease above — kept for completeness, de-emphasised for clarity.
7 medicines meet Open Targets' target-level approved-medicine definition; the 4 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
FK506-binding protein 1A inhibitor
Indicated for Delayed Graft Function, Eye Diseases, Tuberous Sclerosis, Neoplasms
FK506-binding protein 1A inhibitor
Indicated for Astrocytoma, Breast Neoplasms, Carcinoma, Renal Cell, Neuroendocrine Tumors
FK506-binding protein 1A inhibitor
Indicated for Delayed Graft Function, Dermatitis, Atopic, Eczema, Immune System Diseases
FK506-binding protein 1A inhibitor
Indicated for Carcinoma, Renal Cell, Lymphoma, Mantle-Cell, Neoplasms
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene FKBP1A
Gene-level evidence surfaced through the gene FKBP1A that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
View evidence synthesis (5)Hide
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.
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Drug development
7 compounds recorded · 7 approved
View all recorded compounds (7)Hide
Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Antibodies — Emerging
Protein degraders — Emerging
View underlying tractability evidence (10)Hide
Raw Open Targets tractability assessment buckets, by modality.
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 3 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Label change
Label change: SIROLIMUS (NDA213312)
- Trial status changed
A Prospective Study of Optimal Cord Selection for Haplo-Cord Transplantation: Targeting the Inherited Paternal Antigen (IPA) and Matching for the Non-Inherited Maternal Antigen (NIMA)
- Trial status changed
A Randomized, Open-label, Phase III Study of SIM0270 Combined With Everolimus Versus Treatment of Physician's Choice in Patients With CDK4/6 Inhibitors Previously Treated , ER+/HER2- Locally Advanced or Metastatic Breast Cancer
- Trial results posted
A Phase II, Single-Arm Study of RAD001 (Everolimus), Letrozole, and Metformin in Patients With Advanced or Recurrent Endometrial Carcinoma
- Label change
Label change: TACROLIMUS (ANDA203740)
- Trial status changed
Haploidentical Allogeneic Peripheral Blood Transplantation: Clinical Trial and Laboratory Correlates Examining Checkpoint Immune Regulators' Expression
- Regulatory approval
Approval: EVEROLIMUS (ANDA219464)
- Label change
Label change: TACROLIMUS (ANDA090402)
- New publicationTargeting PI3K/AKT/mTOR and MAPK Signaling Pathways in Gastric Cancer.
- New publicationPI3K-AKT/mTOR Signaling in Psychiatric Disorders: A Valuable Target to Stimulate or Suppress?
- New publicationMultifaceted role of mTOR (mammalian target of rapamycin) signaling pathway in human health and disease.
- New publicationA novel rapamycin cream formulation improves facial angiofibromas associated with tuberous sclerosis complex: a double-blind randomized placebo-controlled trial.
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.