Protein / target
Peptidyl-prolyl cis-trans isomerase FKBP1A
Protein at a glance
Biological role
Type I transforming growth factor beta receptor binding
Primary system
Immune system
Strongest disease association
atopic eczema
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
7 approved
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
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.
View supporting evidenceHide supporting evidence
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.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
FK506-binding protein 1A inhibitor
Appears in clinical studies involving blue rubber bleb nevus, Venous malformation, Gorham-Stout disease, vascular neoplasm
FK506-binding protein 1A inhibitor
Appears in clinical studies involving angiomyolipoma, tuberous sclerosis, astrocytoma (excluding glioblastoma), neuroendocrine neoplasm
FK506-binding protein 1A inhibitor
Appears in clinical studies involving conjunctivitis, graft versus host disease, graft versus host disease, Eczematoid dermatitis
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Highest overall evidence
Remaining associations by Open Targets' aggregated evidence score.
Show all associationsHide all associations
Open Targets ranks 1,462 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 7 total
renal cell carcinoma · mantle cell lymphoma · renal cell carcinoma
conjunctivitis · graft versus host disease · graft versus host disease
atopic eczema · atopic eczema · Eczematoid dermatitis
angiomyolipoma · tuberous sclerosis · astrocytoma (excluding glioblastoma)
coronary artery disorder
blue rubber bleb nevus · Venous malformation · Gorham-Stout disease
conjunctivitis · graft versus host disease · graft versus host disease
Tractability
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.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. 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 underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through 3 drugs that target this protein, so each event is news about that drug rather than about the protein directly.
- Industry developmentAutism-Like Traits in Mice Improved After Single Rapamycin Dose
- Trial status changed
Phase I Study of the Pan-ERBB Inhibitor Neratinib Given in Combination With Everolimus, Palbociclib, or Trametinib in Advanced Cancer Subjects With EGFR Mutation/Amplification, HER2 Mutation/Amplification, or HER3/4 Mutation or KRAS Mutation
- 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 publicationRapamycin extenuates experimental colitis by modulating the gut microbiota.
- New publicationAutophagy and autophagy signaling in Epilepsy: possible role of autophagy activator.
- 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.
- New publicationGut microbiome modulates tacrolimus pharmacokinetics through the transcriptional regulation of ABCB1.
- New publicationThe PI3K-Akt-mTOR and Associated Signaling Pathways as Molecular Drivers of Immune-Mediated Inflammatory Skin Diseases: Update on Therapeutic Strategy Using Natural and Synthetic Compounds.
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.