Page last updated: 2024-08-07 16:53:21
Peptidyl-prolyl cis-trans isomerase FKBP1A
A peptidyl-prolyl cis-trans isomerase FKBP1A that is encoded in the genome of human. [PRO:DNx, UniProtKB:P62942]
Synonyms
PPIase FKBP1A;
EC 5.2.1.8;
12 kDa FK506-binding protein;
12 kDa FKBP;
FKBP-12;
Calstabin-1;
FK506-binding protein 1A;
FKBP-1A;
Immunophilin FKBP12;
Rotamase
Research
Bioassay Publications (23)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (4.35) | 18.7374 |
| 1990's | 10 (43.48) | 18.2507 |
| 2000's | 6 (26.09) | 29.6817 |
| 2010's | 3 (13.04) | 24.3611 |
| 2020's | 3 (13.04) | 2.80 |
Compounds (11)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| cycloheximide | Homo sapiens (human) | IC50 | 3.6000 | 1 | 1 |
| cycloheximide | Homo sapiens (human) | Ki | 3.4000 | 1 | 1 |
| 3-(3-pyridyl)-1-propyl-(2s)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate | Homo sapiens (human) | IC50 | 1.2400 | 1 | 1 |
| 3-(3-pyridyl)-1-propyl-(2s)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate | Homo sapiens (human) | Ki | 0.0050 | 3 | 3 |
| tacrolimus | Homo sapiens (human) | IC50 | 7.8618 | 5 | 5 |
| tacrolimus | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| biricodar | Homo sapiens (human) | IC50 | 0.0170 | 1 | 1 |
| l 683590 | Homo sapiens (human) | IC50 | 0.0021 | 2 | 2 |
| cyclosporine | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| sirolimus | Homo sapiens (human) | IC50 | 0.0042 | 6 | 6 |
| sirolimus | Homo sapiens (human) | Ki | 1.3505 | 4 | 4 |
| timcodar | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| thiabendazole | Homo sapiens (human) | Kd | 60.0000 | 1 | 1 |
| tacrolimus | Homo sapiens (human) | EC50 | 0.0009 | 1 | 1 |
| N-(2-fluorophenyl)-2-[2-(4-thiazolyl)-1-benzimidazolyl]acetamide | Homo sapiens (human) | Kd | 4,000.0000 | 1 | 1 |
| l 683590 | Homo sapiens (human) | EC50 | 0.0016 | 2 | 2 |
| sirolimus | Homo sapiens (human) | EC50 | 0.0364 | 1 | 1 |
| bastadin 5 | Homo sapiens (human) | EC50 | 2.2000 | 1 | 1 |
Enables
This protein enables 11 target(s):
| Target | Category | Definition |
|---|---|---|
| peptidyl-prolyl cis-trans isomerase activity | molecular function | Catalysis of the reaction: peptidyl-proline (omega=180) = peptidyl-proline (omega=0). [EC:5.2.1.8] |
| transforming growth factor beta receptor binding | molecular function | Binding to a transforming growth factor beta receptor. [GOC:ai] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| macrolide binding | molecular function | Binding to a macrolide, any of a large group of structurally related antibiotics produced by Streptomyces species. [GOC:jl, ISBN:0198506732] |
| FK506 binding | molecular function | Binding to a 23-membered macrolide lactone FK506. [GOC:jl] |
| channel regulator activity | molecular function | Binds to and modulates the activity of a channel. A channel catalyzes energy-independent facilitated diffusion, mediated by passage of a solute through a transmembrane aqueous pore or channel. [GOC:mah] |
| signaling receptor inhibitor activity | molecular function | Binds to and modulates the activity of a signaling receptor. [GOC:ceb] |
| type I transforming growth factor beta receptor binding | molecular function | Binding to a type I transforming growth factor beta receptor. [GOC:BHF, GOC:mah] |
| transmembrane transporter binding | molecular function | Binding to a transmembrane transporter, a protein or protein complex that enables the transfer of a substance, usually a specific substance or a group of related substances, from one side of a membrane to the other. [GOC:BHF, GOC:jl, PMID:33199372] |
| I-SMAD binding | molecular function | Binding to an inhibitory SMAD signaling protein. [GOC:BHF, GOC:vk, PMID:19114992] |
| activin receptor binding | molecular function | Binding to an activin receptor. [GOC:BHF, GOC:vk] |
Located In
This protein is located in 7 target(s):
| Target | Category | Definition |
|---|---|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| terminal cisterna | cellular component | The portion of sarcoplasmic reticulum devoted to calcium ion storage and calcium ion release. [GOC:mtg_muscle] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| sarcoplasmic reticulum | cellular component | A fine reticular network of membrane-limited elements that pervades the sarcoplasm of a muscle cell; continuous over large portions of the cell and with the nuclear envelope; that part of the endoplasmic reticulum specialized for calcium release, uptake and storage. [GOC:mtg_muscle, ISBN:0124325653, ISBN:0198547684] |
| Z disc | cellular component | Platelike region of a muscle sarcomere to which the plus ends of actin filaments are attached. [GOC:mtg_muscle, ISBN:0815316194] |
| cytoplasmic side of membrane | cellular component | The side of a membrane that faces the cytoplasm. [GOC:dos] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|---|---|
| sarcoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the sarcoplasmic reticulum. [GOC:rph] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|---|---|
| ryanodine receptor complex | cellular component | A voltage-gated calcium-release channel complex of the sarcoplasmic or endoplasmic reticulum. It plays an important role in the excitation-contraction (E-C) coupling of muscle cells. RyR comprises a family of ryanodine receptors, widely expressed throughout the animal kingdom. [GOC:ame, PMID:22822064] |
Involved In
This protein is involved in 21 target(s):
| Target | Category | Definition |
|---|---|---|
| protein peptidyl-prolyl isomerization | biological process | The modification of a protein by cis-trans isomerization of a proline residue. [GOC:krc, PMID:16959570] |
| heart morphogenesis | biological process | The developmental process in which the heart is generated and organized. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:dph, GOC:isa_complete] |
| protein folding | biological process | The process of assisting in the covalent and noncovalent assembly of single chain polypeptides or multisubunit complexes into the correct tertiary structure. [GOC:go_curators, GOC:rb] |
| 'de novo' protein folding | biological process | The process of assisting in the folding of a nascent peptide chain into its correct tertiary structure. [GOC:mb] |
| regulation of skeletal muscle contraction by regulation of release of sequestered calcium ion | biological process | Any process that modulates the frequency, rate or extent of skeletal muscle contraction via the regulation of the release of sequestered calcium ion by sarcoplasmic reticulum into cytosol. The sarcoplasmic reticulum is the endoplasmic reticulum of striated muscle, specialised for the sequestration of calcium ions that are released upon receipt of a signal relayed by the T tubules from the neuromuscular junction. [GOC:mtg_muscle] |
| protein maturation by protein folding | biological process | The process of assisting in the covalent and noncovalent assembly of single chain polypeptides or multisubunit complexes into the correct tertiary structure that results in the attainment of the full functional capacity of a protein. [GOC:isa_complete] |
| negative regulation of transforming growth factor beta receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of any TGF-beta receptor signaling pathway. [GOC:mah] |
| positive regulation of protein binding | biological process | Any process that activates or increases the frequency, rate or extent of protein binding. [GOC:mah] |
| regulation of protein localization | biological process | Any process that modulates the frequency, rate or extent of any process in which a protein is transported to, or maintained in, a specific location. [GOC:dph, GOC:mah, GOC:tb] |
| negative regulation of activin receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the activity of any activin receptor signaling pathway. [GOC:BHF, GOC:rl] |
| protein refolding | biological process | The process carried out by a cell that restores the biological activity of an unfolded or misfolded protein, using helper proteins such as chaperones. [GOC:mb] |
| T cell activation | biological process | The change in morphology and behavior of a mature or immature T cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:mgi_curators, ISBN:0781735149] |
| positive regulation of canonical NF-kappaB signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl] |
| regulation of immune response | biological process | Any process that modulates the frequency, rate or extent of the immune response, the immunological reaction of an organism to an immunogenic stimulus. [GOC:ai] |
| ventricular cardiac muscle tissue morphogenesis | biological process | The process in which the anatomical structures of cardiac ventricle muscle is generated and organized. [GOC:devbiol] |
| regulation of ryanodine-sensitive calcium-release channel activity | biological process | Any process that modulates the activity of a ryanodine-sensitive calcium-release channel. The ryanodine-sensitive calcium-release channel catalyzes the transmembrane transfer of a calcium ion by a channel that opens when a ryanodine class ligand has been bound by the channel complex or one of its constituent parts. [GOC:BHF, GOC:dph, GOC:tb] |
| heart trabecula formation | biological process | The process of creating a trabecula in the heart. A trabecula is a tissue element in the form of a small beam, strut or rod. [GOC:dph] |
| calcium ion transmembrane transport | biological process | A process in which a calcium ion is transported from one side of a membrane to the other by means of some agent such as a transporter or pore. [GOC:mah] |
| supramolecular fiber organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a supramolecular fiber, a polymer consisting of an indefinite number of protein or protein complex subunits that have polymerised to form a fiber-shaped structure. [GOC:pr] |
| regulation of amyloid precursor protein catabolic process | biological process | Any process that modulates the frequency, rate or extent of amyloid precursor protein catabolic process. [GO_REF:0000058, GOC:PARL, GOC:rl, GOC:TermGenie, PMID:24499793] |
| amyloid fibril formation | biological process | The generation of amyloid fibrils, insoluble fibrous protein aggregates exhibiting beta sheet structure, from proteins. [GOC:cvs, GOC:jj, GOC:ppm, GOC:sj, PMID:21148556, PMID:22817896, PMID:28937655, PMID:29654159] |