Gene Symbol: FKBP12
Description: FK506 binding protein 1A
Alias: FKBP-12, FKBP-1A, FKBP1, FKBP12, PKC12, PKCI2, PPIASE, peptidyl-prolyl cis-trans isomerase FKBP1A, 12 kDa FK506-binding protein, 12 kDa FKBP, FK506 binding protein 1A, 12kDa, FK506 binding protein12, FK506-binding protein 1, FK506-binding protein 12, FK506-binding protein, T-cell, 12-kD, FKBP12-Exip3, PPIase FKBP1A, calstabin-1, immunophilin FKBP12, protein kinase C inhibitor 2, rotamase
Species: human
Products:     FKBP12

Top Publications

  1. Harding M, Galat A, Uehling D, Schreiber S. A receptor for the immunosuppressant FK506 is a cis-trans peptidyl-prolyl isomerase. Nature. 1989;341:758-60 pubmed
  2. Liang J, Choi J, Clardy J. Refined structure of the FKBP12-rapamycin-FRB ternary complex at 2.2 A resolution. Acta Crystallogr D Biol Crystallogr. 1999;55:736-44 pubmed
    The structure of the FKBP12-rapamycin-FRB ternary complex has now been refined at 2.2 A resolution...
  3. Jeyakumar L, Ballester L, Cheng D, McIntyre J, Chang P, Olivey H, et al. FKBP binding characteristics of cardiac microsomes from diverse vertebrates. Biochem Biophys Res Commun. 2001;281:979-86 pubmed publisher
    FK506 binding protein (FKBP) is a cytosolic receptor for the immunosuppressive drug FK-506. The common isoform, FKBP12, was found to be associated with the calcium release channel (ryanodine receptor 1) of different species of vertebrate ..
  4. Sugata H, Matsuo K, Nakagawa T, Takahashi M, Mukai H, Ono Y, et al. A peptidyl-prolyl isomerase, FKBP12, accumulates in Alzheimer neurofibrillary tangles. Neurosci Lett. 2009;459:96-9 pubmed publisher
    We investigated a possible role in Alzheimer's disease (AD) for FKBP12, a peptidyl-prolyl cis-trans isomerase known to be important in protein assembly, folding and transportation by using Western blotting and microscopic analyses in ..
  5. Rosen M, Michnick S, Karplus M, Schreiber S. Proton and nitrogen sequential assignments and secondary structure determination of the human FK506 and rapamycin binding protein. Biochemistry. 1991;30:4774-89 pubmed
    ..Long-range NOEs are used to demonstrate that FKBP has a novel folding topology consisting of a five-stranded antiparallel beta sheet with +3, +1, -3, +1 loop connectivity. ..
  6. Griffith J, Kim J, Kim E, Sintchak M, Thomson J, Fitzgibbon M, et al. X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex. Cell. 1995;82:507-22 pubmed
    The X-ray structure of the ternary complex of a calcineurin A fragment, calcineurin B, FKBP12, and the immunosuppressant drug FK506 (also known as tacrolimus) has been determined at 2...
  7. Lam E, Martin M, Timerman A, Sabers C, Fleischer S, Lukas T, et al. A novel FK506 binding protein can mediate the immunosuppressive effects of FK506 and is associated with the cardiac ryanodine receptor. J Biol Chem. 1995;270:26511-22 pubmed
    FK506, an immunosuppressant that prolongs allograft survival, is a co-drug with its intracellular receptor, FKBP12. The FKBP12.FK506 complex inhibits calcineurin, a critical signaling molecule during T-cell activation...
  8. Shou W, Aghdasi B, Armstrong D, Guo Q, Bao S, Charng M, et al. Cardiac defects and altered ryanodine receptor function in mice lacking FKBP12. Nature. 1998;391:489-92 pubmed
    b>FKBP12, a cis-trans prolyl isomerase that binds the immunosuppressants FK506 and rapamycin, is ubiquitously expressed and interacts with proteins in several intracellular signal transduction systems...
  9. Huse M, Chen Y, Massague J, Kuriyan J. Crystal structure of the cytoplasmic domain of the type I TGF beta receptor in complex with FKBP12. Cell. 1999;96:425-36 pubmed
    ..both the GS region and the catalytic domain, has been determined in complex with the FK506-binding protein FKBP12. TbetaR-I adopts an inactive conformation that is maintained by the unphosphorylated GS region...

More Information

Publications120 found, 100 shown here

  1. Gaburjakova M, Gaburjakova J, Reiken S, Huang F, Marx S, Rosemblit N, et al. FKBP12 binding modulates ryanodine receptor channel gating. J Biol Chem. 2001;276:16931-5 pubmed
    ..of skeletal muscle is comprised of four 565,000-dalton RyR1s, each of which binds one FK506 binding protein (FKBP12). RyR1 is required for excitation-contraction coupling in skeletal muscle...
  2. Fulton K, Jackson S, Buckle A. Energetic and structural analysis of the role of tryptophan 59 in FKBP12. Biochemistry. 2003;42:2364-72 pubmed
    Tryptophan 59 forms the seat of the hydrophobic ligand-binding site in the small immunophilin FKBP12. Mutating this residue to phenylalanine or leucine stabilizes the protein by 2.72 and 2.35 kcal mol(-1), respectively...
  3. Wear M, Patterson A, Walkinshaw M. A kinetically trapped intermediate of FK506 binding protein forms in vitro: chaperone machinery dominates protein folding in vivo. Protein Expr Purif. 2007;51:80-95 pubmed
    ..One construct has a short hexa-his tag (6H-FKBP12); the second longer fusion protein (6HL-FKBP12) contains an additional thrombin protease cleavage site; the third ..
  4. Seidler T, Loughrey C, Zibrova D, Kettlewell S, Teucher N, Kogler H, et al. Overexpression of FK-506 binding protein 12.0 modulates excitation contraction coupling in adult rabbit ventricular cardiomyocytes. Circ Res. 2007;101:1020-9 pubmed
    ..was studied in adult rabbit ventricular myocytes after transfection with a recombinant adenovirus coding for human FKBP12.0 (Ad-FKBP12.0). Western blots confirmed overexpression (by 2.6+/-0.4 fold, n=5). FKBP12...
  5. Gerard M, Debyser Z, Desender L, Baert J, Brandt I, Baekelandt V, et al. FK506 binding protein 12 differentially accelerates fibril formation of wild type alpha-synuclein and its clinical mutants A30P or A53T. J Neurochem. 2008;106:121-33 pubmed publisher
    ..In this paper, we investigated in detail the effect of FKBP12 on early aggregation and on fibril formation of wild-type, A53T and A30P alpha-SYN...
  6. Mustafi S, Chen H, Li H, LeMaster D, HERNANDEZ G. Analysing the visible conformational substates of the FK506-binding protein FKBP12. Biochem J. 2013;453:371-80 pubmed publisher
    The 1H-15N 2D NMR correlation spectrum of the widely studied FK506-binding protein FKBP12 (FK506-binding protein of 12 kDa) contains previously unreported peak doublings for at least 31 residues that arise from a minor conformational ..
  7. Roskoski R. Properties of FDA-approved small molecule protein kinase inhibitors. Pharmacol Res. 2019;144:19-50 pubmed publisher
    ..One of the vexing problems is the near universal development of resistance that is associated with the use of small molecule protein kinase inhibitors for the treatment of cancer. ..
  8. Wang X, Hayashi S, Umezaki M, Yamamoto T, Kageyama Yahara N, Kondo T, et al. Shikonin, a constituent of Lithospermum erythrorhizon exhibits anti-allergic effects by suppressing orphan nuclear receptor Nr4a family gene expression as a new prototype of calcineurin inhibitors in mast cells. Chem Biol Interact. 2014;224:117-27 pubmed publisher
    ..Therefore, shikonin has therapeutic potential for the treatment of allergic diseases as a new calcineurin inhibitor. ..
  9. Leach D, Trotta A, Need E, Risbridger G, Taylor R, Buchanan G. The prognostic value of stromal FK506-binding protein 1 and androgen receptor in prostate cancer outcome. Prostate. 2017;77:185-195 pubmed publisher
    ..Prostate 77:185-195, 2017. © 2016 Wiley Periodicals, Inc. ..
  10. De Cicco M, Milroy L, Dames S. Target of rapamycin FATC domain as a general membrane anchor: the FKBP-12 like domain of FKBP38 as a case study. Protein Sci. 2017;: pubmed publisher
  11. Le Douairon Lahaye S, Gratas Delamarche A, Malardé L, Zguira S, Vincent S, Lemoine Morel S, et al. Combined insulin treatment and intense exercise training improved basal cardiac function and Ca(2+)-cycling proteins expression in type 1 diabetic rats. Appl Physiol Nutr Metab. 2012;37:53-62 pubmed publisher
    ..Cardiac expression of the main Ca(2+)-cycling proteins (RyR2, FKBP 12.6, SERCA2, PLB, NCX1) was assessed by Western blot...
  12. Guduru S, Arya P. Synthesis and biological evaluation of rapamycin-derived, next generation small molecules. Medchemcomm. 2018;9:27-43 pubmed publisher
    ..Herein, we report selected case studies related to the synthesis of rapamycin-derived compounds and hybrid molecules to explore their biological properties. ..
  13. Matus M, Kucerova D, Kruzliak P, Adameova A, Doka G, Turcekova K, et al. Upregulation of SERCA2a following short-term ACE inhibition (by enalaprilat) alters contractile performance and arrhythmogenicity of healthy myocardium in rat. Mol Cell Biochem. 2015;403:199-208 pubmed publisher
    ..CSQ, calsequestrin; TRD, triadin; PLB, phospholamban; Thr(17)-PLB-phosphorylated PLB at threonine-17, FKBP12.6, FK506-binding protein, Cav1...
  14. Wang J, Guo R, Liu S, Chen Q, Zuo S, Yang M, et al. Molecular mechanisms of FK506-induced hypertension in solid organ transplantation patients. Chin Med J (Engl). 2014;127:3645-50 pubmed
    ..First, FK506 binds FK506 binding protein 12 and its related isoform 12.6 (FKBP12/12...
  15. Peng L, Jiang Q, Pan J, Deng C, Yu J, Wu X, et al. Involvement of polyphosphate kinase in virulence and stress tolerance of uropathogenic Proteus mirabilis. Med Microbiol Immunol. 2016;205:97-109 pubmed publisher
    ..As a whole, these results indicate that PPK is an important regulator and plays a crucial role in stress tolerance and virulence in uropathogenic P. mirabilis. ..
  16. Liu Z, Cai H, Zhu H, Toque H, Zhao N, Qiu C, et al. Protein kinase RNA-like endoplasmic reticulum kinase (PERK)/calcineurin signaling is a novel pathway regulating intracellular calcium accumulation which might be involved in ventricular arrhythmias in diabetic cardiomyopathy. Cell Signal. 2014;26:2591-600 pubmed publisher
    ..6) FKBP12.6 disassociation...
  17. Chaurasia N, Mishra Y, Chatterjee A, Rai R, Yadav S, Rai L. Overexpression of phytochelatin synthase (pcs) enhances abiotic stress tolerance by altering the proteome of transformed Anabaena sp. PCC 7120. Protoplasma. 2017;254:1715-1724 pubmed publisher
    ..Such recombinant strains have potential for future use as biofertilizer. ..
  18. Harikishore A, Yoon H. Immunophilins: Structures, Mechanisms and Ligands. Curr Mol Pharmacol. 2015;9:37-47 pubmed
    ..Most Cyps and FKBP family members catalyse peptidyl-prolyl cis/trans isomerase (PPIase) mediated reactions and form binary complexes with their ligands cyclosporine A and FK506...
  19. Nath P, Dong G, Braiman A, Isakov N. In vivo regulation of human CrkII by cyclophilin A and FK506-binding protein. Biochem Biophys Res Commun. 2016;470:411-416 pubmed publisher
    ..FRET-based biosensor, supporting the accumulation of cis conformers of human CrkII1-236 in the presence of PPIase inhibitors...
  20. Hussner J, Sünwoldt J, Seibert I, Gliesche D, zu Schwabedissen H. Pimecrolimus increases the expression of interferon-inducible genes that modulate human coronary artery cells proliferation. Eur J Pharmacol. 2016;784:137-46 pubmed publisher
    ..The crosstalk of interferon and toll-like receptor signaling may be a molecular mechanism that contributed to the failure of pimecrolimus-eluting stents in humans. ..
  21. Yang J, Zhang R, Jiang X, Lv J, Li Y, Ye H, et al. Toll-like receptor 4-induced ryanodine receptor 2 oxidation and sarcoplasmic reticulum Ca2+ leakage promote cardiac contractile dysfunction in sepsis. J Biol Chem. 2018;293:794-807 pubmed publisher
    ..and oxidative stress in RyR2 were increased, whereas the levels of the RyR2-associated FK506-binding protein 1B (FKBP12.6) were decreased...
  22. Liu D, Zheng S, Zheng G, Lv Q, Shen B, Yuan X, et al. Adaptation of the FK506 binding protein 1B to hibernation in bats. Cryobiology. 2018;83:1-8 pubmed publisher
    ..This study provides new insights into the molecular evolution of Fkbp1b in adaptation to bat hibernation. ..
  23. Quistgaard E, Weininger U, Ural Blimke Y, Modig K, Nordlund P, Akke M, et al. Molecular insights into substrate recognition and catalytic mechanism of the chaperone and FKBP peptidyl-prolyl isomerase SlyD. BMC Biol. 2016;14:82 pubmed
    ..SlyD is a two-domain enzyme containing both a PPIase FK506-binding protein (FKBP) domain and an insert-in-flap (IF) chaperone domain...
  24. Fritsch E, Stegeman J, Goldstone J, Nacci D, Champlin D, Jayaraman S, et al. Expression and function of ryanodine receptor related pathways in PCB tolerant Atlantic killifish (Fundulus heteroclitus) from New Bedford Harbor, MA, USA. Aquat Toxicol. 2015;159:156-66 pubmed publisher
    ..displayed increased levels of skeletal muscle RyR1 protein, and increased levels of FK506-binding protein 12 kDa (FKBP12) an accessory protein essential for NDL PCB-triggered changes in RyR channel function...
  25. Waseem M, Ahmad F, Habib S, Gao Y, Li Z. Genome-wide identification of FK506-binding domain protein gene family, its characterization, and expression analysis in tomato (Solanum lycopersicum L.). Gene. 2018;678:143-154 pubmed publisher
    FK506-protein also called FKBP protein belongs to PPIase (peptidylprolylcis-trans isomerase) super family of immune suppressive drugs that act as molecular protein chaperones...
  26. Shi P, Aluri S, Lin Y, Shah M, Edman M, Dhandhukia J, et al. Elastin-based protein polymer nanoparticles carrying drug at both corona and core suppress tumor growth in vivo. J Control Release. 2013;171:330-8 pubmed publisher
    ..Having determined that Rapa can be non-specifically entrapped in the core of ELP nanoparticles, FK506 binding protein 12 (FKBP), which is the cognate protein target of Rapa, was genetically fused to the surface of these ..
  27. Lopez L, Harris S, Luciano M, Liewald D, Davies G, Gow A, et al. Evolutionary conserved longevity genes and human cognitive abilities in elderly cohorts. Eur J Hum Genet. 2012;20:341-7 pubmed publisher
    ..We tested AFG3L2 (MIM: 604581, AFG3 ATPase family gene 3-like 2 (yeast)), FRAP1 (MIM: 601231, a FK506 binding protein 12-rapamycin associated protein), MAT1A, MAT2A (MIM: 610550 and 601468, methionine adenosyltransferases I ..
  28. Ernst K, Schnell L, Barth H. Host Cell Chaperones Hsp70/Hsp90 and Peptidyl-Prolyl Cis/Trans Isomerases Are Required for the Membrane Translocation of Bacterial ADP-Ribosylating Toxins. Curr Top Microbiol Immunol. 2017;406:163-198 pubmed publisher
    ..cell chaperones including Hsp90 and protein-folding helper enzymes of the peptidyl-prolyl cis/trans isomerase (PPIase) type facilitate this membrane translocation of the unfolded A-domain for ADP-ribosylating toxins but not for ..
  29. Edinger A, Linardic C, Chiang G, Thompson C, Abraham R. Differential effects of rapamycin on mammalian target of rapamycin signaling functions in mammalian cells. Cancer Res. 2003;63:8451-60 pubmed
    ..Here, we show that the FKBP12/rapamycin complex is an essentially irreversible inhibitor of mTOR kinase activity in vitro...
  30. Van Acker K, Bultynck G, Rossi D, Sorrentino V, Boens N, Missiaen L, et al. The 12 kDa FK506-binding protein, FKBP12, modulates the Ca(2+)-flux properties of the type-3 ryanodine receptor. J Cell Sci. 2004;117:1129-37 pubmed
  31. Tanaka Y, Amano A, Morisaki M, Sato Y, Sasaki T. Cellular peptidyl-prolyl cis/trans isomerase Pin1 facilitates replication of feline coronavirus. Antiviral Res. 2016;126:1-7 pubmed publisher
    ..Both Cyp and FKBP have peptidyl-prolyl cis-trans isomerase (PPIase) activity...
  32. Chen Y, Terajima M, Banerjee P, Guo H, Liu X, Yu J, et al. FKBP65-dependent peptidyl-prolyl isomerase activity potentiates the lysyl hydroxylase 2-driven collagen cross-link switch. Sci Rep. 2017;7:46021 pubmed publisher
    ..Here, we postulated that peptidyl prolyl isomerase (PPIase) activity of FKBP65 positively modulates LH2 enzymatic activity and is critical for the formation of hydroxylysine-..
  33. Rangu M, Ye Z, Bhatti S, Zhou S, Yang Y, Fish T, et al. Association of Proteomics Changes with Al-Sensitive Root Zones in Switchgrass. Proteomes. 2018;6: pubmed publisher
    ..apical 1-cm root apex tissues were clustered into 25 biological pathways; proteins involved in the cell cycle (rotamase FKBP 1 isoforms, and CDC48 protein) were all at a reduced abundance level compared to the non-treated control ..
  34. DiLella A, Hawkins A, Craig R, Schreiber S, Griffin C. Chromosomal band assignments of the genes encoding human FKBP12 and FKBP13. Biochem Biophys Res Commun. 1992;189:819-23 pubmed
    Human FKBP12 and FKBP13 are encoded by distinct genes designated FKBP1 and FKBP2, respectively. Human FKBP1 was previously characterized. The characterization of human FKBP2 is described. FKBP2 is three kb in length and contains six exons...
  35. Maki N, Sekiguchi F, Nishimaki J, Miwa K, Hayano T, Takahashi N, et al. Complementary DNA encoding the human T-cell FK506-binding protein, a peptidylprolyl cis-trans isomerase distinct from cyclophilin. Proc Natl Acad Sci U S A. 1990;87:5440-3 pubmed
    ..This is in contrast to the result that as many as 20 copies of the cyclophilin gene and possible pseudogenes may be present in the mammalian genome. ..
  36. Yang W, Inouye C, Seto E. Cyclophilin A and FKBP12 interact with YY1 and alter its transcriptional activity. J Biol Chem. 1995;270:15187-93 pubmed
    ..In a yeast two-hybrid screen, two cellular proteins, cyclophilin A (CyPA) and FK506-binding protein 12 (FKBP12), interacted with YY1. These interactions are specific and also occur in mammalian cells...
  37. Yan Y, Wang Y, Zhao L, Jiang S, Loh H, Law P, et al. Role of FK506 binding protein 12 in morphine-induced ?-opioid receptor internalization and desensitization. Neurosci Lett. 2014;566:231-235 pubmed publisher
    ..Previously we reported that FK506 binding protein 12 (FKBP12) specifically interacts with OPRM1 and such interaction attenuates receptor phosphorylation and ..
  38. Baker J, Shelton L, Zheng D, Favretto F, Nordhues B, Darling A, et al. Human cyclophilin 40 unravels neurotoxic amyloids. PLoS Biol. 2017;15:e2001336 pubmed publisher
    ..Here we show that cyclophilin 40 (CyP40), a PPIase, dissolves tau amyloids in vitro...
  39. Peattie D, Hsiao K, Benasutti M, Lippke J. Three distinct messenger RNAs can encode the human immunosuppressant-binding protein FKBP12. Gene. 1994;150:251-7 pubmed
    b>FKBP12 is an 11.8-kDa protein that binds the potent immunosuppressants FK506 and rapamycin. When bound to FK506, FKBP12 forms an inhibitory complex with calcineurin and interferes with signal transduction in activated T lymphocytes...
  40. Hara K, Yonezawa K, Kozlowski M, Sugimoto T, Andrabi K, Weng Q, et al. Regulation of eIF-4E BP1 phosphorylation by mTOR. J Biol Chem. 1997;272:26457-63 pubmed
    ..b>FKBP12 complex acts to dephosphorylate/deactivate the p70 S6 kinase; thus, some mTOR mutants that have lost the ability ..
  41. Menotta M, Biagiotti S, Streppa L, Rossi L, Magnani M. Label-free quantification of Tacrolimus in biological samples by atomic force microscopy. Anal Chim Acta. 2015;884:90-6 pubmed publisher
    ..The AFM biosensor presented herein utilises the endogen drug receptor, FKBP12, to quantify Tacrolimus levels...
  42. Suzuki A, Saeki T, Ikuji H, Uchida C, Uchida T. Brown Algae Polyphenol, a Prolyl Isomerase Pin1 Inhibitor, Prevents Obesity by Inhibiting the Differentiation of Stem Cells into Adipocytes. PLoS ONE. 2016;11:e0168830 pubmed publisher
    ..We showed that Pin1 is required for the differentiation of stem cells into adipocytes. We propose that oral intake of brown algae polyphenol is useful for the treatment of obesity. ..
  43. Risal P, Shrestha N, Chand L, Sylvester K, Jeong Y. Involvement of prolyl isomerase PIN1 in the cell cycle progression and proliferation of hepatic oval cells. Pathol Res Pract. 2017;213:373-380 pubmed publisher
    ..In conclusion, Pin1 plays important role in the cell cycle progression and increase oval cells proliferation which may be crucial in chronic liver injury. ..
  44. Shimizu T, Uchida C, Shimizu R, Motohashi H, Uchida T. Prolyl isomerase Pin1 promotes proplatelet formation of megakaryocytes via tau. Biochem Biophys Res Commun. 2017;493:946-951 pubmed publisher
    ..Pin1 bound tau and promoted microtubule polymerization. Our results show that Pin1 serves as a positive regulatory molecule of proplatelet formation of MKs by enhancing the function of phosphorylated tau. ..
  45. Chen X, Liu M, Tian Y, Li J, Qi Y, Zhao D, et al. Cryo-EM structure of human mTOR complex 2. Cell Res. 2018;28:518-528 pubmed publisher
    ..Rictor and mSin1 together generate steric hindrance to inhibit binding of FKBP12-rapamycin to mTOR, revealing the mechanism for rapamycin insensitivity of mTORC2...
  46. Siekierka J, Wiederrecht G, Greulich H, Boulton D, Hung S, Cryan J, et al. The cytosolic-binding protein for the immunosuppressant FK-506 is both a ubiquitous and highly conserved peptidyl-prolyl cis-trans isomerase. J Biol Chem. 1990;265:21011-5 pubmed
    ..In addition, FKBP from all sources possesses peptidyl-prolyl cis-trans isomerase activity which can be specifically inhibited by FK-506. We conclude that FKBP may serve an important biological function in all eukaryotic cells. ..
  47. Vanwetswinkel S, Heetebrij R, van Duynhoven J, Hollander J, Filippov D, Hajduk P, et al. TINS, target immobilized NMR screening: an efficient and sensitive method for ligand discovery. Chem Biol. 2005;12:207-16 pubmed
    ..TINS can be used in competition mode, allowing rapid characterization of the ligand binding site. TINS may allow screening of targets that are difficult to produce or that are insoluble, such as membrane proteins. ..
  48. Wang L, Wang X, Ren Z, Tang W, Zou Q, Wang J, et al. Oxidative Folding of Conopeptides Modified by Conus Protein Disulfide Isomerase. Protein J. 2017;36:407-416 pubmed publisher
    ..Thus, conus protein disulfide isomerase functions not only as an enzyme that catalyses oxidative process but also a fusion partner in recombinant conotoxin expression. ..
  49. Karuppasamy M, Kusmider B, Oliveira T, Gaubitz C, Prouteau M, Loewith R, et al. Cryo-EM structure of Saccharomyces cerevisiae target of rapamycin complex 2. Nat Commun. 2017;8:1729 pubmed publisher
    ..Density, which we conclude is Avo3, occludes the FKBP12-rapamycin-binding site of Tor2's FRB domain rendering TORC2 rapamycin insensitive and recessing the kinase active ..
  50. Bultynck G, de Smet P, Rossi D, Callewaert G, Missiaen L, Sorrentino V, et al. Characterization and mapping of the 12 kDa FK506-binding protein (FKBP12)-binding site on different isoforms of the ryanodine receptor and of the inositol 1,4,5-trisphosphate receptor. Biochem J. 2001;354:413-22 pubmed
    We investigated the interaction of the 12 kDa FK506-binding protein (FKBP12) with two ryanodine-receptor isoforms (RyR1 and RyR3) and with two myo-inositol 1,4,5-trisphosphate (IP3) receptor isoforms (IP3R1 and IP3R3)...
  51. Ozdamar B, Bose R, Barrios Rodiles M, Wang H, Zhang Y, Wrana J. Regulation of the polarity protein Par6 by TGFbeta receptors controls epithelial cell plasticity. Science. 2005;307:1603-9 pubmed
    ..These studies define how an extracellular cue signals to the polarity machinery to control epithelial cell morphology. ..
  52. Caporale A, Mascanzoni F, Farina B, Sturlese M, Di Sorbo G, Fattorusso R, et al. FRET-Protease-Coupled Peptidyl-Prolyl cis-trans Isomerase Assay: New Internally Quenched Fluorogenic Substrates for High-Throughput Screening. J Biomol Screen. 2016;21:701-12 pubmed publisher
    ..Due to its simplicity and precision in the determination of extent of inhibition and reaction rates required for kinetic analysis, this assay offers many advantages over other commonly used assays. ..
  53. Nabet B, Roberts J, Buckley D, Paulk J, Dastjerdi S, Yang A, et al. The dTAG system for immediate and target-specific protein degradation. Nat Chem Biol. 2018;14:431-441 pubmed publisher
    ..The dTAG system pairs a novel degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest...
  54. Oda T, Yang Y, Uchinoumi H, Thomas D, Chen Izu Y, Kato T, et al. Oxidation of ryanodine receptor (RyR) and calmodulin enhance Ca release and pathologically alter, RyR structure and calmodulin affinity. J Mol Cell Cardiol. 2015;85:240-8 pubmed publisher
    ..We used fluorescent CaM, FKBP12.6, and domain-peptide biosensor (F-DPc10) to measure, directly in cardiac myocytes, (1) RyR2 activation by ..
  55. Storer Samaniego C, Suh J, Chattopadhyay A, Olivares K, Guy N, Sivils J, et al. The FKBP52 Cochaperone Acts in Synergy with β-Catenin to Potentiate Androgen Receptor Signaling. PLoS ONE. 2015;10:e0134015 pubmed publisher
    ..Our data suggest that co-regulation of AR by FKBP52 and β-catenin does not require FKBP52 PPIase catalytic activity, nor FKBP52 binding to Hsp90...
  56. Kosowicz J, Lee J, Peiffer B, Guo Z, Chen J, Liao G, et al. Drug Modulators of B Cell Signaling Pathways and Epstein-Barr Virus Lytic Activation. J Virol. 2017;91: pubmed publisher
    ..of rapamycin complex 2 (mTORC2) contributes to BCR-mediated lytic induction and that FK506-binding protein 12 (FKBP12) binding alone is not adequate to block activation...
  57. Zohlnhofer D, Klein C, Richter T, Brandl R, Murr A, Nührenberg T, et al. Gene expression profiling of human stent-induced neointima by cDNA array analysis of microscopic specimens retrieved by helix cutter atherectomy: Detection of FK506-binding protein 12 upregulation. Circulation. 2001;103:1396-402 pubmed
    ..patterns, such as downregulation of mammary-derived growth inhibitor and upregulation of FK506-binding protein 12 (FKBP12). Upregulation of FKBP12 was confirmed at the protein level in neointimal smooth muscle cells...
  58. Huang C, Hsu S. NMR assignments of the peptidyl-prolyl cis-trans isomerase domain of trigger factor from E. coli. Biomol NMR Assign. 2016;10:149-52 pubmed publisher
    ..Within the SBD, a peptidyl-prolyl cis-trans isomerase (PPIase) domain is inserted leading to an unusual domain insertion, which may provide stabilizing effect to the highly ..
  59. Sengupta P, Satpute Krishnan P, Seo A, Burnette D, Patterson G, Lippincott Schwartz J. ER trapping reveals Golgi enzymes continually revisit the ER through a recycling pathway that controls Golgi organization. Proc Natl Acad Sci U S A. 2015;112:E6752-61 pubmed publisher
    ..from an artifact involving an endogenous ER-localized 13-kD FK506 binding protein (FKBP13) competing with the FKBP12-tagged Golgi enzyme for binding to an FKBP-rapamycin binding domain (FRB)-tagged ER trap...
  60. Dongsheng Z, Zhiguang F, Junfeng J, Zifan L, Li W. Cyclophilin A Aggravates Collagen-Induced Arthritis via Promoting Classically Activated Macrophages. Inflammation. 2017;40:1761-1772 pubmed publisher
    ..transcriptional activity of NF-?B, the pivotal transcriptional factor regulating M1 polarization, dependent of its PPIase activity...
  61. Chen H, Mustafi S, LeMaster D, Li Z, Heroux A, Li H, et al. Crystal structure and conformational flexibility of the unligated FK506-binding protein FKBP12.6. Acta Crystallogr D Biol Crystallogr. 2014;70:636-46 pubmed publisher
    The primary known physiological function of FKBP12.6 involves its role in regulating the RyR2 isoform of ryanodine receptor Ca(2+) channels in cardiac muscle, pancreatic β islets and the central nervous system...
  62. Ruer Laventie J, Simoni L, Schickel J, Soley A, Duval M, Knapp A, et al. Overexpression of Fkbp11, a feature of lupus B cells, leads to B cell tolerance breakdown and initiates plasma cell differentiation. Immun Inflamm Dis. 2015;3:265-79 pubmed publisher
  63. Dawar F, Tu J, Xiong Y, Lan J, Dong X, Liu X, et al. Chemotactic Activity of Cyclophilin A in the Skin Mucus of Yellow Catfish (Pelteobagrus fulvidraco) and Its Active Site for Chemotaxis. Int J Mol Sci. 2016;17: pubmed publisher
    ..enzymes, including cyclophilin A (CypA), a multi-functional protein with peptidyl-prolyl cis/trans isomerase (PPIase) activity. Beside various other immunological functions, CypA induces leucocytes migration in vitro in teleost...
  64. Vivoli M, Renou J, Chevalier A, Norville I, Diaz S, Juli C, et al. A miniaturized peptidyl-prolyl isomerase enzyme assay. Anal Biochem. 2017;536:59-68 pubmed publisher
    ..g. cardiovascular disease, cancer and Alzheimer's. The development of novel PPIase inhibitors has been limited by the lack of a rapid, laboratory-based assay for these enzymes, as their substrates ..
  65. Ojima Kato T, Yamamoto N, Nagai S, Shima K, Akiyama Y, Ota J, et al. Application of proteotyping Strain Solution™ ver. 2 software and theoretically calculated mass database in MALDI-TOF MS typing of Salmonella serotype. Appl Microbiol Biotechnol. 2017;101:8557-8569 pubmed publisher
    ..L17, L21, L25, and S7, Mn-cofactor-containing superoxide dismutase (SodA), peptidyl-prolyl cis-trans isomerase C (PPIase C), and protein Gns, and uncharacterized proteins YibT, YaiA, and YciF, that can allow serotyping of Salmonella...
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    ..analysis of FKBP family proteins revealed that the eight known Drosophila FKBPs share homology with the human FKBP12. This indicates a close evolutionary relationship, and possible origination from a common ancestor...
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    ..the absence of immunosuppressive ligands, is the modulation of intracellular calcium release channel function by FKBP12 and FKBP12.6...
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    ..strength-dependent studies have been carried out on the B3 domain of protein G (GB3) as well as on the immunophilin FKBP12 and a H87V variant of that protein in which the major conformational exchange linebroadening transition is ..
  69. Caraveo G, Soste M, Cappelleti V, Fanning S, van Rossum D, Whitesell L, et al. FKBP12 contributes to ?-synuclein toxicity by regulating the calcineurin-dependent phosphoproteome. Proc Natl Acad Sci U S A. 2017;114:E11313-E11322 pubmed publisher
    ..through the recruitment and inhibition of the 12-kDa cis-trans proline isomerase FK506-binding protein (FKBP12)...
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    ..The differences reflect the influence of intermolecular crystal contacts and have implications for interpretation of the interaction of the FK506/FKBP complex with its putative biological receptor. ..
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    ..Here, we show that FkpA, a heat shock periplasmic peptidyl-prolyl cis/trans isomerase (PPIase), suppresses the formation of inclusion bodies from a defective-folding variant of the maltose-binding protein, ..
  72. Bultynck G, Rossi D, Callewaert G, Missiaen L, Sorrentino V, Parys J, et al. The conserved sites for the FK506-binding proteins in ryanodine receptors and inositol 1,4,5-trisphosphate receptors are structurally and functionally different. J Biol Chem. 2001;276:47715-24 pubmed
    ..with the type 1 and type 3 inositol 1,4,5-trisphosphate receptor (IP(3)R1 and IP(3)R3), using a quantitative GST-FKBP12 and GST-FKBP12.6 affinity assay. We first characterized and mapped the interaction of the FKBPs with the RyR3...
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    ..The numbers of neurons recognized with the anti-FKBP 12 or anti-RyR (type 1 and 2) antibodies were counted in the anterior horn of spinal cords from the MND cases and ..
  74. Yamaguchi T, Kurisaki A, Yamakawa N, Minakuchi K, Sugino H. FKBP12 functions as an adaptor of the Smad7-Smurf1 complex on activin type I receptor. J Mol Endocrinol. 2006;36:569-79 pubmed
    The cytoplasmic immunophilin FKBP12, a 12 kDa FK506-binding protein, has been shown to act as an inhibitor for transforming growth factor-beta (TGF-beta) signaling...
  75. Liu F, Liu T, Kung F. FKBP12 regulates the localization and processing of amyloid precursor protein in human cell lines. J Biosci. 2014;39:85-95 pubmed
    ..We have previously demonstrated that AICD interacts with FKBP12, a peptidyl-prolyl cis-trans isomerase (PPIase) ubiquitous in nerve systems...
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    ..such as everolimus are allosteric mTOR inhibitors acting through interaction with the intracellular immunophilin FKBP12, a prolyl isomerase with different cellular functions...
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    The FK506-binding protein 12 (FKBP12) is a cytoplasmic protein and has been reported to possess multiple functions in signaling transduction based on its interaction with different cellular targets...
  79. DiLella A, Craig R. Exon organization of the human FKBP-12 gene: correlation with structural and functional protein domains. Biochemistry. 1991;30:8512-7 pubmed
    ..The function of rotamase activity in cells and the role of FKBP-12 in immunoregulation is uncertain...
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    ..FKBP-12 is a peptidyl-prolyl isomerase (PPIase), and the structures of the complexes suggest ways in which this catalytic activity could operate...
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  82. Cheng S, Bishop J. Suppressor of Fused represses Gli-mediated transcription by recruiting the SAP18-mSin3 corepressor complex. Proc Natl Acad Sci U S A. 2002;99:5442-7 pubmed
    ..These results provide biochemical evidence that Su(fu) directly participates in modulating the transcriptional activity of Gli. ..
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    ..Our results highlight the importance of incorporating both genetic and clinical, demographic factors into dose prediction. ..
  84. Vervliet T, Parys J, Bultynck G. Bcl-2 and FKBP12 bind to IP3 and ryanodine receptors at overlapping sites: the complexity of protein-protein interactions for channel regulation. Biochem Soc Trans. 2015;43:396-404 pubmed publisher
    The 12- and 12.6-kDa FK506-binding proteins, FKBP12 (12-kDa FK506-binding protein) and FKBP12.6 (12...
  85. Batra J, Tjong H, Zhou H. Electrostatic effects on the folding stability of FKBP12. Protein Eng Des Sel. 2016;29:301-308 pubmed publisher
    ..experimental studies into electrostatic effects on the folding stability of the human 12-kD FK506 binding protein (FKBP12). This protein has a close homologue, FKBP12.6, with amino acid substitutions in only 18 of their 107 residues...
  86. Oh Y, Jeong K, Kim K, Lee Y, Jeong S, Kim S, et al. Cyclophilin B protects SH-SY5Y human neuroblastoma cells against MPP(+)-induced neurotoxicity via JNK pathway. Biochem Biophys Res Commun. 2016;478:1396-402 pubmed publisher
    ..CypB has peptidyl-prolyl cis-trans isomerase (PPIase) activity...
  87. Holland E, Goldstone J, Pessah I, Whitehead A, Reid N, Karchner S, et al. Ryanodine receptor and FK506 binding protein 1 in the Atlantic killifish (Fundulus heteroclitus): A phylogenetic and population-based comparison. Aquat Toxicol. 2017;192:105-115 pubmed publisher
    ..models for NDL PCB neurotoxicity, and we used sequencing databases to characterize teleost RyR and FK506 binding protein 12 or 12.6kDa (genes FKBP1A; FKBP1B), which promote NDL PCB-triggered Ca2+ dysregulation...
  88. Ghanakota P, Carlson H. Comparing pharmacophore models derived from crystallography and NMR ensembles. J Comput Aided Mol Des. 2017;31:979-993 pubmed publisher Growth factor receptor bound protein 2 (Grb2), Src SH2 homology domain (Src-SH2), FK506-binding protein 1A (FKBP12), and Peroxisome proliferator-activated receptor-? (PPAR-?)...
  89. Cameron A, Steiner J, Roskams A, Ali S, Ronnett G, Snyder S. Calcineurin associated with the inositol 1,4,5-trisphosphate receptor-FKBP12 complex modulates Ca2+ flux. Cell. 1995;83:463-72 pubmed
    The immunosuppressant drug FK506 binds to the immunophilin protein FKBP12 and inhibits its prolyl isomerase activity...
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    ..A and FK506, which inhibit CaN after forming complexes with cytoplasmic binding proteins (cyclophilin and FKBP12, respectively). We report here the crystal structures of full-length human CaN at 2...
  91. Rollins C, Rivera V, Woolfson D, Keenan T, Hatada M, Adams S, et al. A ligand-reversible dimerization system for controlling protein-protein interactions. Proc Natl Acad Sci U S A. 2000;97:7096-101 pubmed
  92. George C, Sorathia R, Bertrand B, Lai F. In situ modulation of the human cardiac ryanodine receptor (hRyR2) by FKBP12.6. Biochem J. 2003;370:579-89 pubmed
    ..The precise mode of interaction and modulation of the cardiac RyR (RyR2) channel by FKBP12/FKBP12.6 remains to be fully defined...