FKBP1A (also known as FKBP12) is notable in humans for binding the immunosuppressant molecule tacrolimus (originally designated FK506), which is used in treating patients after organ transplant and patients with autoimmune disorders. [3]

It is also commonly referred to as FKBP-12 or FKBP12 and is a member of a family of FK506-binding proteins .

FKBP12, the 12-kDa FK506-binding protein, is a ubiquitous abundant protein that acts as a receptor for the immunosuppressant drug FK506, binds tightly to intracellular calcium release channels and to the transforming growth factor β (TGF-β) type I receptor.

In this review, we have summarized the information from a study on FKBP12 (FK506 binding protein 12 kDa) with a view to understand its drug-free, physiological roles in transcription of ribosomal protein gene in Saccharomyces cerevisiae.

2001年2月20日 · FKBP12, the 12-kDa FK506-binding protein, is a ubiquitous abundant protein that acts as a receptor for the immunosuppressant drug FK506, binds tightly to intracellular calcium release channels and to the transforming growth factor β (TGF-β) type I receptor.

FK506 binding proteins (FKBPs) are a family of highly conserved proteins in eukaryotes. The prototype of this protein family, FKBP12, is the binding partner for immunosuppressive drugs FK506 and rapamycin. FKBP12 functions as a cis/trans peptidyl prolyl isomerase (PPIase) that catalyzes interconversion between prolyl cis/trans conformations ...

The prototype of this protein family, FKBP12, is the binding partner for immunosuppressive drugs FK506 and rapamycin. FKBP12 functions as a cis/trans peptidyl prolyl isomerase (PPIase) that catalyzes interconversion between prolyl cis/trans conformations.

2020年5月21日 · The 12-kDa FK506-binding protein (FKBP12) is the target of the commonly used immunosuppressive drug FK506. The FKBP12-FK506 complex binds to calcineurin and inhibits its activity, leading to immunosuppression and preventing organ transplant rejection.

2022年12月22日 · The primary target of FK506 in cells is FKBP12; therefore, we tested whether SLF and rapamycin, other FKBP12 inhibitors, can recapitulate the activity of FK506. Both chemicals suppressed cell growth specifically in EMM + S medium, similar to FK506.

2018年12月5日 · FKBP12 and FKBP12.6 are well documented components of RyR complexes, which intracellularly amplify Ca 2+-signaling in myocytes to evoke muscle contraction.

Know comprehensive FKBP12 protein information including protein sequence, molecular weight, theoretical pI, structure, function and protein interaction.

The immunophilin FKBP12 binds to TGF-β family type I receptors, including the BMP type I receptor ALK2. FKBP12 keeps the type I receptor in an inactive state and controls signaling activity. Removal of FKBP12 with drugs such as the FKBP-ligand FK506 enhances BMP activity in various cell types.

2023年1月12日 · The most recently discovered natural FKBP12 ligand, WDB002, was identified in 2020 as a potential FKBP12-binding partner when the genomes of Streptomyces malaysiensis isolates were analyzed for gene clusters similar to those involved in the biosynthesis of rapamycin and FK506. During this search, a series of natural products was identified ...

2002年6月15日 · Results: We found that growth inhibition induced by FK506 is abolished in FKBP12-deficient cells but not in FKBP12.6-deficient cells. Conclusions: FKBP12 is the only FKBP family member that plays a key role in immunosuppressant-mediated immunosuppression.

2011年3月3日 · To investigate the physiological role of FKBP12 in the heart, we created and analyzed cardiomyocyte-restricted FKBP12 conditional knockout (FKBP12 f/f /αMyHC-Cre) and FKBP12 overexpression transgenic (αMyHC-FKBP12) mice.

Some of the most studied regulatory proteins are FK506-binding proteins (FKBPs), which are cis-trans peptidi l-prolyl isomerases that bind the immunosuppressant drugs FK506 (Tacrolimus) and Rapamycin. 5 Two members of the FKBP family are expressed within mammalian cardiac myocytes: FKBP12 (12 KDa, also known as fkbp 1a or calstabin1) and FKBP12 ...

FK506 binding (FKBP) proteins are part of the highly conserved immunophilin family and its members have fundamental roles in the regulation of signalling pathways involved in inflammation, adaptive immune responses, cancer and developmental biology. The original member of this family, FKBP12, is a w …

2018年3月27日 · The binding of Ca 2+ to the EF-hand domain of FKBP12 or FKBP12.6 facilitates the transmembrane helices to form a pore and increases the plausibility of gate opening with large-amplitude collective motion. The suggested mechanism also explains the effect on gating induced by the binding of regulators to the cytoplasmic domain of RyR.

2011年4月4日 · We generated FKBP12 overexpressing transgenic (αMyHC-FKBP12) mice and cardiomyocyte-restricted FKBP12 conditional knockout (FKBP12 f/f /αMyHC-Cre) mice, and analyzed their cardiac electrophysiology in vivo and in vitro. A high incidence (38%) of sudden death was found in αMyHC-FKBP12 mice.

2023年1月30日 · The immunophilin FKBP12 binds to TGF-β family type I receptors, including the BMP type I receptor ALK2. FKBP12 keeps the type I receptor in an inactive state and controls signaling activity. Removal of FKBP12 with drugs such as the FKBP-ligand FK506 enhances BMP activity in various cell types.