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.

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 ...

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.

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.

FKBP12 and various targets show differences in the FKBP12 binding surface, 26 providing a high degree of flexibility and improving the odds of binding with additional targets.

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.

2021年11月18日 · FKBP12 was first described in 1989 by Harding et al. and Siekierka et al. . With a molecular weight of 12 kDa, it is the smallest member of the FKBP family. It contains the PPIase core domain, which is found in many FKBPs. It occurs in most species and tissues and is essential for mammalian life.