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Last update 08 May 2025

FKBP1B

Last update 08 May 2025

Basic Info

Synonyms

12.6 kDa FK506-binding protein, 12.6 kDa FKBP, calstabin 2

+ [18]

Introduction

Has the potential to contribute to the immunosuppressive and toxic effects of FK506 and rapamycin. PPIases accelerate the folding of proteins. It catalyzes the cis-trans isomerization of proline imidic peptide bonds in oligopeptides.

Drugs associated with FKBP1B

Argirhein

Target

FKBP1A x FKBP1B

Mechanism

FKBP12 inhibitors [+1]

Active Org.

China Pharmaceutical University

Originator Org.

China Pharmaceutical University

Active Indication

Arrhythmias, Cardiac

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with FKBP1B

100 Translational Medicine associated with FKBP1B

0 Patents (Medical) associated with FKBP1B

367

Literatures (Medical) associated with FKBP1B

01 Apr 2025·Anesthesiology

Protein Alterations in Patients with Delirium after Cardiac Surgery: An Exploratory Case–Control Substudy of the VISION Cardiac Surgery Biobank

Article

Author: Spence, Jessica ; Bashir, Shaheena ; Lamy, Andre ; Belley-Côté, Emilie ; McIntyre, William F. ; Sun, Tao ; Wang, Chew Yin ; Chan, Matthew T. V. ; Chong, Michael ; Devereaux, P. J. ; Brady, Katheryn ; Paré, Guillaume ; Whitlock, Richard P.

Background:Delirium is an acute state of confusion associated with adverse postoperative outcomes. Delirium is diagnosed clinically using screening tools; most cases go undetected. Identifying a delirium biomarker would allow for accurate diagnosis, application of therapies, and insight into causal pathways. To agnostically discover novel biomarkers of delirium, a case–control substudy was conducted using the Vascular Events in Surgery Patients Cohort Evaluation (VISION) Cardiac Surgery Biobank. The objective was to identify candidate biomarkers to investigate in future studies.Methods:The study gathered a convenience sample of 30 patients with delirium on postoperative day 1 matched to 30 controls by age, sex, ethnicity, center, and cardiopulmonary bypass time. The Olink Explore 3K platform was used to identify blood protein alterations on postoperative day 3. Protein concentrations were expressed as normalized protein expression units (log2 fold scale). Protein expression was compared between cases and controls using a paired t test and identified significantly different biomarkers based on a false discovery rate–adjusted P value of less than 0.05.Results:Of 2,865 unique serum proteins, 26 (0.9%) were significantly associated with delirium status; all were elevated in cases versus controls at a false discovery rate of less than 0.05. Pathway analysis identified calcium-release channel activity (Padj = 0.02) and GTP-binding (Padj = 0.005) functions as characteristic of proteins associated with delirium. The top three differentially expressed biomarkers were FKBP1B (Padj = 0.003), C2CD2L (Padj = 0.004), and RAB6B (Padj = 0.004). The inflammatory biomarker interleukin-8 (CXCL8; mean difference = 2.36; P = 3.6 × 10−4) was also associated with delirium.Conclusions:The study identified 26 biomarkers significantly associated with delirium; all are novel except for interleukin-8. An association between delirium and recognized neuroinflammatory proteins or markers of brain injury was not identifed, which supports using biomarkers to differentiate between delirium and other neurologic conditions. While exploratory, the study’s findings support using biomarkers to diagnose postoperative delirium and validate using agnostic screens to identify potential delirium biomarkers.

26 Mar 2025·Investigative Ophthalmology & Visual Science

Topical Administration of Novel FKBP12 Ligand MP-004 Improves Retinal Function and Structure in Retinitis Pigmentosa Models

Article

Author: Vallejo-Illarramendi, Ainara ; Milla-Navarro, Santiago ; Ruiz-Ederra, Javier ; Sagartzazu-Aizpurua, Maialen ; Escudero-Arrarás, Leire ; Miranda, José Ignacio ; Aizpurua, Jesús María ; de la Villa, Pedro ; Sarasola-Gastesi, Miren ; Gonzalez-Imaz, Klaudia ; de Munain, Adolfo López ; Rodríguez-Hidalgo, María ; Lara-López, Araceli

PurposeThis study evaluates the therapeutic potential of MP-004, a novel FKBP12 ligand, in the treatment of inherited retinal dystrophies (IRDs). MP-004 targets the FKBP12/RyR interaction, which is disrupted in several neurologic disorders with underlying oxidative stress.MethodsThe toxicity and efficacy of MP-004 were examined in vitro in 661W cells. Efficacy was evaluated in phototoxic and H2O2-induced damage using impedance assays, calcium imaging, and in situ PLA. In vivo, MP-004 efficacy was evaluated in the rd10 mouse model of retinitis pigmentosa (RP) by topical ocular instillation. Retinal function was assessed by electroretinography (ERG), visual acuity was measured using a water maze test, and retinal structure was analyzed morphometrically.ResultsMP-004 exhibited low toxicity (LD50: 1.22 mM) and effectively protected 661W cells from phototoxicity (EC50: 30.6 nM). Under oxidative stress conditions, MP-004 preserved the FKBP12.6/RyR2 interaction, restored cytosolic and endoplasmic reticulum calcium levels, and prevented cell death. In vivo, MP-004 significantly preserved retinal function in rd10 mice, with ERG wave amplitude increases of up to 50% in scotopic and 71% in photopic conditions, corresponding to rod and cone functions, respectively. Additionally, MP-004 improved visual acuity for low spatial frequency patterns and preserved retinal structure, with a 23% increase in outer nuclear layer thickness and preservation in the number of rods and cones and their segment length.ConclusionsMP-004 shows promise as a therapeutic agent for RP, preserving retinal structure and function, likely through modulation of the FKBP12.6/RyR2 interaction. Further studies are needed to explore its pharmacokinetics and efficacy in other IRD models.

06 Mar 2025·Current Medicinal Chemistry

Knockdown of FKBP12.6 may Cause Bladder Dysfunction in Mice by Affecting IP3R/TRPM4 Function

Article

Author: Wu, Ronghua ; Liu, Yu ; Wang, Jun ; wang, Yangcai ; Nyirimigabo, Eric ; Zhou, Hao ; Zhao, Jiang ; Zhai, Kui ; Zheng, Ji

Background:FKBP12.6 is a crucial calcium regulatory molecule involved in the regulation of bladder excitatory contraction. This study employed FKBP12.6 knockout mice to investigate the impact of FKBP12.6 on the expression and function of IP3R/TRPM4 and its subsequent effect on bladder contraction function.Methods:The study selected 129S2/SvPasCrl and FKBP12.6 knockout mice and constructed a Partial Bladder Outlet Obstruction (PBOO) mouse model. GSE1595 data were utilized to analyze calcium signaling pathway changes. Void spot assays, urodynamic tests, and visceromotor response were employed to evaluate bladder function, while HE staining was used to assess bladder morphology. Immunofluorescence, co-immunoprecipitation, and Western blot techniques were employed to detect the localization, expression, and binding changes of FKBP12.6, Inositol-1,4,5 trisphosphate Receptor (IP3R), and TRPM4.Results:FKBP12.6 was significantly downregulated in PBOO mice (0.9998±0.07 vs. 0.2911±0.04; p <0.05). The micturition frequency (31.42±4.93 vs. 12.17±3.186), bladder sensitivity (1.59 ± 0.22 vs. 3.57± 0.43; p<0.01), detrusor instability, and muscle strip sensitivity (3.470.51 vs. 5.77±0.35; p<0.01) were increased significantly in FKBP12.6 Knockout (KO) mice (p <0.05). FKBP12.6 knockout did not affect the expressions of IP3R and TRPM4 proteins, but FKBP12.6 directly bound to IP3R in mouse bladder detrusor. IP3R/TRPM4 pathway inhibitors, 2-APB and 9-PHE, notably inhibited detrusor sensitivity, micturition frequency, and urination urgency in FKBP12.6 KO mice.Conclusion:The expression of FKBP12.6 was decreased in the bladder of PBOO mice, and the deletion of FKBP12.6 may lead to bladder dysfunction in mice by affecting the functional activity of IP3R/TRPM4.

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FKBP1B

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