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Last update 23 Jan 2025

FABP6

Last update 23 Jan 2025

Basic Info

Synonyms

FABP6, fatty acid binding protein 6, fatty acid binding protein 6, ileal

+ [15]

Introduction

Binds to bile acids and is involved in enterohepatic bile acid metabolism. Required for efficient apical to basolateral transport of conjugated bile acids in ileal enterocytes (By similarity). In vitro binds to bile acids in the order: deoxycholic acid > cholic acid > chenodeoxycholic acid and respective BA conjugation modifies affinities in the order taurine-conjugated > glycine-conjugated > unconjugated bile acids. Stimulates gastric acid and pepsinogen secretion (By similarity). Essential for the survival of colon cancer cells to bile acid-induced apoptosis.

Drugs associated with FABP6

Colesevelam Hydrochloride

Target

FABP6

Mechanism

FABP6 modulators

Active Org.

CHEPLAPHARM Arzneimittel GmbH [+2]

Originator Org.

Genzyme Corp.

Active Indication

Diabetes Mellitus, Type 2 [+3]

Inactive Indication

Diabetes Mellitus, Noninsulin-Dependent, 2 [+1]

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date26 May 2000

Colestyramine

Target

FABP6

Mechanism

FABP6 modulators

Active Org.

Albireo Pharma, Inc.

Originator Org.

Albireo Pharma, Inc.

Active Indication

Bile acid malabsorption

Inactive Indication

Cholestasis, Progressive Familial Intrahepatic 1 [+1]

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

SKF-97426

Target

FABP6

Mechanism

FABP6 modulators

Active Org.-

Originator Org.

GSK Plc

Active Indication-

Inactive Indication

Hypercholesterolemia

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with FABP6

ISRCTN68585853

/ RecruitingPhase 2

A randomised, double-blind, multicentre, international placebo-controlled phase II study aimed at investigating the efficacy and safety of a novel modified-release tablet formulation of colesevelam hydrochloride in patients with idiopathic bile acid diarrhoea

Start Date16 Dec 2024

Sponsor / Collaborator

Cosmo Technologies Ltd.

NCT06197763

/ Not yet recruitingPhase 1/2IIT

Impact of Therapy Using Colesevelam Treatment Reducing Bile Acids in Patients With Fontan Circulation (MYSTIC) Pilot Study.

This is the first pilot study proposing a novel therapeutic option treating patients with Fontan circulation (FC), a high-risk condition that has no definite treatment options available, other than heart or heart-liver transplantation. The investigator's identification of elevated BA and their association with adverse clinical - investigational features in Fontan patients are novel.

Start Date01 Jun 2024

Sponsor / Collaborator

St. Boniface Hospital

CTR20233461

/ RecruitingPhase 3

评价盐酸考来维仑片在原发性高胆固醇血症患者中的有效性和安全性：一项随机、双盲、安慰剂对照、多中心 III 期临床研究

[Translation] Evaluation of the efficacy and safety of colesevelam hydrochloride tablets in patients with primary hypercholesterolemia: a randomized, double-blind, placebo-controlled, multicenter phase III clinical study

主要目的：评价盐酸考来维仑片在原发性高胆固醇血症患者中的有效性。次要目的：评价盐酸考来维仑片在原发性高胆固醇血症患者中的安全性。

[Translation]

Primary objective: To evaluate the efficacy of colesevelam hydrochloride tablets in patients with primary hypercholesterolemia. Secondary objective: To evaluate the safety of colesevelam hydrochloride tablets in patients with primary hypercholesterolemia.

Start Date22 Dec 2023

Sponsor / Collaborator

Zhejiang Jingxin Pharmaceutical Co., Ltd.

100 Clinical Results associated with FABP6

100 Translational Medicine associated with FABP6

0 Patents (Medical) associated with FABP6

441

Literatures (Medical) associated with FABP6

01 Jan 2025·Protein Science

Structural dynamics and binding of Caenorhabditis elegans lifespan‐extending lipid binding protein‐3 to polyunsaturated fatty acids

Article

Author: Ortlund, Eric A. ; Wang, Meng C. ; Tillman, Matthew C. ; Cuevas, André R.

AbstractIntracellular lipid binding proteins (iLBPs) play crucial roles in lipid transport and cellular metabolism across the animal kingdom. Recently, a fat‐to‐neuron axis was described in Caenorhabditis elegans, in which lysosomal activity in the fat liberates polyunsaturated fatty acids (PUFAs) that signal to neurons and extend lifespan with durable fecundity. In this study, we investigate the structure and binding mechanisms of a lifespan‐extending lipid chaperone, lipid binding protein‐3 (LBP‐3), which shuttles dihomo‐γ‐linolenic (DGLA) acid from intestinal fat to neurons. We present the first high‐resolution crystal structure of LBP‐3, which reveals a classic iLBP fold with an unexpected and unique homodimeric arrangement via interstrand interactions that is incompatible with ligand binding. We identify key ionic interactions that mediate DGLA binding within the lipid binding pocket. Molecular dynamics simulations further elucidate LBP‐3's preferential binding to DGLA due to its rotational freedom and access to favorable binding conformations compared to other 20‐carbon PUFAs. We also propose that LBP‐3 dimerization may be a unique regulatory mechanism for lipid chaperones.

01 Dec 2024·Luminescence

Polyethylene Glycol‐Based Refolding Kinetic Modulation of CRABP I Protein

Article

Author: Sahoo, Harekrushna ; Subadini, Suchismita ; Bera, Krishnendu ; Behera, Devi Prasanna ; Hritz, Jozef

ABSTRACTCrowding environment has a significant impact on the folding and stability of protein in biological systems. In this work, we have used four different sizes of a molecular crowder, polyethylene glycol (PEG), to analyze the unfolding and refolding kinetics of an iLBP protein, CRABP I, using urea as chemical denaturant. In general, the stability of the native state of the protein is boosted by the presence of crowding agents in the solution. However, our findings show that not only the type of crowder but also the crowder size played a key role in the effects of excluded volume. In case of lower molecular weight of PEG (M.W. 400), even at 200 g/L concentration, only the viscosity effect is observed, whereas for higher molecular weight of PEG (M.W. 1000), both the viscosity effect and excluded volume effect are noticed, and even at a higher concentration (200 g/L) of PEG 1000, the excluded volume predominates over the viscosity effect. Using the transition state theory, we were also able to determine the free energies of activation for the unfolding and refolding studies from their respective rate constants. Additionally, MD simulation studies provide strong support for our experimental observation. Analysis of secondary structure propensity (SSP) reveals a marked decline in the presence of structural elements (β‐sheet, β‐bridge, turn, and α‐helix) from 81% to 43% over the 1 μs time scale unfolding MD simulation under 8 M urea conditions. Conversely, in a 200 ns refolding simulation, the rate of refolding notably increases at a concentration of 200 g/L PEG 1000.

23 Nov 2024·Translational Neuroscience

Identifying key biomarkers and therapeutic candidates for post-COVID-19 depression through integrated omics and bioinformatics approaches

Article

Author: Wang, Yue ; Zhang, Haidong ; Zhang, Qiyao ; Zhou, Yi ; Yang, Chunhua ; Sui, Xingling ; Dong, Hongyu ; Zhou, Jing

AbstractIntroductionDepression, the leading cause of disability worldwide, is known to be exacerbated by severe acute respiratory syndrome coronavirus 2 infection, worsening coronavirus disease 2019 (COVID-19) outcomes. However, the mechanisms and treatments for this comorbidity are not well understood.MethodsThis study utilized Gene Expression Omnibus datasets for COVID-19 and depression, combined with protein–protein interaction networks, to identify key genes. Gene ontology and Kyoto Encyclopedia of Genes and Genomes analyses were performed to understand gene functions. The CIBERSORT algorithm and NetworkAnalyst were used to examine the relationship of immune cell infiltration with gene expression and to predict transcription factors (TFs) and microRNAs (miRNAs) interactions. The Connectivity Map database was used to predict drug interactions with these genes.ResultsTRUB1, PLEKHA7, and FABP6 were identified as key genes enriched in pathways related to immune cell function and signaling. Seven TFs and nineteen miRNAs were found to interact with these genes. Nineteen drugs, including atorvastatin and paroxetine, were predicted to be significantly associated with these genes and potential therapeutic agents for COVID-19 and depression.ConclusionsThis research provides new insights into the molecular mechanisms of post-COVID-19 depression and suggests potential therapeutic strategies, marking a step forward in understanding and treating this complex comorbidity.

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