Bile acid receptors as targets for drug development

Bile salt biotransformations by human intestinal bacteria

Ridlon, J. M., Kang, D.-J., & Hylemon, P. B. (2006) · Journal of Lipid Research · doi:10.1194/jlr.r500013-jlr200 · Cited by 2,829

Identification of a nuclear receptor for bile acids

Makishima, M., Okamoto, A. Y., Repa, J. J., Tu, H., Learned, R. M., Luk, A., Hull, M. V., Lustig, K. D., Mangelsdorf, D. J., & Shan, B. (1999) · Science · doi:10.1126/science.284.5418.1362 · Cited by 2,714

Gut microbiota regulates bile acid metabolism by reducing the levels of tauro-beta-muricholic acid, a naturally occurring FXR antagonist

Sayin, S. I., Wahlström, A., Felin, J., Jäntti, S., Marschall, H.-U., Bamberg, K., Angelin, B., Hyötyläinen, T., Orešič, M., & Bäckhed, F. (2013) · Cell Metabolism · doi:10.1016/j.cmet.2013.01.003 · Cited by 2,331

Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation

Watanabe, M., Houten, S. M., Mataki, C., Christoffolete, M. A., Kim, B. W., Sato, H., Messaddeq, N., Harney, J. W., Ezaki, O., Kodama, T., et al. (2006) · Nature · doi:10.1038/nature04330 · Cited by 2,220

The Enzymes, Regulation, and Genetics of Bile Acid Synthesis

Russell, D. W. (2003) · Annual Review of Biochemistry · doi:10.1146/annurev.biochem.72.121801.161712 · Cited by 2,069

A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis

Goodwin, B., Jones, S. A., Price, R. R., Watson, M. A., McKee, D. D., Moore, L. B., Galardi, C., Wilson, J. G., Lewis, M. C., Roth, M. E., et al. (2000) · Molecular Cell · doi:10.1016/s1097-2765(00)00051-4 · Cited by 1,940

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

Thomas, C., Gioiello, A., Noriega, L., Strehle, A., Oury, J., Rizzo, G., Macchiarulo, A., Yamamoto, H., Mataki, C., Pruzanski, M., et al. (2009) · Cell Metabolism · doi:10.1016/j.cmet.2009.08.001 · Cited by 1,885

Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis

Inagaki, T., Choi, M., Moschetta, A., Peng, L., Cummins, C. L., McDonald, J. G., Luo, G., Jones, S. A., Goodwin, B., Richardson, J. A., et al. (2005) · Cell Metabolism · doi:10.1016/j.cmet.2005.09.001 · Cited by 1,865

EASL Clinical Practice Guidelines: management of cholestatic liver diseases

European Association for the Study of the Liver (2009) · Journal of Hepatology · doi:10.1016/j.jhep.2009.04.009 · Cited by 1,729

A G Protein-coupled Receptor Responsive to Bile Acids

Kawamata, Y., Fujii, R., Hosoya, M., Harada, M., Yoshida, H., Miwa, M., Fukusumi, S., Habata, Y., Itoh, T., Shintani, Y., et al. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m209706200 · Cited by 1,628

Age-dependent pharmacokinetics of nifedipine in spontaneous hypertensive rats are associated with changes in gut microbiota and hepatic CYP3A1 expression

Xiong, Y., Xiong, Y., Yang, H., Guo, F., Yin, J., Liao, S., Chen, Z., Zhang, W., Zhou, H.-H., Weng, C., et al. (2025) · Drug Metabolism and Disposition · doi:10.1016/j.dmd.2025.100116 · Cited by 1

Work in Progress

Webb, G. J., & Hirschfield, G. M. (2018) · Clinics in Liver Disease · doi:10.1016/j.cld.2018.03.004 · Cited by 1

A phenotypic approach to probing cellular outcomes using heterobivalent constructs

Bhadoria, R., Ping, K., Lohk, C., Järving, I., & Starkov, P. (2020) · Chemical Communications · doi:10.1039/c9cc09595k · Cited by 1

INSIGHTS INTO THE IMPACT OF FXR ACTIVATION ON HEPATIC AUTOPHAGY IN A NON-ALCOHOLIC STEATOHEPATITIS MODEL

Tawfiq, R. A., Attia, Y. M., Nassar, N. N., Hammam, O. A., Elmazar, M. M., & Abdallah, D. M. (2021) · Bulletin of Pharmaceutical Sciences Assiut · doi:10.21608/bfsa.2021.174153 · Cited by 1

Mechanisms of Bile Formation and the Pathogenesis of Cholestasis

Karpen, S. J. (2021) · Cambridge University Press eBooks · doi:10.1017/9781108918978.003 · Cited by 1

An Update on Management of Nonalcoholic Fatty Liver Disease & Nonalcoholic Steatohepapititis is the Time Ripe for Achieving Resolution of NAFLD & NASH Soon

Kaur, K. K., Allahbadia, G., & Singh, M. (2021) · Journal of Endocrinology Research · doi:10.30564/jer.v3i2.3580 · Cited by 1

Avenir de la chirurgie bariatrique au-delà de la surcharge pondérale : la chirurgie métabolique

Caiazzo, R. J., Marciniak, C., Rémond, A., Baud, G., & Pattou, F. N. (2023) · Journal de Chirurgie Viscérale · doi:10.1016/j.jchirv.2023.01.002 · Cited by 1

Primary Biliary Cholangitis (Formerly Primary Biliary Cirrhosis)

Trivedi, P. J., & Hirschfield, G. M. (2019) · Wiley eBooks · doi:10.1002/9781119211419.ch38 · Cited by 1

Hepatobiliary Diseases

Pirschel, W., & Kremer, A. E. (2016) · Springer eBooks · doi:10.1007/978-3-319-33142-3_34 · Cited by 1

A physiologically-based model of bile acid metabolism in humansPreprint

Kister, B., Blank, L. M., Pollmanns, M. R., Wirtz, T. H., & Kuepfer, L. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.07.19.665677 · Cited by 1

Gut microbial regulation of bile acid metabolism and signaling

Sayin, S. I. (2016) · Gothenburg University Publications Electronic Archive (Gothenburg University)

Bile Acids and NAFLD/NASH

Kitamura, T., & Watanabe, S. (2017) · Springer eBooks · doi:10.1007/978-4-431-56062-3_10

Liver immunology and Cross-talk

Iqbal, A., & Shalimar (2016) · Tropical Gastroenterology · doi:10.7869/tg.368

Microbial modulation of metabolic diseases

Molinaro, A. (2018) · Gothenburg University Publications Electronic Archive (Gothenburg University)

Was der (Viszeral-)Chirurg als neue Erkenntnisse über die Gallensäuren und deren Zusammenspiel mit dem Darmmikrobiom wissen sollte

Schönfeld, P., & Meyer, F. P. (2020) · Zeitschrift für Gastroenterologie · doi:10.1055/a-1071-8219

Investigations of 12α-Hydroxylated Bile Acid Signaling in Intestinal Organoids

Ahmad, T. R. (2019) · doi:10.7916/d8-gv4d-bm97

Role of bile acid receptors in the regulation of cardiovascular diseases

Shiozaki, Y., Keenan, A. L., & Miyazaki, M. (2020) · Elsevier eBooks · doi:10.1016/b978-0-12-819404-1.00020-8

Pharmacological Options for NASH

Stern, C., & Ratziu, V. (2020) · Springer eBooks · doi:10.1007/978-3-319-95828-6_17

Review: Uremic Toxins and Gut Microbiome

Suzuki, T., & Abe, T. (2020) · Springer eBooks · doi:10.1007/978-981-15-7793-2_2

Bile Acids and Bilirubin in Liver Immunology

Zhu, C., Claudel, T., & Trauner, M. (2020) · Springer eBooks · doi:10.1007/978-3-030-51709-0_7

Gut Microbiome and Liver Cancer

McVey, J. C., Zhang, Q., Greten, T. F., & Ma, C. (2021) · Physiology in health and disease · doi:10.1007/978-3-030-67951-4_7

The Relationship between Bile Acid Metabolism and Colorectal Polyps

董, 书. (2021) · Advances in Clinical Medicine · doi:10.12677/acm.2021.116369

Targeting bile salt-FGF19 signaling

Chang, X. (2021) · Research Publications (Maastricht University) · doi:10.26481/dis.20211026xc

Faculty Opinions recommendation of Lipid signaling and lipotoxicity in metaflammation: indications for metabolic disease pathogenesis and treatment.

Weiss, L. M. (2019) · Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature · doi:10.3410/f.726441904.793562577

Faculty Opinions recommendation of Farnesoid X receptor agonist INT-767 attenuates liver steatosis and inflammation in rat model of nonalcoholic steatohepatitis.

Aguilar-Salinas, C. A. (2019) · Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature · doi:10.3410/f.733689584.793558336

Peroxisomal Disorders

Wanders, R. J. A., & Waterham, H. R. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-812535-9.00015-7 · Cited by 1

Postoperative liver (dys)function

van Mierlo, K. M. C. (2022) · Research Publications (Maastricht University) · doi:10.26481/dis.20220708km

Development of a mouse model for postresectional liver failurePreprint

van Mierlo, K. M. C., Himbeeck, C. V., Lebrun, V., Jansen, P. L. M., Dejong, C. H. C., Leclercq, I. A., Damink, S. W. M. O., & Schaap, F. G. (2022) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2022.11.10.515992

The FXR agonist obeticholic acid does not stimulate liver regeneration in hepatectomized micePreprint

van Mierlo, K. M. C., Dahrenmöller, C., Lebrun, V., Jansen, P. L. M., Dejong, C. H. C., Leclercq, I. A., Damink, S. W. M. O., & Schaap, F. G. (2022) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2022.11.10.515905

A Study to Evaluate Relative Bioavailability, Food Effect, and Pharmacodynamics of Tropifexor, a Farnesoid X Receptor Agonist, in Healthy Participants

Stringer, R. A., Chen, J., Shah, B., Gu, J., Zhang, Y., Prince, W., Klickstein, L. B., & Woessner, R. (2022) · Clinical Pharmacology in Drug Development · doi:10.1002/cpdd.1208

Pathophysiology of Bile Acid Regulation

Sujka, J. A., & DuCoin, C. G. (2023) · Springer eBooks · doi:10.1007/978-3-031-25828-2_7

Distal Feeding and Hydration

Lacaze, L., Picot, D., & Thibault, R. (2023) · Springer eBooks · doi:10.1007/978-3-031-22265-8_43

Cholapod and Cholaphanes for Recognition of Anions

Chahar, M., Khaturia, S., & Bishnoi, A. (2023) · Current Organic Chemistry · doi:10.2174/0113852728272205231122055645

[Lithocholic acid decreases mRNA stability of nuclear receptor PPARα by upregulating miR-21 expression in hepatoma HepG2 cells].

Pang, B., Huang, N., Huang, X., Li, X., Xiong, W., Kong, B., & Yao, Y. (2023) · PubMed Central · doi:10.12122/j.issn.1673-4254.2023.12.13

Research Progress of Cholestatic Liver Disease-Related Pruritus in Chinese Medicine and Western Medicine

Dai, W., & Nie, H. (2024) · Chinese medicine and natural products · doi:10.1055/s-0044-1787705

The relationship between obesity and gut microbiota

Cai, S. (2025) · Theoretical and Natural Science · doi:10.54254/2753-8818/2024.la19353

Research Progress on Rifaximin in Modulating Gut Microbiota for the Treatment of Nonalcoholic Fatty Liver Disease

范, 裕. (2025) · Advances in Clinical Medicine · doi:10.12677/acm.2025.151161

Microbiota-host interaction: a novel mechanism of gut microbiota in modulating bile acid metabolism to mitigate diarrhea

Gao, R., & Liu, G. (2025) · Scientia Sinica Vitae · doi:10.1360/ssv-2025-0053

Chemical dissection of sterol and bile acid signaling via clickable photoaffinity probes

Xu, M., Chen, X., Ma, J., & Yang, X. (2025) · Biophysics Reports · doi:10.52601/bpr.2025.250029

Bile acids for metabolic dysfunction-associated steatotic liver disease in adults

Ashmawy, R. E., Blyuss, O. B., Nikolova, D., Pavlov, C. S., Gluud, C. N., & Andrenacci, P. J. (2025) · Cochrane Database of Systematic Reviews · doi:10.1002/14651858.cd014850

Secondary bile acid lithocholic acid ameliorates colitis-like inflammation in a human intestine-on-chip system

Kaden, T., Allwang, M., Stallhofer, J., Graf, K., Raasch, M., & Mosig, A. S. (2026) · Frontiers in Immunology · doi:10.3389/fimmu.2026.1761539

Additional file 2 of The gut metagenomics and metabolomics signature in patients with inflammatory bowel disease

Xu, X., Ocansey, D. K. W., Hang, S., Wang, B., Amoah, S., Yi, C., Zhang, X., Liu, L., & Mao, F. (2022) · Figshare · doi:10.6084/m9.figshare.20115656

Additional file 1 of The gut metagenomics and metabolomics signature in patients with inflammatory bowel disease

Xu, X., Ocansey, D. K. W., Hang, S., Wang, B., Amoah, S., Yi, C., Zhang, X., Liu, L., & Mao, F. (2022) · Figshare · doi:10.6084/m9.figshare.20115653

Additional file 3 of The pregnane X receptor drives sexually dimorphic hepatic changes in lipid and xenobiotic metabolism in response to gut microbiota in mice

Barretto, S. A., Lasserre, F., Huillet, M., Régnier, M., Polizzi, A., Lippi, Y., Fougerat, A., Person, E., Bruel, S., Bétoulières, C., et al. (2021) · Figshare · doi:10.6084/m9.figshare.14456699

Additional file 13 of The pregnane X receptor drives sexually dimorphic hepatic changes in lipid and xenobiotic metabolism in response to gut microbiota in mice

Barretto, S. A., Lasserre, F., Huillet, M., Régnier, M., Polizzi, A., Lippi, Y., Fougerat, A., Person, E., Bruel, S., Bétoulières, C., et al. (2021) · Figshare · doi:10.6084/m9.figshare.14456690

Additional file 1 of Gut microbial metabolite deoxycholic acid facilitates Th17 differentiation through modulating cholesterol biosynthesis and participates in high-fat diet-associated colonic inflammation

Li, D., Zhou, J., Wang, L., Gong, Z., Le, H., Huang, Y., Xu, C., Tian, C., Cai, W., & Wu, J. (2023) · Figshare · doi:10.6084/m9.figshare.24240099

Additional file 2 of The pregnane X receptor drives sexually dimorphic hepatic changes in lipid and xenobiotic metabolism in response to gut microbiota in mice

Barretto, S. A., Lasserre, F., Huillet, M., Régnier, M., Polizzi, A., Lippi, Y., Fougerat, A., Person, E., Bruel, S., Bétoulières, C., et al. (2021) · Figshare · doi:10.6084/m9.figshare.14456696

Additional file 14 of The pregnane X receptor drives sexually dimorphic hepatic changes in lipid and xenobiotic metabolism in response to gut microbiota in mice

Barretto, S. A., Lasserre, F., Huillet, M., Régnier, M., Polizzi, A., Lippi, Y., Fougerat, A., Person, E., Bruel, S., Bétoulières, C., et al. (2021) · Figshare · doi:10.6084/m9.figshare.14456693

Additional file 1 of Oleanolic acid improved intestinal immune function by activating and potentiating bile acids receptor signaling in E. coli-challenged piglets

Xue, C., Jia, H., Cao, R., Cai, W., Hong, W., Tu, J., Wang, S., Jiang, Q., Bi, C., Shan, A., et al. (2024) · Figshare · doi:10.6084/m9.figshare.25853012

Additional file 8 of The pregnane X receptor drives sexually dimorphic hepatic changes in lipid and xenobiotic metabolism in response to gut microbiota in mice

Barretto, S. A., Lasserre, F., Huillet, M., Régnier, M., Polizzi, A., Lippi, Y., Fougerat, A., Person, E., Bruel, S., Bétoulières, C., et al. (2021) · Figshare · doi:10.6084/m9.figshare.14456714

Additional file 5 of The pregnane X receptor drives sexually dimorphic hepatic changes in lipid and xenobiotic metabolism in response to gut microbiota in mice

Barretto, S. A., Lasserre, F., Huillet, M., Régnier, M., Polizzi, A., Lippi, Y., Fougerat, A., Person, E., Bruel, S., Bétoulières, C., et al. (2021) · Figshare · doi:10.6084/m9.figshare.14456705

Additional file 10 of The pregnane X receptor drives sexually dimorphic hepatic changes in lipid and xenobiotic metabolism in response to gut microbiota in mice

Barretto, S. A., Lasserre, F., Huillet, M., Régnier, M., Polizzi, A., Lippi, Y., Fougerat, A., Person, E., Bruel, S., Bétoulières, C., et al. (2021) · Figshare · doi:10.6084/m9.figshare.14456681

Additional file 12 of The pregnane X receptor drives sexually dimorphic hepatic changes in lipid and xenobiotic metabolism in response to gut microbiota in mice

Barretto, S. A., Lasserre, F., Huillet, M., Régnier, M., Polizzi, A., Lippi, Y., Fougerat, A., Person, E., Bruel, S., Bétoulières, C., et al. (2021) · Figshare · doi:10.6084/m9.figshare.14456687

Additional file 11 of The pregnane X receptor drives sexually dimorphic hepatic changes in lipid and xenobiotic metabolism in response to gut microbiota in mice

Barretto, S. A., Lasserre, F., Huillet, M., Régnier, M., Polizzi, A., Lippi, Y., Fougerat, A., Person, E., Bruel, S., Bétoulières, C., et al. (2021) · Figshare · doi:10.6084/m9.figshare.14456684

Bile Physiology and Pathophysiology: A Comprehensive Narrative Review

Tavartkiladze, A. A., & Reiter, R. J. (2025) · International Journal of Science and Research (IJSR) · doi:10.21275/sr251219204625

Bile Acids and Healthy Ageing

Attema, B. J., & Kuipers, F. (2026) · Engineering · doi:10.1016/j.eng.2026.01.002 · Cited by 1

Exploring the interaction of obesity and allergy and the potential roles of gut microbiota in the development of this comorbidity in male mice

Miao, Z., Jiang, F., Li, J., Wu, S., Zhang, X., Mao, Y., Su, S., Han, W., He, F., Wu, X., et al. (2026) · International Journal of Obesity · doi:10.1038/s41366-026-02041-2

Étude du lien entre maladie alcoolique du foie, microbiote intestinal et acides biliaires : rôles spécifiques de la pectine et du récepteur aux acides biliaires TGR5

Spatz, M. (2018) · theses.fr (ABES) · doi:10.70675/b092156fz2e11z40fbza4cbz9262830ab0c1

Insights into the bidirectional interactions between the gut microbiota and the xenobiotic receptors CAR and PXR

Barretto, S. A. (2019) · theses.fr (ABES) · doi:10.70675/fa5edab1z50c0z4b21z96d3z01d01036532a

Rôle de LECT2 dans les maladies stéatosiques non alcooliques du foie

Pham, S. (2020) · theses.fr (ABES) · doi:10.70675/3693bfe6z9d91z4045za9a9zc37497dc9c1b

Identification de souches bactériennes à potentiel probiotique dans la diminution des hyperperméabilités intestinales et détermination de leur(s) mécanisme(s) d’action

Chamignon, C. (2020) · theses.fr (ABES) · doi:10.70675/4a201bc9z4ec7z4ccfza054z308f73c4fdd2

Influence of bile acids metabolism on hepatic immunity in mice

Guinot, V. (2022) · theses.fr (ABES) · doi:10.70675/b69bb11eza30fz4874z9af2za6e31b2d5ad8

Les bactéries comme actrices du microbiote intestinal entre inflammation, métabolisme des acides biliaires et interaction avec les bactériophages

Chaffringeon, L. (2022) · theses.fr (ABES) · doi:10.70675/5333e3cdz0991z4f94z82faz68b44fe0a84b

Etude de la zonation des voies métaboliques du glucose en fonction du statut nutritionnel : implication du récepteur nucléaire Farnesoid X Receptor (FXR)

Loubota, A. C. N. (2024) · theses.fr (ABES) · doi:10.70675/406936f5zb422z453ez84d1z38c3f35b82e9

Dihydromyricetin mitigates T2DM progression by modulating bile acid metabolism through SHP/PPARγ pathway

Lv, Q., Guan, Y., Bai, X., Wang, X., & Jiang, B. (2026) · Chinese Herbal Medicines · doi:10.1016/j.chmed.2026.04.002

Obeticholic acid accelerates portal vein embolization-induced liver hypertrophy in rabbits by improving bile salt homeostasis

Chang, X., Olthof, P. B., Jin, H., Chau, S., Soons, Z. I. T. A., van Eijk, H. M. H., van Golen, R. F., van Gulik, T. M., Jansen, P. L. M., Damink, S. W. M. O., et al. (2026) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2026.119368

Targeting cancer-associated fibroblast by biomimetic nanomissiles to remodel tumor stromal microenvironment for colorectal cancer liver metastasis

Wu, Y., Rong, C., Yi, J., Chen, G. D., 吴东平, Li, Z., Tang, W., Liang, X., & Wei, M. (2026) · Materials Today Advances · doi:10.1016/j.mtadv.2026.100799

On the use of UDCA beyond cholestatic liver disease: How bile acid-driven intestinal GLP-1 signalling keeps the joints healthy

Trampert, D. C. (2026) · Journal of Hepatology · doi:10.1016/j.jhep.2026.05.008

ACAT3 controls hepatic cholesterol metabolism and modulates systemic energy homeostasis of male mice

Ma, Z., Chen, Q., Zhang, J. Y., Huang, Z., Wu, Q., Shi, T., Liu, X., Shu, H., Ma, Y., Cheng, K., et al. (2026) · Life Sciences · doi:10.1016/j.lfs.2026.124519

Diet–Microbiota–Immune Interactions in Hepatocellular Carcinoma: An Immunometabolic and Spatial Perspective

Salem, A. E., Nassar, N., Emam, S. M., Negm, S. H., Talib, W. H., & Raposa, B. L. (2026) · Nutrients · doi:10.3390/nu18121911

Elevated circulating bile acids alleviate acute pancreatitis by restoring mitochondrial function via acinar cell uptake

Chen, H., Fan, Y., Huang, N., Wang, Q., Wang, B., Sun, J., Zhang, S., & Li, J. (2026) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.00172.2026

Bile Acid Metabolism in Gout Pathogenesis from Gut–Liver–Joint Crosstalk to Therapeutic Opportunities

Chen, B., Chen, X., Li, J., Gao, S., Wang, X. L., & Han, J. (2026) · Metabolites · doi:10.3390/metabo16070464

Impact of Gut Microbiota Metabolites on Serotonin Levels in Irritable Bowel Syndrome

Gao, N., Liu, Y., Sun, S., Bin, L., Li, S. N., Yang, T., Yang, W. F. Z., & Wu, J. (2026) · Gut Medicine · doi:10.1002/gtm2.70017

Engineered novel protease-stable multifunctional peptides attenuate metabolic dysfunction-associated steatotic liver disease via disrupting bile acid micelle and activating PPAR pathway

Li, Y. C., Deng, W., Li, Q., Zhou, C., Sun, N., Liu, W. T., Zhao, X., Xie, M., Zhu, M., Wang, X., et al. (2026) · Pharmacological Research · doi:10.1016/j.phrs.2026.108341

Chenodeoxycholic acid restrains tumor growth via TGR5-dependent type 1 dendritic cells cross-priming

Zeng, F., Zhao, F., Zhou, P., Li, Y., Wang, X., Hu, Y., Yu, J., Li, G., Yue, C., Feng, Y., et al. (2026) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-026-02777-3

Carbonate alkalinity disrupts the bile acid liver-gut axis and impairs growth in Carassius auratus

Yang, Y., Wu, S., Cheng, H., Jin, X., Liu, Q., You, S., Wang, J., & Sun, Y. (2026) · Water Biology and Security · doi:10.1016/j.watbs.2026.100702

The gut-liver axis in hepatic ischemia-reperfusion injury: from microbiota dysbiosis to remote organ dysfunction

de Oliveira, T. H. C., & Gonçalves, G. K. N. (2026) · Journal of Gastrointestinal Surgery · doi:10.1016/j.gassur.2026.102568

Chemical constituents from Hypericum japonicum and their PXR agonistic activity

Su, H., Yuan, F.-Y., & Zheng, L. (2026) · Phytochemistry Letters · doi:10.1016/j.phytol.2026.104247

Admission Gut and Plasma‐Derived Signatures Associated With Severity and 90‐day Outcome in Hepatitis A–Related and Drug‐Induced Acute Liver Failure

Saxena, A., Maiwall, R., Meena, B. L., Maras, J. S., Suroliya, V., Kumar, G., Sarin, S. K., & Trehanpati, N. (2026) · Journal of Medical Virology · doi:10.1002/jmv.71150

Bile acid-based therapeutics: recent advances in bile acid conjugates and derivatives

Seo, M., Lee, J.-H., Yang, S.-B., Ma, G., Lee, H., Han, J., Ryu, Y., & Park, J. (2026) · Journal of Pharmaceutical Investigation · doi:10.1007/s40005-026-00830-5

Thermo- and pH-responsive hydrogel film with embedded liquid crystal droplets for the optical detection of bile acids

Sharma, D., Nayak, N., Panda, A., Singhal, S., & Dan, A. (2026) · Colloids and Surfaces A Physicochemical and Engineering Aspects · doi:10.1016/j.colsurfa.2026.141991

From Structural Modification to Diverse Pharmacological Activities: Recent Advances and Future Perspectives of Bile Acids

Zhu, H., Chen, H., Gong, Q., Chen, Z., Zhang, C., Xu, J., & Wang, T. (2026) · Medicinal Research Reviews · doi:10.1002/med.70116

Targeted deoxycholic acid-loaded nanoliposomes enhance cell-associated uptake and modulate polarization-associated markers in THP-1-derived M2-like macrophages

Darmanto, W., Wahyuningsih, S. P. A., Dewi, F. R. P., Kafesa, A., Herdiansyah, M. A., Putri, R. A. R. K., Bin, L. K., & Abidin, I. Z. Z. (2026) · Scientific Reports · doi:10.1038/s41598-026-73503-w

Avaliação dos efeitos do d-limoneno no metabolismo de ácidos biliares hepáticos em camundongos c57/bl6

Genaro, B. (2021) · doi:10.11606/003069118

MOLECULAR PERSPECTIVES ON THE IMPACT OF INFLAMMATORY PROCESSES ON DRUG METABOLISM

Arcan, O. D., Vasincu, A., ABABEI, D.-C., Bulea, D., Macadan, I., RUSU, R.-N., Neamţu, M., & Bild, V. (2026) · FARMACIA · doi:10.31925/farmacia.2026.1.2

BindingDB Entry 50019878: Discovery of HPG1860, a Structurally Novel Nonbile Acid FXR Agonist Currently in Clinical Development for the Treatment of Nonalcoholic Steatohepatitis.

BindingDB (2024) · UC San Diego · doi:10.7270/q2pv6qsq

BindingDB Entry 50046196: Modification on ursodeoxycholic acid (UDCA) scaffold. discovery of bile acid derivatives as selective agonists of cell-surface G-protein coupled bile acid receptor 1 (GP-BAR1).

BindingDB (2016) · UC San Diego · doi:10.7270/q2wq05j5

BindingDB Entry 50001642: Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.

BindingDB (2020) · UC San Diego · doi:10.7270/q2r213xv

BindingDB Entry 50019592: Chemical exploration of TGR5 functional hot-spots: Synthesis and structure-activity relationships of C7- and C23-Substituted cholic acid derivatives.

BindingDB (2024) · UC San Diego · doi:10.7270/q2542szc

BindingDB Entry 50021045: Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation.

BindingDB (2025) · UC San Diego · doi:10.7270/q2d22375

BindingDB Entry 50013000: Structural modifications that increase gut restriction of bile acid derivatives.

BindingDB (2022) · UC San Diego · doi:10.7270/q2sj1qbt

BindingDB Entry 50017303: Discovery of (

BindingDB (2023) · UC San Diego · doi:10.7270/q2k35zr8

BindingDB Entry 50018775: Recent Progress on Bile Acid Receptor Modulators for Treatment of Metabolic Diseases.

BindingDB (2024) · UC San Diego · doi:10.7270/q2445rqn

BindingDB Entry 50002485: Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5).

BindingDB (2020) · UC San Diego · doi:10.7270/q2b56nch

BindingDB Entry 50011703: Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.

BindingDB (2022) · UC San Diego · doi:10.7270/q2df6vvn

BindingDB Entry 50017588: Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis.

BindingDB (2023) · UC San Diego · doi:10.7270/q2tt4w12

BindingDB Entry 50000464: Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).

BindingDB (2019) · UC San Diego · doi:10.7270/q2h997n6

BindingDB Entry 50046218: Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists.

BindingDB (2016) · UC San Diego · doi:10.7270/q261122x

Bile acid receptors as targets for drug

Schaap, G., Trauner, M. A., & Jansen, P. L. M. (2013)

Farnesoid X Receptor Agonists and Other Bile Acid Signaling Strategies for Treatment of Liver Disease

Halilbasic, E., Fuchs, C. D., Traussnigg, S., & Trauner, M. (2016) · Digestive Diseases · doi:10.1159/000445268 · Cited by 39

Bile Acid as Therapeutic Agents

Yamanashi, Y., Takada, T., & Suzuki, H. (2017) · Springer eBooks · doi:10.1007/978-4-431-56062-3_5 · Cited by 1

Recent Progress on Bile Acid Receptor Modulators for Treatment of Metabolic Diseases

Xu, Y. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00342 · Cited by 75

Bile Acid Receptor Therapeutics Effects on Chronic Liver Diseases

Meadows, V., Kennedy, L. L., Kundu, D., Alpini, G. D., & Francis, H. (2020) · Frontiers in Medicine · doi:10.3389/fmed.2020.00015 · Cited by 31