Cargando…

Structure Optimization of 12β-O-γ-Glutamyl Oleanolic Acid Derivatives Resulting in Potent FXR Antagonist/Modulator for NASH Therapy

The farnesoid X receptor (FXR) plays a crucial role in regulating the metabolism of bile acids, lipids, and sugars. Consequently, it is implicated in the treatment of various diseases, including cholestasis, diabetes, hyperlipidemia, and cancer. The advancement of novel FXR modulators holds immense...

Descripción completa

Detalles Bibliográficos
Autores principales:	Ma, Hao, Bao, Yunyang, Niu, Shuaishuai, Wang, Shaorong, Li, Yiming, He, Hongwei, Zhang, Na, Fang, Weishuo
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	MDPI 2023
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10221314/ https://www.ncbi.nlm.nih.gov/pubmed/37242541 http://dx.doi.org/10.3390/ph16050758

Ejemplares similares

Design and Synthesis of a Dual Linker for Solid Phase Synthesis of Oleanolic Acid Derivatives
por: Wang, Shaorong, et al.
Publicado: (2011)

FXR and NASH: an avenue for tissue-specific regulation
por: Henry, Zakiyah, et al.
Publicado: (2023)

Discovery of Natural Products as Novel and Potent FXR Antagonists by Virtual Screening
por: Diao, Yanyan, et al.
Publicado: (2018)

Multiple pathways for the formation of the γ-glutamyl peptides γ-glutamyl-valine and γ- glutamyl-valyl-glycine in Saccharomyces cerevisiae
por: Sofyanovich, Olga A., et al.
Publicado: (2019)

Role of FXR in Bile Acid and Metabolic Homeostasis in NASH: Pathogenetic Concepts and Therapeutic Opportunities
por: Radun, Richard, et al.
Publicado: (2021)

Discovery of 9,11-Seco-Cholesterol Derivatives as Novel FXR Antagonists
por: Zhou, Jia-Xu, et al.
Publicado: (2022)

γ-Glutamyl transferase and breast cancer risk
por: Fentiman, I S, et al.
Publicado: (2010)

The application of L‐glutaminase for the synthesis of the immunomodulatory γ‐D‐glutamyl‐L‐tryptophan and the kokumi‐imparting γ‐D‐glutamyl peptides
por: Yang, Juan, et al.
Publicado: (2020)

In vivo detection of γ-glutamyl-transferase up-regulation in glioma using hyperpolarized γ-glutamyl-[1-(13)C]glycine
por: Batsios, Georgios, et al.
Publicado: (2020)

Transcriptional Regulation of Metabolic Pathways via Lipid-Sensing Nuclear Receptors PPARs, FXR, and LXR in NASH
por: Cariello, Marica, et al.
Publicado: (2021)

Investigation and identification of protein γ-glutamyl carboxylation sites
por: Lee, Tzong-Yi, et al.
Publicado: (2011)

Identification of an irreversible PPARγ antagonist with potent anticancer activity
por: Peng, Youyi, et al.
Publicado: (2020)

Ageing Fxr Deficient Mice Develop Increased Energy Expenditure, Improved Glucose Control and Liver Damage Resembling NASH
por: Bjursell, Mikael, et al.
Publicado: (2013)

Transcriptome Analysis of Dual FXR and GPBAR1 Agonism in Rodent Model of NASH Reveals Modulation of Lipid Droplets Formation
por: Carino, Adriana, et al.
Publicado: (2019)

The Non-Steroidal FXR Agonist Cilofexor Improves Portal Hypertension and Reduces Hepatic Fibrosis in a Rat NASH Model
por: Schwabl, Philipp, et al.
Publicado: (2021)

Association of γ-glutamyl transferase with premature coronary artery disease
por: GHATGE, MADANKUMAR, et al.
Publicado: (2016)

Serum alkaline phosphatase and γ-glutamyl transferase in acute pyelonephritis
por: Han, Chaehoon, et al.
Publicado: (2019)

Lysophosphatidic acid receptor 1 antagonist (EPGN2154) causes regression of NASH in preclinical NASH models
por: Bhattacharjee, Jashdeep, et al.
Publicado: (2023)

Combinatorial therapy with BAR502 and UDCA resets FXR and GPBAR1 signaling and reverses liver histopathology in a model of NASH
por: Marchianò, Silvia, et al.
Publicado: (2023)

BRD4 inhibition and FXR activation, individually beneficial in cholestasis, are antagonistic in combination
por: Jung, Hyunkyung, et al.
Publicado: (2020)

The Synergistic Biologic Activity of Oleanolic and Ursolic Acids in Complex with Hydroxypropyl-γ-Cyclodextrin
por: Soica, Codruţa, et al.
Publicado: (2014)

Solubility and Permeability Enhancement of Oleanolic Acid by Solid Dispersion in Poloxamers and γ-CD
por: De Stefani, Chiara, et al.
Publicado: (2022)

Immobilization of E. coli expressing γ-glutamyltranspeptidase on its surface for γ-glutamyl compound production
por: Arai, Shintaro, et al.
Publicado: (2023)

γ-Glutamyl transferase 7 is a novel regulator of glioblastoma growth
por: Bui, Timothy T, et al.
Publicado: (2015)

Garlic γ-glutamyl transpeptidases that catalyze deglutamylation of biosynthetic intermediate of alliin
por: Yoshimoto, Naoko, et al.
Publicado: (2015)

Fearful dogs have increased plasma glutamine and γ-glutamyl glutamine
por: Puurunen, Jenni, et al.
Publicado: (2018)

Human germ cell tumours: expression of γ-glutamyl transpeptidase and sensitivity to cisplatin
por: Hanigan, M H, et al.
Publicado: (1999)

Diabetic and non-diabetic human cornea and tear γ-glutamyl transpeptidase activity
por: Burnham, Jordan M, et al.
Publicado: (2013)

Rapid intraoperative visualization of breast lesions with γ-glutamyl hydroxymethyl rhodamine green
por: Ueo, Hiroki, et al.
Publicado: (2015)

Osteodystrophy in Cholestatic Liver Diseases Is Attenuated by Anti-γ-Glutamyl Transpeptidase Antibody
por: Kawazoe, Yusuke, et al.
Publicado: (2015)

γ-Glutamyl Transferase Is an Independent Biomarker of Splanchnic Thrombosis in Patients With Myeloproliferative Neoplasm
por: Görtzen, Jan, et al.
Publicado: (2016)

Role of Gln79 in Feedback Inhibition of the Yeast γ-Glutamyl Kinase by Proline
por: Nishimura, Akira, et al.
Publicado: (2021)

Oleanolic Acid Enhances the Beneficial Effects of Preconditioning on PC12 Cells
por: Ndlovu, Babongile C., et al.
Publicado: (2014)

γ-glutamyl transferase-to-platelet ratio based nomogram predicting overall survival of gallbladder carcinoma
por: Sun, Le-Jia, et al.
Publicado: (2020)

γ-Glutamyltransferase enzyme activity of cancer cells modulates L-γ-glutamyl-p-nitroanilide (GPNA) cytotoxicity
por: Corti, Alessandro, et al.
Publicado: (2019)

(E)-7-Ethylidene-lithocholic Acid (7-ELCA) Is a Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells
por: Stefela, Alzbeta, et al.
Publicado: (2021)

Acceleration of Anaerobic Cysteine Transformations to Sulfane Sulfur Consequent to γ-Glutamyl Transpeptidase Inhibition
por: Kwiecień, Inga, et al.
Publicado: (2012)

Synthesis, characterization, and biological evaluation of poly(L-γ-glutamyl-glutamine)- paclitaxel nanoconjugate
por: Van, Sang, et al.
Publicado: (2010)

Covalent Immobilization of Bacillus licheniformis γ-Glutamyl Transpeptidase on Aldehyde-Functionalized Magnetic Nanoparticles
por: Chen, Yi-Yu, et al.
Publicado: (2013)

Critical Roles of the Cysteine–Glutathione Axis in the Production of γ-Glutamyl Peptides in the Nervous System
por: Fujii, Junichi, et al.
Publicado: (2023)

Cannot write session to /tmp/vufind_sessions/sess_in3eno8pe236r427jl6c97iqiq