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PubMed Journals Articles About "Protein Coupled Bile Acid Receptor Pipeline Review 2019" RSS

07:05 EST 25th January 2020 | BioPortfolio

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Showing "Protein Coupled Bile Acid Receptor Pipeline Review 2019" PubMed Articles 1–25 of 48,000+

Gluco-metabolic effects of pharmacotherapy-induced modulation of bile acid physiology.

The discovery and characterization of the bile acid specific receptors farnesoid X receptor (FXR) and Takeda G protein-coupled receptor 5 (TGR5) have facilitated a wealth of research focusing on the link between bile acid physiology and glucose metabolism. Modulation of FXR and TGR5 activation have been demonstrated to impact the secretion of glucagon-like peptide 1, insulin and glucagon as well as energy expenditure and gut microbiota composition with potential beneficial effects on glucose metabolism.


The Pharmacology of Bile Acids and Their Receptors.

This review provides a historical perspective of bile acids and their receptors as therapeutic targets. Bile acids are atypical steroids generated by the liver from cholesterol and have been used for almost half a century for treating liver and biliary disorders. Since the early 1970s of the last century, chenodeoxycholic acid (CDCA), a primary bile acid, and ursodeoxycholic acid (UDCA), a secondary bile acid and the 7βepimer of CDCA, have been shown effective in promoting the dissolution of cholesterol ga...

Bile Acid-Activated Receptors: A Review on FXR and Other Nuclear Receptors.

Nuclear receptors (NRs) are ligand-dependent transcription factors that are involved in various biological processes including metabolism, reproduction, and development. Upon activation by their ligands, NRs bind to their specific DNA elements, exerting their biological functions by regulating their target gene expression. Bile acids are detergent-like molecules that are synthesized in the liver. They not only function as a facilitator for the digestion of lipids and fat-soluble vitamins but also serve as s...


Open-label phase 3 continuation study of cholic acid in patients with inborn errors of bile acid synthesis.

In patients with bile acid synthesis disorders (BASD), impairment in the primary bile acid synthetic pathway leads to reduced primary bile acids, upregulated synthesis of cholesterol, and production and accumulation of hepatotoxic atypical bile acids. Primary bile acid therapy downregulates bile acid synthesis, reduces the production of hepatotoxic intermediates, and produces a functional bile acid pool fostering normal liver function.

Semisynthetic bile acids: a new therapeutic option for metabolic syndrome.

Bile acids are endogenous emulsifiers with peculiar amphiphilic structure synthesized from cholesterol. The beneficial effects on human health that have been recognized since ancient times have enormously expanded by discovering their role as signaling molecules. Activation of farnesoid X receptor (FXR) and Takeda G-protein receptor-5 (TGR5) signaling pathways by bile acids, regulating glucose, lipid and energy metabolism, have become attractive avenue for metabolic syndrome treatment. Therefore, an extensi...

Obeticholic Acid: An Update of Its Pharmacological Activities in Liver Disorders.

Obeticholic acid (OCA), 6α-ethyl-3α,7α-dihydroxy-5-cholan-24-oic acid, is a semisynthetic derivative of the chenodeoxycholic acid (CDCA, 3α,7α-dihydroxy-5-cholan-24-oic acid), a relatively hydrophobic primary bile acid synthesized in the liver from cholesterol. OCA, also known as 6-ethyl-CDCA or INT-747, was originally described by investigators at the Perugia University in 2002 as a selective ligand for the bile acid sensor, farnesoid-X-receptor (FXR). In addition to FXR and similarly to CDCA, OCA als...

Association between the perturbation of bile acid homeostasis and valproic acid-induced hepatotoxicity.

Valproic acid (VPA), a widely prescribed antiepileptic drug, is known to induce hepatotoxicity. However, the mechanisms underlying this toxicity are not well understood. In this study, we performed a nontargeted metabolomic analysis of children with epilepsy treated with VPA (n=23). Metabolic pathway analysis showed that the fatty acid pathway, citrate cycle, urea cycle, amino acid metabolism, and bile acid pathway were altered in children with epilepsy exhibiting VPA hepatotoxicity. In particular, the VPA-...

The gut microbiota at the intersection of bile acids and intestinal carcinogenesis: an old story, yet mesmerizing.

The prevalence of colorectal cancer (CRC) dramatically increased worldwide in the last decade. Alterations of bile acid metabolism and gut microbiota have been reported to play vital roles in intestinal carcinogenesis. About trillions of bacteria inhabited in the human gut and maintained the balance of host metabolism. Bile acids are one of numerous metabolites that are synthesized in the liver and further metabolized by the gut microbiota, and are essential in maintaining the normal gut microbiota and lipi...

Receptor component protein, an endogenous allosteric modulator of family B G protein coupled receptors.

Receptor component protein (RCP) is a 148 amino acid intracellular peripheral membrane protein, previously identified as promoting the coupling of CGRP to cAMP production at the CGRP receptor, a heterodimer of calcitonin receptor like-receptor (CLR), a family B G protein-coupled receptor (GPCR) and receptor activity modifying protein 1 (RAMP1). We extend these observations to show that it selectively enhances CGRP receptor coupling to Gs but not Gq or pERK activation. At other family B GPCRs, it enhances cA...

Rifampicin, Not Vitamin E, Suppresses Parenteral Nutrition Associated Liver Disease Development through Pregnane X Receptor Pathway in Piglets.

Infants receiving long-term parenteral nutrition (PN) develop PN associated liver disease (PNALD). We previously showed that PN containing soy-based lipid supplemented with vitamin E (α-tocopherol) prevents the development of PNALD. We hypothesize that this occurs via vitamin E-activation of pregnane X receptor (PXR) mediated pathways involved in bile acid metabolism. Neonatal piglets received PN for 14 d containing Intralipid (IL, soy-based lipid emulsion), IL supplemented with 12.6 mg/kg*d vitamin E (VIT...

Sphingosine 1-phosphate receptor 2/adenylyl cyclase/protein kinase A pathway is involved in taurolithocholate-induced internalization of Abcc2 in rats.

Taurolithocholate (TLC) is a cholestatic bile salt that induces disinsertion of the canalicular transporter Abcc2 (Mrp2, multidrug resistance-associated protein 2). This internalization is mediated by different intracellular signaling proteins such as PI3K, PKCε and MARCK but the initial receptor of TLC remains unknown. A few G protein-coupled receptors interact with bile salts in hepatocytes. Among them, sphingosine-1 phosphate receptor 2 (S1PR2) represents a potential initial receptor for TLC. The aim of...

Decrease in major secondary bile acid, hyodeoxycholic acid, was the main alteration in hepatic bile acid compositions in a hypertensive nonalcoholic fatty liver disease model.

Previous findings on hepatic bile acid compositions in nonalcoholic fatty liver disease (NAFLD) have been inconsistent and complicated. The aim of this study was to investigate the effects of steatosis on hepatic bile acid composition in a hypertensive NAFLD model without obesity and diabetes mellitus and compare hepatic BA composition between hypertensive rats with and without steatosis.

G-protein coupled receptor 40 expression in human melanoma - correlation with tumor thickness, AJCC stage and survival.

In melanoma, preclinical data suggests a possible role of polyunsaturated fatty acids inhibiting cell growth. A new target molecule for free fatty acids, the G-protein coupled receptor GPR40, was identified in melanoma cells.

TGR5 Signaling Mitigates Parenteral Nutrition Associated Liver Disease.

Bile acid receptors regulate the metabolic and immune functions of circulating enterohepatic bile acids. This process is disrupted by administration of parenteral nutrition (PN), which may induce progressive hepatic injury for unclear reasons, especially in the newborn, leading to PN-associated liver disease. To explore the role of bile acid signaling on neonatal hepatic function, we initially observed that TGR5-specific bile acids were negatively correlated with worsening clinical disease markers in the pl...

A adenosine receptor activation mechanisms: molecular dynamics analysis of inactive, active, and fully active states.

We investigated the Gi-coupled A adenosine receptor (AAR) activation mechanism by running 7.2 µs of molecular dynamics (MD) simulations. Based on homology to G protein-coupled receptor (GPCR) structures, three constitutively active mutant (CAM) and the wild-type (WT) AARs in the apo form were modeled. Conformational signatures associated with three different receptor states (inactive R, active R*, and bound to Gi protein mimic) were predicted by analyzing and comparing the CAMs with WT receptor and by co...

Lactoferrin promotes bile acid metabolism and reduces hepatic cholesterol deposition by inhibiting the farnesoid X receptor (FXR)-mediated enterohepatic axis.

Lactoferrin (LF) is a multifunctional glycoprotein that can regulate lipid metabolism, lower cholesterol, reduce body weight, and prevent atherosclerosis. Bile acid (BA) metabolism plays an important role in removing excess cholesterol from the body. However, studies on the effects of LF on BA metabolism are limited and inconsistent.

The five dimensions of receptor pharmacology exemplified by melatonin receptors: An opinion.

Receptology has been complicated with enhancements in our knowledge of G-protein-coupled-receptor (GPCR) biochemistry. This complexity is exemplified by the pharmacology of melatonin receptors. Here, we describe the complexity of GPCR biochemistry in five dimensions: (a) receptor expression, particularly in organs/tissues that are only partially understood; (b) ligands and receptor-associated proteins (interactome); (c) receptor function, which might be more complex than the known G-protein-coupled systems;...

International Union of Basic and Clinical Pharmacology. CVII. Structure and Pharmacology of the Apelin Receptor with a Recommendation that Elabela/Toddler Is a Second Endogenous Peptide Ligand.

The predicted protein encoded by the APJ gene discovered in 1993 was originally classified as a class A G protein-coupled orphan receptor but was subsequently paired with a novel peptide ligand, apelin-36 in 1998. Substantial research identified a family of shorter peptides activating the apelin receptor, including apelin-17, apelin-13, and [Pyr]apelin-13, with the latter peptide predominating in human plasma and cardiovascular system. A range of pharmacological tools have been developed, including radiolab...

Yangonin protects against estrogen-induced cholestasis in a farnesoid X receptor-dependent manner.

Estrogen-induced cholestasis is a common etiology of hepatic diseases in women with contraceptives administration, pregnancy or hormone replacement therapy. Farnesoid X receptor (FXR) is a member of nuclear receptor super family of ligand-activated transcription factors that is highly expressed in liver. FXR is acknowledged to contribute to the bile acid homeostasis, as well as the pathogenesis and progression of cholestasis. Specific targeting of FXR is an innovative approach for the treatment of cholestas...

The role of G protein-coupled estrogen receptor 1 on neurological disorders.

G protein-coupled estrogen receptor 1 (GPER) is a membrane-associated estrogen receptor (ER) associated with rapid estrogen-mediated effects. Over recent years GPER emerged has a potential therapeutic target to induce neuroprotection, avoiding the side effects elicited by the activation of classical ERs. The putative neuroprotection triggered by GPER selective activation was demonstrated in mood disorders, Alzheimer's disease or Parkinsońs disease of male and female in vivo rodent models. In others, like i...

Protein Sorting in Healthy and Diseased Photoreceptors.

Rods and cones are retinal photoreceptor neurons required for our visual sensation. Because of their highly polarized structures and well-characterized processes of G protein-coupled receptor-mediated phototransduction signaling, these photoreceptors have been excellent models for studying the compartmentalization and sorting of proteins. Rods and cones have a modified ciliary compartment called the outer segment (OS) as well as non-OS compartments. The distinct membrane protein compositions between OS and ...

Androgen receptor, aromatase, estrogen receptor α/β, and G-protein-coupled receptor 30 expression in the testes and epididymides of adult sheep.

The androgen receptor (AR) plays a key role in reproduction, and aromatase (P450arom), nuclear estrogen receptors (ERs) α and β, and G-protein-coupled receptor 30 (GPR30) are important for testicular and epididymal cell proliferation and development. In the study, we have investigated the expression and localization of AR, P450arom, ERα, ERβ and GPR30 in testes and epididymides of sexually mature sheep by quantitative reverse transcription-polymerase chain reaction, western blotting, and immunohistochem...

G-protein-coupled receptor 40 agonist GW9508 potentiates glucose-stimulated insulin secretion through activation of protein kinase Cα and ε in INS-1 cells.

The mechanism by which G-protein-coupled receptor 40 (GPR40) signaling amplifies glucose-stimulated insulin secretion through activation of protein kinase C (PKC) is unknown. We examined whether a GPR40 agonist, GW9508, could stimulate conventional and novel isoforms of PKC at two glucose concentrations (3 mM and 20 mM) in INS-1D cells.

Filling a gYap in Hepato-Biliary Tissue Integration in Liver Homeostasis and Regeneration.

Liver bile ducts serve primarily as drainage for bile and undergo extensive remodeling in response to hepatocyte injuries. In this issue of Cell Stem Cell, Pepe-Mooney et al. (2019) and Planas-Paz et al. (2019) show that Yap signaling can be activated by bile acids and is critical for biliary tissue homeostasis and dynamics.

Modulation of bile acid profile by gut microbiota in chronic hepatitis B.

Chronic hepatitis B (CHB) is a global epidemic disease that may progress to fibrosis, cirrhosis and hepatocellular carcinoma. The role of the liver-bile acid-microbiota axis in CHB remains unclear. The aims of this study are to elucidate the alteration of the gut microbiota and its functions in bile acid homeostasis in CHB patients with different degrees of fibrosis. In the present study, we evaluated serum and faecal bile acid profiles in healthy controls and CHB patients with biopsy-proven diagnosis: pati...


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