Academic literature on the topic 'Novel Bile Acid Conjugates'

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Journal articles on the topic "Novel Bile Acid Conjugates"

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Mishra, Satyendra, and Sejal Patel. "Design, Synthesis, and Anti-bacterial Activity of Novel Deoxycholic Acid- Amino Alcohol Conjugates." Medicinal Chemistry 16, no. 3 (April 17, 2020): 385–91. http://dx.doi.org/10.2174/1573406415666190206231002.

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Background: Numerous synthetic bile acid derivatives have been recognized for their various biological activities. Among these, bile acid amides have emerged as an attractive antibacterial agent. We herein illustrate the synthesis and antibacterial evaluation of deoxycholic acidamino alcohols conjugates. Objective: Design and Synthesis of novel deoxycholic acid-amino alcohol conjugates to investigate their antibacterial activity against E. coli and S. aureus. Methods: Novel deoxycholic acid-amino alcohol conjugates were synthesized, from conjugation of deoxycholic acid-NHS ester with amino alcohols. Various amino alcohols moieties were appended to the C24 position of deoxycholic acid to yield deoxycholic acid-amino alcohol conjugates. All the synthesized compounds were characterized by 1H NMR, 13C NMR, IR and massspectroscopy. The entire synthesized deoxycholic acid-amino alcohol conjugates were evaluated for their antibacterial activity against E. coli and S. aureus using the broth dilution method. Results: The outcome illustrated that some of the novel deoxycholic acid-amino alcohol conjugates exhibited enhanced anti-bacterial activities. Amongst them, deoxycholic acid-amino alcohol conjugate containing (-R)-2-aminocyclohexanol (1) demonstrated promising efficacy against both strains S. aureus ATCC 25923 (MIC 15 μg/mL) and E. coli ATCC 25922 (MIC 45 μg/mL) and was identified as a lead molecule. Conclusion: Numbers of novel deoxycholic acid-amino alcohol conjugates were synthesized and their antimicrobial activities provided useful information that the potency was strongly depending on the structures of deoxycholic acid-amino alcohol conjugates.
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Ahonen, Kari V., Manu K. Lahtinen, Miika S. Löfman, Anniina M. Kiesilä, Arto M. Valkonen, Elina I. Sievänen, Nonappa, and Erkki T. Kolehmainen. "Structural studies of five novel bile acid-4-aminopyridine conjugates." Steroids 77, no. 11 (September 2012): 1141–51. http://dx.doi.org/10.1016/j.steroids.2012.06.003.

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Chong, Hyun-Soon, Yunwei Chen, Chi Soo Kang, Xiang Sun, and Ningjie Wu. "Novel 64Cu-radiolabeled bile acid conjugates for targeted PET imaging." Bioorganic & Medicinal Chemistry Letters 25, no. 5 (March 2015): 1082–85. http://dx.doi.org/10.1016/j.bmcl.2015.01.008.

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Li, Yan, Weijun Chu, and Yong Ju. "Novel bile acid derivedH-phosphonate conjugates: Synthesis and spectroscopic characterization." Heteroatom Chemistry 19, no. 4 (2008): 402–7. http://dx.doi.org/10.1002/hc.20447.

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Jin, Xue-Yuan, Chuan-Bao Zhu, Shi-Yong Fan, Jia-Lin Sun, Yu-Cong Shi, Chu-Han Wang, Hui-Fen Wang, Bo-Hua Zhong, Yi-Shan Yao, and Wei-Guo Shi. "Novel hypolipidemic conjugates of fatty acid and bile acid with lysine for linkage." Drug Development and Industrial Pharmacy 45, no. 6 (March 20, 2019): 995–98. http://dx.doi.org/10.1080/03639045.2019.1590393.

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Koivukorpi, Juha, and Erkki Kolehmainen. "Novel bile acid conjugates with aryl/alkenyl linker: Synthesis and characterization." Journal of Molecular Structure 889, no. 1-3 (October 2008): 211–16. http://dx.doi.org/10.1016/j.molstruc.2008.01.050.

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Noponen, Virpi, Shreedhar Bhat, Elina Sievänen, and Erkki Kolehmainen. "Novel two-step synthesis of gold nanoparticles capped with bile acid conjugates." Materials Science and Engineering: C 28, no. 7 (August 2008): 1144–48. http://dx.doi.org/10.1016/j.msec.2007.10.001.

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Blagbrough, I. S., A. J. Geall, and A. P. Neal. "Polyamines and novel polyamine conjugates interact with DNA in ways that can be exploited in non-viral gene therapy." Biochemical Society Transactions 31, no. 2 (April 1, 2003): 397–406. http://dx.doi.org/10.1042/bst0310397.

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As a part of our continuing studies on ‘Polyamines and their role in human disease’ we are investigating how polyamines, and especially how novel polyamine conjugates, interact with DNA. We are studying how these conjugates interact with circular plasmids in order to produce nanometre-sized particles suitable for transfecting cells. Our considerations of structure--activity relationships (SAR) within naturally occurring and synthetic polyamines have shown the significance of the inter-atomic distances between the basic nitrogen atoms. As these atoms are typically fully protonated under physiological conditions, they exist in equilibrium as polyammonium ions. The covalent addition of a lipid moiety, typically one or two alkyl or alkenyl chains, or a steroid, allows much greater efficiency in DNA condensation and in the cellular transfection achieved. Thus efficient DNA condensation and subsequently drug delivery (i.e. with DNA as the drug) can be brought about using novel polyamine conjugates. Taking further advantage of the functionalization of specific steroids (e.g. cholesterol and certain bile acids), we have designed and prepared novel fluorescent molecular probes as tools to throw light on the problematic steps in non-viral gene delivery which still impede efficient gene therapy. Thus, the current aims of our research are to understand, design and prepare small-molecule lipopolyamines for non-viral gene therapy (NVGT). The rational design and practical preparation of non-symmetrical polyamine carbamates and amides, based on steroid templates of cholesterol and the bile acid lithocholic acid as the lipid moiety, provides fluorescent molecular probes that condense DNA. These novel lipopolyamine conjugates mimic the positive charge distribution found in the triamine spermidine and the tetra-amine spermine alkaloids. After optimizing their SAR, these fluorescent probes will be useful in monitoring gene delivery in NVGT.
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Yang, Min, Yu Gu, Lingfeng Li, Tianyu Liu, Xueli Song, Yue Sun, Xiaocang Cao, Bangmao Wang, Kui Jiang, and Hailong Cao. "Bile Acid–Gut Microbiota Axis in Inflammatory Bowel Disease: From Bench to Bedside." Nutrients 13, no. 9 (September 9, 2021): 3143. http://dx.doi.org/10.3390/nu13093143.

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Inflammatory bowel disease (IBD) is a chronic, relapsing inflammatory disorder of the gastrointestinal tract, with increasing prevalence, and its pathogenesis remains unclear. Accumulating evidence suggested that gut microbiota and bile acids play pivotal roles in intestinal homeostasis and inflammation. Patients with IBD exhibit decreased microbial diversity and abnormal microbial composition marked by the depletion of phylum Firmicutes (including bacteria involved in bile acid metabolism) and the enrichment of phylum Proteobacteria. Dysbiosis leads to blocked bile acid transformation. Thus, the concentration of primary and conjugated bile acids is elevated at the expense of secondary bile acids in IBD. In turn, bile acids could modulate the microbial community. Gut dysbiosis and disturbed bile acids impair the gut barrier and immunity. Several therapies, such as diets, probiotics, prebiotics, engineered bacteria, fecal microbiota transplantation and ursodeoxycholic acid, may alleviate IBD by restoring gut microbiota and bile acids. Thus, the bile acid–gut microbiota axis is closely connected with IBD pathogenesis. Regulation of this axis may be a novel option for treating IBD.
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Thorpe, Cheleste M., Xi Qian, Karin Yanagi, Anne Kane, Nicholas Alden, David R. Snydman, and Kyongbum Lee. "2567. Effect of Broad vs. Narrow-Spectrum Clostridioides difficile Treatment on Human Stool Bile Acid Composition Over Time." Open Forum Infectious Diseases 6, Supplement_2 (October 2019): S891. http://dx.doi.org/10.1093/ofid/ofz360.2245.

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Abstract Background Secondary bile acid production by a diverse commensal flora may be a critical factor in preventing recurrence of Clostridioides difficile infection (CDI). Key enzymes involved are bacterial-encoded bile salt hydrolases (BSHs), felt to be “gatekeepers” to secondary bile acid synthesis. Ridinilazole, a novel narrow-spectrum drug for CDI, demonstrated superior sustained clinical response compared with vancomycin in Phase 2. Longitudinal sampling during this trial allowed for assessment of metabolites differentially present in stools during/after therapy with either broad or narrow-spectrum anti-CDI agent. Previous work characterizing subject’s fecal microbiota in this trial showed that unlike vancomycin, ridinilazole has little effect on commensal flora during and after therapy. We hypothesized that ridinilazole’s microbiota-preserving effect is associated with lack of accumulation of conjugated primary bile acids and/or reaccumulation/persistence of secondary bile acids over the course of CDI treatment, when compared with vancomycin-treated subjects. Furthermore, we hypothesized that we would observe correlations between bile acid profiles and predicted BSH gene abundances. Methods Sequential stool samples were obtained from 44 subjects treated with either ridinilazole or vancomycin (22 in each arm), ranging from time of CDI diagnosis, at end-of-therapy, and up to 40 days after diagnosis. Bile acids were quantitated by liquid chromatography-mass spectrometry. Using the PICRUSt algorithm, metagenomic predictions of BSH gene abundances were performed. Results Stool bile acid compositions differed between ridinilazole-treated and vancomycin-treated subjects at end-of-therapy. In vancomycin-treated subjects, stool composition became dominated by conjugated primary bile acids and decreased levels of secondary bile acids compared with baseline; the ratio of stool conjugated bile acids to secondary bile acids significantly predicted treatment arm. This ratio was also associated with predicted BSH gene abundance in ridinilazole-treated subjects. Conclusion Microbiota-preserving CDI treatment with ridinilazole preserves bile acid composition, which may decrease likelihood of recurrence. Disclosures All authors: No reported disclosures.
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Dissertations / Theses on the topic "Novel Bile Acid Conjugates"

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CHINAGLIA, Nicola. "Design, synthesis and biological evaluation of novel nucleoside and oligonucleotide conjugates of bio-medical interest." Doctoral thesis, Università degli studi di Ferrara, 2019. http://hdl.handle.net/11392/2487947.

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Bioconjugation is the process of linking or connecting a biological molecule with another moiety. This moiety may include another biomolecule: in this case a hybrid is formed, in which the properties of the parent molecules are integrated, yielding a single entity with two different functions. With the aim to discover new nucleoside-based compounds of bio-medical interest, we consider bioconjugation as a powerful approach. In light of the well-known therapeutic potential of nucleosides as antitumorals and antivirals, in the first work reported in this thesis a conjugate between 2'-deoxyadenosine and a molecule called "photocage" was synthesized: the latter is in fact able to release under irradiation nitric oxide, whose activity in various bioregulatory systems has been proven in recent studies. Furthermore, two other bioconjugates were synthesized between the same photocage and the ursodeoxycholic and chenodeoxycholic bile acids, using click chemistry reactions. The novel bioconjugates were subjected to cytotoxicity tests and subsequently to photobiological studies that confirmed the combination of chemo- and phototherapeutic effects. In the second work the amphiphilic nature of bile acids was considered, which makes them suitable carriers for poorly lipophilic molecules, as in our case the nucleosides, increasing their cellular uptake. Therefore, new bioconjugates were made using CuAAC reactions between 2'-deoxyadenosine, 2'-deoxyguanosine, 2'-deoxyuridine, adenosine and guanosine alkyne derivatives, and azide derivatives of cheno-, urso-, nor-cheno-, nor-urso- and taurourso-deoxycholic acids. Biological and structure-activity relationship tests on new hybrids have shown that cytoselectivity is mainly driven by the nature of the bile acid and can be fine-tuned by the nature of the nucleoside. The ability of bile acids as carrier molecules has also been exploited in the third work: here the ursodeoxycholic acid and other lipophilic molecules have been conjugated to an antisense oligonucleotide able to associate with the exon of the human dystrophin gene which is more frequently responsible for Duchenne Muscular Dystrophy, in order to improve exon skipping approach. For the synthesis of the oligonucleotide the classic phosphoramidite chemistry in solid phase was used, using the oligosyntesizer "Äkta Oligopilot Plus". By inserting suitable amino linkers to the 3'- and 5'-ends of the oligonucleotide and by the activation of the carboxylic groups present on the lipophilic molecules as N-succinimide esters, it was possible to carry out the bioconjugation by means of amide bonds. Following the tests performed in vitro and in vivo, an increase in the amount of dystrophin in the muscle cells treated with the oligonucleotide conjugated with ursodeoxycholic acid has emerged compared to those treated with the unconjugated oligonucleotide. In the last work of this thesis, bioconjugation was used to synthesize biomimetic compounds of UDP-GlcNAc, a natural substrate of glycosyltransferases, in which the β-phosphate was replaced by an alkyl chain or a triazole ring. These new compounds were then studied as glycosyltransferase inhibitors, as the dysregulation of these enzymes is related to various diseases, including cancer and neurodegenerative syndromes. Uridine monophosphate was conjugated with glucose, N-acetylglucosamine or a pyrrolidine ring substituted in various ways. Enzymatic, spectroscopic and computational studies were in agreement, highlighting how the absence of β-phosphate should be adequately counterbalanced in glycomimetics to have inhibition at micromolar concentrations.
La bioconiugazione è il processo di collegamento di una molecola biologica con un'altra entità chimica. Quest’ultima può includere un'altra biomolecola: in questo caso si forma un ibrido, nel quale le proprietà delle molecole genitrici si integrano, producendo una singola entità con due differenti funzioni. Allo scopo di scoprire nuovi composti di interesse bio-medico a base di nucleosidi, abbiamo considerato la bioconiugazione una valida strategia. Alla luce del ben noto potenziale terapeutico dei nucleosidi come antitumorali e antivirali, nel primo lavoro riportato in questa tesi è stato sintetizzato un coniugato tra 2'-deossiadenosina e una molecola definita “fotogabbia”: quest’ultima è infatti in grado di rilasciare sotto stimolo luminoso ossido nitrico, la cui attività in vari sistemi bioregolatori è stata provata in recenti studi. Sono stati inoltre sintetizzati altri due bioconiugati tra la stessa fotogabbia e gli acidi biliari ursodesossicolico e chenodesossicolico, utilizzando reazioni di click chemistry. I nuovi bioconiugati sono stati sottoposti a test di citotossicità e successivamente a studi fotobiologici che ne hanno confermato la combinazione di effetti chemo- e fototerapeutici. Nel secondo lavoro è stata considerata la natura anfifilica degli acidi biliari, che li rende adeguati carrier per molecole scarsamente lipofiliche, come nel nostro caso i nucleosidi, aumentandone l’uptake cellulare. Sono quindi stati realizzati nuovi bioconiugati utilizzando reazioni CuAAC tra derivati alchinici di 2'-deossiadenosina, 2'-deossiguanosina, 2'-deossiuridina, adenosina e guanosina, e derivati azidici degli acidi cheno-, urso-, nor-cheno-, nor-urso- e taurourso-desossicolico. Test biologici e di relazione struttura-attività sui nuovi ibridi hanno mostrato come la citoselettività sia guidata principalmente dalla natura dell'acido biliare e possa essere affinata dalla natura del nucleoside. L’abilità degli acidi biliari come molecole carrier è stata sfruttata anche nel terzo lavoro: qui l’acido ursodesossicolico e altre molecole lipofiliche sono stati coniugati ad un oligonucleotide antisenso in grado di associarsi all’esone del gene della distrofina umana che è più di frequente responsabile della Distrofia Muscolare di Duchenne, in modo da migliorarne l’exon skipping. Per la sintesi dell'oligonucleotide è stata utilizzata la chimica classica del fosforoammidito in fase solida, impiegando l'oligosintetizzatore "Äkta Oligopilot Plus". Attraverso l’inserimento di adeguati linker amminici alle estremità 3' e 5' dell’oligonucleotide e all’attivazione dei gruppi carbossilici presenti sulle molecole lipofiliche come esteri N-succinimmidici, è stato possibile realizzare la bioconiugazione per mezzo di legami ammidici. In seguito ai test eseguiti in vitro e in vivo, è emerso un effettivo aumento della quantità di distrofina nelle cellule muscolari trattate con l’oligonucleotide coniugato con l’acido ursodesossicolico rispetto a quelle trattate con l’oligonucleotide non coniugato. Nell’ultimo lavoro di questa tesi, la bioconiugazione è stata utilizzata per realizzare composti biomimetici di UDP-GlcNAc, substrato naturale di glicosiltransferasi, nei quali il β-fosfato è stato rimpiazzato da una catena alchilica o da un anello triazolico. Questi nuovi composti sono poi stati studiati come inibitori di glicosiltransferasi, in quanto la disregolazione di questi enzimi è connessa a vari disturbi, tra cui cancro e malattie neurodegenerative. L’uridina monofosfato è stata coniugata con glucosio, N-acetilglucosammina o con un anello pirrolidinico sostituito in vari modi. Test enzimatici, spettroscopici e computazionali sono risultati in accordo, evidenziando come l’assenza del β-fosfato debba essere adeguatamente controbilanciata nei glicomimetici per avere inibizione a concentrazioni micromolari.
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Trusova, Tatyana. "Quantitative estimation of bile acid conjugates in human bile using HPLC /." Connect to online version, 1995. http://hdl.handle.net/1989/3555.

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Hurley, J. P. "Novel bile acid-hydrogel systems as potential nedical device biomaterials." Thesis, Queen's University Belfast, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.269055.

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Tierney, Juliann Jude. "The synthesis and testing of novel cholic acid based stationary phases." Thesis, University of Bristol, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.247854.

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Bhattacharya, Shiladitya. "Novel folate amphiphile conjugates for targeted drug delivery." Scholarly Commons, 2008. https://scholarlycommons.pacific.edu/uop_etds/2360.

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Cancer is not only difficult to treat but the patients also suffer from the pain associated with anticancer treatments. Targeted chemotherapeutics can reduce the adverse effects by reducing the dose required for tumor cell kill. Cancers of various origins often have characteristic marker molecules that distinguish them from the normal tissues. Folate receptors are such marker molecules present in ovarian and cervical cancers. The hypothesis for the current study is that amphiphiles constructed out of folic acid, the natural ligand for the folate receptor, can deliver paclitaxel, a chemotherapeutic compound, to folate receptor expressing cancer cells. To test this hypothesis, amphiphilic molecules were synthesized out of folic acid and fatty acids or long chain aliphatic amines. The gamma carboxylic group of folic acid was converted to an N-alkyl substituted amide. The alkyl group had various chain lengths varying from eleven methylene groups to seventeen methylene groups giving rise to a number of amphiphiles. The amphiphiles formed micelles in aqueous solutions. The critical micellization concentrations of the amphiphiles were measured by pyrene fluorescence and were found to be in the range of 10–70μM. HeLa and Caco-2 cells were taken as in vitro tumor models. Folate receptor expression was verified in HeLa and Caco-2 cells by western blot analysis. HeLa showed more than forty fold expression of the receptor when compared to Caco-2 and was chosen as receptor positive cell line while Caco-2 served as a negative control. Uptake of the folate labeled delivery system in the cell lines was tested by a fluorescent probe (aminocoumarin) labeled amphiphile. To test the specificity of the delivery system towards the receptor positive HeLa cells, the receptors were knocked down (70%) by folate receptor specific siRNA. Fluorescent amphiphile uptake in the knockdown cells was comparable to that of the negative control, Caco-2. Finally cytotoxicity studies were performed for paclitaxel formulated with the folate labeled amphiphiles and compared to free drug treatment in HeLa and Caco-2. IC50 values in HeLa for formulations with the folate labeled amphiphiles were ten folds less than those observed for free drug treatment whereas in Caco-2 no significant difference was noted.
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Duncan, Kenneth William. "Development of a synthetic methodology towards novel bile acid and cholesterol analogues." Thesis, University of Strathclyde, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.248838.

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Gopaul, Vedwatee Sashi. "The identification, characterization and profiling of novel thiol and amino acid conjugates of valproic acid in humans and animals." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1998. http://www.collectionscanada.ca/obj/s4/f2/dsk2/tape17/PQDD_0007/NQ34524.pdf.

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Trujillo, Jesse, and Jesse Trujillo. "A Novel Mechanism for Bile Acid Induced Activation of Estrogen Receptor β in Colorectal Cancer." Diss., The University of Arizona, 2016. http://hdl.handle.net/10150/622961.

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Primary bile acids are a group of cholesterol metabolites that are synthesized in the liver and stored in the gallbladder. The main role of bile acids is to aid in the digestion of dietary fats and lipids. More recently, a signaling role for bile acids has been characterized. Secondary bile acids are formed when the bacteria of the colon metabolize primary bile acids. Secondary bile acids that escape enterohepatic re-uptake to the liver can have a deleterious effect in the colon. Deoxycholic acid (DCA) and ursodeoxycholic acid (UDCA) are two secondary bile acids that have been studied for their biological effects in the colon. More recently, these bile acids have been found to induce intracellular signaling in the colon. Although much is known about bile acids and their link to tumorigenesis or chemoprevention, there is very little known about how they induce the intracellular signaling of cells. In short, it is our goal to understand the mechanism of how bile acids like DCA and UDCA induce the activation of signaling pathways. For several years, bile acids have slowly been characterized as hormonal molecules due to their ability to naturally bind to the farnesoid x receptor (FXR) and pregnane x receptor (PXR). Moreover, DCA and UDCA have also been researched for their gender specific role. In animal models, UDCA was found to be a chemopreventive agent in males, but a tumor-promoting agent in females. In our studies, we identified a novel nuclear receptor that bile acids exert their effect on. Estrogen receptor β (ERβ) is highly predominant in the colon and a regulator of colorectal cancer. Using human colorectal adenocarcinoma cell lines, we identified a key serine residue (Serine-87) on ERβ that is highly regulated by the MAPK pathway. We found that DCA and UDCA induce the phosphorylation and subsequent up-regulation of estrogen receptor regulated genes. Moreover, we found that phosphorylation was occurring mainly in the nucleus of our cells, indicative of activation of ERβ. Remarkably, we also identified a tumorigenic role for UDCA. UDCA-treated cells showed increased migration, which was blocked when the MAPK and ERβ pathways were inhibited. Collectively, this data reveals a novel signaling mechanism for bile acids in colorectal cancer and uncovers an adverse role for UDCA.
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Almarghalani, Daniyah Abduljalil. "Molecular Cloning, Expression, and Characterization of A Novel ZebrafishCytosolic Sulfotransferase, SULT5A1." University of Toledo Health Science Campus / OhioLINK, 2016. http://rave.ohiolink.edu/etdc/view?acc_num=mco1470097207.

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Delsol, Anne Aline Germaine. "Microbial 7-hydroxylation of the steroid lithocholic acid : a novel approach to produce bile acids for gallstone therapy." Thesis, University of Exeter, 1999. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.297640.

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Book chapters on the topic "Novel Bile Acid Conjugates"

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Kuipers, Folkert, Charles M. A. Bijleveld, C. M. Frank Kneepkens, John Fernandes, and Roel J. Vonk. "Sulfated Lithocholic Acid Conjugates and Cholestasis: Clinical Implications and Protecting Factors." In Liver, Nutrition, and Bile Acids, 225–34. Boston, MA: Springer US, 1985. http://dx.doi.org/10.1007/978-1-4615-9427-7_20.

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Xie, W., and T. Wada. "Novel roles of liver X receptor in bile acid homeostasis and haptobiliary diseases." In Bile Acid Biology and Therapeutic Actions, 115–25. Dordrecht: Springer Netherlands, 2009. http://dx.doi.org/10.1007/978-1-4020-9644-0_16.

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Barton, Derek H. R., Jocelyne Wozniak, and Samir Z. Zard. "A SHORT AND EFFICIENT DEGRADATION OF THE BILE ACID SIDE CHAIN.: SOME NOVEL REACTIONS OF SULPHINES AND α-KETOESTERS." In World Scientific Series in 20th Century Chemistry, 710–20. WORLD SCIENTIFIC / IMPERIAL COLLEGE PRESS, 1996. http://dx.doi.org/10.1142/9789812795984_0116.

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Conference papers on the topic "Novel Bile Acid Conjugates"

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Šnajdr, Ivan, Zbyněk Janoušek, and Martin Kotora. "Synthesis of novel C-(o-carboranyl)-2-deoxy-D-ribose conjugates." In XVth Symposium on Chemistry of Nucleic Acid Components. Prague: Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 2011. http://dx.doi.org/10.1135/css201112465.

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Sapra, Puja Sapra, Lioudmila Tchistiakova, Russell Dushin, Mauricio Leal, John DiJoseph, Robert Veneziale, Eric Feyfant, et al. "Abstract 5691: Novel site-specific antibody drug conjugates based on novel amino acid incorporation technology have improved pharmaceutical properties over conventional antibody drug conjugates." In Proceedings: AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-5691.

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Atkins, Jonathan S., Brian G. Keevil, and James M. Hawley. "P164 Bile acid malabsorption: the development of a novel serum 7α-hydroxy-4-cholesten-3-one (C4) method to aid diagnosis." In BSG LIVE’23, 19–22 June, ACC Liverpool. BMJ Publishing Group Ltd and British Society of Gastroenterology, 2023. http://dx.doi.org/10.1136/gutjnl-2023-bsg.235.

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Goldman, Aaron, Mohammad Shahidullah, Hwudaurw Chen, Nicholas Delamere, and Katerina Dvorak. "Abstract 4105: Nitric-oxide-mediated inhibition of Na+/H+ exchange (NHE) is a novel mechanism of bile acid induced damage: Relevance to esophageal carcinogenesis." In Proceedings: AACR 101st Annual Meeting 2010‐‐ Apr 17‐21, 2010; Washington, DC. American Association for Cancer Research, 2010. http://dx.doi.org/10.1158/1538-7445.am10-4105.

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Reports on the topic "Novel Bile Acid Conjugates"

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Shapira, Roni, Judith Grizzle, Nachman Paster, Mark Pines, and Chamindrani Mendis-Handagama. Novel Approach to Mycotoxin Detoxification in Farm Animals Using Probiotics Added to Feed Stuffs. United States Department of Agriculture, May 2010. http://dx.doi.org/10.32747/2010.7592115.bard.

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T-2 toxin, a toxic product belongs to the trichothecene mycotoxins, attracts major interest because of its severe detrimental effects on the health of human and farm animals. The occurrence of trichothecenes contamination is global and they are very resistant to physical or chemical detoxification techniques. Trichothecenes are absorbed in the small intestine into the blood stream. The hypothesis of this project was to develop a protecting system using probiotic bacteria that will express trichothecene 3-O-acetyltransferase (Tri101) that convert T-2 to a less toxic intermediate to reduce ingested levels in-situ. The major obstacle that we had faced during the project is the absence of stable and efficient expression vectors in probiotics. Most of the project period was invested to screen and isolate strong promoter to express high amounts of the detoxify enzyme on one hand and to stabilize the expression vector on the other hand. In order to estimate the detoxification capacity of the isolated promoters we had developed two very sensitive bioassays.The first system was based on Saccharomyces cerevisiae cells expressing the green fluorescent protein (GFP). Human liver cells proliferation was used as the second bioassay system.Using both systems we were able to prove actual detoxification on living cells by probiotic bacteria expressing Tri101. The first step was the isolation of already discovered strong promoters from lactic acid bacteria, cloning them downstream the Tri101 gene and transformed vectors to E. coli, a lactic acid bacteria strain Lactococcuslactis MG1363, and a probiotic strain of Lactobacillus casei. All plasmid constructs transformed to L. casei were unstable. The promoter designated lacA found to be the most efficient in reducing T-2 from the growth media of E. coli and L. lactis. A prompter library was generated from L. casei in order to isolate authentic probiotic promoters. Seven promoters were isolated, cloned downstream Tri101, transformed to bacteria and their detoxification capability was compared. One of those prompters, designated P201 showed a relatively high efficiency in detoxification. Sequence analysis of the promoter region of P201 and another promoter, P41, revealed the consensus region recognized by the sigma factor. We further attempted to isolate an inducible, strong promoter by comparing the protein profiles of L. casei grown in the presence of 0.3% bile salt (mimicking intestine conditions). Six spots that were consistently overexpressed in the presence of bile salts were isolated and identified. Their promoter reigns are now under investigation and characterization.
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