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List of works by Angela Zampella

2 - GPBAR1 (TGR5) Agonism Reverses Endothelial Dysfunction and Liver Injury in a Dietetic Model of Steatohepatitis

scholarly article published in May 2018

241 - GPBAR1 (TGR5) is a Modulator of Liver Immunity and Reverses Liver Inflammation in a Mouse Models of Acute Hepatitis

scholarly article published in May 2018

4-Methylenesterols from Theonella swinhoei sponge are natural pregnane-X-receptor agonists and farnesoid-X-receptor antagonists that modulate innate immunity

scientific article published on 20 January 2012

Agonism for the bile acid receptor GPBAR1 reverses liver and vascular damage in a mouse model of steatohepatitis

article

Amphiasterins: a new family of cytotoxic metabolites from the marine sponge Plakortis quasiamphiaster

Anti-inflammatory cyclopeptides from the marine sponge Theonella swinhoei

article published in 2012

BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis

scientific article published on 16 February 2017

Bengamides and Related New Amino Acid Derivatives from the New Caledonian Marine SpongeJaspis carteri

Bile Acids Activated Receptors Regulate Innate Immunity

scientific article published on 13 August 2018

Bile acid modulators for the treatment of nonalcoholic steatohepatitis (NASH)

scientific article published on 19 June 2020

Bile acid-activated receptors and the regulation of macrophages function in metabolic disorders

scientific article published on 29 May 2020

Binding mechanism of the farnesoid X receptor marine antagonist suvanine reveals a strategy to forestall drug modulation on nuclear receptors. Design, synthesis, and biological evaluation of novel ligands.

scientific article

Bioactive cembrane derivatives from the Indian Ocean soft coral, Sinularia kavarattiensis

scientific article

Callipeltin A: sodium ionophore effect and tension development in vascular smooth muscle

scientific article published in October 2004

Callipeltins F–I: new antifungal peptides from the marine sponge Latrunculia sp

Chemical Proteomics Reveals Heat Shock Protein 60 To Be the Main Cellular Target of the Marine Bioactive Sesterterpene Suvanine

scientific article published on 24 July 2012

Chemistry and Pharmacology of GPBAR1 and FXR Selective Agonists, Dual Agonists, and Antagonists

scientific article published on 01 January 2019

Concise Synthesis of All Stereoisomers of β-Methoxytyrosine and Determination of the Absolute Configuration of the Residue in Callipeltin A

scientific article published on 01 August 2005

Concise synthesis of AHMHA unit in perthamide C. Structural and stereochemical revision of perthamide C

Conicasterol E, a small heterodimer partner sparing farnesoid X receptor modulator endowed with a pregnane X receptor agonistic activity, from the marine sponge Theonella swinhoei.

scientific article

Coscinolactams A and B: new nitrogen-containing sesterterpenoids from the marine sponge Coscinoderma mathewsi exerting anti-inflammatory properties

article published in 2009

Crellastatin A: A Cytotoxic Bis-Steroid Sulfate from the Vanuatu Marine SpongeCrellasp.†

scholarly article by Maria Valeria D'Auria et al published October 1998 in Journal of Organic Chemistry

Cystathionine γ-lyase, a H2S-generating enzyme, is a GPBAR1-regulated gene and contributes to vasodilation caused by secondary bile acids

article

Decoding the role of the nuclear receptor SHP in regulating hepatic stellate cells and liver fibrogenesis

scientific article published on 24 January 2017

Decoding the vasoregulatory activities of bile acid-activated receptors in systemic and portal circulation: role of gaseous mediators

scientific article

Design, synthesis, and biological evaluation of potent dual agonists of nuclear and membrane bile acid receptors.

scientific article published on 17 January 2014

Determination of Gymnemic Acid I as a Protein Biosynthesis Inhibitor Using Chemical Proteomics.

scientific article

Development of FXR, PXR and CAR agonists and antagonists for treatment of liver disorders

scientific article

Discovery of ((1,2,4-oxadiazol-5-yl)pyrrolidin-3-yl)ureidyl derivatives as selective non-steroidal agonists of the G-protein coupled bile acid receptor-1

scientific article published on 21 February 2019

Discovery of sulfated sterols from marine invertebrates as a new class of marine natural antagonists of farnesoid-X-receptor

scientific article

Discovery that theonellasterol a marine sponge sterol is a highly selective FXR antagonist that protects against liver injury in cholestasis

scientific article (publication date: 2012)

Disruption of TFGβ-SMAD3 pathway by the nuclear receptor SHP mediates the antifibrotic activities of BAR704, a novel highly selective FXR ligand

scientific article published on 9 March 2018

Epoxide functionalization on cholane side chains in the identification of G-protein coupled bile acid receptor (GPBAR1) selective agonists

scholarly article in RSC Advances, vol. 7 no. 52, 2017

Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands.

scientific article

FXR mediates a chromatin looping in the GR promoter thus promoting the resolution of colitis in rodents.

scientific article published in September 2013

Farnesoid X receptor agonist for the treatment of liver and metabolic disorders: focus on 6-ethyl-CDCA.

scientific article

Farnesoid X receptor modulators (2011 - 2014): a patent review

scientific article published on August 2015

Farnesoid X receptor modulators 2014-present: a patent review

scientific article published on 13 April 2018

GPBAR1 Activation by C6-Substituted Hyodeoxycholane Analogues Protect against Colitis

scientific article published on 02 March 2020

GPBAR1 Functions as Gatekeeper for Liver NKT Cells and provides Counterregulatory Signals in Mouse Models of Immune-Mediated Hepatitis

scientific article published on 18 June 2019

Glucocorticoid receptor mediates the gluconeogenic activity of the farnesoid X receptor in the fasting condition.

scientific article published on 23 March 2012

Gpbar1 agonism promotes a Pgc-1α-dependent browning of white adipose tissue and energy expenditure and reverses diet-induced steatohepatitis in mice.

scientific article

Gracilioethers E–J, new oxygenated polyketides from the marine sponge Plakinastrella mamillaris

article

Heat shock proteins as key biological targets of the marine natural cyclopeptide perthamide C.

scientific article published on 10 February 2012

Heteronemin, a marine sponge terpenoid, targets TDP-43, a key factor in several neurodegenerative disorders

scientific article published in January 2014

Hijacking SARS-CoV-2/ACE2 Receptor Interaction by Natural and Semi-synthetic Steroidal Agents Acting on Functional Pockets on the Receptor Binding Domain

scientific article published on 23 October 2020

Homophymine A, an anti-HIV cyclodepsipeptide from the sponge Homophymia sp.

scientific article

Homophymines B-E and A1-E1, a family of bioactive cyclodepsipeptides from the sponge Homophymia sp.

scientific article published on 22 July 2009

Hyodeoxycholic acid derivatives as liver X receptor α and G-protein-coupled bile acid receptor agonists

scientific article

Identification of Cysteinyl-leukotriene-receptor 1 antagonists as ligands for the bile acid receptor GPBAR1

scientific article published on 21 April 2020

Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling

scientific article published on 15 July 2015

Incisterols, highly degraded marine sterols, are a new chemotype of PXR agonists.

scientific article

Insights on FXR selective modulation. Speculation on bile acid chemical space in the discovery of potent and selective agonists.

scientific article published on 7 January 2016

Insights on pregnane-X-receptor modulation. Natural and semisynthetic steroids from Theonella marine sponges.

scientific article

Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties

scientific article published on 16 March 2019

Investigation around the Oxadiazole Core in the Discovery of a New Chemotype of Potent and Selective FXR Antagonists

scientific article published on 10 January 2019

Investigation on bile acid receptor regulators. Discovery of cholanoic acid derivatives with dual G-protein coupled bile acid receptor 1 (GPBAR1) antagonistic and farnesoid X receptor (FXR) modulatory activity

scientific article published on 19 November 2015

Isolation and structural elucidation of the crellastatins I-M: cytotoxic bis-steroid derivatives from the vanuatu marine sponge Crella sp

scholarly article by Clelia Giannini et al published November 1999 in Tetrahedron

Isolation of Plakinamine I: A New Steroidal Alkaloid from the Marine SpongeCorticiumsp. and Synthesis of an Analogue Model Compound

Isolation of callipeltins A–C and of two new open-chain derivatives of callipeltin A from the marine sponge Latrunculia sp. A revision of the stereostructure of callipeltins

Isoswinholide B and swinholide K, potently cytotoxic dimeric macrolides from Theonella swinhoei.

scientific article published on 15 June 2013

Jaspamides H–L, new actin-targeting depsipeptides from the sponge Jaspis splendans

Jaspamides M–P: new tryptophan modified jaspamide derivatives from the sponge Jaspis splendans

Marine and semi-synthetic hydroxysteroids as new scaffolds for pregnane X receptor modulation

scientific article

Marine sponge steroids as nuclear receptor ligands.

scientific article

Mo2014 – Comparative Effects of Bar502, a Dual Fxr and Gpbar1 Agonist, Obeticholic Acid and Ursodeoxycholic Acid in a Rodent Model of Nash

scholarly article

Modification in the side chain of solomonsterol A: discovery of cholestan disulfate as a potent pregnane-X-receptor agonist.

scientific article

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)

scientific article published on 07 September 2014

Molecular decodification of gymnemic acids from Gymnema sylvestre. Discovery of a new class of liver X receptor antagonists.

scientific article

Natural ligands for nuclear receptors: biology and potential therapeutic applications.

scientific article published on January 2012

Navigation in bile acid chemical space: discovery of novel FXR and GPBAR1 ligands

scientific article

New Jaspamide Derivatives from the Marine SpongeJaspis splendansCollected in Vanuatu1

New antimalarial polyketide endoperoxides from the marine sponge Plakinastrella mamillaris collected at Fiji Islands

New isomalabaricane derivatives from a new species of Jaspis sponge collected at the Vanuatu islands.

scientific article

New jaspamide derivatives with antimicrofilament activity from the sponge Jaspis splendans

New tridecapeptides of the theonellapeptolide family from the Indonesian sponge Theonella swinhoei.

scientific article published on 13 August 2013

Novel Isoxazole Derivatives with Potent FXR Agonistic Activity Prevent Acetaminophen-Induced Liver Injury

scientific article published on 06 December 2018

Opposite effects of the FXR agonist obeticholic acid on Mafg and Nrf2 mediate the development of acute liver injury in rodent models of cholestasis

scientific article published on 01 May 2020

Oxygenated polyketides from Plakinastrella mamillaris as a new chemotype of PXR agonists.

scientific article published on 2 July 2013

Perthamides C and D, two new potent anti-inflammatory cyclopeptides from a Solomon Lithistid sponge Theonella swinhoei

Perthamides C–F, potent human antipsoriatic cyclopeptides

Plakilactones G and H from a marine sponge. Stereochemical determination of highly flexible systems by quantitative NMR-derived interproton distances combined with quantum mechanical calculations of (13)C chemical shifts

scientific article published on 30 December 2013

Plakilactones from the marine sponge Plakinastrella mamillaris. Discovery of a new class of marine ligands of peroxisome proliferator-activated receptor γ.

scientific article

Preliminary structure-activity relationship on theonellasterol, a new chemotype of FXR antagonist, from the marine sponge Theonella swinhoei

scientific article published on 5 November 2012

Quantitative NMR-derived interproton distances combined with quantum mechanical calculations of 13C chemical shifts in the stereochemical determination of conicasterol F, a nuclear receptor ligand from Theonella swinhoei

scientific article published on 23 January 2012

Quantum Mechanical Calculation of Coupling Constants in the Configurational Analysis of Flexible Systems: Determination of the Configuration of Callipeltin A

Retracted: Perthamide C Inhibits eNOS and iNOS Expression and Has Immunomodulating Activity In Vivo

retracted article

Reversal of Endothelial Dysfunction by GPBAR1 Agonism in Portal Hypertension Involves a AKT/FOXOA1 Dependent Regulation of H2S Generation and Endothelin-1.

scientific article published on 5 November 2015

Role of nuclear receptors in lipid dysfunction and obesity-related diseases.

scientific article

Solomonamides A and B, new anti-inflammatory peptides from Theonella swinhoei.

scientific article published on 22 February 2011

Solomonsterol A, a marine pregnane-X-receptor agonist, attenuates inflammation and immune dysfunction in a mouse model of arthritis.

scientific article published on 24 December 2013

Solomonsterols A and B from Theonella swinhoei. The first example of C-24 and C-23 sulfated sterols from a marine source endowed with a PXR agonistic activity

scientific article published on 9 December 2010

Stereochemical assignment of the C23–C35 portion of sphinxolide/reidispongiolide class of natural products by asymmetric synthesis

Stereoselective synthesis of (2R,3R,4R)-3-hydroxy-2,4,6-trimethylheptanoic acid and determination of the absolute stereochemistry of the natural product from callipeltin A

Steroidal scaffolds as FXR and GPBAR1 ligands: from chemistry to therapeutical application

scientific article published on July 2015

Structural insights into Estrogen Related Receptor-β modulation: 4-methylenesterols from Theonella swinhoei sponge as the first example of marine natural antagonists.

scientific article published on 4 December 2013

Structure-based drug design targeting the cell membrane receptor GPBAR1: exploiting the bile acid scaffold towards selective agonism

scientific article published on 16 November 2015

Structures of microfilament destabilizing toxins bound to actin provide insight into toxin design and activity

scientific article

Studies towards the synthesis of superstolide A. Synthesis and stereochemical assignment of the C(21)C(26) fragment of superstolide A

Su1053 - Bar704, a Potent and Selective Fxr Agonist Protects Against Intestinal Fibrosis

scholarly article published in May 2018

Swinholide J, a potent cytotoxin from the marine sponge Theonella swinhoei

scientific article published on 22 June 2011

Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors

scientific article published on March 2006

Synthetic and pharmacological studies on new simplified analogues of the potent actin-targeting Jaspamide.

scientific article

Synthetic studies on callipeltin A: stereoselective synthesis of (2 R ,3 R ,4 S )-3-hydroxy-2,4,6-trimethylheptanoic acid

Synthetic studies on homophymine A: stereoselective synthesis of (2R,3R,4R,6R)-3-hydroxy-2,4,6-trimethyloctanoic acid

Targeting Bile Acid Receptors: Discovery of a Potent and Selective Farnesoid X Receptor Agonist as a New Lead in the Pharmacological Approach to Liver Diseases

scientific article published on 30 March 2017

The Bile Acid Receptor GPBAR1 Modulates CCL2/CCR2 Signaling at the Liver Sinusoidal/Macrophage Interface and Reverses Acetaminophen-Induced Liver Toxicity

scientific article published on 25 March 2020

The Bile Acid Receptor GPBAR1 Regulates the M1/M2 Phenotype of Intestinal Macrophages and Activation of GPBAR1 Rescues Mice from Murine Colitis.

scientific article

The First Total Synthesis of Solomonsterol B, a Marine Pregnane X Receptor Agonist

The bile acid activated receptors GPBAR1 and FXR exert antagonistic effects on autophagy

scientific article published on 01 January 2021

The bile acid receptor GPBAR1 (TGR5) is expressed in human gastric cancers and promotes epithelial-mesenchymal transition in gastric cancer cell lines.

scientific article published on 07 July 2016

The bile acid sensor FXR is required for immune-regulatory activities of TLR-9 in intestinal inflammation

scientific journal article

The nuclear receptor FXR regulates hepatic transport and metabolism of glutamine and glutamate

scientific article

Theonellasterols and conicasterols from Theonella swinhoei. Novel marine natural ligands for human nuclear receptors.

scientific article

Theonellasterone, a steroidal metabolite isolated from a Theonella sponge, protects peroxiredoxin-1 from oxidative stress reactions

scientific article

Total synthesis and pharmacological characterization of solomonsterol A, a potent marine pregnane-X-receptor agonist endowed with anti-inflammatory activity

scientific article published on 3 June 2011

Towards new ligands of nuclear receptors. Discovery of malaitasterol A, an unique bis-secosterol from marine sponge Theonella swinhoei

scientific article published on 16 May 2011

Transcriptome Analysis of Dual FXR and GPBAR1 Agonism in Rodent Model of NASH Reveals Modulation of Lipid Droplets Formation.

scientific article

Tu1546 – Gpbar1 is a Modulator of Liver Immunity and Its Agonism Reverses Acetaminophen-Induced Hepatotoxicity by Modulating Recruitment of Liver Macrophages

scholarly article

Ursodeoxycholic acid is a GPBAR1 agonist and resets liver/intestinal FXR signaling in a model of diet-induced dysbiosis and NASH

scientific article published on 17 July 2019

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