List of works - Valentina Sepe

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

scientific article published on 19 June 2020

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

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

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

scientific article published on 17 January 2014

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)

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 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

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

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 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 callipeltins J–M: antifungal peptides from the marine sponge Latrunculia sp

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

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

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

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

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

scientific article published on 06 December 2018

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

Perthamides C–F, potent human antipsoriatic cyclopeptides

Phallusiasterols A and B: two new sulfated sterols from the Mediterranean tunicate Phallusia fumigata and their effects as modulators of the PXR receptor.

scientific article published on 3 April 2014

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

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

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

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

scientific article published on July 2015

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

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

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

List of works by Valentina Sepe

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

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

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

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

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.

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

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

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

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

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.

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

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

Farnesoid X receptor modulators 2014-present: a patent review

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

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

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

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

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

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

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

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

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

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

Isolation and structural elucidation of callipeltins J–M: antifungal peptides from the marine sponge Latrunculia sp

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

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

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

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)

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

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

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

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

Perthamides C–F, potent human antipsoriatic cyclopeptides

Phallusiasterols A and B: two new sulfated sterols from the Mediterranean tunicate Phallusia fumigata and their effects as modulators of the PXR receptor.

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

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

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

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

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

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

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

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

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

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

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

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

Triterpenoid profile and bioactivity study of Oenothera maritima