List of works - Francesco Saverio Di Leva

Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase

scientific article

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

Biselectivity of isoDGR peptides for fibronectin binding integrin subtypes α5β1 and αvβ6: conformational control through flanking amino acids

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 N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75.

scientific article published on 22 June 2015

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

Exploring the N-Terminal Region of C-X-C Motif Chemokine 12 (CXCL12): Identification of Plasma-Stable Cyclic Peptides As Novel, Potent C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonists

scientific article

Exploring the chemical space of G-quadruplex binders: discovery of a novel chemotype targeting the human telomeric sequence

scientific article published on 27 November 2013

From a Helix to a Small Cycle: Metadynamics-Inspired αvβ6 Integrin Selective Ligands.

scientific article published on 16 April 2018

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

scientific article

Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by Diketo acid derivatives

scientific article

Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: A first round of lead optimization

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

Lead Discovery of Dual G-Quadruplex Stabilizers and Poly(ADP-ribose) Polymerases (PARPs) Inhibitors: A New Avenue in Anticancer Treatment.

scientific article

Ligand-Based NMR Study of C-X-C Chemokine Receptor Type 4 (CXCR4)-Ligand Interactions on Living Cancer Cells

scientific article published on 9 March 2018

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

scientific article

Mechanistic insight into ligand binding to G-quadruplex DNA

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

Monothiocarbamates Strongly Inhibit Carbonic Anhydrases in Vitro and Possess Intraocular Pressure Lowering Activity in an Animal Model of Glaucoma

scientific article published on 2 June 2016

N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase

scientific article

New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H.

scientific article

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

scientific article published on 06 December 2018

Overcoming the Lack of Oral Availability of Cyclic Hexapeptides: Design of a Selective and Orally Available Ligand for the Integrin αvβ3.

scientific article

Pharmacophoric modifications lead to superpotent αvβ3 integrin ligands with suppressed α5β1 activity

scientific article

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors

scientific article published on 16 September 2013

Protein flexibility in virtual screening: the BACE-1 case study

scientific article

Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides

scientific article

Stable Peptides Instead of Stapled Peptides: Highly Potent αvβ6-Selective Integrin Ligands

scientific article published on 9 December 2015

State-of-the-art methodologies for the discovery and characterization of DNA G-quadruplex binders.

scientific article published on January 2012

Structural Insight into the Binding Mode of FXR and GPBAR1 Modulators

scientific article published on 01 January 2019

Structure-Activity Relationships and Biological Characterization of a Novel, Potent, and Serum Stable C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonist

scientific article published on 10 November 2017

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

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 ring residue proline 8 is crucial for the thermal stability of the lasso peptide caulosegnin II

scientific article

List of works by Francesco Saverio Di Leva

Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase

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.

Biselectivity of isoDGR peptides for fibronectin binding integrin subtypes α5β1 and αvβ6: conformational control through flanking amino acids

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

Discovery of N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75.

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

Exploring the N-Terminal Region of C-X-C Motif Chemokine 12 (CXCL12): Identification of Plasma-Stable Cyclic Peptides As Novel, Potent C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonists

Exploring the chemical space of G-quadruplex binders: discovery of a novel chemotype targeting the human telomeric sequence

From a Helix to a Small Cycle: Metadynamics-Inspired αvβ6 Integrin Selective Ligands.

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

Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by Diketo acid derivatives

Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: A first round of lead optimization

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

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

Lead Discovery of Dual G-Quadruplex Stabilizers and Poly(ADP-ribose) Polymerases (PARPs) Inhibitors: A New Avenue in Anticancer Treatment.

Ligand-Based NMR Study of C-X-C Chemokine Receptor Type 4 (CXCR4)-Ligand Interactions on Living Cancer Cells

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

Mechanistic insight into ligand binding to G-quadruplex DNA

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)

Monothiocarbamates Strongly Inhibit Carbonic Anhydrases in Vitro and Possess Intraocular Pressure Lowering Activity in an Animal Model of Glaucoma

N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase

New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H.

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

Overcoming the Lack of Oral Availability of Cyclic Hexapeptides: Design of a Selective and Orally Available Ligand for the Integrin αvβ3.

Pharmacophoric modifications lead to superpotent αvβ3 integrin ligands with suppressed α5β1 activity

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors

Protein flexibility in virtual screening: the BACE-1 case study

Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides

Stable Peptides Instead of Stapled Peptides: Highly Potent αvβ6-Selective Integrin Ligands

State-of-the-art methodologies for the discovery and characterization of DNA G-quadruplex binders.

Structural Insight into the Binding Mode of FXR and GPBAR1 Modulators

Structure-Activity Relationships and Biological Characterization of a Novel, Potent, and Serum Stable C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonist

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

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 ring residue proline 8 is crucial for the thermal stability of the lasso peptide caulosegnin II