F. S. Di Leva

发表

Targeting the KRAS Oncogene: Synthesis, Physicochemical and Biological Evaluation of Novel G-Quadruplex DNA Binders.

E. Novellino, G. Salgado, F. Da Settimo, 2020, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

The organometallic ferrocene exhibits amplified anti-tumor activity by targeted delivery via highly selective ligands to αvβ3, αvβ6, or α5β1 integrins.

H. Kessler, S. Di Maro, U. Reuning, 2021, Biomaterials.

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

E. Novellino, M. Schwaiger, H. Kessler, 2016, Angewandte Chemie.

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

E. Novellino, H. Kessler, F. Rechenmacher, 2014, Journal of medicinal chemistry.

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

A. Carino, S. Marchianò, C. Finamore, 2019, ACS medicinal chemistry letters.

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

Y. Pommier, E. Novellino, F. Da Settimo, 2013, Journal of medicinal chemistry.

The Inhibition of DNA Viruses by the Amphibian Antimicrobial Peptide Temporin G: A Virological Study Addressing HSV-1 and JPCyV

L. Nencioni, A. Palamara, A. Carotenuto, 2022, International journal of molecular sciences.

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

E. Novellino, H. Kessler, D. Brancaccio, 2018, Angewandte Chemie.

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

E. Novellino, H. Kessler, F. Rechenmacher, 2017, Angewandte Chemie.

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

E. Novellino, S. Zahler, M. Marahiel, 2014, Journal of medicinal chemistry.

GPBAR1 Activation by C6-Substituted Hyodeoxycholane Analogues Protect against Colitis.

E. Novellino, A. Carino, S. Marchianò, 2020, ACS medicinal chemistry letters.

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

E. Novellino, L. Portella, S. Scala, 2018, Journal of medicinal chemistry.

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

E. Novellino, A. Carino, S. Marchianò, 2018, ACS medicinal chemistry letters.

Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities

V. Summa, F. S. Di Leva, A. Beccari, 2020, Journal of medicinal chemistry.

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

Y. Pommier, E. Novellino, S. L. Le Grice, 2015, Journal of medicinal chemistry.

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

E. Novellino, F. Da Settimo, S. Taliani, 2012, European journal of medicinal chemistry.

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

E. Novellino, C. Supuran, A. Scozzafava, 2016, Journal of medicinal chemistry.

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

S. Marchianò, V. Sepe, E. Distrutti, 2017, Front. Pharmacol..

Identification of Highly Conserved Residues Involved in Inhibition of HIV-1 RNase H Function by Diketo Acid Derivatives

E. Novellino, O. Delelis, R. Di Santo, 2014, Antimicrobial Agents and Chemotherapy.

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

V. Sepe, A. Zampella, S. Fiorucci, 2014, Journal of medicinal chemistry.

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

S. Marchianò, V. Sepe, C. Finamore, 2019, Molecules.

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

E. Novellino, B. Pagano, Valeria La Pietra, 2012, Current pharmaceutical design.

Mechanistic insight into ligand binding to G-quadruplex DNA

A. Cavalli, M. Parrinello, E. Novellino, 2014, Nucleic acids research.

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

E. Novellino, O. Delelis, R. Di Santo, 2016, Antiviral research.

Basic Quinolinonyl Diketo Acid Derivatives as Inhibitors of HIV Integrase and their Activity against RNase H Function of Reverse Transcriptase

Y. Pommier, E. Novellino, S. L. Le Grice, 2014, Journal of medicinal chemistry.

Selective Targeting of Integrin αvβ8 by a Highly Active Cyclic Peptide.

M. Schwaiger, H. Kessler, S. Di Maro, 2019, Journal of medicinal chemistry.

Marine and Semi-Synthetic Hydroxysteroids as New Scaffolds for Pregnane X Receptor Modulation

E. Novellino, V. Sepe, A. Zampella, 2014, Marine drugs.

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

E. Novellino, B. Pagano, L. Botta, 2017, Journal of medicinal chemistry.

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).

E. Novellino, V. Sepe, A. Zampella, 2014, Journal of medicinal chemistry.

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

E. Novellino, L. Portella, S. Scala, 2017, Journal of medicinal chemistry.

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.

E. Novellino, L. Portella, C. Ieranò, 2016, Journal of medicinal chemistry.

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

E. Novellino, H. Kessler, J. Spatz, 2013, Journal of medicinal chemistry.

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

S. Marchianò, C. Finamore, A. Zampella, 2019, Scientific Reports.

Disulfide bond replacement with 1,4- and 1,5-disubstituted [1,2,3]-triazole on C-X-C chemokine receptor type 4 (CXCR4) peptide ligands: small changes that make big differences.

E. Novellino, C. Ieranò, S. Scala, 2020, Chemistry.

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

A. Cavalli, E. Novellino, B. Pagano, 2013, Journal of medicinal chemistry.

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

E. Novellino, R. Di Santo, R. Costi, 2015, European journal of medicinal chemistry.

Bioinformatics and Biosimulations as Toolbox for Peptides and Peptidomimetics Design: Where Are We?

Vittorio Limongelli, Ilda D’Annessa, Francesco Saverio Di Leva, 2020, Frontiers in Molecular Biosciences.

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

E. Novellino, S. Marchianò, C. Finamore, 2017, Scientific Reports.

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

Ettore Novellino, Vittorio Limongelli, Francesco Saverio Di Leva, 2015, Scientific Reports.

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

E. Novellino, M. Marahiel, L. Marinelli, 2016, Molecular bioSystems.

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.

E. Novellino, A. Zampella, S. Fiorucci, 2013, Journal of medicinal chemistry.

Discovery of dihydroxyindole-2-carboxylic acid derivatives as dual allosteric HIV-1 Integrase and Reverse Transcriptase associated Ribonuclease H inhibitors.

E. Novellino, L. Naesens, R. Di Santo, 2019, Antiviral research.

Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.

E. Novellino, F. Da Settimo, S. Taliani, 2018, Journal of medicinal chemistry.

Theoretical and experimental studies on the interaction of biphenyl ligands with human and murine PD-L1: Up-to-date clues for drug design

P. Seneci, L. Cerofolini, M. Fragai, 2023, Computational and structural biotechnology journal.

Structural Insight into the Binding Mode of FXR and GPBAR1 Modulators.

V. Limongelli, F. S. Di Leva, D. Di Marino, 2019, Handbook of experimental pharmacology.

Broad-spectrum coronavirus 3C-like protease peptidomimetic inhibitors effectively block SARS-CoV-2 replication in cells: Design, synthesis, biological evaluation, and X-ray structure determination

M. Brindisi, V. Summa, P. Storici, 2023, European Journal of Medicinal Chemistry.

Exploring the 1,3-benzoxazine chemotype for cannabinoid receptor 2 as a promising anti-cancer therapeutic.

M. Maccarrone, L. Marinelli, F. S. Di Leva, 2023, European journal of medicinal chemistry.

Halting the Spread of Herpes Simplex Virus-1: The Discovery of an Effective Dual αvβ6/αvβ8 Integrin Ligand

E. Novellino, H. Kessler, G. Quilici, 2021, Journal of medicinal chemistry.

Molecular View on the iRGD Peptide Binding Mechanism: Implications for Integrin Activity and Selectivity Profiles

L. Marinelli, F. S. Di Leva, M. Baiula, 2023, Journal of chemical information and modeling.

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.

E. Novellino, L. Portella, C. Ieranò, 2016, Journal of medicinal chemistry.

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

E. Novellino, M. Marahiel, L. Marinelli, 2016, Molecular bioSystems.

Discovery of 2,3-Diaminoindole Derivatives as a Novel Class of NOD Antagonists.

A. Carotenuto, L. Marinelli, F. S. Di Leva, 2024, Journal of medicinal chemistry.