Daniela Arosio
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View article: Identification of new selective CD36 inhibitors to potentiate HER2-targeted therapy in HER2-positive breast cancer
Identification of new selective CD36 inhibitors to potentiate HER2-targeted therapy in HER2-positive breast cancer Open
HER2 overexpression/amplification (HER2+) occurs in approximately 15-20% of breast cancer (BC) and identifies a highly aggressive BC subtype. The cure rate of HER2 + BC has been significantly increased through recent clinical achievements;…
View article: Synthesis and Preliminary Evaluation of Tanshinone Mimic Conjugates for Mechanism of Action Studies
Synthesis and Preliminary Evaluation of Tanshinone Mimic Conjugates for Mechanism of Action Studies Open
Human antigen R (HuR) is an RNA binding protein (RBP) belonging to the ELAV (Embryonic Lethal Abnormal Vision) family, which stabilizes mRNAs and regulates the expression of multiple genes. Its altered expression or localization is related…
View article: Novel, soluble 3-heteroaryl-substituted tanshinone mimics attenuate the inflammatory response in murine macrophages
Novel, soluble 3-heteroaryl-substituted tanshinone mimics attenuate the inflammatory response in murine macrophages Open
View article: A combined approach of structure‐based virtual screening and NMR to interrupt the PD‐1/PD‐L1 axis: Biphenyl‐benzimidazole containing compounds as novel PD‐L1 inhibitors
A combined approach of structure‐based virtual screening and NMR to interrupt the PD‐1/PD‐L1 axis: Biphenyl‐benzimidazole containing compounds as novel PD‐L1 inhibitors Open
Immunotherapy has emerged as a game‐changing approach for cancer treatment. Although monoclonal antibodies (mAbs) targeting the programmed cell death protein 1/programmed cell death protein 1 ligand 1 (PD‐1/PD‐L1) axis have entered the mar…
View article: HuR modulation counteracts lipopolysaccharide response in murine macrophages
HuR modulation counteracts lipopolysaccharide response in murine macrophages Open
Lipopolysaccharide (LPS) exposure to macrophages induces an inflammatory response, which is regulated at the transcriptional and post-transcriptional levels. HuR (ELAVL1) is an RNA-binding protein that regulates cytokines and chemokines tr…
View article: HuR modulation with tanshinone mimics impairs LPS response in murine macrophages
HuR modulation with tanshinone mimics impairs LPS response in murine macrophages Open
Lipopolysaccharide exposure to macrophages induces an inflammatory response that is heavily regulated at the transcriptional and post-transcriptional levels. HuR (ELAVL1) is an RNA binding protein that binds and regulates the maturation an…
View article: RGD Cyclopeptide Equipped with a Lysine‐Engaging Salicylaldehyde Showing Enhanced Integrin Affinity and Cell Detachment Potency
RGD Cyclopeptide Equipped with a Lysine‐Engaging Salicylaldehyde Showing Enhanced Integrin Affinity and Cell Detachment Potency Open
Salicylaldehyde (SA) derivatives are emerging as useful fragments to obtain reversible‐covalent inhibitors interacting with the lysine residues of the target protein. Here the SA installation at the C terminus of an integrin‐binding cyclop…
View article: Theoretical and experimental studies on the interaction of biphenyl ligands with human and murine PD-L1: Up-to-date clues for drug design
Theoretical and experimental studies on the interaction of biphenyl ligands with human and murine PD-L1: Up-to-date clues for drug design Open
View article: Tanshinone Mimics Bearing a 3-Heterocyclic Ring Endowed with Increased Solubility and Anti-Inflammatory Properties
Tanshinone Mimics Bearing a 3-Heterocyclic Ring Endowed with Increased Solubility and Anti-Inflammatory Properties Open
View article: Squalene-Based Nano-Assemblies Improve the Pro-Autophagic Activity of Trehalose
Squalene-Based Nano-Assemblies Improve the Pro-Autophagic Activity of Trehalose Open
The disaccharide trehalose is a well-established autophagy inducer, but its therapeutic application is severely hampered by its low potency and poor pharmacokinetic profile. Thus, we targeted the rational design and synthesis of trehalose-…
View article: HuR-targeted agents: An insight into medicinal chemistry, biophysical, computational studies and pharmacological effects on cancer models
HuR-targeted agents: An insight into medicinal chemistry, biophysical, computational studies and pharmacological effects on cancer models Open
View article: Interfering with the Tumor–Immune Interface: Making Way for Triazine-Based Small Molecules as Novel PD-L1 Inhibitors
Interfering with the Tumor–Immune Interface: Making Way for Triazine-Based Small Molecules as Novel PD-L1 Inhibitors Open
The inhibition of the PD-1/PD-L1 axis by monoclonal antibodies has achieved remarkable success in treating a growing number of cancers. However, a novel class of small organic molecules, with BMS-202 (1) as the lead, is emerging as …
View article: Cyclic RGD and isoDGR Integrin Ligands Containing cis-2-amino-1-cyclopentanecarboxylic (cis-β-ACPC) Scaffolds
Cyclic RGD and isoDGR Integrin Ligands Containing cis-2-amino-1-cyclopentanecarboxylic (cis-β-ACPC) Scaffolds Open
Integrin ligands containing the tripeptide sequences Arg-Gly-Asp (RGD) and iso-Asp-Gly- Arg (isoDGR) were actively investigated as inhibitors of tumor angiogenesis and directing unit in tumor-targeting drug conjugates. Reported herein is t…
View article: Multimeric Presentation of RGD Peptidomimetics Enhances Integrin Binding and Tumor Cell Uptake
Multimeric Presentation of RGD Peptidomimetics Enhances Integrin Binding and Tumor Cell Uptake Open
The use of multimeric ligands is considered as a promising strategy to improve tumor targeting for diagnosis and therapy. Herein, tetrameric RGD (Arg‐Gly‐Asp) peptidomimetics were designed to target α v β 3 integrin‐expressing tumor cells.…
View article: Kiss and Run: Promoting Effective and Targeted Cellular Uptake of a Drug Delivery Vehicle Composed of an Integrin-Targeting Diketopiperazine Peptidomimetic and a Cell-Penetrating Peptide
Kiss and Run: Promoting Effective and Targeted Cellular Uptake of a Drug Delivery Vehicle Composed of an Integrin-Targeting Diketopiperazine Peptidomimetic and a Cell-Penetrating Peptide Open
Cell-penetrating peptides (CPPs) have emerged as powerful tools in terms of drug delivery. Those short, often cationic peptides are characterized by their usually low toxicity and their ability to transport diverse cargos inside almost any…
View article: Conjugates of Cryptophycin and RGD or <i>iso</i>DGR Peptidomimetics for Targeted Drug Delivery
Conjugates of Cryptophycin and RGD or <i>iso</i>DGR Peptidomimetics for Targeted Drug Delivery Open
RGD‐cryptophycin and iso DGR‐cryptophycin conjugates were synthetized by combining peptidomimetic integrin ligands and cryptophycin, a highly potent tubulin‐binding antimitotic agent across lysosomally cleavable Val‐Ala or uncleavable link…
View article: Intracisternal delivery of PEG-coated gold nanoparticles results in high brain penetrance and long-lasting stability
Intracisternal delivery of PEG-coated gold nanoparticles results in high brain penetrance and long-lasting stability Open
View article: Rational Design of Antiangiogenic Helical Oligopeptides Targeting the Vascular Endothelial Growth Factor Receptors
Rational Design of Antiangiogenic Helical Oligopeptides Targeting the Vascular Endothelial Growth Factor Receptors Open
Tumor angiogenesis, essential for cancer development, is regulated mainly by vascular endothelial growth factors (VEGFs) and their receptors (VEGFRs), which are overexpressed in cancer cells. Therefore, the VEGF/VEGFR interaction represent…
View article: Synthesis and Biological Evaluation of RGD and <i>iso</i>DGR–Monomethyl Auristatin Conjugates Targeting Integrin α<sub>V</sub>β<sub>3</sub>
Synthesis and Biological Evaluation of RGD and <i>iso</i>DGR–Monomethyl Auristatin Conjugates Targeting Integrin α<sub>V</sub>β<sub>3</sub> Open
This work reports the synthesis of a series of small‐molecule–drug conjugates containing the α V β 3 ‐integrin ligand cyclo [DKP‐RGD] or cyclo [DKP‐ iso DGR], a lysosomally cleavable Val‐Ala (VA) linker or an “uncleavable” version devoid o…
View article: A dimeric bicyclic RGD ligand displays enhanced integrin binding affinity and strong biological effects on U-373 MG glioblastoma cells
A dimeric bicyclic RGD ligand displays enhanced integrin binding affinity and strong biological effects on U-373 MG glioblastoma cells Open
AC2-symmetric dimeric bicyclic integrin ligand, bearing two RGD motifs, displays enhanced biological effects compared to monovalent RGD analogues.
View article: β-Glucuronidase triggers extracellular MMAE release from an integrin-targeted conjugate
β-Glucuronidase triggers extracellular MMAE release from an integrin-targeted conjugate Open
A non-internalizing conjugate targeting αvβ3 integrin inhibits the proliferation of integrin-expressing cancer cells in the presence of β-glucuronidase.
View article: Neutrophil Elastase Promotes Linker Cleavage and Paclitaxel Release from an Integrin‐Targeted Conjugate
Neutrophil Elastase Promotes Linker Cleavage and Paclitaxel Release from an Integrin‐Targeted Conjugate Open
This work takes advantage of one of the hallmarks of cancer, that is, the presence of tumor infiltrating cells of the immune system and leukocyte‐secreted enzymes, to promote the activation of an anticancer drug at the tumor site. The pept…
View article: Synthesis and Biological Evaluation of Paclitaxel Conjugates Involving Linkers Cleavable by Lysosomal Enzymes and α<sub>V</sub>β<sub>3</sub>‐Integrin Ligands for Tumor Targeting
Synthesis and Biological Evaluation of Paclitaxel Conjugates Involving Linkers Cleavable by Lysosomal Enzymes and α<sub>V</sub>β<sub>3</sub>‐Integrin Ligands for Tumor Targeting Open
Two cyclo [DKP‐RGD]‐PTX (PTX = paclitaxel) and two cyclo [RGDfK]‐PTX conjugates containing the Gly‐Phe‐Leu‐Gly (GFLG) linker, which is cleavable by lysosomal enzymes, were synthesized and compared to two cyclo [DKP‐RGD]‐Val‐Ala‐PTX conjuga…
View article: Synthesis and biological evaluation of RGD and isoDGR peptidomimetic-α-amanitin conjugates for tumor-targeting
Synthesis and biological evaluation of RGD and isoDGR peptidomimetic-α-amanitin conjugates for tumor-targeting Open
RGD-α-amanitin and isoDGR-α-amanitin conjugates were synthesized by joining integrin ligands to α-amanitin via various linkers and spacers. The conjugates were evaluated for their ability to inhibit biotinylated vitronectin binding to the …
View article: Stereodivergent synthesis of 5-aminopipecolic acids and application in the preparation of a cyclic RGD peptidomimetic as a nanomolar α<sub>V</sub>β<sub>3</sub> integrin ligand
Stereodivergent synthesis of 5-aminopipecolic acids and application in the preparation of a cyclic RGD peptidomimetic as a nanomolar α<sub>V</sub>β<sub>3</sub> integrin ligand Open
A stereodivergent preparation of trans and cis-5-aminopipecolic acids (5-APAs) was developed to obtain constrained amino acids useful for peptidomimetics.
View article: Investigating the Interaction of Cyclic RGD Peptidomimetics with αVβ6 Integrin by Biochemical and Molecular Docking Studies
Investigating the Interaction of Cyclic RGD Peptidomimetics with αVβ6 Integrin by Biochemical and Molecular Docking Studies Open
The interaction of a small library of cyclic RGD (Arg-Gly-Asp) peptidomimetics with αVβ6 integrin has been investigated by means of competitive solid phase binding assays to the isolated receptor and docking calculations in the crystal str…
View article: Multivalency Increases the Binding Strength of RGD Peptidomimetic‐Paclitaxel Conjugates to Integrin α<sub>V</sub>β<sub>3</sub>
Multivalency Increases the Binding Strength of RGD Peptidomimetic‐Paclitaxel Conjugates to Integrin α<sub>V</sub>β<sub>3</sub> Open
This work reports the synthesis of three multimeric RGD peptidomimetic‐paclitaxel conjugates featuring a number of α V β 3 integrin ligands ranging from 2 to 4. These constructs were assembled by conjugation of the integrin α V β 3 ligand …
View article: Targeting Integrin α <sub>V</sub> β <sub>3</sub> with Theranostic RGD‐Camptothecin Conjugates Bearing a Disulfide Linker: Biological Evaluation Reveals a Complex Scenario
Targeting Integrin α <sub>V</sub> β <sub>3</sub> with Theranostic RGD‐Camptothecin Conjugates Bearing a Disulfide Linker: Biological Evaluation Reveals a Complex Scenario Open
Theranostic RGD‐camptothecin conjugates, possessing a disulfide linker and a fluorescent naphthalimide moiety, were synthesized and biologically evaluated. The conjugates showed nanomolar affinity for the purified α V β 3 ‐integrin recepto…
View article: Tumor Targeting with an <i>iso</i>DGR–Drug Conjugate
Tumor Targeting with an <i>iso</i>DGR–Drug Conjugate Open
Herein we report the first example of an iso DGR–drug conjugate ( 2 ), designed to release paclitaxel selectively within cancer cells expressing integrin α V β 3 . Conjugate 2 was synthesized by connecting the iso DGR peptidomimetic 5 with…
View article: 4-Connected azabicyclo[5.3.0]decane Smac mimetics-Zn2+ chelators as dual action antitumoral agents
4-Connected azabicyclo[5.3.0]decane Smac mimetics-Zn2+ chelators as dual action antitumoral agents Open