Alberto Dal Corso
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View article: Late-stage peptide modification with salicylaldehyde tag enhances affinity for nuclear factor-kappa B essential modulator
Late-stage peptide modification with salicylaldehyde tag enhances affinity for nuclear factor-kappa B essential modulator Open
We introduce a versatile click-chemistry strategy for a tailored insertion of salicylaldehyde (SA) tags onto peptides, aimed at forming imine adducts with lysine residues on target proteins, thereby enhancing binding affinity and complex s…
View article: Bifunctional Photocatalysts Display Proximity-Enhanced Catalytic Activity in Metallaphotoredox C–O Coupling
Bifunctional Photocatalysts Display Proximity-Enhanced Catalytic Activity in Metallaphotoredox C–O Coupling Open
Dual catalytic reactions may be made more effective through improved integration of the catalytic cycles achieved using bifunctional catalysts. Herein, we describe two bifunctional photocatalysts consisting of a photoactive donor-acceptor …
View article: Achieving High Affinity for a Bacterial Lectin with Reversible Covalent Ligands
Achieving High Affinity for a Bacterial Lectin with Reversible Covalent Ligands Open
High-affinity monovalent ligands for lectins are challenging to develop due to weak binding interactions. This study investigates the potential of rationally designed covalent ligands targeting the N-terminal domain of BC2L-C lectin from B…
View article: Bifunctional photocatalysts display proximity-enhanced catalytic activity in metallaphotoredox C–O coupling
Bifunctional photocatalysts display proximity-enhanced catalytic activity in metallaphotoredox C–O coupling Open
Dual catalytic reactions may be made more effective through an improved integration of the catalytic cycles achieved using bifunctional catalysts. Herein we describe new bifunctional photocatalysts consisting of a photoactive donor-accepto…
View article: Synthesis of Noncoded Amino Acids Bearing a Salicylaldehyde Tag for the Design of Reversible‐Covalent Peptides
Synthesis of Noncoded Amino Acids Bearing a Salicylaldehyde Tag for the Design of Reversible‐Covalent Peptides Open
Insertion of electrophilic species on the structure of small molecule ligands or peptides is a well‐known strategy to increase their binding affinity for the target protein of interest. Among these reactive units, the salicylaldehyde (SA) …
View article: Amine‐Carbamate Self‐Immolative Spacers Counterintuitively Release 3° Alcohol at Much Faster Rates than 1° Alcohol Payloads
Amine‐Carbamate Self‐Immolative Spacers Counterintuitively Release 3° Alcohol at Much Faster Rates than 1° Alcohol Payloads Open
Self‐immolative (SI) spacers are degradable chemical connectors widely used in prodrugs and drug conjugates to release pharmaceutical ingredients in response to specific stimuli. Amine‐carbamate SI spacers are particularly versatile, as th…
View article: Ex vivo mass spectrometry-based biodistribution analysis of an antibody-Resiquimod conjugate bearing a protease-cleavable and acid-labile linker
Ex vivo mass spectrometry-based biodistribution analysis of an antibody-Resiquimod conjugate bearing a protease-cleavable and acid-labile linker Open
Immune-stimulating antibody conjugates (ISACs) equipped with imidazoquinoline (IMD) payloads can stimulate endogenous immune cells to kill cancer cells, ultimately inducing long-lasting anticancer effects. A novel ISAC was designed, featur…
View article: A Tight Contact: The Expanding Application of Salicylaldehydes in Lysine‐Targeting Covalent Drugs
A Tight Contact: The Expanding Application of Salicylaldehydes in Lysine‐Targeting Covalent Drugs Open
The installation of aldehydes into synthetic protein ligands is an efficient strategy to engage protein lysine residues in remarkably stable imine bonds and augment the compound affinity and selectivity for their biological targets. The hi…
View article: Visible Light-Promoted β-Functionalization of Carbonyl Compounds in the Presence of Organic Dyes
Visible Light-Promoted β-Functionalization of Carbonyl Compounds in the Presence of Organic Dyes Open
Herein, we investigate the use of organic photocatalysts in the visible light-promoted β-functionalization of carbonyl compounds. In particular, we studied the addition of aliphatic aldehydes to α,β-unsaturated compounds (β-Michael additio…
View article: Data from Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma
Data from Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma Open
In most cases, cytotoxic drugs do not preferentially accumulate at the tumor site, causing unwanted toxicities and preventing dose escalation to therapeutically active regimens. Here, we show that acetazolamide derivatives, which bind to c…
View article: Data from Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma
Data from Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma Open
In most cases, cytotoxic drugs do not preferentially accumulate at the tumor site, causing unwanted toxicities and preventing dose escalation to therapeutically active regimens. Here, we show that acetazolamide derivatives, which bind to c…
View article: Supplementary Materials from Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma
Supplementary Materials from Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma Open
Herein we describe detailed synthetic procedures and characterization of the presented compounds (i.e., HPLC purity of final products, MS and NMR data, SPR assays), together with additional biological data (i.e., stability of 4a in the pre…
View article: Supplementary Materials from Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma
Supplementary Materials from Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma Open
Herein we describe detailed synthetic procedures and characterization of the presented compounds (i.e., HPLC purity of final products, MS and NMR data, SPR assays), together with additional biological data (i.e., stability of 4a in the pre…
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: Metallaphotoredox C−O and C−N Cross‐Coupling Using Donor‐Acceptor Cyanoarene Photocatalysts
Metallaphotoredox C−O and C−N Cross‐Coupling Using Donor‐Acceptor Cyanoarene Photocatalysts Open
Herein we report a study on the use of donor‐acceptor cyanoarenes as photocatalysts for C−O and C−N coupling reactions promoted by nickel. We found that some of these stable and readily available organic compounds can replace the precious …
View article: Advanced Pyrrolidine‐Carbamate Self‐Immolative Spacer with Tertiary Amine Handle Induces Superfast Cyclative Drug Release
Advanced Pyrrolidine‐Carbamate Self‐Immolative Spacer with Tertiary Amine Handle Induces Superfast Cyclative Drug Release Open
Amine‐carbamate self‐immolative (SI) spacers represent practical and versatile tools in targeted prodrugs, but their slow degradation mechanism limits drug activation at the site of disease. We engineered a pyrrolidine‐carbamate SI spacer …
View article: Functionalized 2‐Hydroxybenzaldehyde‐PEG Modules as Portable Tags for the Engagement of Protein Lysine ϵ‐Amino Groups
Functionalized 2‐Hydroxybenzaldehyde‐PEG Modules as Portable Tags for the Engagement of Protein Lysine ϵ‐Amino Groups Open
The formation of reversible‐covalent interactions between a small‐molecule ligand and its protein target is emerging as a general strategy to design binders with increased affinity. In this context, 2‐hydroxybenzaldehyde (2HB) has been rec…
View article: A trifunctional self-immolative spacer enables drug release with two non-sequential enzymatic cleavages
A trifunctional self-immolative spacer enables drug release with two non-sequential enzymatic cleavages Open
The enzymatic dephosphorylation of a self-immolative spacer accelerates cargo release and acts as an additional and independent trigger in protease-sensitive prodrugs.
View article: Targeted Small‐Molecule Conjugates: The Future is Now
Targeted Small‐Molecule Conjugates: The Future is Now Open
In recent years, novel classes of small hetero‐bifunctional compounds have been developed as tools for the treatment of cancer and other diseases through different approaches, from radio/chemotherapy and imaging to immunotherapy and protei…
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: Fast Cyclization of a Proline‐Derived Self‐Immolative Spacer Improves the Efficacy of Carbamate Prodrugs
Fast Cyclization of a Proline‐Derived Self‐Immolative Spacer Improves the Efficacy of Carbamate Prodrugs Open
Self‐immolative (SI) spacers are sophisticated chemical constructs designed for molecular delivery or material degradation. We describe herein a ( S )‐2‐(aminomethyl)pyrrolidine SI spacer that is able to release different types of anticanc…
View article: Frontispiece: Innovative Linker Strategies for Tumor‐Targeted Drug Conjugates
Frontispiece: Innovative Linker Strategies for Tumor‐Targeted Drug Conjugates Open
Improvement of the pharmacological effects of cytotoxic agents with a concomitant decrease of systemic toxicity has been investigated for decades in order to reduce the side effects of tumor-targeting drugs. In their Review article, A. Dal…
View article: Innovative Linker Strategies for Tumor‐Targeted Drug Conjugates
Innovative Linker Strategies for Tumor‐Targeted Drug Conjugates Open
The covalent conjugation of potent cytotoxic agents to either macromolecular carriers or small molecules represents a well‐known approach to increase the therapeutic index of these drugs, thus improving treatment efficacy and minimizing si…
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: CCDC 1885148: Experimental Crystal Structure Determination
CCDC 1885148: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
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…