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Progresses in the pursuit of aldose reductase inhibitors: the structure-based lead optimization step.
Aldose reductase (ALR2) is a crucial enzyme in the development of the major complications of diabetes mellitus. Very recently it has been demonstrated that the ARL2 inhibitor, fidarestat,Expand
Pharmacological folding chaperones act as allosteric ligands of Frizzled4.
Upon binding, ligands can chaperone their protein targets by preventing them from misfolding and aggregating. Thus, an organic molecule that works as folding chaperone for a protein might be itsExpand
Bax Activation Blocks Self-Renewal and Induces Apoptosis of Human Glioblastoma Stem Cells.
Glioblastoma (GBM) is characterized by a poor response to conventional chemotherapeutic agents, attributed to the insurgence of drug resistance mechanisms and to the presence of a subpopulation ofExpand
To each his own: isonitriles for all flavors. Functionalized isocyanides as valuable tools in organic synthesis.
The term functionalized isocyanides refers to all those isocyanides in which a neighbouring functional group can finely tune the reactivity of the isocyano group or can be exploited inExpand
Shooting for selective druglike G-quadruplex binders: evidence for telomeric DNA damage and tumor cell death.
Targeting of DNA secondary structures, such as G-quadruplexes, is now considered an appealing opportunity for drug intervention in anticancer therapy. So far, efforts made in the discovery ofExpand
Replacement of the double bond of antitubulin chalcones with triazoles and tetrazoles: Synthesis and biological evaluation.
In the chalcone scaffold, it is thought that the double bond is an important structural linker but it is likely not essential for the interaction with tubulin. Yet, it may be a potential site ofExpand
Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents.
The first direct activator of BAX, a pro-apoptotic member of the BCL-2 family, has been recently identified. Herein, a structure-based lead optimization turned out into a small series of analogues,Expand
Amino Acid Derivatives as New Zinc Binding Groups for the Design of Selective Matrix Metalloproteinase Inhibitors
A number of matrix metalloproteinases (MMPs) are important medicinal targets for conditions ranging from rheumatoid arthritis to cardiomyopathy, periodontal disease, liver cirrhosis, multipleExpand
Targeting the BCL2 Gene Promoter G‐Quadruplex with a New Class of Furopyridazinone‐Based Molecules
Targeting of G‐quadruplex‐forming DNA in the BCL2 gene promoter to inhibit the expression of anti‐apoptotic Bcl‐2 protein is an attractive approach to cancer treatment. So far, efforts made in theExpand
Novel peptidomimetics as BACE-1 inhibitors: synthesis, molecular modeling, and biological studies.
Aiming at identifying new scaffolds for BACE-1 inhibition devoid of the pharmacokinetic drawbacks of peptide-like structures, we investigated a series of novel peptidomimetics based on aExpand