Protein binding heavily modulates drug activity. Therefore, the binding features need to be elucidated when chemistry researchers study new molecules to be used as drugs. This short review concerns the analysis of the binding of small molecules to a fluorescent protein (the golden standard serum albumin) by using direct fluorescence titrations. This widely used technique is valuable, but often much more tricky than it might appear at first sight. We aim to share a mechanistic approach, discussing the critical aspects for correctly designing the experiments and treating the data.
Congratulations to our Ph.D. student Francesca Binacchi for her recent scientific pubblication entitled: "On the Different Mode of Action of Au(I)/Ag(I)-NHC Bis-Anthracenyl Complexes Towards Selected Target Biomolecules" Gold and silver N-heterocyclic carbenes (NHCs) are emerging for therapeutic applications. Multiple techniques are here used to unveil the mechanistic details of the binding to different biosubstrates of bis(1-(anthracen-9-ylmethyl)-3-ethylimidazol-2-ylidene) silver chloride [Ag(EIA)2]Cl and bis(1-(anthracen-9-ylmethyl)-3-ethylimidazol-2-ylidene) gold chloride [Au(EIA)2]Cl.
Congratulations to our Ph.D. students Simona Braccini and Gianni Pecorini for their scientific publication entitled “Adhesion of fibroblast cells on thin films representing surfaces of polymeric scaffolds of human urethra rationalized by molecular models of integrin binding: cell adhesion on polymeric scaffolds for regenerative medicine” in the journal “Journal of Biotechnology”.
An inexpensive and new triphenylphosphine‐based palladacycle has been developed as a pre‐catalyst leading to highly effective Stille cross coupling reactions in water under mild conditions. Only 500‐1000 ppm of Pd suffices for couplings involving a variety of aryl/heteroaryl halides with aryl/hetaryl stannanes. Several drug intermediates can be prepared using this catalyst in aqueous nanoreactors formed by 2 wt % Brij‐30 in water.
New bis-quinolinium chiral ionic liquids (CILs) were synthesized in good yields starting from isomannide and isosorbide by a straightforward procedure that maintains the absolute stereostructure of the isohexide scaffolds. Thermal gravimetric analysis and differential scanning calorimetry, aimed at investigating the short thermal stability and the thermal behaviour of the synthesized ionic compounds are presented.
We present a fluorescent pH biosensor based on a conjugated coumarin-triazine scaffold that is excitable in the visible range, shows pseudo-linear ratiometric response over more than 6 pH units with a single fluorogenic unit, and allows imaging of the whole endo-lysosomal pH landscape of living cells with a single acquisition. The probe can discriminate, on the basis of intracellular acidity, between physiologic and tumor cells, being potentially suitable in perspective as diagnostic tool.