The coordination capacity of thiosemicarbazone ligands and their synergism with palladium(II) ions modulate their reactivity, allowing custom design. Using thiosemicarbazones with two potential stable...

In Europa: Caroline de Gruyter

We are looking for a highly motivated PhD candidate to join the Montenegro Lab and carry out a doctoral thesis focused on the synthesis, functionalization, and evaluation of boron clusters and chaotro...

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The blood-brain barrier represents a significant challenge in delivering anticancer drugs for glioblastoma treatment. The study investigates the potential of a series of octahedral photoactivatable cyclometalated iridium complexes (Ir1–Ir10) with the general formula [Ir(ttpy)(C∧N)Cl]PF6 as photoactivated therapy candidates for the treatment of this aggressive tumor. These complexes, which include the terdentate ligand 4′-(p-tolyl)-2,2′:6′,2″-terpyridine (ttpy), and a C∧N ligand based on the deprotonated 2-arylbenzimidazole backbone, were tested on human glioblastoma using 2D cell cultures and 3D spheroidal models, including a fusion system comprising cerebral organoids from nonmalignant human-induced pluripotent stem cells and spheroids derived from malignant brain cells. The iridium complexes catalyze NADH photooxidation and photogenerate 1O2 and/or •OH under blue light irradiation. Blood-brain barrier penetration was assessed using various in vitro models. The complex Ir4, containing deprotonated methyl 1-butyl-2-phenylbenzimidazolecarboxylate, shows promise for targeted therapy of resistant brain tumors when photoactivated with blue light. Ir4 induces rapid and sustained ROS-mediated cytotoxicity and selectively accumulates in tumor tissue. This suggests its potential for fluorescently guided-PDT cooperative resection of glioblastoma. Notably, Ir4 significantly reduces glioblastoma growth even under dark conditions compared to conventional Temozolomide treatment without affecting healthy brain tissue.

We report a steered molecular dynamics (SMD) investigation into how substitution-inert polynuclear platinum complexes (SI-PPCs) influence the binding affinity between heparan sulphate (HS) and the enz...

Here we report a C3-symmetric metal-binding tripeptide, BTMA-1, that self-assembles in water into either a chiral supramolecular helical polymer or a discrete CoII peptide helicate, depending on metal coordination. The CoII peptide helicate exhibits high affinity and selectivity toward DNA three-way junctions (3WJ), a class of noncanonical DNA structures with emerging biological relevance. Importantly, we demonstrate that the recognition process can be triggered dynamically by adding CoII ions to a dispersion of the supramolecular polymer, which acts as an inert precursor reservoir in physiological media. In this way, our strategy shows that chiral supramolecular helical polymers can form temporarily inactive aggregates that release discrete helicates for biomolecular recognition, such as 3WJ binding, upon metal ion coordination. Overall, this mechanism reveals a previously unexplored capability of this class of materials and offers a new approach for the design of responsive supramolecular systems for nucleic acid recognition and anticancer therapy.