Gianfranco Cavallaro

Dysregulation of Human ClpP Using Small Molecules with Piperazine-Based Scaffold for Diffuse Intrinsic Pontine Glioma Therapy Validated by Patient-Derived Tumor Organoids

Morena Miciaccia, Domenico Armenise, Olga Maria Baldelli, Anselma Liturri et autres

Diffuse intrinsic pontine glioma (DIPG) is a dismal pediatric brainstem tumor with a median survival of approximately 12 months and no curative treatments. ONC201, the most clinically characterized small-molecule, selectively activates human caseinolytic protease P (hClpP). Guided by X-ray structure of the …

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Dysregulation of human ClpP using small molecules with piperazine-based scaffold for diffuse intrinsic pontine glioma therapy validated by patient-derived tumor organoids

Antonio Scilimati, Morena Miciaccia, Domenico Armenise, Olga Maria Baldelli et autres

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Influence of Extraction Method on the Bioactivity of Pistacia vera L. Extracts: Metabolic and Gene Expression Changes in Colorectal Cancer Cells

Giulia Zerbo, Paolo Giuseppe Bonacci, Morena Terrana, Valentina Greco et autres

Sustainable extraction methods represent a key strategy in green chemistry and nutraceutical development, aiming to replace conventional solvent-based techniques while maintaining extract quality and safety. This study compared pistachio (Pistacia vera L.) extracts obtained by Ultrasound-Assisted Extraction (UAE) and a classical solvent-based …

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Influence of Extraction Method on the Bioactivity of Pistachio Extracts: Metabolic and Gene Expression Changes in Colorectal Cancer Cells

Giulia Zerbo, Paolo Giuseppe Bonacci, Morena Terrana, Valentina Greco et autres

Sustainable extraction methods represent a key strategy in green chemistry and nutraceutical development, aiming to replace conventional solvent-based techniques while maintaining extract quality and safety. This study compared pistachio ( Pistacia vera L.) extracts obtained by ultrasound-assisted extraction (UAE) and a traditional …

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Redefine tumor spheroids heterogeneity via PCA-coupled biophysical characterization

Domenico A. Cristaldi, Martina Bedeschi, Gianfranco Cavallaro, Azzurra Sargenti et autres

Spheroids, a part of 3D cell culture systems, are crucial models for bridging in-vitro and in-human studies. However, achieving reliable standardization remains difficult, even when comparing spheroids of similar diameters. The challenge arises due to their cross-sectional architecture, which increases heterogeneity and …

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Mitochondrial Protease ClpP: Cancer Marker and Drug Target

Domenico Armenise, Olga Maria Baldelli, Anselma Liturri, Gianfranco Cavallaro et autres

Background: The human mitochondrial ClpP is a serine protease located in the mitochondrial matrix responsible for degrading short lived regulatory proteins as well as misfolded or damaged proteins, thereby maintaining cellular homeostasis. Proteastasis dysregulation is linked to tumor progression. Methods: We conducted …

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From SARS to MERS and SARS-CoV-2: Comparative Spike Protein Remodeling and Ligand-Binding Hot-Spots Revealed by Multiscale Simulations

Gianfranco Cavallaro, Giuseppe Forte, Carmela Bonaccorso, Federica Sipala et autres

The COVID-19 pandemic has prompted the scientific community to develop new weapons against the SARS-CoV-2 spike protein. The study of its mutations is important to understand how it interacts with human receptors and how to prevent a future pandemic. In this study, …

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ONC201-Derived Tetrahydropyridopyrimidindiones as Powerful ClpP Protease Activators to Tackle Diffuse Midline Glioma

Morena Miciaccia, Olga Maria Baldelli, Cosimo G. Fortuna, Gianfranco Cavallaro et autres

Pediatric diffuse intrinsic pontine glioma (DIPG), classified under diffuse midline glioma, is a deadly tumor, with no effective treatments. The human mitochondrial protease h ClpP is a potential DIPG therapeutic target, and this study describes the synthesis of two new series of …

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Halloysite Nanotube-Based Delivery of Pyrazolo[3,4-d]pyrimidine Derivatives for Prostate and Bladder Cancer Treatment

Marina Massaro, Rebecca Ciani, Giancarlo Grossi, Gianfranco Cavallaro et autres

Background/Objectives: The development of therapies targeting unregulated Src signaling through selective kinase inhibition using small-molecule inhibitors presents a significant challenge for the scientific community. Among these inhibitors, pyrazolo[3,4-d]pyrimidine heterocycles have emerged as potent agents; however, their clinical application is hindered by low …

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Harmaline to Human Mitochondrial Caseinolytic Serine Protease Activation for Pediatric Diffuse Intrinsic Pontine Glioma Treatment

Morena Miciaccia, Francesca Rizzo, Antonella Centonze, Gianfranco Cavallaro et autres

Diffuse intrinsic pontine glioma (DIPG), affecting children aged 4–7 years, is a rare, aggressive tumor that originates in the pons and then spreads to nearby tissue. DIPG is the leading cause of death for pediatric brain tumors due to its infiltrative nature …

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Harmaline and Human ClpP Activation for Pediatric Diffuse Intrinsic Pontine Glioma (DIPG) Treatment

Morena Miciaccia, Francesca Rizzo, Antonella Centonze, Gianfranco Cavallaro et autres

Diffuse intrinsic pontine glioma (DIPG), affecting children aged 4-7 years, is a rare, aggressive tumor that originates in the pons and then spreads to nearby tissue. DIPG is the leading cause of death for pediatric brain tumors due to its infiltrative nature …

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Different In Silico Approaches Using Heterocyclic Derivatives against the Binding between Different Lineages of SARS-CoV-2 and ACE2

Federica Sipala, Gianfranco Cavallaro, Giuseppe Forte, Cristina Satriano et autres

Over the last few years, the study of the SARS-CoV-2 spike protein and its mutations has become essential in understanding how it interacts with human host receptors. Since the crystallized structure of the spike protein bound to the angiotensin-converting enzyme 2 (ACE2) …

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