A5071309513- Peptidase Inhibition and Analysis
- Chronic Myeloid Leukemia Treatments
- Epigenetics and DNA Methylation
- Cancer therapeutics and mechanisms
- Lung Cancer Treatments and Mutations
- Histone Deacetylase Inhibitors Research
- Protein Degradation and Inhibitors
- Cancer-related Molecular Pathways
- Sarcoma Diagnosis and Treatment
- CAR-T cell therapy research
- GDF15 and Related Biomarkers
- Retinoids in leukemia and cellular processes
- Genetics and Neurodevelopmental Disorders
- Synthesis and biological activity
- DNA Repair Mechanisms
- MicroRNA in disease regulation
- Click Chemistry and Applications
- Ubiquitin and proteasome pathways
- Bioactive Compounds and Antitumor Agents
- Cell death mechanisms and regulation
- Biochemical and Molecular Research
- HER2/EGFR in Cancer Research
- Cancer, Lipids, and Metabolism
- Cancer Mechanisms and Therapy
- RNA Interference and Gene Delivery
Fondazione IRCCS Istituto Nazionale dei Tumori
2015-2024
University of Milan
2014-2015
Sigma Tau (Italy)
2010-2013
Mario Negri Institute for Pharmacological Research
2010
University of Rome Tor Vergata
2010
Centro Cardiologico Monzino
2003
Istituto Dermopatico dell'Immacolata
2003
Epigenetic dependencies have become evident in many cancers. On the basis of antagonism between BAF/SWI-SNF and PRC2 SMARCB1-deficient sarcomas, we recently completed clinical trial EZH2 inhibitor tazemetostat. However, principles tumor response to epigenetic therapy general, tazemetostat particular, remain unknown. Using functional genomics diverse experimental models, define molecular mechanisms resistance tumors. We found distinct acquired mutations that converge on RB1/E2F axis decouple...
Radiotherapy is one of the main treatment options for non-metastatic prostate cancer (PCa). Although technical optimization has greatly improved local tumor control, a considerable fraction patients still experience relapse due to development resistance. Radioresistance complex and poorly understood phenomenon involving deregulation variety signaling pathways as consequence several genetic epigenetic abnormalities. In this context, cumulative evidence supports functional role microRNAs in...
Abstract Objectives Among gynaecologic malignancies, ovarian cancer (OC) represents the leading cause of death for women worldwide. Current OC treatment involves cytoreductive surgery followed by platinum‐based chemotherapy, which is associated with severe side effects and development drug resistance. Therefore, new therapeutic strategies are urgently needed. Herein, we evaluated anti‐tumour Vitamin E‐derived δ‐tocotrienol (δ‐TT) in two human cell lines, IGROV‐1 SKOV‐3 cells. Materials...
Preclinical studies support the therapeutic potential of histone deacetylases inhibitors (HDACi) in combination with taxanes. The efficacy has been mainly ascribed to a cooperative effect on microtubule stabilization following tubulin acetylation. In present study we investigated paclitaxel two novel HDACi, ST2782 or ST3595, able induce p53 and hyperacetylation. A synergistic paclitaxel/ST2782 (or ST3595) was found wild-type ovarian carcinoma cells, but not mutant subline, spite marked Such...
A series of 22 derivatives the [1,2]oxazolo[5,4-e]isoindole system were synthesized through an efficient and versatile procedure that involves annelation [1,2]oxazole moiety to isoindole ring, producing with a wide substitution pattern. The structure–activity relationship indicates N-4-methoxybenzyl group appears crucial for potent activity. In addition, presence 6-phenyl is important best activity reached 3,4,5-trimethoxy substituent. most active compound, bearing both structural features,...
The value of microRNAs (miRNAs) as novel targets for cancer therapy is now widely recognized. However, no information currently available on the expression/functional role miRNAs in diffuse malignant peritoneal mesothelioma (DMPM), a rapidly lethal disease, poorly responsive to conventional treatments, which development new therapeutic strategies urgently needed. Here, we evaluated expression and biological effects miR-34a—one most deregulated lipid-formulated mimic already clinically...
Abstract BACKGROUND Defects in the cell cycle machinery of prostate cancer cells might impair efficiency checkpoints and affect response to chemotherapeutic drugs. We examined relationship between status microtubule damage‐activated hormone‐refractory paclitaxel. METHODS The two lines DU145 PC3 harboring defects at proteins involved regulation activated by damage were for sensitivity, apoptotic response, RESULTS In spite a comparable sensitivity antiproliferative effects paclitaxel,...
ABSTRACT This study exploited a novel patient-derived xenograft (PDX) of desmoplastic small round cell tumor (DSRCT), which reproduces histomorphological and molecular characteristics the clinical tumor, to assess activity cytotoxic targeted anticancer agents. Antitumor effect was moderate for doxorubicin, pazopanib larotrectenib [maximum volume inhibition (max TVI), 55-66%], while trabectedin had higher TVI, 82%). Vinorelbine, irinotecan eribulin achieved nearly complete growth 96-98%),...
The novel atypical retinoid E-3-(4'-hydroxy-3'-adamantylbiphenyl-4-yl)acrylic acid (ST1926, 4) exhibited a potent antiproliferative activity on large panel of human tumor cells. Despite almost complete loss ability to activate RARs, the compound was an effective apoptosis inducer and surprisingly produced DNA damage, that likely contributes proapoptotic activity. Following oral administration, 4 well tolerated caused growth inhibition in ovarian carcinoma, A2780/DX, melanoma, MeWo, growing...
Epithelioid sarcoma (ES) is a rare mesenchymal malignancy marked by SMARCB1/INI1 deficiency. Retrospective clinical data report on the activity of anthracycline- and gemcitabine-based regimens. EZH2 inhibitors are currently being tested in trials. Since comparisons these agents unlikely to be prospectively evaluated clinics, we took advantage an INI1-deficient proximal-type ES patient-derived xenograft (PDX ES-1) comparatively assess its preclinical antitumor activity. Mice were treated with...