A5053091621- Protein Degradation and Inhibitors
- Multiple Myeloma Research and Treatments
- Ubiquitin and proteasome pathways
- Histone Deacetylase Inhibitors Research
- Synthesis of Organic Compounds
- Prostate Cancer Treatment and Research
- Synthesis and biological activity
- Cancer-related gene regulation
- Microtubule and mitosis dynamics
- Plant chemical constituents analysis
- Cancer Treatment and Pharmacology
- Click Chemistry and Applications
- Cancer, Hypoxia, and Metabolism
- Protease and Inhibitor Mechanisms
- Epigenetics and DNA Methylation
- Receptor Mechanisms and Signaling
- Synthesis and Biological Activity
- Cancer-related Molecular Pathways
- Neuropeptides and Animal Physiology
- Protein Tyrosine Phosphatases
- Polyamine Metabolism and Applications
- Long-Term Effects of COVID-19
- FOXO transcription factor regulation
- Intraperitoneal and Appendiceal Malignancies
- Mast cells and histamine
Laboratoire Vision Action Cognition
2020-2022
Center for Genomic Science
2021
Italian Institute of Technology
2021
International Drug Development
2021
Università della Svizzera italiana
2019
Institute of Oncology Research
2017-2019
Mario Negri Institute for Pharmacological Research
2013-2016
Istituti di Ricovero e Cura a Carattere Scientifico
2014-2016
Zero to Three
2016
Experimental Medicine and Biology Institute
2007-2013
Triple-negative breast cancer (TNBC) is an aggressive and heterogeneous subgroup of tumors clinically defined by the lack estrogen, progesterone HER2 receptors, limiting use targeted therapies employed in other malignancies. Recent evidence indicates that c-MYC a key driver TNBC. The BET-bromodomain inhibitor OTX015 (MK-8628) has potent antiproliferative activity accompanied down-regulation several tumor types, demonstrated synergism with mTOR everolimus different models. aim this study was...
// Maria E. Riveiro 1 , Lucile Astorgues-Xerri Ramiro Vazquez 2 Roberta Frapolli Ivo Kwee 3, 5 Andrea Rinaldi 3 Elodie Odore 6 Keyvan Rezai Mohamed Bekradda Giorgio Inghirami 7, 9 Maurizio D’Incalci Kay Noel 10 Esteban Cvitkovic 1, Eric Raymond 11 Francesco Bertoni 12 Oncology Therapeutic Development, Clichy, France IRCCS-Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy Lymphoma and Genomics Research Program, IOR Institute of Research, Bellinzona, Switzerland 4 Dalle Molle...
It has recently been reported that a large proportion of human malignant pleural mesothelioma (MPM) cell lines and patient tissue samples present high expression the c-MYC oncogene. This gene drives several tumorigenic processes is overexpressed in many cancers. Although strategic target to restrain cancer processes, no drugs acting as inhibitors are available. The novel thienotriazolodiazepine small-molecule bromodomain inhibitor OTX015/MK-8628 shown potent antiproliferative activity...
Abstract In the search for alternative chemotherapeutic strategies against leukemia, various 1‐indanone thiosemicarbazones, as well eight novel platinum(II) and palladium(II) complexes, with formula [MCl 2 (HL)] [M(HL)(L)]Cl, derived from two thiosemicarbazones were synthesized tested antiproliferative activity human leukemia U937 cell line. The crystal structure of [Pt(HL1)(L1)]Cl . M eOH, where L1=1‐indanone thiosemicarbazone, was solved by X‐ray diffraction. Free thiosemicarbazone ligands...
Chemotherapy is the treatment of choice for metastatic castration-resistant prostate cancer (mCRPC) nonresponsive to androgen receptor-targeted therapies. Nevertheless, impact chemotherapy on patient survival limited and clinical outcome remain dismal. Bromodomain extraterminal inhibitors (BETis) are attractive therapeutic agents currently in trials be tested their efficacy patients.In this study, we evaluated activity two stage BETis, INCB054329 INCB057643, alone combination with...
Abstract Cancer of the prostate is one most common malignancies and second leading cause cancer death in men developed countries. There increasing evidence that stem-like cells (CSCs) are implicated CRPC disease progression treatment resistance. Transcriptional, epigenetic metabolic reprogramming key features for acquisition maintenance properties. Understanding factors regulating self-renewal survival CSCs may offer novel targets innovative therapeutic strategies. LSD1/KDM1A a lysine...
Abstract Background. BET bromodomain proteins recognize chromatin modifications and act as epigenetic readers contributing to gene transcription. OTX015, a novel inhibitor currently in clinical Phase Ib studies hematologic malignancies solid tumors, including lung cancer. We have shown vitro vivo activity of OTX015 NSCLC SCLC models (Riveiro et al; EORTC 2014), however the mechanism action relevant affected genes are not fully characterized. This study aimed elucidate pathways affecting...
VE-cadherin is an essential adhesion molecule in endothelial adherens junctions, and the integrity of these complexes thought to be regulated by tyrosine phosphorylation. We have previously shown that adrenomedullin (AM) blockade correlates with elevated levels phosphorylated (pVE-cadherinY731) cells, associated impaired barrier function a persistent increase vascular cell permeability. However, mechanism underlying this effect unknown. In article, we demonstrate AM-mediated...
Abstract Background: TNBC is an aggressive and heterogeneous subtype group of breast cancers clinically defined by the lack estrogen progesterone receptors, as well human epidermal growth factor receptor 2 (HER2). Few therapeutic options have shown clinical benefit beyond cytotoxic chemotherapy. Clinical studies demonstrated that more than 50% present a much lower median O2 partial pressure normal tissue, correlating with chemo- radio-resistance. We previously reported in vivo effects...
Abstract Prostate cancer is a leading cause of death worldwide. Deregulated transcriptional factors and epigenetic effectors contribute to prostate progression castration resistance providing ideal targets for developing new therapeutic strategies. Bromodomain extra-terminal (BET) proteins act co-activators interacting with multiple co-regulatory molecules at gene promoters enhancers. BET inhibitors (BETi) disrupt regulatory complexes have broad anticancer activity. INCB054329 INCB057643 are...