Search Results - "Botrugno, A"
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ATR addiction in multiple myeloma: synthetic lethal approaches exploiting established therapies
Published in Haematologica (Roma) (01-10-2020)“…Therapeutic strategies designed to tinker with cancer cell DNA damage response have led to the widespread use of PARP inhibitors for BRCA1/2-mutated cancers…”
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Interplay between oncogene-induced DNA damage response and heterochromatin in senescence and cancer
Published in Nature cell biology (01-03-2011)“…Different mechanisms have been implicated in the induction of senescence. Two of these mechanisms, the DNA damage response, which induces a replicative…”
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Biochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases LSD1 and LSD2
Published in Journal of the American Chemical Society (19-05-2010)“…LSD1 and LSD2 histone demethylases are implicated in a number of physiological and pathological processes, ranging from tumorigenesis to herpes virus…”
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Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent
Published in Journal of medicinal chemistry (25-02-2016)“…We report the stereoselective synthesis and biological activity of a novel series of tranylcypromine (TCPA) derivatives (14a–k, 15, 16), potent inhibitors of…”
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Thieno[3,2‑b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure–Activity Relationship
Published in Journal of medicinal chemistry (09-03-2017)“…The balance of methylation levels at histone H3 lysine 4 (H3K4) is regulated by KDM1A (LSD1). KDM1A is overexpressed in several tumor types, thus representing…”
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Thieno[3,2‑b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration
Published in Journal of medicinal chemistry (09-03-2017)“…Lysine specific demethylase 1 KDM1A (LSD1) regulates histone methylation and it is increasingly recognized as a potential therapeutic target in oncology. We…”
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Tranylcypromine‐Based LSD1 Inhibitors: Structure‐Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation
Published in ChemMedChem (03-04-2020)“…: LSD1 is a lysine demethylase highly involved in initiation and development of cancer. To design highly effective covalent inhibitors, a strategy is to fill…”
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Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: A novel class of irreversible inhibitors of histone demethylase KDM1A
Published in European journal of medicinal chemistry (30-10-2014)“…Histone demethylase KDM1A (also known as LSD1) has become an attractive therapeutic target for the treatment of cancer as well as other disorders such as viral…”
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A Novel RGD-4C-Saporin Conjugate Inhibits Tumor Growth in Mouse Models of Bladder Cancer
Published in Frontiers in oncology (11-04-2022)“…Although toxin may have some advantages compared to chemotherapeutic drugs in cancer therapy, e.g. a potent cytotoxic activity and a reduced risk of…”
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Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts
Published in European journal of medicinal chemistry (13-04-2015)“…The pure enantiomers of the N-(2-, 3-, and 4-(2-aminocyclopropyl)phenyl)benzamides hydrochlorides 11a–j were prepared and tested against LSD1 and MAO enzymes…”
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Recruitment of the Histone Methyltransferase SUV39H1 and Its Role in the Oncogenic Properties of the Leukemia-Associated PML-Retinoic Acid Receptor Fusion Protein
Published in Molecular and Cellular Biology (01-02-2006)“…Article Usage Stats Services MCB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Liver receptor homolog 1 controls the expression of the scavenger receptor class B type I
Published in EMBO reports (01-12-2002)“…The scavenger receptor class B type I (SR‐BI), which mediates selective cellular cholesterol uptake from high‐density lipoproteins (HDLs), plays a key role in…”
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Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies
Published in ACS medicinal chemistry letters (12-02-2015)“…The pure four diastereomers (11a–d) of trans-benzyl (1-((4-(2-aminocyclopropyl)phenyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate hydrochloride 11, previously…”
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The Small Heterodimer Partner Interacts with the Liver X Receptor α and Represses Its Transcriptional Activity
Published in Molecular endocrinology (Baltimore, Md.) (01-09-2002)“…The small heterodimer partner SHP (NR0B2) is an unusual nuclear receptor that lacks the typical DNA binding domain common to most nuclear receptors. SHP has…”
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Soft X-ray measurements in magnetic fusion plasma physics
Published in Nuclear instruments & methods in physics research. Section A, Accelerators, spectrometers, detectors and associated equipment (11-11-2010)“…Soft X-ray diagnostic systems and their successful application in the field of magnetic fusion plasma physics are discussed. Radiation with wavelength in the…”
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Scalable integration of multiomic single-cell data using generative adversarial networks
Published in Bioinformatics (Oxford, England) (02-05-2024)“…Abstract Motivation Single-cell profiling has become a common practice to investigate the complexity of tissues, organs, and organisms. Recent technological…”
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Peaked density profiles in neon and lithium doped discharges on FTU
Published in Fusion engineering and design (01-12-2014)“…Peaked density profiles are observed in FTU discharges when the recycling condition of the chamber is influenced by the action of the liquid lithium limiter…”
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Genomic Instability and Replicative Stress in Multiple Myeloma: The Final Curtain?
Published in Cancers (22-12-2021)“…Multiple Myeloma (MM) is a genetically complex and heterogeneous hematological cancer that remains incurable despite the introduction of novel therapies in the…”
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HDACs link the DNA damage response, processing of double-strand breaks and autophagy
Published in Nature (London) (03-03-2011)“…Protein acetylation is mediated by histone acetyltransferases (HATs) and deacetylases (HDACs), which influence chromatin dynamics, protein turnover and the DNA…”
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Leveraging the potential of 1.0-mm i.d. columns in UHPLC-HRMS-based untargeted metabolomics
Published in Analytical and bioanalytical chemistry (24-10-2024)“…Untargeted metabolomics UHPLC-HRMS workflows typically employ narrowbore 2.1-mm inner diameter (i.d.) columns. However, the wide concentration range of the…”
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