C. Mercurio

发表

CELL CYCLE REGULATION AND HUMAN LEUKEMIAS : THE ROLE OF p 16 INK 4 GENE INACTIVATION IN THE DEVELOPMENT OF HUMAN ACUTE LYMPHOBLASTIC LEUKEMIA

F. Ragione, C. Mercurio, A. Iolascon, 2005 .

Cell cycle regulation and human leukemias: the role of p16INK4 gene inactivation in the development of human acute lymphoblastic leukemia.

F. Ragione, C. Mercurio, A. Iolascon, 1995, Haematologica.

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.

A. Isacchi, E. Casale, C. Mercurio, 2010, Journal of medicinal chemistry.

Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.

A. Mai, S. Minucci, C. Mercurio, 2010, Journal of medicinal chemistry.

Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.

S. Minucci, C. Mercurio, M. Varasi, 2013, European journal of medicinal chemistry.

Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.

L. Altucci, A. Nebbioso, C. Mercurio, 2013, European journal of medicinal chemistry.

Towards Selective Inhibition of Histone Deacetylase Isoforms: What Has Been Achieved, Where We Are and What Will Be Next

C. Mercurio, F. Thaler, 2014, ChemMedChem.

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.

S. Minucci, C. Mercurio, L. Moretti, 2017, Journal of medicinal chemistry.

Drf1, a novel regulatory subunit for human Cdc7 kinase

R. Bosotti, A. Montagnoli, J. Berthelsen, 2002, The EMBO journal.

New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.

C. Martini, A. Coluccia, R. Silvestri, 2018, European journal of medicinal chemistry.

Diversity Oriented Virtual Compound Selection Strategy for High Throughput Cell-Based Screening of Potential Anticancer Agents

Ismael Zamora, Jordi Mestres, Simona Distinto, 2008 .

Transcriptional Analysis of an E2F Gene Signature as a Biomarker of Activity of the Cyclin-Dependent Kinase Inhibitor PHA-793887 in Tumor and Skin Biopsies from a Phase I Clinical Study

R. Bosotti, E. Scacheri, A. Isacchi, 2010, Molecular Cancer Therapeutics.

Chiral Resolution and Pharmacological Characterization of the Enantiomers of the Hsp90 Inhibitor 2‐Amino‐7‐[4‐fluoro‐2‐(3‐pyridyl)phenyl]‐4‐methyl‐7,8‐dihydro‐6H‐quinazolin‐5‐one Oxime

S. Minucci, C. Mercurio, R. Amici, 2014, ChemMedChem.

High-throughput screening identifies histone deacetylase inhibitors that modulate GTF2I expression in 7q11.23 microduplication autism spectrum disorder patient-derived cortical neurons

C. Mercurio, M. Varasi, M. Gabriele, 2020, Molecular Autism.

Dual modulation of MCL-1 and mTOR determines the response to sunitinib

B. Teh, S. Minucci, C. Mercurio, 2017, The Journal of clinical investigation.

New targets to modulate the DNA damage response.

C. Mercurio, M. Varasi, 2018, Future medicinal chemistry.

Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.

Y. Ni, E. Novellino, B. Maresca, 2013, Journal of medicinal chemistry.

Down-regulation of protein kinase CKII activity by sodium butyrate.

V. Della Pietra, D. Marshak, C. Mercurio, 1997, Biochemical and biophysical research communications.

Beclin 1 restrains tumorigenesis through Mcl-1 destabilization in an autophagy-independent reciprocal manner

S. Minucci, C. Miracco, C. Mercurio, 2014, Nature Communications.

Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.

S. Minucci, C. Mercurio, L. Moretti, 2016, European journal of medicinal chemistry.

Synthesis and Biological Characterization of Amidopropenyl Hydroxamates as HDAC Inhibitors

A. Mai, S. Minucci, C. Mercurio, 2010, ChemMedChem.

Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.

A. Mai, S. Minucci, C. Mercurio, 2011, Journal of medicinal chemistry.

GTF2I dosage regulates neuronal differentiation and social behavior in 7q11.23 neurodevelopmental disorders

T. Bonaldi, C. Mercurio, M. Varasi, 2022, bioRxiv.

Dual Targeting of CDK and Tropomyosin Receptor Kinase Families by the Oral Inhibitor PHA-848125, an Agent with Broad-Spectrum Antitumor Efficacy

A. Isacchi, C. Mercurio, F. Colotta, 2010, Molecular Cancer Therapeutics.

Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.

A. Mai, S. Minucci, C. Mercurio, 2015, ACS medicinal chemistry letters.

Compounds and methods for inhibiting histone demethylases: a patent evaluation of US20160102096A1

C. Mercurio, F. Thaler, 2016, Expert opinion on therapeutic patents.

Purification and characterization of recombinant human 5'-methylthioadenosine phosphorylase: definite identification of coding cDNA.

V. Della Pietra, C. Mercurio, F. Della Ragione, 1996, Biochemical and biophysical research communications.

Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models.

S. Minucci, C. Mercurio, C. So, 2020, ACS medicinal chemistry letters.

Tranylcypromine‐Based LSD1 Inhibitors: Structure‐Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation

A. Mai, S. Minucci, C. Mercurio, 2020, ChemMedChem.

Spiro[chromane‐2,4′‐piperidine]‐Based Histone Deacetylase Inhibitors with Improved in vivo Activity

S. Minucci, C. Mercurio, M. Varasi, 2012, ChemMedChem.

3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.

J. Bischoff, C. Mercurio, A. Vulpetti, 2006, Bioorganic & medicinal chemistry letters.

Design and synthesis of novel isoxazole-based HDAC inhibitors.

Laura Sola, Roberta Ettari, Ciro Mercurio, 2010, European journal of medicinal chemistry.

Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.

A. Isacchi, E. Casale, C. Mercurio, 2009, Journal of medicinal chemistry.

Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.

Ettore Novellino, Andrea Brancale, Ilaria Granata, 2011, Journal of medicinal chemistry.

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.

Anna Vulpetti, Enrico Pesenti, Ciro Mercurio, 2005, Journal of medicinal chemistry.

New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.

E. Novellino, L. Di Marcotullio, C. Martini, 2015, Journal of medicinal chemistry.

New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.

Ettore Novellino, Andrea Brancale, Ruoli Bai, 2014, Journal of medicinal chemistry.

Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A.

A. Mai, S. Minucci, M. Tortorici, 2014, European journal of medicinal chemistry.

Human Cdc25 A inactivation in response to S phase inhibition and its role in preventing premature mitosis

M. Molinari, C. Mercurio, G. Draetta, 2000, EMBO reports.

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.

S. Minucci, C. Mercurio, L. Moretti, 2017, Journal of medicinal chemistry.

Novel potent inhibitors of the histone demethylase KDM1A (LSD1), orally active in a murine promyelocitic leukemia model.

S. Minucci, C. Mercurio, M. Villa, 2017, Future medicinal chemistry.

Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent.

A. Mai, S. Minucci, C. Mercurio, 2016, Journal of medicinal chemistry.

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

A. Isacchi, E. Casale, J. Bischoff, 2010, Bioorganic & medicinal chemistry.

Molecular Cancer apeutics linical Development l Targeting of CDK and Tropomyosin Receptor Kinase ilies by the Oral Inhibitor PHA-848125 , an Agent Ther Broad-Spectrum Antitumor Efficacy

A. Isacchi, C. Mercurio, F. Colotta, 2010 .

Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts.

A. Mai, S. Minucci, C. Mercurio, 2015, European journal of medicinal chemistry.

Anti‐tumour efficacy on glioma models of PHA‐848125, a multi‐kinase inhibitor able to cross the blood–brain barrier

C. Mercurio, M. Ciomei, F. Fiorentini, 2013, British journal of pharmacology.

Targeting Cyclin-Dependent Kinases with Small Molecule Inhibitors

J. Bischoff, C. Mercurio, P. Pevarello, 2010 .

Cyclin-dependent kinase 2 functions in normal DNA repair and is a therapeutic target in BRCA1-deficient cancers.

Kum Kum Khanna, Ciro Mercurio, K. Khanna, 2006, Cancer research.

Interplay between oncogene-induced DNA damage response and heterochromatin in senescence and cancer

W. Hahn, S. Minucci, V. Gorgoulis, 2011, Nature Cell Biology.

6‐Substituted Pyrrolo[3,4‐c]pyrazoles: An Improved Class of CDK2 Inhibitors

C. Mercurio, A. Vulpetti, D. Ballinari, 2007, ChemMedChem.

Targeting the scaffolding role of LSD1 (KDM1A) poises acute myeloid leukemia cells for retinoic acid–induced differentiation

G. Pavesi, R. Ravasio, A. Mai, 2020, Science Advances.

Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells

A. Mai, S. Minucci, C. Mercurio, 2015 .

Histone deacetylases and epigenetic therapies of hematological malignancies.

S. Minucci, P. Pelicci, C. Mercurio, 2010, Pharmacological research.

Protective effects of butyric acid in colon cancer.

V. Della Pietra, C. Mercurio, V. Zappia, 1999, Advances in experimental medicine and biology.

Alteration of cell division cycle regulation in human cancers: The role of CDKN2A gene

F. Ragione, C. Mercurio, A. Iolascon, 1998 .

p16INK4 gene deletions in childhood acute lymphoblastic leukemias.

S. Perrotta, C. Mercurio, F. Della Ragione, 1995, Leukemia research.

Biochemical Characterization of p16INK4- and p18-containing Complexes in Human Cell Lines*

Ciro Mercurio, F. Ragione, C. Mercurio, 1996, The Journal of Biological Chemistry.

Alterations of Histone Modifications in Cancer

S. Minucci, C. Mercurio, S. Plyte, 2012 .

Pathology tissue–chromatin immunoprecipitation, coupled with high-throughput sequencing, allows the epigenetic profiling of patient samples

S. Minucci, P. Pelicci, G. Viale, 2010, Proceedings of the National Academy of Sciences.

Novel Pyridine‐Based Hydroxamates and 2′‐Aminoanilides as Histone Deacetylase Inhibitors: Biochemical Profile and Anticancer Activity

L. Altucci, A. Mai, A. Nebbioso, 2020, ChemMedChem.

LSD1-directed therapy affects glioblastoma tumorigenicity by deregulating the protective ATF4-dependent integrated stress response

S. Minucci, B. Costanza, B. Pollo, 2021, Science Translational Medicine.

Fragment‐based Identification of Hsp90 Inhibitors

Mark Whittaker, Thomas Hesterkamp, Dirk Winkler, 2009, ChemMedChem.

Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells.

L. Altucci, A. Mai, A. Nebbioso, 2022, European journal of medicinal chemistry.

Cross platform microarray analysis for robust identification of differentially expressed genes

Sandra Healy, Luca Sartori, Raffaele Calogero, 2007, BMC Bioinformatics.

The Antidiabetic Agent Sodium Tungstate Activates Glycogen Synthesis through an Insulin Receptor-independent Pathway*

M. Muñoz, C. Mercurio, R. Gomis, 2003, Journal of Biological Chemistry.

3-Aroyl-1,4-diarylpyrroles Inhibit Chronic Myeloid Leukemia Cell Growth through an Interaction with Tubulin.

A. Coluccia, A. Brancale, R. Silvestri, 2017, ACS medicinal chemistry letters.

tert‐Butylcarbamate‐Containing Histone Deacetylase Inhibitors: Apoptosis Induction, Cytodifferentiation, and Antiproliferative Activities in Cancer Cells

E. Novellino, D. Trisciuoglio, L. Altucci, 2013, ChemMedChem.

Further insights into the SAR of α-substituted cyclopropylamine derivatives as inhibitors of histone demethylase KDM1A.

C. Mercurio, M. Villa, M. Varasi, 2015, European journal of medicinal chemistry.

Valproic acid induces differentiation and transient tumor regression, but spares leukemia-initiating activity in mouse models of APL

S. Minucci, C. Mercurio, R. D. Zuffo, 2012, Leukemia.

STRUCTURE OF CDK2-CYCLIN A WITH PHA-630529

J. Bischoff, C. Mercurio, A. Vulpetti, 2005 .

Beclin 1 restrains tumorigenesis through Mcl-1 destabilization in an autophagy-independent reciprocal manner

S. Minucci, C. Miracco, C. Mercurio, 2014, Nature Communications.

Triazole-modified histone deacetylase inhibitors as a rapid route to drug discovery.

C. Mercurio, P. Canonico, G. Tron, 2008, Journal of combinatorial chemistry.

New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.

E. Novellino, L. Di Marcotullio, A. Brancale, 2014, Journal of medicinal chemistry.

Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.

Y. Ni, E. Novellino, B. Maresca, 2013, Journal of medicinal chemistry.