A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity

…, V Patton, R Alzani, A Ciavolella, F Sola… - Nature chemical …, 2008 - nature.com
Cdc7 is an essential kinase that promotes DNA replication by activating origins of replication.
Here, we characterized the potent Cdc7 inhibitor PHA-767491 ( 1 ) in biochemical and cell-…

Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase

…, M Caldarelli, M Mennecozzi, ML Giorgini, F Sola… - Cancer research, 2010 - AACR
MPS1 kinase is a key regulator of the spindle assembly checkpoint (SAC), a mitotic mechanism
specifically required for proper chromosomal alignment and segregation. It has been …

Cdc7 inhibition reveals a p53-dependent replication checkpoint that is defective in cancer cells

A Montagnoli, P Tenca, F Sola, D Carpani… - Cancer research, 2004 - AACR
Cdc7 is an evolutionarily conserved kinase that regulates S phase by promoting replication
origin activation. Down-regulation of Cdc7 by small interfering RNA in a variety of tumor cell …

NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies

…, J Lansen, E Pesenti, S Rizzi, M Rocchetti, F Sola… - Molecular cancer …, 2012 - AACR
Polo-like kinase 1 (PLK1) is a serine/threonine protein kinase considered to be the master
player of cell-cycle regulation during mitosis. It is indeed involved in centrosome maturation, …

PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity

…, ML Giorgini, P Cappella, D Ballinari, F Sola… - Clinical Cancer …, 2006 - AACR
Purpose: Aurora kinases play critical roles during mitosis in chromosome segregation and
cell division. The aim of this study was to determine the preclinical profile of a novel, highly …

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly …

…, F Riccardi-Sirtori, A Scolaro, F Sola… - Journal of medicinal …, 2015 - ACS Publications
The nuclear protein poly(ADP-ribose) polymerase-1 (PARP-1) has a well-established role
in the signaling and repair of DNA and is a prominent target in oncology, as testified by the …

Synthesis and biological evaluation of RGD peptidomimetic–paclitaxel conjugates bearing lysosomally cleavable linkers

…, F Gasparri, A Marsiglio, F Sola… - … A European Journal, 2015 - Wiley Online Library
Two small‐molecule–drug conjugates (SMDCs, 6 and 7) featuring lysosomally cleavable
linkers (namely the Val–Ala and Phe–Lys peptide sequences) were synthesized by …

Essential role of human CDT1 in DNA replication and chromatin licensing

M Rialland, F Sola, C Santocanale - Journal of cell science, 2002 - journals.biologists.com
Formation of pre-replicative complexes at origins is an early cell cycle event essential for
DNA duplication. A large body of evidence supports the notion that Cdc6 protein, through its …

Quantification of the proliferation index of human dermal fibroblast cultures with the ArrayScan™ high-content screening reader

F Gasparri, M Mariani, F Sola… - Journal of biomolecular …, 2004 - journals.sagepub.com
High-throughput cell-based assays are becoming a powerful approach in the drug discovery
process. The ArrayScan™ high-content screening (HCS) reader is a cytometer based on a …

Phosphorylation of TCTP as a marker for polo-like kinase-1 activity in vivo

U Cucchi, LM Gianellini, A De Ponti, F Sola… - Anticancer …, 2010 - ar.iiarjournals.org
Polo-like kinase 1 (PLK1) is the master regulator of mitosis and a target for anticancer therapy.
To develop a marker of PLK1 activity in cells and tumour tissues, this study focused on …