Výsledky vyhledávání - "Stefania Re Depaolini"

Identification of unprecedented ATP-competitive choline kinase inhibitors

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 51:128310

In this article we describe the identification of unprecedented ATP-competitive ChoKα inhibitors starting from initial hit NMS-P830 that binds to ChoKα in an ATP concentration-dependent manner. This result is confirmed by the co-crystal structure o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b28088bfd6a53b4154d2a1addbdf62e8
https://doi.org/10.1016/j.bmcl.2021.128310

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Structural Insight into Maternal Embryonic Leucine Zipper Kinase (MELK) Conformation and Inhibition toward Structure-Based Drug Design

Autor: Elena Casale, Patrizia Carpinelli, Claudia Perrera, Ulisse Cucchi, Giulia Canevari, Barbara Forte, Eduard R. Felder, J.A. Bertrand, Stefania Re Depaolini

Publikováno v: Biochemistry. 52:6380-6387

Maternal embryonic leucine zipper kinase (MELK) is upregulated in several types of tumor, including breast, prostate, and brain tumors. Its expression is generally associated with cell survival, cell proliferation, and resistance to apoptosis. Theref

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f56ee0275ac4a58b46b034f4411bab56
https://doi.org/10.1021/bi4005864

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Identification of candidate substrates for poly(ADP-ribose) polymerase-2 (PARP2) in the absence of DNA damage using high-density protein microarrays

Autor: Luisa Rusconi, Sandrine Thieffine, Rita Perego, Rosita Lupi, Roberta Bosotti, Sonia Troiani, Stefania Re Depaolini

Publikováno v: FEBS Journal. 278:3676-3687

Poly(ADP-ribose) polymerase-2 (PARP2) belongs to the ADP-ribosyltransferase family of enzymes that catalyze the addition of ADP-ribose units to acceptor proteins, thus affecting many diverse cellular processes. In particular, PARP2 shares with PARP1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d05c3b1de2940b8ad6975b9af9b2c55e
https://doi.org/10.1111/j.1742-4658.2011.08286.x

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NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor

Autor: Roberto Bossi, Daniele Pezzetta, Gabriele Fachin, Barbara Forte, Alessandra Scolaro, Italo Beria, Walter Ceccarelli, Enrico Pesenti, Michele Caruso, Francesco Fiorentini, Stefania Re Depaolini, Marina Fasolini, Helena Posteri, Barbara Valsasina, Maria Gabriella Brasca

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:2969-2974

As part of our drug discovery effort, we identified and developed 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as PLK1 inhibitors. We now report the optimization of this class that led to the identification of NMS-P937, a potent, selective a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1eb1c72f2e8179a8a325d3bbb4369e24
https://doi.org/10.1016/j.bmcl.2011.03.054

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Targeting the Mitotic Checkpoint for Cancer Therapy with NMS-P715, an Inhibitor of MPS1 Kinase

Autor: Arturo Galvani, Maria Laura Giorgini, Nilla Avanzi, Luisa Rusconi, Francesco Sola, Riccardo Colombo, Paolo Cappella, Stefania Re Depaolini, Claudia Perrera, Antonella Isacchi, Daniele Donati, Francesco Colotta, Ulisse Cucchi, Roberto Bossi, Marina Caldarelli, Enrico Pesenti, Milena Mennecozzi, Jürgen Moll, J.A. Bertrand

Publikováno v: Cancer Research. 70:10255-10264

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 found aberrantly overexpressed in a wide range of human tumors and is nec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ad1d4d987ed709eb7439c66638602f27
https://doi.org/10.1158/0008-5472.can-10-2101

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Abstract 3795: Novel and selective MELK kinase inhibitors active in breast cancer cell lines

Autor: Sabrina Cribioli, Giulia Canevari, Antonella Isacchi, Maria Gabriella Brasca, Daniele Donati, Riccardo Colombo, Marina Ciomei, Eduard R. Felder, Alessia Montagnoli, Marisa Montemartini, Arturo Galvani, Nadia Amboldi, Helena Posteri, Dario Ballinari, Patrizia Carpinelli, Walter Ceccarelli, Nilla Avanzi, Stefania Re Depaolini

Publikováno v: Cancer Research. 76:3795-3795

Maternal Embryonic Leucine zipper Kinase (MELK) is a serine-threonine kinase implicated in stem cell renewal, override of cell cycle checkpoints, pre-mRNA splicing and resistance to apoptosis, while MELK gene expression levels correlate inversely wit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::626bb24c033b311039827a4d551d066f
https://doi.org/10.1158/1538-7445.am2016-3795

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Identification of candidate substrates for poly(ADP-ribose) polymerase-2 (PARP2) in the absence of DNA damage using high-density protein microarrays

Autor: Sonia, Troiani, Rosita, Lupi, Rita, Perego, Stefania Re, Depaolini, Sandrine, Thieffine, Roberta, Bosotti, Luisa, Rusconi

Publikováno v: The FEBS journal. 278(19)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::0e535defbc98835a453c1139d4ec0ac6
https://pubmed.ncbi.nlm.nih.gov/21812934

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