Properly substituted analogues of BIX-01294 lose inhibition of G9a histone methyltransferase and gain selective anti-DNA methyltransferase 3A activity.

Autor: Dante Rotili, Domenico Tarantino, Biagina Marrocco, Christina Gros, Véronique Masson, Valérie Poughon, Fréderic Ausseil, Yanqi Chang, Donatella Labella, Sandro Cosconati, Salvatore Di Maro, Ettore Novellino, Michael Schnekenburger, Cindy Grandjenette, Celine Bouvy, Marc Diederich, Xiaodong Cheng, Paola B Arimondo, Antonello Mai

Publikováno v: PLoS ONE, Vol 9, Iss 5, p e96941 (2014)

Chemical manipulations performed on the histone H3 lysine 9 methyltransferases (G9a/GLP) inhibitor BIX-01294 afforded novel desmethoxyquinazolines able to inhibit the DNA methyltransferase DNMT3A at low micromolar levels without any significant inhib

Externí odkaz: https://doaj.org/article/281a01d650e04497b3316ad698b79eb4

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities

Autor: Donatella Labella, Lucia Altucci, Anthony Tumber, Biagina Marrocco, Clarence Yapp, Giuseppe Ciossani, Dante Rotili, Oliver N. King, Marcello Tortorici, Sergio Valente, Richard J. Hopkinson, Stefano Tomassi, Mariarosaria Conte, Andrea Mattevi, Akane Kawamura, Ettore Novellino, Rosaria Benedetti, Antonello Mai, Christopher J. Schofield

Publikováno v: Journal of Medicinal Chemistry; Vol 57
Journal of Medicinal Chemistry
Journal of medicinal chemistry 57 (2014): 42–55. doi:10.1021/jm4012802
info:cnr-pdr/source/autori:Rotili, Dante; Tomassi, Stefano; Conte, Mariarosaria; Benedetti, Rosaria; Tortorici, Marcello; Ciossani, Giuseppe; Valente, Sergio; Marrocco, Biagina; Labella, Donatella; Novellino, Ettore; Mattevi, Andrea; Altucci, Lucia; Tumber, Anthony; Yapp, Clarence; King, Oliver N. F.; Hopkinson, Richard J.; Kawamura, Akane; Schofield, Christopher J.; Mai, Antonello/titolo:Pan-Histone Demethylase Inhibitors Simultaneously Targeting Jumonji C and Lysine-Specific Demethylases Display High Anticancer Activities/doi:10.1021%2Fjm4012802/rivista:Journal of medicinal chemistry/anno:2014/pagina_da:42/pagina_a:55/intervallo_pagine:42–55/volume:57

In prostate cancer, two different types of histone lysine demethylases (KDM), LSD1/KDM1 and JMJD2/KDM4, are co-expressed and co-localize with the androgen receptor. We designed and synthesized hybrid LSD1/JmjC - "pan-KDM" - inhibitors 1-6, by couplin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9d1aef50dc49a0e68c8bb117a66e669
https://ora.ox.ac.uk/objects/uuid:bfd82582-e57e-451d-89ac-492128dcfdfb

An Analog of BIX-01294 Selectively Inhibits a Family of Histone H3 Lysine 9 Jumonji Demethylases

Autor: Xing Zhang, Xiaodong Cheng, Ruogu Hu, Antonello Mai, Ji Woong Han, Donatella Labella, Yanqi Chang, Young Sup Yoon, Anup K. Upadhyay, Dante Rotili

Publikováno v: Journal of Molecular Biology; Vol 416

BIX-01294 and its analogs were originally identified and subsequently designed as potent inhibitors against histone H3 lysine 9 (H3K9) methyltransferases G9a and G9a-like protein. Here, we show that BIX-01294 and its analog E67 can also inhibit H3K9

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d61bb130809ed3bdf84f2aec5c229699
https://doi.org/10.1016/j.jmb.2011.12.036

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

Autor: Andrea Mattevi, Giovanni Ruoppolo, Oronza A. Botrugno, Ciro Mercurio, Paola Dessanti, Saverio Minucci, Sergio Valente, Giuseppe Ciossani, Biagina Marrocco, Mario Varasi, Antonello Mai, Donatella Labella, Roberto Cirilli, Veronica Rodriguez, Bruna Saponara, Paola Vianello

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 described by us as LSD1 inhibitor, were obtained by enantiospecific synthesis/chiral HPLC se

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4351fe8c5c835e50b71e3891d7e2ca86
https://europepmc.org/articles/PMC4329595/

1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells

Autor: Marco Miceli, Antonello Mai, Gerald Brosch, Alessia Lenoci, Donatella Del Bufalo, Angela Nebbioso, Lucia Altucci, Giulio Dondio, Daniela Trisciuoglio, Sergio Valente, Teresa De Luca, Donatella Labella, Chiara Bigogno

Publikováno v: Journal of medicinal chemistry 57 (2014): 6259–6265. doi:10.1021/jm500303u
info:cnr-pdr/source/autori:Valente, Sergio; Trisciuoglio, Daniela; De Luca, Teresa; Nebbioso, Angela; Labella, Donatella; Lenoci, Alessia; Bigogno, Chiara; Dondio, Giulio; Miceli, Marco; Brosch, Gerald; Del Bufalo, Donatella; Altucci, Lucia; Mai, Antonello/titolo:1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells/doi:10.1021%2Fjm500303u/rivista:Journal of medicinal chemistry/anno:2014/pagina_da:6259/pagina_a:6265/intervallo_pagine:6259–6265/volume:57

We describe 1,3,4-oxadiazole-containing hydroxamates (2) and 2-aminoanilides (3) as histone deacetylase inhibitors. Among them, 2t, 2x, and 3i were the most potent and selective against HDAC1. In U937 leukemia cells, 2t was more potent than SAHA in i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ef6fa0a6448bf020104ae8557502636
https://publications.cnr.it/doc/287245