Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach

Autor: Yuri Takada, Yuki Kitao, Yoshie Fujiwara, Chika Yamamoto, Mitsuhiro Terao, Dan Ohtan Wang, Elghareeb E. Elboray, Yasunobu Yamashita, Yukihiro Itoh, Paolo Mellini, Rohini Roy, Yukari Takahashi, Makoto Oba, Masayuki Kotoku, Takao Yamaguchi, Satoshi Obika, Ritesh Singh, Muthuraj Prakash, Takayoshi Suzuki

Publikováno v: Journal of medicinal chemistry. 64(21)

Fat mass obesity-associated protein (FTO) is a DNA/RNA demethylase involved in the epigenetic regulation of various genes and is considered a therapeutic target for obesity, cancer, and neurological disorders. Here, we aimed to design novel FTO-selec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cda13918510b1de8b8f693d2d156f972
https://pubmed.ncbi.nlm.nih.gov/34727689

Novel small molecule SIRT2 inhibitors induce cell death in leukemic cell lines

Autor: Shin-ichiro Honda, Akiyoshi Aikawa, Takeo Ohsugi, Yuichiro Uchida, Takayoshi Suzuki, Tomohiro Kozako, Paolo Mellini

Publikováno v: BMC Cancer, Vol 18, Iss 1, Pp 1-10 (2018)
BMC Cancer

Background Sirtuin 2 (SIRT2) is a member of the sirtuin family, nicotinamide adenine dinucleotide+-dependent deacylases, which participates in modulation of cell cycle control, neurodegeneration, and tumorigenesis. SIRT2 expression increases in acute

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4eeeda85ed28d3fb1cc3a54424ff0a39
http://link.springer.com/article/10.1186/s12885-018-4710-1

Correction to 'Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells'

Autor: Sergio Valente, Diana Borovika, Biagina Marrocco, Clemens Zwergel, Peteris Trapencieris, Ilaria Carnevale, Elisabetta Ferretti, Paolo Mellini, Giulia Stazi, Lucia Polletta, Serena Saladini, Marco Tafani, Antonello Mai

Publikováno v: Philosophical transactions of the Royal Society of London. Series B, Biological sciences. 373(1755)

Novel pyrazole-based EZH2 inhibitors have been prepared through a molecular pruning approach from known inhibitors bearing a bicyclic moiety as a central scaffold. The hit compound 1o (N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-methyl-1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc07f92006f21a1b59359e1224816fbc
https://pubmed.ncbi.nlm.nih.gov/29685965

Potent mechanism-based sirtuin-2-selective inhibition by an in situ-generated occupant of the substrate-binding site, 'selectivity pocket' and NAD+-binding site

Autor: Takayoshi Suzuki, Hiroki Tsumoto, Natsuko Tokuda, Maija Lahtela-Kakkonen, Paolo Mellini, Jun Takeuchi, Yukihiro Itoh, Taeko Kakizawa, Ying Li, Yuri Miura, Miki Suzuki

Sirtuin 2 (SIRT2), a member of the NAD+-dependent histone deacetylase family, has recently received increasing attention due to its potential involvement in neurodegenerative diseases and the progression of cancer. Potent and selective SIRT2 inhibito

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f13317153fe675bc8fbbc29ce95052e
https://erepo.uef.fi/handle/123456789/5136

1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells

Autor: Paolo Mellini, Donatella Del Bufalo, Sébastien Moniot, Lucia Polletta, Clemens Steegborn, Marco Tafani, Ilaria Carnevale, Roberta Budriesi, Maria Tardugno, Lucia Altucci, Chiara Gabellini, Sandra Atlante, Daniela Trisciuoglio, Antonello Mai, Vincenzo Carafa, Angela Nebbioso, Serena Saladini, Sergio Valente, Francesco Spallotta, Clemens Zwergel, Chiara Cencioni, Carlo Gaetano

Publikováno v: Journal of medicinal chemistry (2016).
info:cnr-pdr/source/autori:Valente S, Mellini P, Spallotta F, Carafa V, Nebbioso A, Polletta L, Carnevale I, Saladini S, Trisciuoglio D, Gabellini C, Tardugno M, Zwergel C, Cencioni C, Atlante S, Moniot S, Steegborn C, Budriesi R, Tafani M, Del Bufalo D, Altucci L, Gaetano C, Mai A./titolo:1,4-Dihydropyridines Active on the SIRT1%2FAMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells./doi:/rivista:Journal of medicinal chemistry/anno:2016/pagina_da:/pagina_a:/intervallo_pagine:/volume

Modulators of sirtuins are considered promising therapeutic targets for the treatment of cancer, cardiovascular, metabolic, inflammatory, and neurodegenerative diseases. Here we prepared new 1,4-dihydropyridines (DHPs) bearing changes at the C2/C6, C

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a4bbdf098839e19177d1bd2f68f8889
http://hdl.handle.net/11573/870523