P
Paolo Di Fruscia
Researcher at Istituto Italiano di Tecnologia
Publications - 12
Citations - 648
Paolo Di Fruscia is an academic researcher from Istituto Italiano di Tecnologia. The author has contributed to research in topics: Potentiator & SIRT2. The author has an hindex of 8, co-authored 11 publications receiving 547 citations. Previous affiliations of Paolo Di Fruscia include Imperial College London & Scripps Research Institute.
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Journal ArticleDOI
SIRT Inhibitors Induce Cell Death and p53 Acetylation through Targeting Both SIRT1 and SIRT2
Barrie Peck,Chun-Yuan Chen,Ka-Kei Ho,Paolo Di Fruscia,Stephen S. Myatt,R. Charles Coombes,Matthew J. Fuchter,Chwan-Deng Hsiao,Eric Lam +8 more
TL;DR: It is suggested that SIRT inhibitors require combined targeting of both SIRT1 and SIRT2 to induce p53 acetylation and cell death and that p53 mediates the cytotoxic function of Sirtinol and Salermide.
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The discovery of a highly selective 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one SIRT2 inhibitor that is neuroprotective in an in vitro Parkinson's disease model.
Paolo Di Fruscia,Emmanouil Zacharioudakis,Chang Liu,Sébastien Moniot,Sasiwan Laohasinnarong,Mattaka Khongkow,Ian F. Harrison,Konstantina Koltsida,Christopher R. Reynolds,Karin Schmidtkunz,Manfred Jung,Kathryn L. Chapman,Clemens Steegborn,David T. Dexter,Michael J.E. Sternberg,Eric Lam,Matthew J. Fuchter +16 more
TL;DR: In concordance with the recent reports that suggest SIRT2 inhibition is a potential strategy for the treatment of Parkinson’s disease, compound ICL‐SIRT078 has a significant neuroprotective effect in a lactacystin‐induced model of Parkinsonian neuronal cell death in the N27 cell line.
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Perspectives on natural product epigenetic modulators in chemical biology and medicine.
Fanny L. Cherblanc,Robert W. M. Davidson,Paolo Di Fruscia,Nitipol Srimongkolpithak,Matthew J. Fuchter +4 more
TL;DR: This review will give a perspective on the current status of natural product epigenetic modulators, highlighting the limitations, challenges and opportunities for currently identified molecules, as well as potential strategies for novel compound discovery moving forward.
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Thienopyrimidinone Based Sirtuin-2 (SIRT2)-Selective Inhibitors Bind in the Ligand Induced Selectivity Pocket
Sandeep Sundriyal,Sébastien Moniot,Zimam Mahmud,Shang Yao,Paolo Di Fruscia,Christopher R. Reynolds,David T. Dexter,Michael J.E. Sternberg,Eric Lam,Clemens Steegborn,Matthew J. Fuchter +10 more
TL;DR: An extensive SAR study of this chemical series reveals a cocrystal structure of one of the compounds bound to SIRT2 that reveals the formation of a previously reported selectivity pocket but to bind in an inverted fashion to what might be intuitively expected.
Journal ArticleDOI
Discovery of a picomolar potency pharmacological corrector of the mutant CFTR chloride channel.
Nicoletta Pedemonte,Fabio Bertozzi,Emanuela Caci,Federico Sorana,Paolo Di Fruscia,Valeria Tomati,Loretta Ferrera,Alejandra Rodríguez-Gimeno,Francesco Berti,Emanuela Pesce,Elvira Sondo,Ambra Gianotti,Paolo Scudieri,Tiziano Bandiera,Luis J. V. Galietta +14 more
TL;DR: A small molecule that, at picomolar concentrations, rescues mutant CFTR chloride channel from protein degradation is identified and represents a high-affinity probe for CFTR structure-function studies.