Effects of structurally distinct human HDAC6 and HDAC6/HDAC8 inhibitors against S. mansoni larval and adult worm stages.

Autor: Roberto Gimmelli, Giuliana Papoff, Fulvio Saccoccia, Cristiana Lalli, Sandra Gemma, Giuseppe Campiani, Giovina Ruberti

Publikováno v: PLoS Neglected Tropical Diseases, Vol 18, Iss 2, p e0011992 (2024)

Schistosomiasis is a major neglected parasitic disease that affects more than 240 million people worldwide caused by Platyhelminthes of the genus Schistosoma. The treatment of schistosomiasis relies on the long-term application of a single safe drug,

Externí odkaz: https://doaj.org/article/0dfe90516e1e4bc0866785472651d7ce

Identification of novel multi-stage histone deacetylase (HDAC) inhibitors that impair Schistosoma mansoni viability and egg production

Autor: Alessandra Guidi, Fulvio Saccoccia, Nadia Gennari, Roberto Gimmelli, Emanuela Nizi, Cristiana Lalli, Giacomo Paonessa, Giuliana Papoff, Alberto Bresciani, Giovina Ruberti

Publikováno v: Parasites & Vectors, Vol 11, Iss 1, Pp 1-10 (2018)

Abstract Background Novel anti-schistosomal multi-stage drugs are needed because only a single drug, praziquantel, is available for the treatment of schistosomiasis and is poorly effective on larval and juvenile stages of the parasite. Schistosomes h

Externí odkaz: https://doaj.org/article/45af4f283f4a4d728d531a94827cf54e

Comparative metabolic profiling by 1H-NMR spectroscopy analysis reveals the adaptation of S. mansoni from its host to in vitro culture conditions: a pilot study with ex vivo and GSH-supplemented medium-cultured parasites

Autor: Valentina Fustaino, Roberto Gimmelli, Alessandra Guidi, Sara Lentini, Fulvio Saccoccia, Greta Petrella, Daniel Oscar Cicero, Giovina Ruberti

Publikováno v: Parasitology Research. 121:1191-1198

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de0a497e5c73ebbc84ec6925a92b39a4
https://doi.org/10.1007/s00436-022-07426-6

Discovery by organism based high-throughput screening of new multi-stage compounds affecting Schistosoma mansoni viability, egg formation and production.

Autor: Alessandra Guidi, Cristiana Lalli, Roberto Gimmelli, Emanuela Nizi, Matteo Andreini, Nadia Gennari, Fulvio Saccoccia, Steven Harper, Alberto Bresciani, Giovina Ruberti

Publikováno v: PLoS Neglected Tropical Diseases, Vol 11, Iss 10, p e0005994 (2017)

Schistosomiasis, one of the most prevalent neglected parasitic diseases affecting humans and animals, is caused by the Platyhelminthes of the genus Schistosoma. Schistosomes are the only trematodes to have evolved sexual dimorphism and the constant p

Externí odkaz: https://doaj.org/article/bacaa2ac7d364a01a33cfbf94adc8cb1

Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation

Autor: Francesca Vanni, Niamh H McCabe, Stefania Lamponi, Cristina Ulivieri, Federica Sarno, Fulvio Saccoccia, Sandra Gemma, Giulia Chemi, David W. Christianson, Ola Ibrahim, Margherita Brindisi, Simone Brogi, Giovina Ruberti, Stefano Federico, Manfred Jung, Giuseppe Campiani, Nicola Relitti, Vincent P. Kelly, Daniela M. Zisterer, Stefania Butini, Richard C. Turkington, Antonella Di Costanzo, Patricia Hannon Barroeta, Rebecca Amet, Lucia Altucci, Magda Ghanim, Jeff O'Sullivan, Alessandro Grillo, Jeremy D. Osko, A Prasanth Saraswati, Daniel Herp

Publikováno v: Saraswati, A P, Relitti, N, Brindisi, M, Osko, J D, Chemi, G, Federico, S, Grillo, A, Brogi, S, McCabe, N H, Turkington, R C, Ibrahim, O, O'Sullivan, J, Lamponi, S, Ghanim, M, Kelly, V P, Zisterer, D, Amet, R, Hannon Barroeta, P, Vanni, F, Ulivieri, C, Herp, D, Sarno, F, Di Costanzo, A, Saccoccia, F, Ruberti, G, Jung, M, Altucci, L, Gemma, S, Butini, S, Christianson, D W & Campiani, G 2020, ' Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation ', ACS MEDICINAL CHEMISTRY LETTERS, vol. 11, no. 11, pp. 2268-2276 . https://doi.org/10.1021/acsmedchemlett.0c00395
ACS Med Chem Lett
ACS medicinal chemistry letters (2020). doi:10.1021/acsmedchemlett.0c00395
info:cnr-pdr/source/autori:A Prasanth Saraswati 1, Nicola Relitti 1, Margherita Brindisi 1, Jeremy D Osko 2, Giulia Chemi 1, Stefano Federico 1, Alessandro Grillo 1, Simone Brogi 3, Niamh H McCabe 4, Richard C Turkington 4, Ola Ibrahim 5, Jeffrey O'Sullivan 5, Stefania Lamponi 1, Magda Ghanim 6, Vincent P Kelly 6, Daniela Zisterer 6, Rebecca Amet 6, Patricia Hannon Barroeta 6, Francesca Vanni 7, Cristina Ulivieri 7, Daniel Herp 8, Federica Sarno 9, Antonella Di Costanzo 9, Fulvio Saccoccia 10, Giovina Ruberti 10, Manfred Jung 8, Lucia Altucci 9, Sandra Gemma 1, Stefania Butini 1, David W Christianson 2, Giuseppe Campiani/titolo:Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation/doi:10.1021%2Facsmedchemlett.0c00395/rivista:ACS medicinal chemistry letters/anno:2020/pagina_da:/pagina_a:/intervallo_pagine:/volume
ACS Medicinal Chemistry Letters

[Image: see text] Histone deacetylase inhibitors (HDACi) have emerged as promising therapeutics for the treatment of neurodegeneration, cancer, and rare disorders. Herein, we report the development of a series of spiroindoline-based HDAC6 isoform-sel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2bdda0b9bb58feac3ff72ae889a7ab41
https://pure.qub.ac.uk/en/publications/spiroindolinecapped-selective-hdac6-inhibitors-design-synthesis-structural-analysis-and-biological-evaluation(5bed77f3-2eb8-4bef-8802-360242d740c1).html