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

Fatty acid acylated peptide therapeutics: discovery of omega-n oxidation of the lipid chain as a novel metabolic pathway in preclinical species

Autor: Simone Esposito, Alain Krick, Olivier Pasquier, Fabrice Bonche, Raffaele Ingenito, Paola Magotti, Elisabetta Bianchi, Edith Monteagudo, Mariana Gallo, Daniel Oscar Cicero, Laura Orsatti, Maria Veneziano, Fulvia Caretti, Riccardo Mele, Daniela Roversi, Nadia Gennari, Denis Brasseur, Laurence Gauzy-Lazo, Olivier Duclos, Christine Mauriac, Stephane Illiano, Sergio Mallart

Publikováno v: Journal of Pharmaceutical and Biomedical Analysis
Journal of Pharmaceutical and Biomedical Analysis, 2023, 227, pp.115256. ⟨10.1016/j.jpba.2023.115256⟩

International audience; We recently described C18 fatty acid acylated peptides as a new class of potent long-lasting single-chain RXFP1 agonists that displayed relaxin-like activities in vivo. Early pharmacokinetics and toxicological studies of these

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe48f7e018f9c4ba38832ba51bf5e8f5
https://hdl.handle.net/2108/313607

Optimization of 2-(1H-imidazo-2-yl)piperazines series of Trypanosoma brucei growth inhibitors as potential treatment for the second stage of HAT

Autor: Nadia Gennari, Maria Vittoria Orsale, Vincenzo Summa, Rita Graziani, Simona Ponzi, Jesus Maria Ontoria Ontoria, Alina Ciammaichella, Steven J. Harper, Andreina Basta, Giacomo Paonessa, Ilaria Biancofiore, Valentina Nardi, Federica Ferrigno, Ivan Fini, Melania D'Amico

A previous publication from our laboratory reported the identification of a new class of 2-(1H-imidazo-2-yl)piperazines as potent T. brucei growth inhibitors as potential treatment for Human African Trypanosomiasis (HAT). This work describes the stru

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1eb99b1d9838b8c3597fae42fc68fd91
http://hdl.handle.net/11588/828220

Discovery of 2-(1H-imidazo-2-yl)piperazines as a new class of potent and non-cytotoxic inhibitors of Trypanosoma brucei growth in vitro

Autor: Annalise Di Marco, Steven J. Harper, Savina Malancona, Nadia Gennari, Simona Ponzi, Jesus Maria Ontoria Ontoria, Marcel Kaiser, Rita Graziani, Ilaria Biancofiore, Giacomo Paonessa, Alberto Bresciani, Federica Ferrigno, Vincenzo Summa

Publikováno v: Bioorganicmedicinal chemistry letters. 28(23-24)

The identification of a new series of growth inhibitors of Trypanosoma brucei rhodesiense, causative agent of Human African Trypanosomiasis (HAT), is described. A selection of compounds from our in-house compound collection was screened in vitro agai

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8cf46768ec11c331900bbf1c794ff7cb
https://pubmed.ncbi.nlm.nih.gov/30482621

Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins

Autor: Alberto Bresciani, Alessio Sferrazza, Matteo Andreini, Steven J. Harper, Rita Graziani, Danilo Fabbrini, Emanuela Nizi, Giacomo Paonessa, Valentina Nardi, Nadia Gennari

Publikováno v: Bioorganicmedicinal chemistry letters. 28(9)

Falcipain-2 (FP2) is an essential enzyme in the lifecycle of malaria parasites such as Plasmodium falciparum, and its inhibition is viewed as an attractive mechanism of action for new anti-malarial agents. Selective inhibition of FP2 with respect to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed75866f82fe905ee5ae0e3c42fe3690
https://pubmed.ncbi.nlm.nih.gov/29615344