Absolutely thrilled to present our paper accepted for publication in #JMedChem. #Strongyloidiasis is a neglected tropical disease caused primarily by the roundworm Strongyloides stercoralis. It is estimated to infect more than 200 million people worldwide with up to 2.5% of these infections progressing into a hyperinfection syndrome and a mortality rate of 90% if untreated. In preclinical models, the activation of ssDAF-12 receptor was able to suppress infection and to reduce lethality. Despite these remarkable evidences, only scarce efforts have been devoted to the field. In this work, we report the discovery of unprecedented ssDAF-12 modulators that have the potential to interfere with the lifecycle of the nematode Strongyloides stercoralis and to modulate the parasitic infection making it vulnerable to therapeutic intervention. We provide novel insights into the SAR profile and properties of steroidal modulators that might enable progress in targeting ssDAF-12 for treating #parasitism. It has been a long journey with a great collaborative effort from the chemical #synthesis of challenging #steroids to #computationalchemistry, #screening assays and #metabolic studies. Thanx and congrats to all involved Giada Ceccarelli, Laura Goracci, Andrea Carotti, Federico Paccoia, Daniela Passeri, Marco Cipolloni, Stefano Di Bona, Gabriele Cruciani, roberto pellicciari Università degli Studi di Perugia Tes Pharma S.r.l. Molecular Horizon #MedChem #Strongyloidiasis #Parasitism #Drugdiscovery Have a look: https://lnkd.in/gFVpXkpJ
Congrats Antimo!
Congratulations, Antimo!
Felicidades!!!!!!!!!!!!
Lucia Ricci
7mo
Congratulazioni!!
Pharmaceutical Chemistry and Technology Graduate
7moCongratulation!!!