Show simple item record

dc.creatorBrai, Annalaura
dc.creatorRiva, Valentina
dc.creatorClementi, Letizia
dc.creatorFalsitta, Lucia
dc.creatorZamperini, Claudio
dc.creatorSinigiani, Virginia
dc.creatorFestuccia, Claudio
dc.creatorSabetta, Samantha
dc.creatorAiello, Davide
dc.creatorRoselli, Camilla
dc.creatorGarbelli, Anna
dc.creatorTrivisani, Claudia Immacolata
dc.creatorMaccari, Laura
dc.creatorBugli, Francesca
dc.creatorSanguinetti, Maurizio
dc.creatorCalandro, Pierpaolo
dc.creatorChiariello, Mario
dc.creatorQuaranta, Paola
dc.creatorBotta, Lorenzo
dc.creatorAngelucci, Adriano
dc.creatorMaga, Giovanni
dc.creatorBotta, Maurizio
dc.date.accessioned2022-04-29T19:21:43Z
dc.date.available2022-04-29T19:21:43Z
dc.date.issued2021-11-07
dc.identifier.citationBrai A, Riva V, Clementi L, Falsitta L, Zamperini C, Sinigiani V, Festuccia C, Sabetta S, Aiello D, Roselli C, Garbelli A, Trivisani CI, Maccari L, Bugli F, Sanguinetti M, Calandro P, Chiariello M, Quaranta P, Botta L, Angelucci A, Maga G, Botta M. Targeting DDX3X Helicase Activity with BA103 Shows Promising Therapeutic Effects in Preclinical Glioblastoma Models. Cancers. 2021; 13(21):5569. https://doi.org/10.3390/cancers13215569
dc.identifier.issn2072-6694
dc.identifier.doihttp://dx.doi.org/10.34944/dspace/7602
dc.identifier.urihttp://hdl.handle.net/20.500.12613/7624
dc.description.abstractDDX3X is an ATP-dependent RNA helicase that has recently attracted interest for its involvement in viral replication and oncogenic progression. Starting from hit compounds previously identified by our group, we have designed and synthesized a new series of DDX3X inhibitors that effectively blocked its helicase activity. These new compounds were able to inhibit the proliferation of cell lines from different cancer types, also in DDX3X low-expressing cancer cell lines. According to the absorption, distribution, metabolism, elimination properties, and antitumoral activity, compound BA103 was chosen to be further investigated in glioblastoma models. BA103 determined a significant reduction in the proliferation and migration of U87 and U251 cells, downregulating the oncogenic protein β-catenin. An in vivo evaluation demonstrated that BA103 was able to reach the brain and reduce the tumor growth in xenograft and orthotopic models without evident side effects. This study represents the first demonstration that DDX3X-targeted small molecules are feasible and promising drugs also in glioblastoma.
dc.format.extent26 pages
dc.languageEnglish
dc.language.isoeng
dc.relation.ispartofFaculty/ Researcher Works
dc.relation.haspartCancers, Vol. 13, No. 21
dc.relation.isreferencedbyMDPI
dc.rightsAttribution CC BY
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.subjectDDX3X
dc.subjectGlioblastoma
dc.subjectAnticancer
dc.subjectXenograft
dc.subjectHelicase inhibitors
dc.titleTargeting DDX3X Helicase Activity with BA103 Shows Promising Therapeutic Effects in Preclinical Glioblastoma Models
dc.typeText
dc.type.genreJournal article
dc.contributor.groupCenter for Biotechnology, Sbarro Institute for Cancer Research and Molecular Medicine (Temple University)
dc.description.departmentBiology
dc.relation.doihttps://doi.org/10.3390/cancers13215569
dc.ada.noteFor Americans with Disabilities Act (ADA) accommodation, including help with reading this content, please contact scholarshare@temple.edu
dc.description.schoolcollegeTemple University. College of Science and Technology
dc.temple.creatorBotta, Maurizio
refterms.dateFOA2022-04-29T19:21:43Z


Files in this item

Thumbnail
Name:
Botta-JournalArticle-2021.pdf
Size:
4.304Mb
Format:
PDF

This item appears in the following Collection(s)

Show simple item record

Attribution CC BY
Except where otherwise noted, this item's license is described as Attribution CC BY