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Pregled bibliografske jedinice broj: 958331

Inhibition of glioblastoma cell proliferation, invasion, and mechanism of action of a novel hydroxamic acid hybrid molecule


Zhang, Issan; Beus, Maja; Stochaj, Ursula; Le, Phuong, Uyen; Zorc, Branka; Rajić, Zrinka; Petrecca, Kevin; Maysinger, Dusica
Inhibition of glioblastoma cell proliferation, invasion, and mechanism of action of a novel hydroxamic acid hybrid molecule // Cell Death Discovery, 5 (2018), 41; -, 14 doi:10.1038/s41420-018-0103-0 (međunarodna recenzija, članak, znanstveni)


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Naslov
Inhibition of glioblastoma cell proliferation, invasion, and mechanism of action of a novel hydroxamic acid hybrid molecule

Autori
Zhang, Issan ; Beus, Maja ; Stochaj, Ursula ; Le, Phuong, Uyen ; Zorc, Branka ; Rajić, Zrinka ; Petrecca, Kevin ; Maysinger, Dusica

Izvornik
Cell Death Discovery (2058-7716) 5 (2018), 41; 14

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
glioblastoma ; hybrid molecule ; histone deacetylase inhibitor

Sažetak
Glioblastoma multiforme is one of the most aggressive brain tumors and current therapies with temozolomide or suberoylanilide hydroxamic acid (SAHA, vorinostat) show considerable limitations. SAHA is a histone deacetylase (HDAC) inhibitor that can cause undesirable side effects due to the lack of selectivity. We show here properties of a novel hybrid molecule, sahaquine, which selectively inhibits cytoplasmic HDAC6 at nanomolar concentrations without markedly suppressing class I HDACs. Inhibition of HDAC6 leads to significant α- tubulin acetylation, thereby impairing cytoskeletal organization in glioblastoma cells. The primaquine moiety of sahaquine reduced the activity of Pglycoprotein, which contributes to glioblastoma multiforme drug resistance. We propose the mechanism of action of sahaquine to implicate HDAC6 inhibition together with suppression of epidermal growth factor receptor and downstream kinase activity, which are prominent therapeutic targets in glioblastoma multiforme. Sahaquine significantly reduces the viability and invasiveness of glioblastoma tumoroids, as well as brain tumor stem cells, which are key to tumor survival and recurrence. These effects are augmented with the combination of sahaquine with temozolomide, the natural compound quercetin or buthionine sulfoximine, an inhibitor of glutathione biosynthesis. Thus, a combination of agents disrupting glioblastoma and brain tumor stem cell homeostasis provides an effective anti–cancer intervention

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija



POVEZANOST RADA


Projekt / tema


Ustanove
Farmaceutsko-biokemijski fakultet, Zagreb

Profili:

Avatar Url Zrinka Rajić (autor)

Avatar Url Branka Zorc (autor)

Avatar Url Maja Beus (autor)

Citiraj ovu publikaciju

Zhang, Issan; Beus, Maja; Stochaj, Ursula; Le, Phuong, Uyen; Zorc, Branka; Rajić, Zrinka; Petrecca, Kevin; Maysinger, Dusica
Inhibition of glioblastoma cell proliferation, invasion, and mechanism of action of a novel hydroxamic acid hybrid molecule // Cell Death Discovery, 5 (2018), 41; -, 14 doi:10.1038/s41420-018-0103-0 (međunarodna recenzija, članak, znanstveni)
Zhang, I., Beus, M., Stochaj, U., Le, Phuong, Uyen, Zorc, B., Rajić, Z., Petrecca, K. & Maysinger, D. (2018) Inhibition of glioblastoma cell proliferation, invasion, and mechanism of action of a novel hydroxamic acid hybrid molecule. Cell Death Discovery, 5 (41), -, 14 doi:10.1038/s41420-018-0103-0.
@article{article, year = {2018}, pages = {14}, DOI = {10.1038/s41420-018-0103-0}, chapter = {-}, keywords = {glioblastoma, hybrid molecule, histone deacetylase inhibitor}, journal = {Cell Death Discovery}, doi = {10.1038/s41420-018-0103-0}, volume = {5}, number = {41}, issn = {2058-7716}, title = {Inhibition of glioblastoma cell proliferation, invasion, and mechanism of action of a novel hydroxamic acid hybrid molecule}, keyword = {glioblastoma, hybrid molecule, histone deacetylase inhibitor}, chapternumber = {-} }

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