GARGANTILLA, Marta, Leentje PERSOONS, Tereza KAUEROVÁ, Natalia DEL RIO, Dirk DAELEMANS, Eva-Maria PRIEGO, Peter KOLLÁR a Maria-Jesus PEREZ-PEREZ. Hybridization Approach to Identify Salicylanilides as Inhibitors of Tubulin Polymerization and Signal Transducers and Activators of Transcription 3 (STAT3). Pharmaceuticals. BASEL: MDPI, 2022, roč. 15, č. 7, s. 1-18. ISSN 1424-8247. Dostupné z: https://dx.doi.org/10.3390/ph15070835.
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Základní údaje
Originální název Hybridization Approach to Identify Salicylanilides as Inhibitors of Tubulin Polymerization and Signal Transducers and Activators of Transcription 3 (STAT3)
Autoři GARGANTILLA, Marta, Leentje PERSOONS, Tereza KAUEROVÁ (203 Česká republika, domácí), Natalia DEL RIO, Dirk DAELEMANS, Eva-Maria PRIEGO, Peter KOLLÁR (203 Česká republika, garant, domácí) a Maria-Jesus PEREZ-PEREZ.
Vydání Pharmaceuticals, BASEL, MDPI, 2022, 1424-8247.
Další údaje
Originální jazyk angličtina
Typ výsledku Článek v odborném periodiku
Obor 30104 Pharmacology and pharmacy
Stát vydavatele Švýcarsko
Utajení není předmětem státního či obchodního tajemství
WWW URL
Impakt faktor Impact factor: 4.600
Kód RIV RIV/00216224:14160/22:00126409
Organizační jednotka Farmaceutická fakulta
Doi http://dx.doi.org/10.3390/ph15070835
UT WoS 000833255500001
Klíčová slova anglicky tubulin polymerization inhibitors; colchicine site; salicylanilides; niclosamide; signal transducer and activator of transcription (STAT3) inhibitors
Štítky rivok, ÚFTo
Příznaky Mezinárodní význam, Recenzováno
Změnil Změnila: JUDr. Sabina Krejčiříková, učo 383857. Změněno: 11. 8. 2022 07:41.
Anotace
The superimposition of the X-ray complexes of cyclohexanediones (i.e., TUB015), described by our research group, and nocodazole, within the colchicine binding site of tubulin provided an almost perfect overlap of both ligands. This structural information led us to propose hybrids of TUB015 and nocodazole using a salicylanilide core structure. Interestingly, salicylanilides, such as niclosamide, are well-established signal transducers and activators of transcription (STAT3) inhibitors with anticancer properties. Thus, different compounds with this new scaffold have been synthesized with the aim to identify compounds inhibiting tubulin polymerization and/or STAT3 signaling. As a result, we have identified new salicylanilides (6 and 16) that showed significant antiproliferative activity against a panel of cancer cells. Both compounds were able to reduce the levels of p-STAT3(Tyr705) without affecting the total expression of STAT3. While compound 6 inhibited tubulin polymerization and arrested the cell cycle of DU145 cells at G2/M, similar to TUB015, compound 16 showed a more potent effect on inhibiting STAT3 phosphorylation and arrested the cell cycle at G1/G0, similar to niclosamide. In both cases, no toxicity towards PBMC cells was detected. Thus, the salicylanilides described here represent a new class of antiproliferative agents affecting tubulin polymerization and/or STAT3 phosphorylation.
VytisknoutZobrazeno: 21. 7. 2024 13:22