-
Design of new potent and selective thiophene-based Kv1.3 inhibitors and their potential for anticancer activity [Elektronski vir]Gubič, Špela ...The voltage-gated potassium channel KV1.3 has been recognized as a tumor marker and represents a promising new target for the discovery of new anticancer drugs. We designed a novel structural class ... of KV1.3 inhibitors through structural optimization of benzamide-based hit compounds and structure-activity relationship studies. The potency and selectivity of the new KV1.3 inhibitors were investigated using whole-cell patch- and voltage-clamp experiments. 2D and 3D cell models were used to determine antiproliferative activity. Structural optimization resulted in the most potent and selective KV1.3 inhibitor 44 in the series with an IC50 value of 470 nM in oocytes and 950 nM in Ltk− cells. KV1.3 inhibitor 4 induced significant apoptosis in Colo-357 spheroids, while 14, 37, 43, and 44 significantly inhibited Panc-1 proliferation.Vir: Cancers [Elektronski vir]. - ISSN 2072-6694 (Vol. 14, no. 11, art. no. 2595, 2022, str. 1-20)Vrsta gradiva - e-članek ; neleposlovje za odrasleLeto - 2022Jezik - angleškiCOBISS.SI-ID - 109409795
Avtor
Gubič, Špela |
Hendrickx, Louise Antonia |
Shi, Xiaoyi |
Toplak, Žan |
Možina, Štefan, kemik |
Van Theemsche, Kenny M. |
Lopes Pinheiro-Junior, Ernesto |
Peigneur, Steve |
Tomašič, Tihomir |
Peterlin-Mašič, Lucija
Teme
Rak (medicina) |
Apoptoza |
Farmacevtska kemija |
Kv1.3 |
kalijevi ionski kanali |
antiproliferativno delovanje |
zdravila proti raku |
Kv1.3 |
potassium ion channels |
antiproliferative activity |
apoptosis |
anticancer drugs
![loading ... loading ...](themes/default/img/ajax-loading.gif)
Vnos na polico
Trajna povezava
- URL:
Faktor vpliva
Dostop do baze podatkov JCR je dovoljen samo uporabnikom iz Slovenije. Vaš trenutni IP-naslov ni na seznamu dovoljenih za dostop, zato je potrebna avtentikacija z ustreznim računom AAI.
Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
---|---|---|---|---|---|---|---|---|
JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Baze podatkov, v katerih je revija indeksirana
Ime baze podatkov | Področje | Leto |
---|
Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
---|---|
Gubič, Špela | 53671 |
Hendrickx, Louise Antonia | ![]() |
Shi, Xiaoyi | ![]() |
Toplak, Žan | 52375 |
Možina, Štefan, kemik | 36492 |
Van Theemsche, Kenny M. | ![]() |
Lopes Pinheiro-Junior, Ernesto | ![]() |
Peigneur, Steve | ![]() |
Tomašič, Tihomir | 28334 |
Peterlin-Mašič, Lucija | 19317 |
Izberite prevzemno mesto:
Prevzem gradiva po pošti
Obvestilo
Gesla v Splošnem geslovniku COBISS
Izbira mesta prevzema
Mesto prevzema | Status gradiva | Rezervacija |
---|
Prosimo, počakajte trenutek.