| Autor: |
Sadakane K; Department of Bioinformatics, Graduate School of Engineering Soka University, 1-236 Tangi-cho, Hachioji, Tokyo, Japan., Alrazi IMD; Department of Bioinformatics, Graduate School of Engineering Soka University, 1-236 Tangi-cho, Hachioji, Tokyo, Japan., Maruta S; Department of Bioinformatics, Graduate School of Engineering Soka University, 1-236 Tangi-cho, Hachioji, Tokyo, Japan. |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of biochemistry [J Biochem] 2018 Oct 01; Vol. 164 (4), pp. 295-301. |
| DOI: |
10.1093/jb/mvy051 |
| Abstrakt: |
Mitotic kinesin Eg5 plays an important physiological role in cell division. Several small-molecule inhibitors of Eg5 are the focus of cancer therapies. Azobenzene is a photochromic compound exhibiting cis-trans isomerization upon ultraviolet (UV) and visible (VIS) light irradiation. Photochromic compounds of azobenzene derivatives, mimicking Eg5-specific inhibitors of STLC, indicated photoreversible inhibitory effects on Eg5 ATPase activity; however, the photoreversible switching efficiency was not significant. This study presents a novel synthesized photochromic Eg5 inhibitor 2, 3-bis[(2,5-dioxo-1-{4-[(E)-2-phenyldiazen-1-yl]phenyl}pyrrolidin-3-yl)sulfanyl] butanedioic acid (BDPSB), which is composed of two azobenzenes. BDPSB exhibited cis-trans isomerization with UV and VIS light irradiation. The trans form of BDPSB significantly inhibited microtubule-dependent ATPase activity of Eg5, with an IC50 of 74 μM. Cis BDPSB showed weak effects on the microtubule-dependent ATPase activity. The results suggest that the novel photochromic Eg5 inhibitor BDPSB, which exhibits highly efficient photoswitching, shows a switch 'ON' and 'OFF' behaviour with VIS and UV light irradiation. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
|
Nepřihlášeným uživatelům se plný text nezobrazuje |
K zobrazení výsledku je třeba se přihlásit.
|
