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1.
Eur J Pharmacol ; 971: 176518, 2024 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-38556119

RESUMEN

XAV-939(XAV) is a chemical compound that inhibits the activity of tankyrase. However, the precise way in which XAV alters membrane ionic currents is not well understood. In this study,our goal was to examine the impact of XAV on the ionic currents in mouse MA-10 Leydig cells, specifically focusing on the magnitude, gating properties,and voltage-dependent hysteresis of erg-mediated K+currents(IK(erg)). In our whole-cell current recordings we observed that the addition of XAV inhibited the density of IK(erg) in a concentration-dependent manner with an IC50 of 3.1 µM. Furthermore we found that continued exposure to XAV, further addition of neither liraglutide nor insulin-like growth factor-1 counteracted XAV-mediated inhibition of IK(erg). Additionally the presence of XAV suppressed the mean current versus voltage relationship of IK(erg) across the entire voltage-clamp step analyzed. This compound shifted the steady-state activation curve of IK(erg) to a less negative potential by approximately 12 mV. The presence of XAV increased the time constant of deactivating IK(erg) in MA-10 cells. The voltage-dependent clockwise hysteresis of IK(erg) responding to prolonged upright isosceles-triangular ramp voltage became diminished by adding XAV; moreover subsequent addition of NS3623 effectively reversed XAV-induced decrease of hysteretic area of IK(erg). XAV also inhibited the proliferation of this cell line and the IC50 value of XAV-induced inhibition of cell proliferation was 2.8M. Overall the suppression of IK(erg) by XAV may serve as a significant ionic mechanism that contribute to the functional properties of MA-10 cells. However, it is important to note that this effect cannot be attributed solely to the inhibition of tankyrase.


Asunto(s)
Compuestos Heterocíclicos con 3 Anillos , Neoplasias , Tanquirasas , Ratones , Masculino , Animales , Línea Celular
2.
Urol Case Rep ; 24: 100840, 2019 May.
Artículo en Inglés | MEDLINE | ID: mdl-31211051

RESUMEN

Renal calyceal diverticulum is congenital outpouchings of the renal calyx and communicate with the main collecting system via a narrow channel. Stones have reportedly been found in up to 50% of diverticulum. Surgical intervention is indicated for symptomatic stone. Stenotic infundibulum had been reported but seldom literature reported of calyceal diverticular atresia. Here we presented a case of atretic calyceal diverticular stone which successful managed by retrograde intrarenal surgery safely.

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