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Unsere aktivsten Substanzen

Unsere "Besten" - durch langjährige Kooperation mit der Medizinische Universität Graz (Biophysik) haben wir einige hochinteressante Substanzen entwickelt. 

Diese sind jetzt auch für andere Forschungsgruppen auf Anfrage in geringen Mengen günstig zu haben. Bei Interesse können Sie Dr. Glasnov direkt kontaktieren.

 

Our "Best ones" - in a long-lasting cooperation wit the Medical University of Graz (Biophysics) we have developed highly interesting compounds.

These are now available also for other research groups. Small amounts can be provided upon request and at reasonable prices. If interested, please contact Dr. Glasnov directly.

Pyr6

Pyr6 is a selective inhibitor of calcium release from the endoplasmic reticulum via STIM1/Orai1 mediated, store operated calcium entry (SOCE). Pyr6 blocks SOCE in thapsigargin treated, calcium depleted BRL-2H3 cells (IC50 = 0.49 μM), but has poor activity against carbachol-induced, TRPC3-mediated calcium entry in TRPC3-transfected HEK293 cells (IC50 = 18.46 μM).

Pyr10

Pyr10 is a novel, selective inhibitor of the transient receptor potential channel TRPC3. Pyr10 blocks carbachol-induced calcium entry into TRPC3-transfected HEK293 cells (IC50= 0.72 μM), with significantly lower activity against STIM1/Orai1 mediated release of calcium from endoplasmic reticulum (store operated calcium entry) in BRL-2H3 cells (IC50= 13.08 μM).

Benzimidazole Agonists of TRPC3-Channels

Lipid-gated TRPC channels are highly expressed in cardiovascular and neuronal tissues. Exerting precise pharmacological control over their activity in native cells is expected to serve as a basis for the development of novel therapies. Here we report on new benzimidazoles to generate TRPC agonists. 

Opto-Agonists of TRPC3-Channels

Lipid-gated TRPC channels are highly expressed in cardiovascular and neuronal tissues. Exerting precise pharmacological control over their activity in native cells is expected to serve as a basis for the development of novel therapies. Here we report on a new photopharmacological tool that enables manipulation of TRPC3 channels by light, in a manner independent of lipid metabolism and with higher temporal precision than lipid photopharmacology. Using the azobenzene photoswitch moiety, we modified GSK1702934A to generate light-controlled TRPC agonists. We obtained a light-sensitive molecules that allow us to exert efficient, light-mediated control over TRPC3 activity and the associated cellular Ca2+ signaling. OptoBI-1 enabled high-precision, temporal control of TRPC3-linked cell functions such as neuronal firing and endothelial Ca2+ transients. With these findings, we introduce a novel photopharmacological strategy to control native TRPC conductances.

Diacylglycerol-based lipid messanger (OptoDArG)

Transient receptor potential canonical (TRPC) channels TRPC3, TRPC6 and TRPC7 are able to sense the lipid messenger diacylglycerol (DAG). The DAG-sensing and lipid-gating processes in these ion channels are still unknown. To gain insights into the lipid-sensing principle, we generated a DAG photoswitch, OptoDArG, that enabled efficient control of TRPC3 by light.

 Toma Glasnov

Assoz. Prof. Dr. rer. nat.
Mag. Pharm.
Institut für Chemie
Schubertstr. 1/4

Telefon:+43 (0)316 380 - 8690
Fax:+43 (0)316 380 - 9840

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