| Institution: | 1. Max‐Planck‐Institut für Molekulare Physiologie, Otto‐Hahn‐Strasse 11, 44227 Dortmund (Germany);2. Technische Universit?t Dortmund, Fakult?t Chemie, Lehrbereich Chemische Biologie, Otto‐Hahn‐Strasse 6, 44227 Dortmund (Germany);3. School of Medicine, LIGHT Building, Clarendon Way, University of Leeds, Leeds, LS2 9JT, England (UK);4. School of Pharmacy, Aichi‐Gakuin University, 1‐100 Kusumoto, Chikusa, Nagoya 464‐8650 (Japan);5. Clinical Physiology Department, Faculty of Medicine, Menoufiya University (Egypt);6. Institute of Chemistry and Biochemistry, Freie Universit?t Berlin, Takustrasse 3, 14195 Berlin (Germany) |
| Abstract: | Current therapies for common types of cancer such as renal cell cancer are often ineffective and unspecific, and novel pharmacological targets and approaches are in high demand. Here we show the unexpected possibility for the rapid and selective killing of renal cancer cells through activation of calcium‐permeable nonselective transient receptor potential canonical (TRPC) calcium channels by the sesquiterpene (?)‐englerin A. This compound was found to be a highly efficient, fast‐acting, potent, selective, and direct stimulator of TRPC4 and TRPC5 channels. TRPC4/5 activation through a high‐affinity extracellular (?)‐englerin A binding site may open up novel opportunities for drug discovery aimed at renal cancer. |
