New Diarylamine K_V10.1 Inhibitors and Their Anticancer Potential by Špela Gubič, Žan Toplak, Xiaoyi Shi, Jaka Dernovšek, Louise Antonia Hendrickx, Ernesto Lopes Pinheiro-Junior, Steve Peigneur, Jan Tytgat, Luis A. Pardo, Lucija Peterlin Mašič, Tihomir Tomašič

Subjects: Get full text

3D Pharmacophore-Based Discovery of Novel K_V10.1 Inhibitors with Antiproliferative Activity by Žan Toplak, Louise Antonia Hendrickx, Špela Gubič, Štefan Možina, Bojana Žegura, Alja Štern, Matjaž Novak, Xiaoyi Shi, Steve Peigneur, Jan Tytgat, Tihomir Tomašič, Luis A. Pardo, Lucija Peterlin Mašič

Subjects: Get full text

Identification, Synthesis, Conformation and Activity of an Insulin-like Peptide from a Sea Anemone by Michela L. Mitchell, Mohammed Akhter Hossain, Feng Lin, Ernesto L. Pinheiro-Junior, Steve Peigneur, Dorothy C. C. Wai, Carlie Delaine, Andrew J. Blyth, Briony E. Forbes, Jan Tytgat, John D. Wade, Raymond S. Norton

“…IlO1_i1 did not bind to the insulin or insulin-like growth factor receptors, but showed weak activity against K_V1.2, 1.3, 3.1, and 11.1 (hERG) channels, as well as Na_V1.4 channels. …”
Get full text

Biochemical and Electrophysiological Characterization of Two Sea Anemone Type 1 Potassium Toxins from a Geographically Distant Population of Bunodosoma caissarum by André J. Zaharenko, Jan Tytgat, José C. Freitas, Adriano M. C. Pimenta, José E. P. W. Bicudo, Gabriela G. Montandon, Juliana S. Cassoli, Bruno Madio, Diego J. B. Orts, Steve Peigneur

“…Their functional characterization was performed by means of a wide electrophysiological screening on 12 different subtypes of KV channels (KV1.1–KV1.6; KV2.1; KV3.1; KV4.2; KV4.3; hERG and Shaker IR). BcsTx1 shows a high affinity for rKv1.2 over rKv1.6, hKv1.3, Shaker IR and rKv1.1, while Bcstx2 potently blocked rKv1.6 over hKv1.3, rKv1.1, Shaker IR and rKv1.2. …”
Get full text

Structure-Function Studies of Sponge-Derived Compounds on the Cardiac Ca_V3.1 Channel by Anne-Sophie Depuydt, Piyush A. Patel, Žan Toplak, Chinmaya Bhat, Manuela Voráčová, Irene Eteläinen, Fiammetta Vitulano, Tanja Bruun, Antti Lempinen, Nives Hribernik, Eero Mäki-Lohiluoma, Louise Hendrickx, Ernesto Lopes Pinheiro-Junior, Tihomir Tomašič, Lucija Peterlin Mašič, Jari Yli-Kauhaluoma, Paula Kiuru, Jan Tytgat, Steve Peigneur

“…A selectivity screening showed that these analogs are also active on hERG channels. Collectively, a new class of Ca_V3 channel inhibitors has been discovered and the structure–function studies provide new insights into the synthetic design of drugs and the mechanism of interaction with T-type Ca_V channels.…”
Get full text