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Mostrando publicaciones 1-5 de 5

  • Ion occupancy of the selectivity filter controls opening of a cytoplasmic gate in the K2P channel TALK-2 

    Neelsen, Lea C.; Riel, Elena B.; Rinné, Susanne; Schmid, Freya-Rebecca; Jürs, Björn C.; Bedoya, Mauricio; Langer, Jan P.; Eymsh, Bisher; Kiper, Aytug K.; Cordeiro, Sönke; Decher, Niels; Baukrowitz, Thomas; Schewe, Marcus (2024)
    Two-pore domain K+ (K2P) channel activity was previously thought to be controlled primarily via a selectivity filter (SF) gate. However, recent crystal structures of TASK-1 and TASK-2 revealed a lower gate at the cytoplasmic ...

  • Rational design, synthesis, and evaluation of novel polypharmacological compounds targeting NaV1.5, KV1.5, and K2P channels for atrial fibrillation 

    Camargo-Ayala, Lorena; Bedoya, Mauricio; Dasí, Albert; Prüser, Merten; Schütte, Sven; Prent-Peñaloza, Luis; Adasme-Carreño, Francisco; Kiper, Aytug K.; Rinné, Susanne; Camargo-Ayala, Paola Andrea; Peña-Martínez, Paula A.; Bueno-Orovio, Alfonso; Varela, Diego; Wiedmann, Felix; Márquez Montesinos, José C. E; Mazola, Yuliet; Venturini, Whitney; Zúñiga, Rafael; Zúñiga, Leandro; Schmidt, Constanze; Rodriguez, Blanca; Ravens, Ursula; Decher, Niels; Gutiérrez, Margarita; González, Wendy (2025)
    Atrial fibrillation (AF) involves electrical remodeling of the atria, with ion channels such as NaV1.5, KV1.5, and TASK-1 playing crucial roles. This study investigates acetamide-based compounds designed as multi-target ...

  • Selective TASK-1 inhibitor with a defined structure–activity relationship reduces cancer cell proliferation and viability 

    Arévalo, Bárbara; Bedoya, Mauricio; Kiper, Aytug K.; Vergara, Fernando; Ramírez, David; Mazola, Yuliet; Bustos, Daniel; Zúñiga, Rafael; Cikutovic, Rocio; Cayo, Angel; Rinné, Susanne; Ramirez-Apan, M. Teresa; Sepúlveda, Francisco V.; Cerda, Oscar; López-Collazo, Eduardo; Decher, Niels; Zúñiga, Leandro; Gutiérrez, Margarita; González, Wendy (2021)
    Chemical structures of selective blockers of TASK channels contain aromatic groups and amide bonds. Using this rationale, we designed and synthesized a series of compounds based on 3-benzamidobenzoic acid. These compounds ...

  • Selective TASK-1 inhibitor with a defined structure–activity relationship reduces cancer cell proliferation and viability 

    Arévalo, Bárbara; Bedoya, Mauricio; Kiper, Aytug K.; Vergara, Fernando; Ramírez, David; Mazola, Yuliet; Bustos, Daniel; Zúñiga, Rafael; Cikutovic, Rocio; Cayo, Angel; Rinné, Susanne; Ramirez-Apan, M. Teresa; Sepúlveda, Francisco V.; Cerda, Oscar; López-Collazo, Eduardo; Decher, Niels; Zúñiga, Leandro; Gutierrez, Margarita; González, Wendy (2022)
    Chemical structures of selective blockers of TASK channels contain aromatic groups and amide bonds. Using this rationale, we designed and synthesized a series of compounds based on 3-benzamidobenzoic acid. These compounds ...

  • Structure/activity analysis of TASK-3 channel antagonists based on a 5,6,7,8 tetrahydropyrido[4,3-d]pyrimidine 

    Ramírez, David; Bedoya, Mauricio; Kiper, Aytug K.; Rinné, Susanne; Morales-Navarro, Samuel; Hernández-Rodríguez, Erix W.; Sepúlveda, Francisco V.; Drecher, Niels; González, Wendy (2019)
    TASK-3 potassium (K+) channels are highly expressed in the central nervous system, regulating the membrane potential of excitable cells. TASK-3 is involved in neurotransmitter action and has been identified as an oncogenic ...