Fragment-based discovery of a new family of non-peptidic small-molecule cyclophilin inhibitors with potent antiviral activities

Autor: Abdelhakim Ahmed-Belkacem, Lionel Colliandre, Nazim Ahnou, Quentin Nevers, Muriel Gelin, Yannick Bessin, Rozenn Brillet, Olivier Cala, Dominique Douguet, William Bourguet, Isabelle Krimm, Jean-Michel Pawlotsky, Jean- François Guichou

Publikováno v: Nature Communications, Vol 7, Iss 1, Pp 1-11 (2016)

Cyclophilins play a key role in the life cycle of many viruses and represent important drug targets for broad-spectrum antiviral therapies. Here, the authors use fragment-based drug discovery to develop non-peptidic inhibitors of human cyclophilins w

Externí odkaz: https://doaj.org/article/39ec7c8e931548f1a43d8bd4de43a06f

Pharmacological activation of PIEZO1 in human red blood cells prevents Plasmodium falciparum invasion

Autor: Rakhee Lohia, Benoit Allegrini, Laurence Berry, Hélène Guizouarn, Rachel Cerdan, Manouk Abkarian, Dominique Douguet, Eric Honoré, Kai Wengelnik

Publikováno v: Cellular and Molecular Life Sciences. 80

An inherited gain-of-function variant (E756del) in the mechanosensitive cationic channel PIEZO1 was shown to confer a significant protection against severe malaria. Here, we demonstrate in vitro that human red blood cell (RBC) infection by Plasmodium

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::70296c45ca237e183447e1fb5da1a503
https://doi.org/10.1007/s00018-023-04773-0

Pharmacological activation of PIEZO1 in human red blood cells prevents Plasmodium falciparum invasion

Autor: Rachel Cerdan, Dominique Douguet, Laurence Berry, Hélène Guizouarn, Roberto Bernal, Jordy Le Guet, Rakhee Lohia, Manouk Abkarian, Eric Honoré, Kai Wengelnik

An inherited gain-of–function variant (E756 del) in the mechanosensitive cationic channel PIEZO1 was recently shown to confer a significant protection against severe malaria. Here, we demonstrate in vitro that human red blood cell (RBC) infection b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ce1bcec64d840b02db1001a98e8cd7d
https://hal.archives-ouvertes.fr/hal-03246779

Piezo Ion Channels in Cardiovascular Mechanobiology

Autor: Dominique Douguet, Amanda Patel, Paul M. Vanhoutte, Aimin Xu, Eric Honoré

Publikováno v: Douguet, D, Patel, A, Xu, A, Vanhoutte, P M & Honoré, E 2019, ' Piezo Ion Channels in Cardiovascular Mechanobiology ', Trends in Pharmacological Sciences, vol. 40, no. 12, pp. 956-970 . https://doi.org/10.1016/j.tips.2019.10.002
Trends in Pharmacological Sciences
Trends in Pharmacological Sciences, Elsevier, 2019, ⟨10.1016/j.tips.2019.10.002⟩

International audience; Mechanotransduction plays a key role in vascular development, physiology and disease states. Piezo1 is a mechanosensitive non-selective cationic channel present in endothelial and vascular smooth muscle cells. It is activated

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34ba9d4bdaa8e413a5a2812e0f5ec5a6
https://portal.findresearcher.sdu.dk/da/publications/f778bf53-8c3d-43ca-be29-aedf95fa41da

Mambalgin-1 pain-relieving peptide locks the hinge between α4 and α5 helices to inhibit rat acid-sensing ion channel 1a

Autor: Robert Thai, Daad Sarraf, Miguel Salinas, Pascal Kessler, Nicolo Tonali, Eric Lingueglia, Dominique Douguet, Denis Servent

Publikováno v: Neuropharmacology
Neuropharmacology, 2021, 185, pp.108453. ⟨10.1016/j.neuropharm.2021.108453⟩
Neuropharmacology, Elsevier, 2021, pp.108453. ⟨10.1016/j.neuropharm.2021.108453⟩

International audience; Acid-sensing ion channels (ASICs) are proton-gated cationic channels involved in pain and other processes, underscoring the potential therapeutic value of specific inhibitors such as the three-finger toxin mambalgin-1 (Mamb-1)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcd763fe755d5c5af61a5f75dc5e7088
https://doi.org/10.1016/j.neuropharm.2021.108453