Nature Communications (Aug 2021)
Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen
- Jenna Giubilaro,
- Doris A. Schuetz,
- Tomasz M. Stepniewski,
- Yoon Namkung,
- Etienne Khoury,
- Mónica Lara-Márquez,
- Shirley Campbell,
- Alexandre Beautrait,
- Sylvain Armando,
- Olivier Radresa,
- Jean Duchaine,
- Nathalie Lamarche-Vane,
- Audrey Claing,
- Jana Selent,
- Michel Bouvier,
- Anne Marinier,
- Stéphane A. Laporte
Affiliations
- Jenna Giubilaro
- Department of Pharmacology and Therapeutics, McGill University
- Doris A. Schuetz
- Institute for Research in Immunology and Cancer (IRIC), Université de Montréal
- Tomasz M. Stepniewski
- Research Programme on Biomedical Informatics (GRIB), Department of Experimental and Health Sciences of Pompeu, Fabra University (UPF)-Hospital del Mar Medical Research Institute (IMIM)
- Yoon Namkung
- Research Institute of the McGill University Health Center (RI-MUHC)
- Etienne Khoury
- Department of Medicine, Research Institute of the McGill University Health Center (RI-MUHC), McGill University
- Mónica Lara-Márquez
- Research Institute of the McGill University Health Center (RI-MUHC)
- Shirley Campbell
- Department of Pharmacology and Physiology, Université de Montréal
- Alexandre Beautrait
- Institute for Research in Immunology and Cancer (IRIC), Université de Montréal
- Sylvain Armando
- Department of Medicine, Research Institute of the McGill University Health Center (RI-MUHC), McGill University
- Olivier Radresa
- Department of Medicine, Research Institute of the McGill University Health Center (RI-MUHC), McGill University
- Jean Duchaine
- Institute for Research in Immunology and Cancer (IRIC), Université de Montréal
- Nathalie Lamarche-Vane
- Research Institute of the McGill University Health Center (RI-MUHC)
- Audrey Claing
- Department of Pharmacology and Physiology, Université de Montréal
- Jana Selent
- Research Programme on Biomedical Informatics (GRIB), Department of Experimental and Health Sciences of Pompeu, Fabra University (UPF)-Hospital del Mar Medical Research Institute (IMIM)
- Michel Bouvier
- Institute for Research in Immunology and Cancer (IRIC), Université de Montréal
- Anne Marinier
- Institute for Research in Immunology and Cancer (IRIC), Université de Montréal
- Stéphane A. Laporte
- Department of Pharmacology and Therapeutics, McGill University
- DOI
- https://doi.org/10.1038/s41467-021-24968-y
- Journal volume & issue
-
Vol. 12,
no. 1
pp. 1 – 16
Abstract
While Ras is a promising target for cancer therapy, development of inhibitors targeting Ras signaling has proven challenging. Here, the authors report the discovery of Rasarfin, a small molecule from a phenotypic screen on G protein-coupled receptor (GPCR) endocytosis that acts as a dual Ras and ARF6 inhibitor.
