Characterization of novel covalent and non-covalent drugs against K-Ras surrogate targets

Autor: Okutachi, Sunday Ojochegbe

Mutations in the KRAS gene are associated with approximately 15% of all human cancers. This makes it one of the most frequently mutated oncogenes known. Whilst recent breakthroughs in Ras drug discovery have led to the FDA approval of the first direc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od______2658::d75c4bcd1f0f3c99619a0627c0240c5d
http://orbilu.uni.lu/handle/10993/47512

PDE6D Inhibitors with a New Design Principle Selectively Block K-Ras Activity

Autor: Siddiqui, Farid A, Alam, Catharina, Ora, Mikko, Sabt, Ahmed, Manoharan, Ganesh Babu, Bindu, Lakshman, Okutachi, Sunday, Catillon, Marie, Taylor, Troy, Abdelhafez, Omaima M, Lönnberg, Harri, Stephen, Andrew G, Papageorgiou, Anastassios C, Virta, Pasi, Abankwa, Daniel

The trafficking chaperone PDE6D (also referred to as PDEδ) has been nominated as a surrogate target for K-Ras4B (hereafter K-Ras). Arl2-assisted unloading of K-Ras from PDE6D in the perinuclear area is significant for correct K-Ras localization and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=core_ac_uk__::06ab01e5b4dd1be565d79e401930b95c

PDE6D Inhibitors with a New Design Principle Selectively Block K-Ras Activity.

Autor: Siddiqui FA; Turku Bioscience Centre, University of Turku and Åbo Akademi University, 20520 Turku, Finland., Alam C; Turku Bioscience Centre, University of Turku and Åbo Akademi University, 20520 Turku, Finland., Rosenqvist P; Department of Chemistry, University of Turku, 20014 Turku, Finland., Ora M; Department of Chemistry, University of Turku, 20014 Turku, Finland., Sabt A; Department of Chemistry, University of Turku, 20014 Turku, Finland.; Chemistry of Natural Compounds Department, National Research Centre, Dokki, 12622 Giza, Egypt., Manoharan GB; Cancer Cell Biology and Drug Discovery Group, Life Sciences Research Unit, University of Luxembourg, 4362 Esch-sur-Alzette, Luxembourg., Bindu L; NCI RAS Initiative, Cancer Research Technology Program, Frederick National Laboratory for Cancer Research, 21702 Frederick, Maryland, United States., Okutachi S; Cancer Cell Biology and Drug Discovery Group, Life Sciences Research Unit, University of Luxembourg, 4362 Esch-sur-Alzette, Luxembourg., Catillon M; Cancer Cell Biology and Drug Discovery Group, Life Sciences Research Unit, University of Luxembourg, 4362 Esch-sur-Alzette, Luxembourg., Taylor T; NCI RAS Initiative, Cancer Research Technology Program, Frederick National Laboratory for Cancer Research, 21702 Frederick, Maryland, United States., Abdelhafez OM; Chemistry of Natural Compounds Department, National Research Centre, Dokki, 12622 Giza, Egypt., Lönnberg H; Department of Chemistry, University of Turku, 20014 Turku, Finland., Stephen AG; NCI RAS Initiative, Cancer Research Technology Program, Frederick National Laboratory for Cancer Research, 21702 Frederick, Maryland, United States., Papageorgiou AC; Turku Bioscience Centre, University of Turku and Åbo Akademi University, 20520 Turku, Finland., Virta P; Department of Chemistry, University of Turku, 20014 Turku, Finland., Abankwa D; Turku Bioscience Centre, University of Turku and Åbo Akademi University, 20520 Turku, Finland.; Cancer Cell Biology and Drug Discovery Group, Life Sciences Research Unit, University of Luxembourg, 4362 Esch-sur-Alzette, Luxembourg.

Publikováno v: ACS omega [ACS Omega] 2019 Dec 23; Vol. 5 (1), pp. 832-842. Date of Electronic Publication: 2019 Dec 23 (Print Publication: 2020).