Bioluminescence Resonance Energy Transfer 2 (BRET2)‐based RAS biosensors to characterize RAS inhibitors

Protein‐protein interactions (PPIs) are principle biological processes that control normal cell growth, differentiation, and homeostasis but are also crucial in diseases such as malignancy, neuropathy, and infection. Despite the importance of PPIs in biology, this target class has been very challeng...

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Detalhes bibliográficos
Principais autores: Bery, N, Rabbitts, TH
Formato: Journal article
Idioma:English
Publicado em: Wiley 2019
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author Bery, N
Rabbitts, TH
author_facet Bery, N
Rabbitts, TH
author_sort Bery, N
collection OXFORD
description Protein‐protein interactions (PPIs) are principle biological processes that control normal cell growth, differentiation, and homeostasis but are also crucial in diseases such as malignancy, neuropathy, and infection. Despite the importance of PPIs in biology, this target class has been very challenging to convert to therapeutics. In the last decade, much progress has been made in the inhibition of PPIs involved in diseases, but many remain difficult such as RAS‐effector interactions in cancers. We describe here a protocol for using Bioluminescence Resonance Energy Transfer 2 (BRET2)‐based RAS biosensors to detect and characterize RAS PPI inhibition by macromolecules and small molecules. This method could be extended to any other small GTPases or any other PPIs of interest.
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spelling oxford-uuid:845a6c07-932f-4bc2-a63f-62e68c5980c22022-03-26T21:50:41ZBioluminescence Resonance Energy Transfer 2 (BRET2)‐based RAS biosensors to characterize RAS inhibitorsJournal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:845a6c07-932f-4bc2-a63f-62e68c5980c2EnglishSymplectic Elements at OxfordWiley2019Bery, NRabbitts, THProtein‐protein interactions (PPIs) are principle biological processes that control normal cell growth, differentiation, and homeostasis but are also crucial in diseases such as malignancy, neuropathy, and infection. Despite the importance of PPIs in biology, this target class has been very challenging to convert to therapeutics. In the last decade, much progress has been made in the inhibition of PPIs involved in diseases, but many remain difficult such as RAS‐effector interactions in cancers. We describe here a protocol for using Bioluminescence Resonance Energy Transfer 2 (BRET2)‐based RAS biosensors to detect and characterize RAS PPI inhibition by macromolecules and small molecules. This method could be extended to any other small GTPases or any other PPIs of interest.
spellingShingle Bery, N
Rabbitts, TH
Bioluminescence Resonance Energy Transfer 2 (BRET2)‐based RAS biosensors to characterize RAS inhibitors
title Bioluminescence Resonance Energy Transfer 2 (BRET2)‐based RAS biosensors to characterize RAS inhibitors
title_full Bioluminescence Resonance Energy Transfer 2 (BRET2)‐based RAS biosensors to characterize RAS inhibitors
title_fullStr Bioluminescence Resonance Energy Transfer 2 (BRET2)‐based RAS biosensors to characterize RAS inhibitors
title_full_unstemmed Bioluminescence Resonance Energy Transfer 2 (BRET2)‐based RAS biosensors to characterize RAS inhibitors
title_short Bioluminescence Resonance Energy Transfer 2 (BRET2)‐based RAS biosensors to characterize RAS inhibitors
title_sort bioluminescence resonance energy transfer 2 bret2 based ras biosensors to characterize ras inhibitors
work_keys_str_mv AT beryn bioluminescenceresonanceenergytransfer2bret2basedrasbiosensorstocharacterizerasinhibitors
AT rabbittsth bioluminescenceresonanceenergytransfer2bret2basedrasbiosensorstocharacterizerasinhibitors