Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method

Abstract G-protein coupled receptors (GPCRs) play indispensable physiological roles in cell proliferation, differentiation, and migration; therefore, identifying the mechanisms by which ligands bind to GPCRs is crucial for developing GPCR-targeting pharmaceutics and for understanding critical biolog...

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Autores principales:	Seong-Gu Han, Sanghwan Ko, Won-Kyu Lee, Sang Taek Jung, Yeon Gyu Yu
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2017
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/a95ef854682540e9ad103939b8dbf401
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spelling	oai:doaj.org-article:a95ef854682540e9ad103939b8dbf4012021-12-02T15:06:02ZDetermination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method10.1038/s41598-017-08096-62045-2322https://doaj.org/article/a95ef854682540e9ad103939b8dbf4012017-08-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-08096-6https://doaj.org/toc/2045-2322Abstract G-protein coupled receptors (GPCRs) play indispensable physiological roles in cell proliferation, differentiation, and migration; therefore, identifying the mechanisms by which ligands bind to GPCRs is crucial for developing GPCR-targeting pharmaceutics and for understanding critical biological functions. Although some structural information is available regarding the interactions between GPCRs and their small molecule ligands, knowledge of how GPCRs interact with their corresponding macromolecule ligands, such as peptides and proteins, remains elusive. In this study, we have developed a novel strategy to investigate the precise ligand recognition mechanisms involved in the interaction of endothelin receptor type A (ETA) with its ligand, endothelin-1 (ET-1); we call this method “directed degeneration” method. Through flow cytometric screening of a randomized ETA library, statistical analysis of the identified sequences, and biochemical studies, the ligand interaction map was successfully obtained.Seong-Gu HanSanghwan KoWon-Kyu LeeSang Taek JungYeon Gyu YuNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-9 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Seong-Gu Han Sanghwan Ko Won-Kyu Lee Sang Taek Jung Yeon Gyu Yu Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method
description	Abstract G-protein coupled receptors (GPCRs) play indispensable physiological roles in cell proliferation, differentiation, and migration; therefore, identifying the mechanisms by which ligands bind to GPCRs is crucial for developing GPCR-targeting pharmaceutics and for understanding critical biological functions. Although some structural information is available regarding the interactions between GPCRs and their small molecule ligands, knowledge of how GPCRs interact with their corresponding macromolecule ligands, such as peptides and proteins, remains elusive. In this study, we have developed a novel strategy to investigate the precise ligand recognition mechanisms involved in the interaction of endothelin receptor type A (ETA) with its ligand, endothelin-1 (ET-1); we call this method “directed degeneration” method. Through flow cytometric screening of a randomized ETA library, statistical analysis of the identified sequences, and biochemical studies, the ligand interaction map was successfully obtained.
format	article
author	Seong-Gu Han Sanghwan Ko Won-Kyu Lee Sang Taek Jung Yeon Gyu Yu
author_facet	Seong-Gu Han Sanghwan Ko Won-Kyu Lee Sang Taek Jung Yeon Gyu Yu
author_sort	Seong-Gu Han
title	Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method
title_short	Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method
title_full	Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method
title_fullStr	Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method
title_full_unstemmed	Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method
title_sort	determination of the endothelin-1 recognition sites of endothelin receptor type a by the directed-degeneration method
publisher	Nature Portfolio
publishDate	2017
url	https://doaj.org/article/a95ef854682540e9ad103939b8dbf401
work_keys_str_mv	AT seongguhan determinationoftheendothelin1recognitionsitesofendothelinreceptortypeabythedirecteddegenerationmethod AT sanghwanko determinationoftheendothelin1recognitionsitesofendothelinreceptortypeabythedirecteddegenerationmethod AT wonkyulee determinationoftheendothelin1recognitionsitesofendothelinreceptortypeabythedirecteddegenerationmethod AT sangtaekjung determinationoftheendothelin1recognitionsitesofendothelinreceptortypeabythedirecteddegenerationmethod AT yeongyuyu determinationoftheendothelin1recognitionsitesofendothelinreceptortypeabythedirecteddegenerationmethod
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Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method

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