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.
| Original language | English |
|---|---|
| Article number | 7577 |
| Journal | Scientific reports |
| Volume | 7 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - 2017 Dec 1 |
| Externally published | Yes |
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Cite this
Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method. / Han, Seong Gu; Ko, Sanghwan; Lee, Won Kyu; Jung, Sang Taek; Yu, Yeon Gyu.
In: Scientific reports, Vol. 7, No. 1, 7577, 01.12.2017.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method
AU - Han, Seong Gu
AU - Ko, Sanghwan
AU - Lee, Won Kyu
AU - Jung, Sang Taek
AU - Yu, Yeon Gyu
PY - 2017/12/1
Y1 - 2017/12/1
N2 - 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.
AB - 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.
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U2 - 10.1038/s41598-017-08096-6
DO - 10.1038/s41598-017-08096-6
M3 - Article
VL - 7
JO - Scientific Reports
JF - Scientific Reports
SN - 2045-2322
IS - 1
M1 - 7577
ER -