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| Type |
Poster Presentation |
| Area |
Life Chemistry |
| Room No. |
Exhibition Hall 2 |
| Time |
4월 19일 (금요일) 11:00~12:30 |
| Code |
LIFE.P-384 |
| Subject |
Two Color, Cell-based on-bead Screening for Discovering Ligands of the Viral G Protein-Coupled Receptor |
| Authors |
Junhyung Park, Hyun-Suk Lim1,*
Division of Advanced Materials Science, Pohang University of Science and Technology, Korea
1Department of Chemistry, Pohang University of Science and Technology, Korea
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| Abstract |
Herpesviruses family use their virally encoded GPCRs for viral pathogenesis. It is reported that Kaposi’s sarcoma-associated herpesvirus (KSHV)-infected cells express the virally encoded GPCR. This viral GPCR is highly related to Kaposi’s sarcoma which is the most frequent type of tumor that occurs in HIV-infected patients and remains a significant cause of death in AIDS sufferers.1 Therefore, the viral KSHV GPCR is an attractive therapeutic target for the treatment of Kaposi’s sarcoma.
To develop the specific ligands to the GPCR, knowing crystal structure of GPCR can be a important reference. However, it is very challenging to crystallize the membrane protein due to its inherent instability if it is isolated from plasma membrane. These limitations can be addressed through the formation of chimeric construct with binding partners to stabilize the conformation of GPCR. Thus, discovering ligands for the target GPCR can be a good starting point for crystallization of GPCR as well as identifying ligands for GPCRs.
In this regard, we discovered the ligands for the KSHV GPCR through two color, cell-based on-bead screening method without protein purification. In this method, target receptor expressing cell and parental cell that lacks the receptor of interest are labeled with different quantum dot respectively, which enables to select ligand that specifically binds to the target membrane protein. We used OBOC cyclic peptoid library for screening. Identified ligands is now being used for binding assay against the KSHV GPCR.
References
1. Akrit Sodhi, Silvia Montaner, J. Silvio Gutkind*, Nat. Rev. Mol. Cell. Biol. 2004, 5, 988-1012
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| E-mail |
jhpark0816@postech.ac.kr |
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123rd General Meeting of the KCS