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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Koukos, Georgios Kuliopulos, Athan Bohm, Andrew Corlin, Tiffany Baleja, James D. Covic, Lidija Nguyen, Nga Rana, Rajashree Leger, Andrew J. Zhang, Ping |
| Description | Author Affiliation: Zhang P ( From the Center of Hemostasis and Thrombosis Research, Molecular Oncology Research Institute, Tufts Medical Center, and Departments of Biochemistry and Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111.); Leger AJ ( From the Center of Hemostasis and Thrombosis Research, Molecular Oncology Research Institute, Tufts Medical Center, and Departments of Biochemistry and Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111.); Baleja JD ( From the Center of Hemostasis and Thrombosis Research, Molecular Oncology Research Institute, Tufts Medical Center, and Departments of Biochemistry and Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111.); Rana R ( From the Center of Hemostasis and Thrombosis Research, Molecular Oncology Research Institute, Tufts Medical Center, and Departments of Biochemistry and Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111.); Corlin T ( From the Center of Hemostasis and Thrombosis Research, Molecular Oncology Research Institute, Tufts Medical Center, and Departments of Biochemistry and Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111.); Nguyen N ( From the Center of Hemostasis and Thrombosis Research, Molecular Oncology Research Institute, Tufts Medical Center, and Departments of Biochemistry and Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111.); Koukos G ( From the Center of Hemostasis and Thrombosis Research, Molecular Oncology Research Institute, Tufts Medical Center, and Departments of Biochemistry and Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111.); Bohm A ( From the Center of Hemostasis and Thrombosis Research, Molecular Oncology Research Institute, Tufts Medical Center, and Departments of Biochemistry and Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111.); Covic L ( From the Center of Hemostasis and Thrombosis Research, Molecular Oncology Research Institute, Tufts Medical Center, and Departments of Biochemistry and Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111.); Kuliopulos A ( From the Center of Hemostasis and Thrombosis Research, Molecular Oncology Research Institute, Tufts Medical Center, and Departments of Biochemistry and Medicine, Tufts University School of Medicine, Boston, Massachusetts 02111 athan.kuliopulos@tufts.edu.) |
| Abstract | G protein-coupled receptors (GPCRs) are remarkably versatile signaling systems that are activated by a large number of different agonists on the outside of the cell. However, the inside surface of the receptors that couple to G proteins has not yet been effectively modulated for activity or treatment of diseases. Pepducins are cell-penetrating lipopeptides that have enabled chemical and physical access to the intracellular face of GPCRs. The structure of a third intracellular (i3) loop agonist, pepducin, based on protease-activated receptor-1 (PAR1) was solved by NMR and found to closely resemble the i3 loop structure predicted for the intact receptor in the on-state. Mechanistic studies revealed that the pepducin directly interacts with the intracellular H8 helix region of PAR1 and allosterically activates the receptor through the adjacent (D/N)PXXYYY motif through a dimer-like mechanism. The i3 pepducin enhances PAR1/G subunit interactions and induces a conformational change in fluorescently labeled PAR1 in a very similar manner to that induced by thrombin. As pepducins can potentially be made to target any GPCR, these data provide insight into the identification of allosteric modulators to this major drug target class. |
| ISSN | 00219258 |
| e-ISSN | 1083351X |
| Journal | Journal of Biological Chemistry |
| Issue Number | 25 |
| Volume Number | 290 |
| Language | English |
| Publisher | American Society for Biochemistry and Molecular Biology (United States) |
| Publisher Date | 2015-06-19 |
| Publisher Place | United States |
| Access Restriction | Open |
| Subject Keyword | Biomimetic Materials Chemistry Cell-Penetrating Peptides GTP-Binding Protein Alpha Subunits Receptor, PAR-1 Allosteric Regulation Genetics Amino Acid Motifs Animals COS Cells Cercopithecus Aethiops Metabolism HEK293 Cells Nuclear Magnetic Resonance, Biomolecular Research Support, N.I.H., Extramural Biochemistry Molecular Biology |
| Content Type | Text |
| Resource Type | Article |
| Subject | Cell Biology Biochemistry Molecular Biology |
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