GLP-1 receptor: difference between revisions
Diff·revision 3 → 4·07:57, 11 Jul 2024
Difference between revision 3 and revision 4 of GLP-1 receptor. 2 lines changed; the page grew by 294 bytes.
| Revision 3 — 08:50, 2 Jul 2024 BetaCellBoyd (talk) clarify that the incretin effect is defined by the oral–intravenous comparison 2,831 bytes ±0 | Revision 4 — 07:57, 11 Jul 2024 StubSorterBot (talk) bot: sort category members 3,125 bytes +294 | ||
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| 15 | Cryo-electron microscopy structures of the agonist-bound, G<sub>s</sub>-coupled receptor have resolved the sharp kink in transmembrane helix 6 that accompanies activation. The structures also explain why the first eight residues of the peptide are indispensable while the C-terminal half tolerates extensive modification: acylation, PEGylation and fusion partners are all attached distal to the pharmacophore.{{r|zhang2017}} | 15 | Cryo-electron microscopy structures of the agonist-bound, G<sub>s</sub>-coupled receptor have resolved the sharp kink in transmembrane helix 6 that accompanies activation. The structures also explain why the first eight residues of the peptide are indispensable while the C-terminal half tolerates extensive modification: acylation, PEGylation and fusion partners are all attached distal to the pharmacophore.{{r|zhang2017}} |
| 16 | 16 | ||
| + | 17 | Small-molecule agonists bind a partially overlapping but distinct pocket, closer to the extracellular face of the transmembrane bundle, and do not require the extracellular-domain capture step. This is why an orally absorbable non-peptide agonist is chemically possible at all.{{r|graaf2016}} | |
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| 17 | == References == | 19 | == References == |
| 18 | {{reflist}} | 20 | {{reflist}} |