Dual incretin agonist: difference between revisions
Diff·revision 3 → 4·15:09, 13 Aug 2024
Difference between revision 3 and revision 4 of Dual incretin agonist. 2 lines changed; the page grew by 259 bytes.
| Revision 3 — 19:57, 30 Jul 2024 TirzTaxonomist (talk) expand §Beyond GIP and GLP-1 2,297 bytes ±0 | Revision 4 — 15:09, 13 Aug 2024 INN_Ingrid (talk) reorder the analogues chronologically rather than alphabetically 2,556 bytes +259 | ||
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| 15 | The design proceeds by choosing a backbone, then substituting residues that confer activity at the second receptor while retaining activity at the first. In practice a GIP backbone has proved more tolerant of the substitutions needed for GLP-1 activity than the reverse, which is why tirzepatide is built from GIP rather than from GLP-1.{{r|coskun2018}} | 15 | The design proceeds by choosing a backbone, then substituting residues that confer activity at the second receptor while retaining activity at the first. In practice a GIP backbone has proved more tolerant of the substitutions needed for GLP-1 activity than the reverse, which is why tirzepatide is built from GIP rather than from GLP-1.{{r|coskun2018}} |
| 16 | 16 | ||
| + | 17 | Reported potency ratios are assay-dependent — cell line, readout, incubation time and receptor expression level all move them — and cross-publication comparison of ratios is unreliable. A ratio quoted without its assay system is not a meaningful number. | |
| + | 18 | ||
| 17 | == References == | 19 | == References == |
| 18 | {{reflist}} | 20 | {{reflist}} |