Receptor bias: difference between revisions
Diff·revision 16 → 17·10:35, 14 Jun 2025
Difference between revision 16 and revision 17 of Receptor bias. 5 lines changed; the page grew by 464 bytes.
| Revision 16 — 16:32, 24 May 2025 TSH_Tallulah (talk) move the trial material out of §Physiology into the compound articles 3,536 bytes ±0 | Revision 17 — 10:35, 14 Jun 2025 CiteBot (talk) bot: sort category members 4,000 bytes +464 | ||
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| 27 | [[Tirzepatide|Tirzepatide]] is reported to show cAMP-favouring bias at the GLP-1 receptor, and it also has a potency imbalance between the GIP and GLP-1 receptors. These are two different senses of "bias" and conflating them is a common error. See [[Tirzepatide]].{{r|jones2018}} | 27 | [[Tirzepatide|Tirzepatide]] is reported to show cAMP-favouring bias at the GLP-1 receptor, and it also has a potency imbalance between the GIP and GLP-1 receptors. These are two different senses of "bias" and conflating them is a common error. See [[Tirzepatide]].{{r|jones2018}} |
| 28 | 28 | ||
| + | 29 | == Status of the idea == | |
| + | 30 | Biased agonism has been a productive research programme and a disappointing translational one, at this receptor and at several others. Several biased compounds designed on the principle have failed to show the predicted clinical advantage.{{r|kenakin2013}} | |
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| + | 32 | The honest summary is that the phenomenon is established, its molecular basis is understood, and its clinical exploitation at this target has not been demonstrated.{{r|jones2018}} | |
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| 29 | == References == | 34 | == References == |
| 30 | {{reflist}} | 35 | {{reflist}} |