ReviewACS pharmacology & translational science2026
Kinetic Benefit(s) of Allosteric Receptor Blockade by Positive Allosteric Modulator Antagonists.
Review in ACS pharmacology & translational science, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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0 citing papers in PubMed.
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Authors and funding
2 authors.
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Abstract
This paper discusses how targeted pharmacologic experiments can elucidate the mechanism of allosteric receptor inhibitors (NAMs) to identify NAMs that may have exceptionally useful properties and target residence times in vivo. Specifically, experiments can be done to identify positive allosteric modulator (PAM) antagonists, NAMs that increase the affinity of the receptor for the agonist but decrease agonist efficacy. These molecules would be predicted to have long receptor offset times in vivo (in the presence of ambient concentrations of agonist) and favorable receptor residence times for therapy and also selectively target agonist prebound receptors. Flux analysis is used to demonstrate the salient properties of PAM antagonists and their favorable pharmacodynamic effects for blocking physiological signals.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.