Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 5, Pages 2367-2375Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm201600e
Keywords
-
Categories
Funding
- Australian Research Council [DP110100687]
- National Health and Medical Research Council (NHMRC) of Australia [519461]
Ask authors/readers for more resources
A series of novel 2-amino-3-benzoylthiophenes (2A3BTs) were screened using a functional assay of AIR mediated phosphorylation of extracellular signal-regulated kinases 1 and 2 (ERK1/2) in intact CHO cells to identify potential agonistic effects as well as the ability to allosterically modulate the activity of the orthosteric agonist, R-PIA. Two derivatives, 8h and 8i, differing only in terms of the absence or presence of an electron-withdrawing group on the benzoyl moiety of the 2A3BT scaffold, were identified as biased allosteric agonists and positive allosteric modulators of agonist function at the adenosine A(1) receptor (A(1)R) in two different functional assays. Our findings indicate that subtle structural variations can promote functionally distinct receptor conformational states.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available