Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.

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Xiao Y, Araldi GL, Zhao Z, Brugger N, Karra S, Fischer D, Palmer E

Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4323-7. Epub 2007 May 16.

PubMed ID

17531488 [ View in PubMed

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Abstract

Analogs of PGE(2) with introduction of diene groups at the omega-side chain have been synthesized and evaluated for their binding affinity for EP(2) and EP(4) receptors. An optimized analog (compound 9b) showed high potency and selectivity for the EP(4) receptor over other known receptors.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dinoprostone	Prostaglandin E2 receptor EP1 subtype	Ki (nM)	9.1	N/A	N/A	Details
Dinoprostone	Prostaglandin E2 receptor EP2 subtype	Ki (nM)	4.9	N/A	N/A	Details
Dinoprostone	Prostaglandin E2 receptor EP3 subtype	Ki (nM)	0.33	N/A	N/A	Details
Dinoprostone	Prostaglandin E2 receptor EP4 subtype	Ki (nM)	0.79	N/A	N/A	Details