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- W2901524433 abstract "Abstract: There is significant evidence that internal pools of G protein–coupled receptors (GPCRs) exist and may be affected by both endogenous signaling molecules and hydrophobic pharmaceutical ligands, once assumed to only affect cell surface versions of these receptors. Here, we discuss evidence that the biology of nuclear GPCRs in particular is complex, rich, and highly interactive with GPCR signaling from the cell surface. Caging existing GPCR ligands may be an excellent means of further stratifying the phenotypic effects of known pharmacophores such as β-adrenergic, angiotensin II, and type B endothelin receptor ligands in the cardiovascular system. We describe some synthetic strategies we have used to design ligands to go from in cellulo to in vivo experiments. We also consider how surface and intracellular GPCR signaling might be integrated and ways to dissect this. If they could be selectively targeted, nuclear GPCRs and their associated nucleoligands would represent a completely novel area for exploration by Pharma." @default.
- W2901524433 created "2018-11-29" @default.
- W2901524433 creator A5006334654 @default.
- W2901524433 creator A5021824403 @default.
- W2901524433 creator A5052328017 @default.
- W2901524433 creator A5057160583 @default.
- W2901524433 date "2018-04-01" @default.
- W2901524433 modified "2023-10-18" @default.
- W2901524433 title "Nucleoligands-repurposing G Protein–coupled Receptor Ligands to Modulate Nuclear-localized G Protein–coupled Receptors in the Cardiovascular System" @default.
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