PTGFR binds PTGFR agonists

Stable Identifier
R-HSA-9718020
Type
Reaction [binding]
Species
Homo sapiens
Compartment
ReviewStatus
5/5
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The prostaglandin F receptor (PTGFR) is a prostenoid receptor based on its ability, upon activation by prostaglandin F2α, to contract certain smooth muscle and smooth muscle-containing tissues such as those of the uterus and the eye. PTGFR is highly expressed in the uterine myometrium, the eye and the ovaries. PTGFR agonists (Abramovitz et al. 2000, Sharif et al. 2001, 2002, Neuschäfer-Rube et al. 2003) are primarily used to treat ocular hypertension and gluacoma, as well as eyelash hypotrichosis due to the autoimmune disease alopecia areata. The free acid forms of bimatoprost, latanoprost, tafluprost and travoprost (fluprostenol) are the active forms which are indicated for glaucoma and ocular hypertension. Latanoprostene bunod is a NO-donating analogue of the prostaglandin F2α agonist latanoprost (isopropyl ester) and benefits from the additive hypotensive actions of both the prostaglandin agonist and NO (determined in preclinical models, Kraus et al. 2011). Latanoprostene bunod is the first NO-donating prostaglandin analogue to be granted FDA marketing approval (Kaufman 2017, Fingeret et al. 2019).
Literature References
PubMed ID Title Journal Year
11740958 Bimatoprost and its free acid are prostaglandin FP receptor agonists

Kelly, CR, Williams, GW, Sharif, NA

Eur J Pharmacol 2001
12222762 Agonist activity of bimatoprost, travoprost, latanoprost, unoprostone isopropyl ester and other prostaglandin analogs at the cloned human ciliary body FP prostaglandin receptor

Crider, JY, Kelly, CR, Sharif, NA

J Ocul Pharmacol Ther 2002
12519077 Identification by site-directed mutagenesis of amino acids contributing to ligand-binding specificity or signal transduction properties of the human FP prostanoid receptor

Böer, U, Koch, S, Püschel, GP, Engemaier, E, Neuschäfer-Rube, F

Biochem. J. 2003
10634944 The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs

Adam, M, Labelle, M, Abramovitz, M, Gareau, Y, Sawyer, N, Denis, D, Belley, M, Lamontagne, S, Boie, Y, Metters, KM, Godbout, C, Rochette, C, Tremblay, NM, Dufresne, C, Ouimet, N, Gallant, M, Ruel, R, Carrière, M, Juteau, H

Biochim. Biophys. Acta 2000
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