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The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
Characterization of the human cysteinyl leukotriene CysLT1 receptor
The molecular and pharmacological characterization of the cloned human CysLT1 receptor is reported and the functional activation (calcium mobilization) of this receptor is described by LTD4 and LTC4, and competition for radiolabelled LTD4 binding to this receptor by the cysteinyl leukotrienes and three structurally distinct classes of Cys LT1-receptor antagonists.
Characterization of the Human Cysteinyl Leukotriene 2 Receptor*
- C. Heise, B. O'dowd, Jilly F. Evans
- Biology, MedicineThe Journal of Biological Chemistry
- 29 September 2000
The cloning and characterization of the second cysteinyl leukotriene receptor, CysLT2, a 346-amino acid protein with 38% amino acid identity to the Cys LT1 receptor is described and demonstrated high affinity binding and a rank order of potency for competition of LTC4 = LTD4 ≫ LTE4.
Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Molecular Cloning and Characterization of the Human Prostanoid DP Receptor (*)
- Y. Boie, N. Sawyer, D. Slipetz, K. Metters, M. Abramovitz
- BiologyThe Journal of Biological Chemistry
- 11 August 1995
The cloned and expressed a functional cDNA for the hDP receptor showed the highest degree of identity with the hIP and hEP2 receptors, followed by the hEP4 receptor and the rank order of affinities for prostaglandins and prostaglandsin analogs was as predicted for the DP receptor.
Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2
Functional studies demonstrated that PGD2 activation of recombinant CRTH2 results in decrease of intracellular cAMP in a pertussis toxin‐sensitive manner and showed that CRTH 2 can functionally couple to the G‐protein Gαi/o.
Prostaglandin receptor EP(4) mediates the bone anabolic effects of PGE(2).
The pharmacological evidence presented here provides strong support for the hypothesis that the bone anabolic effect of PGE(2) in rats is mediated by the EP(4) receptor.
Cloning and expression of a cDNA for the human prostanoid FP receptor.
Selective modulation of chemokinesis, degranulation, and apoptosis in eosinophils through the PGD2 receptors CRTH2 and DP.
- F. Gervais, R. P. Cruz, G. O'neill
- Biology, MedicineThe Journal of allergy and clinical immunology
- 1 December 2001
These data support the hypothesis that PGD(2) controls eosinophil functions through 2 pharmacologically distinct receptors with independent functions and suggest a role for CRTH2 in the modulation of eos inophil movement and in triggering the release of cytotoxic proteins.