Title : Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.

Pub. Date : 2003 Oct

PMID : 14500756






3 Functional Relationships(s)
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1 In conclusion, Ki16425 selectively inhibits LPA receptor-mediated actions, especially through LPA1 and LPA3; therefore, it may be useful in evaluating the role of LPA and its receptor subtypes involved in biological actions. 3-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl amino)-3-methyl-5-isoxazolyl) benzylsulfanyl) propanoic acid lysophosphatidic acid receptor 3 Homo sapiens
2 With the cells overexpressing LPA1, LPA2, or LPA3, we examined the selectivity and mode of inhibition by Ki16425 against the LPA-induced actions and compared them with those of dioctyl glycerol pyrophosphate (DGPP 8:0), a recently identified antagonist for LPA receptors. 3-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl amino)-3-methyl-5-isoxazolyl) benzylsulfanyl) propanoic acid lysophosphatidic acid receptor 3 Homo sapiens
3 Ki16425 inhibited the LPA-induced response in the decreasing order of LPA1 >/= LPA3 >> LPA2, whereas DGPP 8:0 preferentially inhibited the LPA3-induced actions. 3-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl amino)-3-methyl-5-isoxazolyl) benzylsulfanyl) propanoic acid lysophosphatidic acid receptor 3 Homo sapiens