YM-254890, a novel platelet aggregation inhibitor produced by Chromobacterium sp. QS3666.
A novel platelet aggregation inhibitor, YM-254890, was isolated from the culture broth of strain QS3666. This strain was isolated from a soil sample collected at Okutama, Tokyo, Japan, and was identified as Chromobacterium sp. by morphological and physiological criteria. YM-254890 was purified from the culture supernatant by solvent extraction, ODS and silica gel flash chromatography, followed by preparative HPLC. YM-254890 inhibited ADP-induced platelet aggregation in human platelet-rich plasma with an IC50 value below 0.6 microM by blocking the P2Y1 receptor-signal transduction pathway.
Taniguchi
Masatoshi
M
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. taniguti@yamanouchi.co.jp
Nagai
Koji
K
Arao
Nakako
N
Kawasaki
Tomihisa
T
Saito
Tetsu
T
Moritani
Yumiko
Y
Takasaki
Jun
J
Hayashi
Kazumi
K
Fujita
Shigeo
S
Suzuki
Ken-ichi
K
Tsukamoto
Shin-ichi
S
D000244:Adenosine Diphosphate / Q000037:antagonists & inhibitors / Q000494:pharmacology; D000818:Animals; D002118:Calcium / Q000378:metabolism; D002861:Chromobacterium / Q000737:chemistry / Q000145:classification / Q000378:metabolism*; D005285:Fermentation; D006801:Humans; D008826:Microbial Sensitivity Tests; D010456:Peptides, Cyclic / Q000096:biosynthesis / Q000302:isolation & purification / Q000494:pharmacology; D010975:Platelet Aggregation Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology; D058919:Purinergic P2 Receptor Antagonists; D051381:Rats; D058472:Receptors, Purinergic P2Y1; D012988:Soil Microbiology; D014407:Tumor Cells, Cultured
C546382:P2RY1 protein, human; D010456:Peptides, Cyclic; D010975:Platelet Aggregation Inhibitors; D058919:Purinergic P2 Receptor Antagonists; D058472:Receptors, Purinergic P2Y1; C475455:YM-254890; D000244:Adenosine Diphosphate; D002118:Calcium