Panosialins, inhibitors of an alpha1,3-fucosyltransferase Fuc-TVII, suppress the expression of selectin ligands on U937 cells.
Panosialins A and B were isolated as inhibitors of an alpha1,3-fucosyltransferase, Fuc-TVII, which is a key enzyme in the biosynthesis of selectin ligands, from culture broth of Streptomyces sp. Panosialins A and B inhibited the Fuc-TVII activity with IC50 values of 4.8 and 5.3 microg/ml, respectively. Panosialin A suppressed expression of selectin ligands on U937 cells, and inhibited the cell adhesion to immobilized E-selectin-immunoglobulin. Panosialins are the first reported Fuc-TVII inhibitors which can suppress the biosynthesis of selectin ligands and then inhibit selectin-mediated cell adhesion.
Shinoda
K
K
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan. katsumi.shinoda@kyowa.co.jp
Shitara
K
K
Yoshihara
Y
Y
Kusano
A
A
Uosaki
Y
Y
Ohta
S
S
Hanai
N
N
Takahashi
I
I
D001555:Benzene Derivatives / Q000494:pharmacology*; D002448:Cell Adhesion / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005434:Flow Cytometry; D005647:Fucosyltransferases / Q000037:antagonists & inhibitors*; D006801:Humans; D007074:Immunoglobulin G / Q000378:metabolism; D008024:Ligands; D011993:Recombinant Fusion Proteins / Q000378:metabolism; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D019087:Selectins / Q000378:metabolism*; D020298:U937 Cells
D001555:Benzene Derivatives; D004791:Enzyme Inhibitors; D007074:Immunoglobulin G; D008024:Ligands; D011993:Recombinant Fusion Proteins; D011994:Recombinant Proteins; D019087:Selectins; C003039:panosialin; D005647:Fucosyltransferases; C031692:galactoside 3-fucosyltransferase