Phenosafranin inhibits nuclear localization of transglutaminase 2 without affecting its transamidase activity.
Transglutaminase 2 (TG2) localizes to the nucleus and induces apoptosis through a crosslinking inactivation of Sp1 in JHH-7 cells treated with acyclic retinoid. We screened an inhibitor suppressing transamidase activity in the nucleus without affecting transamidase activity itself. Phenosafranin was found to inhibit nuclear localization of EGFP-tagged TG2 and dose-dependently reduce nuclear transamidase activity without affecting the activity in a tube. We concluded that phenosafranin was a novel TG2 inhibitor capable of suppressing its nuclear localization.
Micro-Signaling Regulation Technology Unit, RIKEN Center for Life Science Technologies, 2-1 Hirosawa, Wako, Saitama, 351-0198, Japan.
Yutaka
Y
Furutani
Micro-Signaling Regulation Technology Unit, RIKEN Center for Life Science Technologies, 2-1 Hirosawa, Wako, Saitama, 351-0198, Japan.
Mariko
M
Toguchi
Micro-Signaling Regulation Technology Unit, RIKEN Center for Life Science Technologies, 2-1 Hirosawa, Wako, Saitama, 351-0198, Japan.
Rajan
R
Shrestha
Micro-Signaling Regulation Technology Unit, RIKEN Center for Life Science Technologies, 2-1 Hirosawa, Wako, Saitama, 351-0198, Japan. skojima@riken.jp.
Soichi
S
Kojima
D021581:Active Transport, Cell Nucleus / Q000187:drug effects; D000595:Amino Acid Sequence; D045744:Cell Line, Tumor; D002467:Cell Nucleus / Q000187:drug effects* / Q000378:metabolism; D003600:Cytosol / Q000187:drug effects* / Q000378:metabolism; D019204:GTP-Binding Proteins / Q000235:genetics / Q000378:metabolism*; D015870:Gene Expression; D005822:Genetic Vectors / Q000737:chemistry / Q000378:metabolism; D049452:Green Fluorescent Proteins / Q000235:genetics / Q000378:metabolism; D022781:Hepatocytes / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D057166:High-Throughput Screening Assays; D006801:Humans; D010619:Phenazines / Q000494:pharmacology*; D000072417:Protein Domains; D000091345:Protein Glutamine gamma Glutamyltransferase 2; D013194:Staining and Labeling; D014162:Transfection; D011503:Transglutaminases / Q000235:genetics / Q000378:metabolism*; D014212:Tretinoin / Q000031:analogs & derivatives / Q000494:pharmacology
D010619:Phenazines; C485184:enhanced green fluorescent protein; D049452:Green Fluorescent Proteins; D014212:Tretinoin; C011977:phenosafranine; C034534:3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentaenoic acid; D000091345:Protein Glutamine gamma Glutamyltransferase 2; D011503:Transglutaminases; D019204:GTP-Binding Proteins
Inhibitor; Nuclear localization; Phenosafranin; Transglutaminase