Tadashi Watabe

Fibroblast activation protein (FAP), which promotes tumor growth and progression, is overexpressed in cancer-associated fibroblasts of many human epithelial cancers. Because of its low expression in normal organs, FAP is an excellent target for theranostics. In this study, we used radionuclides with relatively long half-lives, ⁶⁴Cu (half-life, 12.7 h) and ²²⁵Ac (half-life, 10 d), to label FAP inhibitors (FAPIs) in mice with human pancreatic cancer xenografts. <b>Methods:</b

7-Hydroxymethyl-12-methylbenz[alpha]anthracene (7-HMBA), a carcinogenic major metabolite of 7,12-dimethylbenz[alpha]anthracene (DMBA) in liver, was transformed by liver cytosolic sulfotransferase to reactive 7-HMBA sulfate, which is mutagenic toward Salmonella typhimurium strain TA98. The mutagenicity of 7-HMBA in the presence of hepatic sulfotransferase was much higher than that of DMBA or 7-HMBA in the presence of hepatic monooxygenase.

Bovine liver microsomes converted four A'-steroids, cholesterol, 5-cholestene, 20-methyl-5-pregnen-3p-01, and pregnenolone, to the corresponding 5,6a-epoxides, 5,6/3-epoxides, and 5a,6/3-glycols in the presence of an NADPH-generating system, ferrous ion, and ADP.All of the metabolites were separated and isolated by high performance liquid chromatography and identified by gas chromatography-mass spectroscopy.The microsomes catalyzed hydrolysis of the a-and &epoxides of all the examined A'-steroid

²¹¹At is an α-emitter that has similar chemical properties to iodine and is used in targeted α-therapy. In the present study, we added ascorbic acid (AA) to ²¹¹At solution to increase the radiochemical purity of astatide and evaluated its efficacy against differentiated thyroid cancer, which is characterized by the expression of sodium/iodide symporter (NIS). <b>Methods:</b> Crude ²¹¹At solution (AA(-)) and ²¹¹At solution treated with AA (AA(+)) were p

It is known that in humans taking soy food, the phytoestrogens, daidzein (DZ) and genistein (GS), exist as sulfates and glucuronides in the plasma and are excreted as conjugates in urine. To investigate which human sulfotransferase (SULT) isoforms participate in the sulfation of these phytoestrogens, the four major cytosolic SULTs, SULT1A1, SULT1A3, SULT1E1, and SULT2A1, occurring in the human liver were bacterially expressed as His-tagged proteins and chromatographically purified to homogeneity

1. Rat liver microsomes converted d-limonene to the 1,2-epoxide (1-methyl-4-(1′-methylethenyl)-7-oxabicyclo[4,1,0]heptane), the 8,9-epoxide (1-methyl-4-(1′-methyl-1′,2′-epoxyethyl)cyclohex-1-ene), and the 8,9-glycol (2-(4′-methylcyclohex-3′-en-1′-yl) propane-1,2-diol) in the presence of NADPH. The 8,9-glycol was formed in the highest yield, the 1,2-epoxide in next highest yield, and the 8,9-epoxide was formed in low yield.2. The absence of the 1,2-glycol (1-methyl-4-(1′-methylethenyl)cyclohexene

Distilled styrene showed mutagenic activity towards Salmonella typhimurium TA 100 after activ ation with hepatic 9,000 X g supernatant fractions (S-9). The S-9 fractions ,had been obtained from rats treated with 3-methylcholanthrene or phenobarbital and fortified with an NADPH-generating system in the presence of 3,3,3-trichloropropene oxide (TCPO), an hepatic microsomal epoxide hydratase inhibitor. No mutagenic activity was observed when either the TCPO was omitted or rats were treated with a p

Phenylalanine derivatives, which target tumors especially through L-type amino acid transporter-1 (LAT1), have elicited considerable attention. In this study, we evaluated the treatment effect of phenylalanine labeled with the alpha emitter astatine (²¹¹At-PA) in tumor bearing mice. The C6 glioma, U-87MG, and GL261 cell lines were subjected to a cellular ²¹¹At-PA uptake analysis that included an evaluation of the uptake inhibition by the system L amino acid transporter inhi