A novel CDC7-selective inhibitor TAK-931 with potent antitumor activity

An abstract of a study by Iwai et al on a novel CDC7-selective inhibitor TAK-931 with potent antitumor activity is presented. The study used the CDC7 enzymatic assay for TAK-931 Transcreener ADP Assay to measure the phosphorylation level of MCM2. TAK-931 was orally administered to nude mice bearing...

Full description

Saved in:
Bibliographic Details
Published in:European journal of cancer (1990) 2016-12, Vol.69, p.S34-S34
Main Authors: Iwai, K, Tadahiro, N, Kurasawa, O, Uchiyama, N, Ohashi, A
Format: Article
Language:English
Subjects:
Adenosine diphosphate
Animal models
Anticancer properties
Antitumor activity
ATP
Cancer
Cancer therapies
Cell growth
Gene expression
Hematology, Oncology and Palliative Medicine
Immunoblotting
Inhibitor drugs
Inhibitors
Kinetics
Oral administration
Pharmacodynamics
Pharmacology
Phosphorylation
Tumor cell lines
Tumors
Xenografts
Xenotransplantation
Citations: Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:An abstract of a study by Iwai et al on a novel CDC7-selective inhibitor TAK-931 with potent antitumor activity is presented. The study used the CDC7 enzymatic assay for TAK-931 Transcreener ADP Assay to measure the phosphorylation level of MCM2. TAK-931 was orally administered to nude mice bearing the xenograft tumors, while pharmacodynamics effect was assessed by evaluating phospho-MCM2 expression in tumor by immunoblotting. Results showed that in xenograft mouse models, TAK-931 potently inhibited CDC7 kinase activity with a time-dependent ATP-competitive kinetics to its ATP-binding pocket. A cellular antiproliferative activity of TAK-931 was observed in multiple cancer cell lines.
ISSN:0959-8049
1879-0852
DOI:10.1016/S0959-8049(16)32683-1