Development of anticancer agents for zinc-proteins related to cancer

2016 Fiscal Year Final Research Report

• Project/Area Number: 26460148
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Kumamoto University
• Principal Investigator: OKAMOTO Yoshinari 熊本大学, 大学院生命科学研究部(薬), 助教 (20194409)
• Co-Investigator(Renkei-kenkyūsha): OTSUKA Masami 熊本大学, 大学院生命科学研究部, 教授 (40126008)
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: 癌 / 浸潤・転移 / ADAM17 / Rasタンパク / 亜鉛配位子

Outline of Final Research Achievements

It is well known that various proteins are relating to cancer. Among them, I focused on a disintegrin and metalloprotease 17 (ADAM17) and farnesyltransferase (FTase).
We are successful to synthesis of a new pyridine /cysteamine based zinc chelator equipped with butynyloxybenzenesulfonyl group (as a ADAM17 inhibitor) or farnesyl group (as a FTase inhibitor) for recognition of these proteins.
IC50 value of ADAM17 inhibitor against the THP-1 cell was 3.22μM, and IC50 value of FTase inhibitor against the dansyl-GCLVS was 0.90μM.

Free Research Field

生体機能分子合成学