| Budget Amount *help |
¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2015: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2014: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
|
|---|
| Outline of Final Research Achievements |
In this research, I tried to identify the primary target of CPZEN-45, which is a promising anti tubercular agent derivatized from natural product caprazamycins. At the beginning of this research, I focused on following three candidate enzymes for the target; (1) MurX which is a target of caprazamycins and involved in peptidoglycan biosynthesis, (2) WecA which is a paralog of MurX and involved in biosynthesis of arabinogalactan (AG), and (3) AG ligase, which has similar function to MurX and WecA.
As the result of this research, it is revealed that CPZEN-45 inhibited the activity of WecA and de novo synthesis of AG. In contrast, CPZEN-45 did not inhibit the activity of MurX, which is a primary target of caprazamycins. These results indicated that CPZEN-45 showed antituberculous activity by inhibiting WecA enzyme and subsequent blocking of AG biosynthesis.
Also, my collaborator and I succeeded to identify AG ligase, which we expected to be a candidate of target of CPZEN-45.
|
