2009 Fiscal Year Final Research Report
Development of novel compound of function selective labeling reagent for proteins and its systematic use
| Project/Area Number |
19685015
|
|---|
| Research Category |
Grant-in-Aid for Young Scientists (A)
|
| Allocation Type | Single-year Grants |
|---|
| Research Field |
Chemistry related to living body
|
|---|
| Research Institution | Hokkaido University |
|---|
Principal Investigator |
HINOU Hiroshi Hokkaido University, 大学院・先端生命科学研究院, 助教 (70333333)
|
|---|
| Project Period (FY) |
2007 – 2009
|
| Keywords | 自殺基質 / 機能選択的 / 特異的阻害 / 触媒部位の同定 / ラベル化 / 非特異的阻害 / 活性化速度 |
|---|
| Research Abstract |
I have tried to develop a novel method of inhibitor design of such enzymes exemplified to a neuraminidase Vibrio cholerae neuraminidase (VCNA) of which crystal structure was reported in 1994 and most potent inhibitor was reported in 1971. As a result, a potent inhibitor for Vibrio cholerae neuramnidase was developed using mechanism-based labeling information of key amino acid residues, design of a skeleton of focused library based on labeling information, screening of the focused library, and elimination of promiscuous inhibitor by detergent-based assay to afford potent (Ki=73nM) and selective inhibitor among viral, bacterial, and mammal neuraminidases.
|
-
[Journal Article] Lucia Mendonca-Previato, Jose O Previato, Adriane R Todeschini "A new class of mechanism-based inhibitors for Trypanosoma cruzi trans-sialidase and their influence on parasite virulence"2010
Author(s)
Sebastiao T Carvalho, Mauro Sola-Penna, Isadora A Oliveira, Samuel Pita, Arlan S Goncalves, Bianca C Neves, Francisco R Sousa, Leonardo Freire-de-Lima, Masaki Kurogochi, Hiroshi Hinou, Shin-Ichiro Nishimura
-
Journal Title
-
-
-
[Journal Article] Functional Neoglycopeptides: Synthesis and Characterization of New Class MUC1 Glycoprotein Models Having Core 2-based O-Glycan and Complex-type N-Glycan Chains2009
Author(s)
Takahiko Matsushita, Reiko Sadamoto, Naoki Oyabu, Hideki Nakata, Masataka Fumoto, Naoki Fujitani, Yasuhiro Takegawa, Takashi Sakamoto, Masaki Kurogochi, Hiroshi Hinou, Hiroki Shimizu, Takaomi Ito, Kentaro Naruchi, Hiroko Togame, HiroshiTakemoto, Hirosato Kondo, Shin-Ichiro Nishimura
-
Journal Title
Biochemistry 48
Pages: 11117-11133
-
-
[Journal Article] An Essential Epitope of Anti-MUC1 Monoclonal Antibody KL-6 Revealed by Focused Glycopeptide Library2009
Author(s)
Naoki Ohyabu, Hiroshi Hinou, Takahiko Matsushita, Ryuko Izumi, Hiroki Shimizu, Keiko Kawamoto, Yoshito Numata, Hiroko Togame, Hiroshi Takemoto, Hirosato Kondo, Shin-Ichiro Nishimura
-
Journal Title
Journal of the American Chemical Society 131
Pages: 17102-17109
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
