語系:
繁體中文
English
說明(常見問題)
登入
回首頁
切換:
標籤
|
MARC模式
|
ISBD
Total synthesis of thielocin B1 as a...
~
Ohsawa, Kosuke.
Total synthesis of thielocin B1 as a protein-protein interaction inhibitor of PAC3 homodimer
紀錄類型:
書目-語言資料,印刷品 : Monograph/item
正題名/作者:
Total synthesis of thielocin B1 as a protein-protein interaction inhibitor of PAC3 homodimer/ by Kosuke Ohsawa.
作者:
Ohsawa, Kosuke.
出版者:
Tokyo :Springer Japan : : 2015.,
面頁冊數:
xiii, 109 p. :ill. (some col.), digital ; : 24 cm.;
Contained By:
Springer eBooks
標題:
Proteins - Inhibitors. -
電子資源:
http://dx.doi.org/10.1007/978-4-431-55447-9
ISBN:
9784431554479 (electronic bk.)
Total synthesis of thielocin B1 as a protein-protein interaction inhibitor of PAC3 homodimer
Ohsawa, Kosuke.
Total synthesis of thielocin B1 as a protein-protein interaction inhibitor of PAC3 homodimer
[electronic resource] /by Kosuke Ohsawa. - Tokyo :Springer Japan :2015. - xiii, 109 p. :ill. (some col.), digital ;24 cm. - Springer theses,2190-5053. - Springer theses..
Introduction -- Total Synthesis of Thielocin B1 and NMR Chemical Shift Perturbation Experiments with PAC3 Homodimer -- Synthesis of Spin-labeled Thielocin B1 and Observation of Paramagnetic Relaxation Enhancement Effects -- An Improved Method for the Direct Formylation ob Substituted Benzenes Using Dichloromethyl Methyl Ether-Silver Trifluoromethanesulfonate -- Conclusions.
This book focuses on thielocin B1 (TB1), which was found to be an inhibitor of protein–protein interactions (PPIs) of proteasome assembling chaperone (PAC) 3 homodimer, and elucidates the mechanism by nuclear magnetic resonance (NMR) studies. Interfaces of PPIs recently have been expected to be novel therapeutic targets, while it is difficult to apply conventional methodology based on lock and key theory. The author achieved the first total synthesis of TB1 and its spin-labeled derivative to carry out NMR experiments because the supply of TB1 from natural sources was limited. Unique 2,2',6,6'-tetrasubstituted diphenyl ether moiety of TB1 was synthesized from a depsidone skeleton by chemoselective reduction of lactone. In the process of elongating side wings, efficient formylation utilizing dichloromethyl methyl ether–silver trifluoromethanesulfonate was developed for the sterically hindered aromatic compound. NMR titration experiments and paramagnetic relaxation enhancement observation of PAC3 homodimer were performed with synthesized TB1 and its molecular probe, respectively. The results of the above NMR studies and additional in silico docking studies suggested that TB1 promotes the dissociation to monomeric PAC3 after interaction with PAC3 homodimer. The rare mechanism shown in this book indicates a potential novel drug target in the interfaces of PPIs with no cavity or groove.
ISBN: 9784431554479 (electronic bk.)
Standard No.: 10.1007/978-4-431-55447-9doiSubjects--Topical Terms:
1065647
Proteins
--Inhibitors.
LC Class. No.: QP551.5
Dewey Class. No.: 572.6
Total synthesis of thielocin B1 as a protein-protein interaction inhibitor of PAC3 homodimer
LDR
:02814nam a2200325 a 4500
001
835948
003
DE-He213
005
20150825134340.0
006
m d
007
cr nn 008maaau
008
160421s2015 ja s 0 eng d
020
$a
9784431554479 (electronic bk.)
020
$a
9784431554462 (paper)
024
7
$a
10.1007/978-4-431-55447-9
$2
doi
035
$a
978-4-431-55447-9
040
$a
GP
$c
GP
041
0
$a
eng
050
4
$a
QP551.5
072
7
$a
PNN
$2
bicssc
072
7
$a
SCI013040
$2
bisacsh
082
0 4
$a
572.6
$2
23
090
$a
QP551.5
$b
.O38 2015
100
1
$a
Ohsawa, Kosuke.
$3
1065646
245
1 0
$a
Total synthesis of thielocin B1 as a protein-protein interaction inhibitor of PAC3 homodimer
$h
[electronic resource] /
$c
by Kosuke Ohsawa.
260
$a
Tokyo :
$c
2015.
$b
Springer Japan :
$b
Imprint: Springer,
300
$a
xiii, 109 p. :
$b
ill. (some col.), digital ;
$c
24 cm.
490
1
$a
Springer theses,
$x
2190-5053
505
0
$a
Introduction -- Total Synthesis of Thielocin B1 and NMR Chemical Shift Perturbation Experiments with PAC3 Homodimer -- Synthesis of Spin-labeled Thielocin B1 and Observation of Paramagnetic Relaxation Enhancement Effects -- An Improved Method for the Direct Formylation ob Substituted Benzenes Using Dichloromethyl Methyl Ether-Silver Trifluoromethanesulfonate -- Conclusions.
520
$a
This book focuses on thielocin B1 (TB1), which was found to be an inhibitor of protein–protein interactions (PPIs) of proteasome assembling chaperone (PAC) 3 homodimer, and elucidates the mechanism by nuclear magnetic resonance (NMR) studies. Interfaces of PPIs recently have been expected to be novel therapeutic targets, while it is difficult to apply conventional methodology based on lock and key theory. The author achieved the first total synthesis of TB1 and its spin-labeled derivative to carry out NMR experiments because the supply of TB1 from natural sources was limited. Unique 2,2',6,6'-tetrasubstituted diphenyl ether moiety of TB1 was synthesized from a depsidone skeleton by chemoselective reduction of lactone. In the process of elongating side wings, efficient formylation utilizing dichloromethyl methyl ether–silver trifluoromethanesulfonate was developed for the sterically hindered aromatic compound. NMR titration experiments and paramagnetic relaxation enhancement observation of PAC3 homodimer were performed with synthesized TB1 and its molecular probe, respectively. The results of the above NMR studies and additional in silico docking studies suggested that TB1 promotes the dissociation to monomeric PAC3 after interaction with PAC3 homodimer. The rare mechanism shown in this book indicates a potential novel drug target in the interfaces of PPIs with no cavity or groove.
650
0
$a
Proteins
$x
Inhibitors.
$3
1065647
650
0
$a
Protein-protein interactions.
$3
668549
650
1 4
$a
Chemistry.
$3
593913
650
2 4
$a
Organic Chemistry.
$3
673440
650
2 4
$a
Pharmacy.
$3
582411
650
2 4
$a
Medicinal Chemistry.
$3
668872
710
2
$a
SpringerLink (Online service)
$3
593884
773
0
$t
Springer eBooks
830
0
$a
Springer theses.
$3
831604
856
4 0
$u
http://dx.doi.org/10.1007/978-4-431-55447-9
950
$a
Chemistry and Materials Science (Springer-11644)
筆 0 讀者評論
多媒體
評論
新增評論
分享你的心得
Export
取書館別
處理中
...
變更密碼[密碼必須為2種組合(英文和數字)及長度為10碼以上]
登入