東華大學圖書館 |

語系: 繁體中文

說明(常見問題)

回圖書館首頁

手機版館藏查詢

登入

回首頁

切換: 標籤 | MARC模式 | ISBD

Total synthesis of thielocin B1 as a...

Ohsawa, Kosuke.

FindBook

Google Book

Amazon

博客來

Total synthesis of thielocin B1 as a protein-protein interaction inhibitor of PAC3 homodimer

紀錄類型:	書目-電子資源 : 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.
內容註:	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.
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:

2133917
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:02814nmm a2200325 a 4500 001 1994848
003 DE-He213
005 20150825134340.0
006 m d
007 cr nn 008maaau
008 151019s2015 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 2133916
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 : $b Springer Japan : $b Imprint: Springer, $c 2015.
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 2133917
650 0 $a Protein-protein interactions. $3 767666
650 1 4 $a Chemistry. $3 516420
650 2 4 $a Organic Chemistry. $3 890856
650 2 4 $a Pharmacy. $3 636101
650 2 4 $a Medicinal Chemistry. $3 892420
710 2 $a SpringerLink (Online service) $3 836513
773 0 $t Springer eBooks
830 0 $a Springer theses. $3 1314442
856 4 0 $u http://dx.doi.org/10.1007/978-4-431-55447-9
950 $a Chemistry and Materials Science (Springer-11644)