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

I) The Development of Deoxycytidine ...

Gipson, Raymond Marshall.

FindBook

Google Book

Amazon

博客來

I) The Development of Deoxycytidine Kinase Inhibitors with Nanomolar Affinity and Improved Metabolic Stability. II) The Synthesis of Ferrocene-Containing Monomers and Biodegradable Polymers Using Azide-Alkyne Click Chemistry and Ring Opening Polymerization.

紀錄類型:	書目-電子資源 : Monograph/item
正題名/作者:	I) The Development of Deoxycytidine Kinase Inhibitors with Nanomolar Affinity and Improved Metabolic Stability. II) The Synthesis of Ferrocene-Containing Monomers and Biodegradable Polymers Using Azide-Alkyne Click Chemistry and Ring Opening Polymerization./
作者:	Gipson, Raymond Marshall.
面頁冊數:	209 p.
附註:	Source: Dissertation Abstracts International, Volume: 76-09(E), Section: B.
Contained By:	Dissertation Abstracts International76-09B(E).
標題:	Organic chemistry. -
電子資源:	http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3704119
ISBN:	9781321762952

I) The Development of Deoxycytidine Kinase Inhibitors with Nanomolar Affinity and Improved Metabolic Stability. II) The Synthesis of Ferrocene-Containing Monomers and Biodegradable Polymers Using Azide-Alkyne Click Chemistry and Ring Opening Polymerization.
Gipson, Raymond Marshall.

I) The Development of Deoxycytidine Kinase Inhibitors with Nanomolar Affinity and Improved Metabolic Stability. II) The Synthesis of Ferrocene-Containing Monomers and Biodegradable Polymers Using Azide-Alkyne Click Chemistry and Ring Opening Polymerization. - 209 p.

Source: Dissertation Abstracts International, Volume: 76-09(E), Section: B.

Thesis (Ph.D.)--University of California, Los Angeles, 2015.

Small molecule dCK inhibitors, in combination with pharmacological perturbations of de novo dNTP biosynthetic pathways, can eliminate acute lymphoblastic leukemia cells in animal models. Our group's previous lead dCK inhibitors had a short half-life in vivo. Part I of this dissertation presents the development of new dCK inhibitors with improved pharmacokinetic properties. Guided by crystal structures of dCK in complex with the lead compound and with derivatives, we delineated the sites of the inhibitor for modification. Crystal structure of the complex between dCK and the racemic mixture of our new lead compound indicated that the R-isomer is responsible for kinase inhibition. This was corroborated by kinetic analysis of the purified enantiomers, which showed that the R-isomer has >60-fold higher affinity than the S-isomer for dCK. This new lead compound has significantly improved metabolic stability, making it a prime candidate for dCK-inhibitor based therapies against hematological malignancies and, potentially, other cancers.

ISBN: 9781321762952Subjects--Topical Terms:

523952
Organic chemistry.

I) The Development of Deoxycytidine Kinase Inhibitors with Nanomolar Affinity and Improved Metabolic Stability. II) The Synthesis of Ferrocene-Containing Monomers and Biodegradable Polymers Using Azide-Alkyne Click Chemistry and Ring Opening Polymerization.
LDR:03003nmm a2200289 4500 001 2077466
005 20161114130316.5
008 170521s2015 ||||||||||||||||| ||eng d
020 $a 9781321762952
035 $a (MiAaPQ)AAI3704119
035 $a AAI3704119
040 $a MiAaPQ $c MiAaPQ
100 1 $a Gipson, Raymond Marshall. $3 3192969
245 1 0 $a I) The Development of Deoxycytidine Kinase Inhibitors with Nanomolar Affinity and Improved Metabolic Stability. II) The Synthesis of Ferrocene-Containing Monomers and Biodegradable Polymers Using Azide-Alkyne Click Chemistry and Ring Opening Polymerization.
300 $a 209 p.
500 $a Source: Dissertation Abstracts International, Volume: 76-09(E), Section: B.
500 $a Advisers: Caius Gabriel Radu; Miguel A. Garcia-Garibay.
502 $a Thesis (Ph.D.)--University of California, Los Angeles, 2015.
520 $a Small molecule dCK inhibitors, in combination with pharmacological perturbations of de novo dNTP biosynthetic pathways, can eliminate acute lymphoblastic leukemia cells in animal models. Our group's previous lead dCK inhibitors had a short half-life in vivo. Part I of this dissertation presents the development of new dCK inhibitors with improved pharmacokinetic properties. Guided by crystal structures of dCK in complex with the lead compound and with derivatives, we delineated the sites of the inhibitor for modification. Crystal structure of the complex between dCK and the racemic mixture of our new lead compound indicated that the R-isomer is responsible for kinase inhibition. This was corroborated by kinetic analysis of the purified enantiomers, which showed that the R-isomer has >60-fold higher affinity than the S-isomer for dCK. This new lead compound has significantly improved metabolic stability, making it a prime candidate for dCK-inhibitor based therapies against hematological malignancies and, potentially, other cancers.
520 $a Part II presents a strategy for functionalizing biodegradable polymers with ferrocene. Small molecule drugs containing ferrocene play an important role in current cancer research, as these novel chemotherapeutics possess redox activity and have the ability to quench damaging free radicals. Current drugs that quench free radicals have adverse side effects, and dosage limits render them less effective in radiotherapy. In the search of more potent and/or selective radioprotective agents, ferrocene functionalized monomers were synthesized via azide-alkyne "click" cycloaddition. Potentially environmentally friendly ferrocene-containing polycarbonates were synthesized via ring opening polymerization (ROP), and they were characterized via NMR spectroscopy, gel permeation chromatography (GPC), thermal analysis, and electrochemical studies.
590 $a School code: 0031.
650 4 $a Organic chemistry. $3 523952
650 4 $a Pharmacology. $3 634543
690 $a 0490
690 $a 0419
710 2 $a University of California, Los Angeles. $b Chemistry 0153. $3 2096181
773 0 $t Dissertation Abstracts International $g 76-09B(E).
790 $a 0031
791 $a Ph.D.
792 $a 2015
793 $a English
856 4 0 $u http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3704119