High-Throughput Chemical Modification of Oligonucleotides for Systematic Structure-Activity Relationship Evaluation

被引：2

作者：

Zewge, Daniel ^{[1
]}

Gosselin, Francis ^{[1
]}

Kenski, Denise M. ^{[1
]}

Li, Jenny ^{[1
]}

Jadhav, Vasant ^{[1
]}

Yuan, Yu ^{[1
]}

Nerurkar, Sandhya S. ^{[1
]}

Tellers, David M. ^{[1
]}

Flanagan, W. Michael ^{[1
]}

Davies, Ian W. ^{[1
]}

机构：

[1] Merck Res Labs, Dept Proc Chem, Rahway, NJ 07065 USA

来源：

BIOCONJUGATE CHEMISTRY | 2014年 / 25卷 / 12期

关键词：

SMALL-INTERFERING RNA; IN-VITRO POTENCY; CLICK CHEMISTRY; BIOLOGICAL-ACTIVITY; SIRNA DELIVERY; SOLID-PHASE; ACID; STABILITY; IMMUNOSTIMULATION; CONJUGATION;

D O I：

10.1021/bc500453q

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Chemical modification of siRNA is achieved in a high-throughput manner (96-well plate format) by copper catalyzed azide-alkyne cycloadditions. This transformation can be performed in one synthetic operation at up to four positions with complete specificity, good yield, and acceptable purity. As demonstrated here, this approach extends the current synthetic options for oligonucleotide modifications and simultaneously facilitates the systematic, rapid biological evaluation of modified siRNA.

引用

页码：2222 / 2232

页数：11

共 50 条

[1] Chemical Modification of Polysaccharides: A Review of Synthetic Approaches, Biological Activity and the Structure-Activity Relationship
Liu, Tianbo
Ren, Qianqian
Wang, Shuang
Gao, Jianing
Shen, Congcong
Zhang, Shengyu
Wang, Yanhong
Guan, Feng
MOLECULES, 2023, 28 (16):
[2] High-throughput screening identifies small molecules that enhance the pharmacological effects of oligonucleotides
Yang, B.
Ming, X.
Cao, C.
Laing, B.
Yuan, A.
Porter, M. A.
Hull-Ryde, E. A.
Maddry, J.
Suto, M.
Janzen, W. P.
Juliano, R. L.
NUCLEIC ACIDS RESEARCH, 2015, 43 (04) : 1987 - 1996
[3] Quantum Chemical Study on Structure-activity Relationship of Several Kinds of Drugs
李小红
程新路
张瑞州
杨向东
Chinese Journal of Structural Chemistry, 2005, (05) : 513 - 520
[4] Quantum chemical study on structure-activity relationship of several kinds of drugs
Li, XH
Cheng, XL
Zhang, RZ
Yang, XD
CHINESE JOURNAL OF STRUCTURAL CHEMISTRY, 2005, 24 (05) : 513 - 520
[5] QUANTUM CHEMICAL PROPERTIES USED IN STRUCTURE-ACTIVITY RELATIONSHIP STUDIES.
Arroio, Agnaldo
Honorio, Kathia M.
da Silva, Alberico B. F.
QUIMICA NOVA, 2010, 33 (03): : 694 - 699
[6] Establishing the Structure-Activity Relationship of Daptomycin
Chow, Hoi Yee
Po, Kathy Hiu Laam
Jin, Kang
Qiao, Guanlin
Sun, Zhenquan
Ma, Wenjie
Ye, Xiyun
Zhou, Ning
Chen, Sheng
Li, Xuechen
ACS MEDICINAL CHEMISTRY LETTERS, 2020, 11 (07): : 1442 - 1449
[7] Synthesis, Herbicidal Evaluation, and Structure-Activity Relationship of Benzophenone Oxime Ether Derivatives
Ma, Jimei
Ma, Mingwei
Sun, Linhao
Zeng, Zhen
Jiang, Hong
JOURNAL OF CHEMISTRY, 2015, 2015
[8] Antioxidant Activity of Eugenol: A Structure-Activity Relationship Study
Gulcin, Ilhami
JOURNAL OF MEDICINAL FOOD, 2011, 14 (09) : 975 - 985
[9] Chemical modifications of dehydrocostus lactone from Saussurea lappa and the study of structure-activity relationship
Setia, R. R.
Kaur, K.
Mankala, R.
Chhabra, B. R.
INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 2007, 46 (05): : 847 - 851
[10] Nature-inspired design of tetraindoles: Optimization of the core structure and evaluation of structure-activity relationship
Abdu-Allah, Hajjaj H. M.
Huang, Shih-Ting
Chang, Tzu Ting
Chen, Chia-Ling
Wu, Han-Chung
Li, Wen-Shan
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 26 (18) : 4497 - 4503

← 1 2 3 4 5 →