Complete, up-to-date coverage of the broad area of nucleic acid chemistry and biology

Assembling contributions from a collection of authors with expertise in all areas of nucleic acids, medicinal chemistry, and therapeutic applications,Medicinal Chemistry of Nucleic Acids presents a thorough overview of nucleic acid chemistrya rapidly evolving and highly challenging discipline directly responsible for the development of antiviral and antitumor drugs. This reliable resource delves into a multitude of subject areas involving the study of nucleic acidssuch as the new advances in genome sequencing, and the processes for creating RNA interference (RNAi) based drugsto assist pharmaceutical researchers in removing roadblocks that hinder their ability to predict drug efficacy. Offering the latest cutting-edge science in this growing field, Medicinal Chemistry of Nucleic Acids includes:

In-depth coverage of the development and application of modified nucleosides and nucleotides in medicinal chemistry

A close look at a large range of current topics on nucleic acid chemistry and biology

Essential information on the use of nucleic acid drugs to treat diseases like cancer

A thorough exploration of siRNA for RNAi and the regulation of microRNA, non-coding RNA (ncRNA), a newly developing and exciting research area

Thorough in its approach and promising in its message,Medicinal Chemistry of Nucleic Acids probes the new domains of pharmaceutical researchand exposes readers to a wealth of new drug discovery opportunities emerging in the dynamic field of nucleic acid chemistry.

LI-HE ZHANG is President of the academic committee of State Key Laboratory of Natural and Biomimetic Drugs, as well as Professor of Medicinal Chemistry at Peking University. He is also a member of the Chinese Academy of Sciences, Fellow of the Royal Society of Chemistry, former vice president of the Chinese Pharmaceutical Association, and past president of the Asian Federation of Medicinal Chemistry.

ZHEN XI, PhD, is Deputy Director of the State Key Laboratory of Elemento-organic Chemistry, as well as Professor of Pesticide Science and Chemical Biology, and Vice Dean of the College of Chemistry at Nankai University. He holds seven patents and has written a number of reviews and book chapters and sixty-four original research articles.

JYOTI CHATTOPADHYAYA, PhD, DSc, is the University Chair of Bioorganic Chemistry and the chair of the Chemical Biology Program at Uppsala University. He is a guest professor of chemistry at both Jilin University and Nankai University. He has written over 410 peer-reviewed original research articles and is also on the editorial boards of several international journals.

FOREWORD vii

CONTRIBUTORS xi

INTRODUCTION xv

1 RECENT ADVANCES IN CARBOCYCLIC NUCLEOSIDES: SYNTHESIS AND BIOLOGICAL ACTIVITY 1
Jianing Wang, Ravindra K. Rawal, and Chung K. Chu

2 STRUCTURES AND FUNCTIONS OF NUCLEIC ACIDS MODIFIED WITH S, Se, AND Te AND COMPLEXED WITH SMALL MOLECULES 101
Wen Zhang, Jia Sheng, and Zhen Huang

3 UNRAVELING OF THE NAD CYCLIZING AND CALCIUM SIGNALING FUNCTIONS OF HUMAN CD38 142
Hon Cheung Lee

4 DNA AND RNA BINDING SMALL MOLECULES 164
Shibo Li and Zhen Xi

5 G-QUADRUPLEX DNA AND ITS LIGANDS IN ANTICANCER THERAPY 206
Zhi-Shu Huang, Jia-Heng Tan, Tian-Miao Ou, Ding Li, and Lian-Quan Gu

6 MOLECULAR MODELING IN NUCLEIC ACID-TARGETED DRUG DESIGN 258
Lidan Sun, Hongwei Jin, Liangren Zhang, and Lihe Zhang

7 STRUCTURE OF 1023 DNAzyme IN COMPLEX WITH THE TARGET RNAIN SILICOA PROGRESS REPORT ON THE MECHANISM OF RNA CLEAVAGE BY DNA ENZYME 272
Oleksandr Plashkevych and Jyoti Chattopadhyaya

8 LABELING OLIGONUCLEOTIDES TOWARD THE BIOMEDICAL PROBE 292
Il Joon Lee and Byeang Hyean Kim

9 LOCKED NUCLEIC ACID OLIGONUCLEOTIDES TOWARD CLINICAL APPLICATIONS 335
Rakesh N. Veedu and Jesper Wengel

10 THE PHARMACOKINETICS RESEARCH OF NUCLEIC ACID DRUGS 349
Shengqi Wang, Dandan Lu, Qingqing Wang, Haifeng Song, Chan Gao, Caihong Liu, and Ying Wang

11 INDUCIBLE RNAi AND DRUG TARGET VALIDATION 390
Wei Xiong, Jing Zhao, Yufan Zhang, Jinxi Wang, Yong-Xiang Zheng, Qiu-Chen He, Li-He Zhang, and De-Min Zhou

12 siRNA: THE SPECIFICITY AND OFF-TARGET EFFECTS 405
Quan Du, Huang Huang, and Zicai Liang

INDEX 423