Covering all areas of the medicinal chemistry and therapeutic applications of nucleic acids, this book provides up-to-date coverage of the broad area of nucleic acid chemistry and biology. The book lays out the basic principles of medicinal chemistry of nucleic acids before focusing on the development and application of modified nucleosides and nucleotides in medicinal chemistry. Cutting-edge subjects for drug discovery like antisense, RNAi, and siRNA are also discussed, and help the target audience of chemists, pharmaceutical researchers, and academics understand the use of nucleic acid drugs to treat diseases.

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 10-23 DNAzyme IN COMPLEX WITH THE TARGET RNA IN SILICO--A 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