Lihe Zhang & Zhen Xi 
Medicinal Chemistry of Nucleic Acids 

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
chemistry–a 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 acids–such as
the new advances in genome sequencing, and the processes for
creating RNA interference (RNAi) based drugs–to 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 si RNA for RNAi and the regulation of
micro RNA, non-coding RNA (nc RNA), 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 research–and exposes readers to a wealth of
new drug discovery opportunities emerging in the dynamic field of
nucleic acid chemistry.

Table of Content

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 si RNA: THE SPECIFICITY AND OFF-TARGET EFFECTS 405

Quan Du, Huang Huang, and Zicai Liang

INDEX 423

About the author

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, Ph D, 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, Ph D, 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.