药学学报, 2013, 48(6): 814-823
引用本文:
何 伟, 佘鹏伟, 方 正, 郭 凯. 动态组合化学的研究进展[J]. 药学学报, 2013, 48(6): 814-823.
HE Wei, SHE Peng-wei, FANG Zheng, GUO Kai. The research progress of dynamic combinatorial chemistry[J]. Acta Pharmaceutica Sinica, 2013, 48(6): 814-823.

动态组合化学的研究进展
何 伟1, 佘鹏伟2, 方 正1, 郭 凯3*
(南京工业大学 1. 药学院, 2. 理学院, 3. 生物与制药工程学院, 江苏 南京210009)
摘要:

作为组合化学中的新兴分支, 动态组合化学是一种集合成与筛选为一体的组合化学研究新方法。在动态组合化合物库中, 通过靶标分子的诱导结合驱动作用, 能够选择性地筛选到与靶标分子存在强相互作用的优势化合物, 因而动态组合化学在药物研发、材料化学等领域有着广泛的应用前景。本文在简单介绍动态组合化学原理和方法的基础上, 着重介绍了动态组合化学的三要素, 即靶点 (生物酶、凝集素、核酸、有机分子、无机分子等)、涉及的化学反应 (二硫化物化学、胺化还原反应、腙化学等) 以及分析方法, 并对现存限制因素和发展前景作了探讨。

关键词:   
The research progress of dynamic combinatorial chemistry
Abstract:

As a novel branch of combinational chemistry, dynamic combinatorial chemistry (DCC) can be viewed as a technique which combines library synthesis and screening in one pot.  By addition of molecular target, ligangds, which show binding affinity or strong interaction with the molecular target, can be amplified an young but rapidly growing branch of combinatorial chemistry, has been widely used in organic chemistry, biochemistry, material fields.  Ligands in the library can be amplified, since synthesis of the library is screened by a molecular target.  Therefore, these structures could be identified easily.  Consequently DCC has been widely used in the lead discovery, material chemistry and other fields.  On the basis of the principle and method of DCC, this review emphasizes the three factors of DCC, including molecular targets (bio-enzyme, lectin, nucleic acid, organic molecule, inorganic molecule); reaction (disulphide chemistry, ammoniation reduction reaction, hydrazone chemistry, etc.) and analytical method.  Meanwhile, limitation, current situation and future development of DCC were also discussed in this paper.

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