Chemoenzymatic Routes to Novel Dendritic Architectures Suitable for Pharmaceutical Applications

树突状分子在其外围含有特定功能基团的多个拷贝，允许在每个这些位点上附着药物样分子。所得到的偶联物通常比原来的单一药物分子具有优越得多的治疗特性。这种现象正在彻底改变药物设计。这一领域的发展受到目前可用的树突分子范围的限制。因此，缺乏变化的三维结构和可用的功能在这些结构的外围是一个严重的缺陷。本提案旨在通过应用申请人开发的新型化学酶方法来纠正这一问题。

Dendritic molecules incorporating multiple copies of a particular functional group on their periphery allow for attachment of drug-like molecules at each of these sites. The resulting conjugates often have vastly superior therapeutic properties relative to the original single drug molecule. This phenomenon is now revolutionizing drug design. Developments in this area are limited by the range of dendritic molecules currently available. Thus, lack of variation in the three-dimensional architecture and the functionality available at the periphery of such constructs is a serious deficiency. This proposal seeks to redress this through the application of novel chemoenzymatic methods developed by the applicant.