摘要
基于动态同位素效应的转态转化分析和计算化学为转化状态的类似物的设计和化学合成提供了静电电位图。这些分子的功用通过对对白血病、自体免疫疾病、通风、实体瘤、细菌群体感应和细菌抗生素的潜在临床效应得到了验证。某种情况下,转化状态类似物担任化学特征使其对新的适应症可以重新设定,其中包括潜在的抗病毒作用。来自这种家族的三种化合物已经进入了临床试验阶段。这种转化状态类似物与他们靶蛋白的绑定具有高亲和力和特异性。这种绑定的物理和结构特性是有价值担任,并且关于紧绑定抑制剂的性质经常有令人惊喜的发现。
关键词: 脱氨酶,Iminoribitols
Current Medicinal Chemistry
Title:The Immucillins: Design, Synthesis and Application of Transition- State Analogues
Volume: 22 Issue: 34
Author(s): Gary B. Evans, Vern L. Schramm and Peter C. Tyler
Affiliation:
关键词: 脱氨酶,Iminoribitols
摘要: Transition-state analysis based on kinetic isotope effects and computational chemistry provides electrostatic potential maps to serve as blueprints for the design and chemical synthesis of transition-state analogues. The utility of these molecules is exemplified by potential clinical applications toward leukemia, autoimmune disorders, gout, solid tumors, bacterial quorum sensing and bacterial antibiotics. In some cases, transition-state analogues have chemical features that have allowed them to be repurposed for new indications, including potential antiviral use. Three compounds from this family have entered clinical trials. The transition-state analogues bind to their target proteins with high affinity and specificity. The physical and structural properties of binding teach valuable and often surprising lessons about the nature of tight-binding inhibitors.
Export Options
About this article
Cite this article as:
Gary B. Evans, Vern L. Schramm and Peter C. Tyler , The Immucillins: Design, Synthesis and Application of Transition- State Analogues, Current Medicinal Chemistry 2015; 22 (34) . https://dx.doi.org/10.2174/0929867322666150821100851
DOI https://dx.doi.org/10.2174/0929867322666150821100851 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |

- Author Guidelines
- Bentham Author Support Services (BASS)
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements