The Immucillins: Design, Synthesis and Application of Transition- State Analogues

Author(s): Gary B. Evans, Vern L. Schramm, Peter C. Tyler

Journal Name: Current Medicinal Chemistry

Volume 22 , Issue 34 , 2015

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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.

Keywords: Deaminases, Iminoribitols, N-ribosyltransferases, nucleoside analogues, transition-state analogues, transition-state theory.

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Article Details

Year: 2015
Page: [3897 - 3909]
Pages: 13
DOI: 10.2174/0929867322666150821100851
Price: $65

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