Structural Perspective on Enzymatic Halogenation

Structural Perspective on Enzymatic Halogenation

Simple halogen substituents frequently afford key structural features that account for the potency and selectivity of natural products, including antibiotics and hormones. For example, when a single chlorine atom on the antibiotic vancomycin is replaced by hydrogen, the resulting antibacterial activity decreases by up to 70% ( Harris , C. M. ; Kannan , R. ; Kopecka , H. ; Harris , T. M. J. Am. ...

Insights into enzymatic halogenation from computational studies

The halogenases are a group of enzymes that have only come to the fore over the last 10 years thanks to the discovery and characterization of several novel representatives. They have revealed the fascinating variety of distinct chemical mechanisms that nature utilizes to activate halogens and introduce them into organic substrates. Computational studies using a range of approaches have already ...

Mechanism of the inhibition of enzymatic halogenation by antithyroid agents.

The structural perspective on CDK5.

Cyclin-dependent kinase 5 (CDK5) plays an essential role in the development of the central nervous system during mammalian embryogenesis. In the adult, CDK5 is required for the maintenance of neuronal architecture. Its deregulation has profound cytotoxic effects and has been implicated in the development of neurodegenerative diseases such as Alzheimer's disease and amyotrophic lateral sclerosis...

The Halogenation of Aromatic Carbinols

In recent years many efforts have been made aiming to define the conditions of the reaction of substitution which lead to inversion of configuration (Walden inversion). The investigations in this direction of Polanyi et al.,’ of Olson,2 of Hughes, Ingold, et aL3 are most outstanding. Polanyi et al. and Olson came to the conclusion that all reactions of substitution by a negative group or ion ar...