2-Azabicyclo[2.2.1]hept-5-en-3-one (γ-lactam or Vince lactam) is an important precursor of carbocyclic nucleoside analogs, such as abacavir which is important chemotherapeutic agent in the treatment of human HIV and hepatitis B viruses. Traditionally, they are synthesized by chemical methods, but enzymatic synthesis of nucleosides can be more efficient and environmetally friendly. Gamma-Lactamase (EC 3.5.2) is a hydrolase that is utilized for the kinetic resolution of racemic γ-lactam to obtain gamma-lactam, the amino acid product from the resolution can also be used for preparation of candidates currently under clinical trials. In this study, we report a newly discovered lactamase to be integrated in the preparation of the antiviral drugs, followed by protein engineering to enhance the catalytic performance.

Discovery and engineering of novel enzymes for the preparation of antiviral drugs abacavir and carbovir

ACS Spring Meeting 2021

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