publication . Thesis

Chemoenzymatic synthesis of isotopically labelled folates

Angelastro, Antonio;
Open Access English
  • Country: United Kingdom
Abstract
Dihydrofolate reductase (DHFR) is a key enzyme in cellular anabolism. It catalyses the reduction of 7,8-dihydrofolate (H2F) to 5,6,7,8-tetrahydrofolate (H4F) via hydride transfer from the C4 position of NADPH to the C6 position of\ud H2F accompanied with protonation at the N5 position of H2F. Due to the importance of DHFR as an anticancer and antimicrobial target, the catalytic mechanism of DHFR has long been the focus of intense research. Kinetic isotope\ud effect (KIE) measurements can provide insight into the mechanism of DHFR catalysis and guide the rational design of novel anti-DHFR drugs. However,because of a lack of a practical strategy to introduce heavy...
Subjects
Medical Subject Headings: parasitic diseases
free text keywords: QD
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