PT  - JOURNAL ARTICLE
AU  - Eduard Melief
AU  - Shilah A. Bonnett
AU  - Edison S. Zuniga
AU  - Tanya Parish
TI  - Activation of 2,4-diaminoquinazoline in <em>Mycobacterium tuberculosis</em> by Rv3161c, a putative dioxygenase
AID  - 10.1101/375519
DP  - 2018 Jan 01
TA  - bioRxiv
PG  - 375519
4099  - http://biorxiv.org/content/early/2018/07/24/375519.short
4100  - http://biorxiv.org/content/early/2018/07/24/375519.full
AB  - The diaminoquinazoline series has good potency against Mycobacterium tuberculosis. Resistant isolates have mutations in Rv3161c, a putative dioxygenase. We carried out metabolite analysis on wild-type and an Rv3161c mutant strain after exposure to a diaminoquinazoline. The parental compound was found in intracellular extracts from the mutant, but not the wild-type. A metabolite consistent with a mono-hydroxylated form was identified in the wild-type. These data support the hypothesis that Rv3161c metabolizes diaminoquinazolines in M. tuberculosis.