Drug intelligence / Profile preview

biotinol-5-amp

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Biotinol-5'-AMP is a synthetic small molecule that mimics the natural reaction intermediate of biotin protein ligase (BPL), an enzyme essential for bacterial metabolism. Structurally, it is a derivative of adenosine monophosphate (AMP) conjugated to a biotin analog. Biotinol-5'-AMP acts as a pan inhibitor of BPLs from various clinically important bacteria, including *Staphylococcus aureus* and *Mycobacterium tuberculosis*. It competitively inhibits the substrate biotin at the enzyme's active site, thereby blocking the ligation of biotin to target proteins—a process critical for fatty acid synthesis in bacteria. This compound has demonstrated antibacterial activity with low micromolar minimum inhibitory concentrations (MICs) against these pathogens and shows no cytotoxicity toward human HepG2 cells[1][6][7]. It is not approved for clinical use but serves as an important tool in biochemical research and drug discovery targeting bacterial BPL.

Other names
Biotinyl-5'-AMP5'-O-[hydroxy({5-[2-oxohexahydrothieno[3,4-d]imidazolyl]pentyl}oxy)phosphoryl]adenosine
02

Targets

BPL (Biotin protein ligase)

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