Drug intelligence / Profile preview

myxopyronin B

Development stage
Discontinued
Lead developer
Roche
Modality
Small Molecules
01

Overview

Myxopyronin B is a natural product antibiotic belonging to the alpha-pyrone class and is classified as an aryl ketone. It was originally isolated from the bacterium Myxococcus fulvus. Myxopyronin B acts as an inhibitor of bacterial DNA-directed RNA polymerase (RNAP), specifically binding to the switch 1 and switch 2 regions of RNAP's "switch region." This mechanism is distinct from other RNAP inhibitors such as rifamycins and fidaxomicin; thus, there is no cross-resistance with these drugs. Myxopyronin B exhibits antibacterial activity against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and has been considered for use in drug-resistant tuberculosis. However, due to high resistance rates and high serum protein binding similar to rifamycins and lipiarmycin, unmodified myxopyronin B has not advanced beyond preclinical development[1][2][7].

Other names
BRN 5162839BRN5162839BRN-516283988192-99-8methyl N-[(E,5R)-5-[5-[(2E,4E)-2,5-dimethylnona-2,4-dienoyl]-4-hydroxy-6-oxopyran-2-yl]hex-1-enyl]carbamate
02

Targets

RNAP (Bacterial dna-dependent RNA polymerase)rpoB (DNA-directed RNA polymerase subunit beta)

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