Small-molecule inhibitor: globomycin
Name
- Common name
- globomycin
Inhibition
- History
- Globomycin, a 19-membered cyclic depsipeptide, was described as an antibiotic compound in 1978, and it was soon recognised to be an inhibitor of signal peptidase II (e.g. Dev et al., 1985).
- Peptidases inhibited
- Signal peptidase II.
- Mechanism
- A half-maximal inhibiting concentration of 0.76 nM was reported for E. coli signal peptidase II by Tokunaga et al. (1984). Dev et al. (1985) found the inhibition of signal peptidase II to be non-competitive, with Ki 36 nM.
- Pharmaceutical relevance
- An analogue of globomycin showed greater antibacterial activity against Gram-negative bacteria than globomycin and also was active against methicillin-resistant Staphylococcus aureus (MRSA) (Kiho et al., 2003).
Chemistry
- CID at PubChem
- 115071
- ChEBI
- 472355
- Structure
![[globomycin (A08.001 inhibitor) structure ]](/merops/smi/structures/globomycin.gif)
- Chemical/biochemical name
- Glycine, N-(N-(N-(N-(N-(3-hydroxy-2-methyl-1-oxononyl)-N-methyl-L-leucyl)-L-alloisoleucyl)-L-seryl)-L-allothreonyl)-, rho-lactone
- Formula weight
- 656
- Related inhibitors
- SF-1902 A(5) (Omoto et al., 1979)
