4IOA

Crystal structure of compound 4e bound to large ribosomal subunit (50S) from Deinococcus radiodurans

Summary for 4IOA

• Entry DOI: 10.2210/pdb4ioa/pdb
• Related: 4IO9 4IOC
• Descriptor: 23S ribosomal RNA, 50S ribosomal protein L14, 50S ribosomal protein L15, ... (32 entities in total)
• Functional Keywords: ribosome-ribosome inhibitor complex, ribosome/ribosome inhibitor
• Biological source: Deinococcus radiodurans; More
• Total number of polymer chains: 30
• Total formula weight: 1366001.10

Authors

Han, S.,Marr, E.S. (deposition date: 2013-01-07, release date: 2013-03-06, Last modification date: 2024-10-30)

Primary citation

Magee, T.V.,Han, S.,McCurdy, S.P.,Nguyen, T.T.,Granskog, K.,Marr, E.S.,Maguire, B.A.,Huband, M.D.,Chen, J.M.,Subashi, T.A.,Shanmugasundaram, V.
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
Bioorg.Med.Chem.Lett., 23:1727-1731, 2013

PubMed Abstract: A novel series of 3-O-carbamoyl erythromycin A derived analogs, labeled carbamolides, with activity versus resistant bacterial isolates of staphylococci (including macrolide and oxazolidinone resistant strains) and streptococci are reported. An (R)-2-aryl substituent on a pyrrolidine carbamate appeared to be critical for achieving potency against resistant strains. Crystal structures showed a distinct aromatic interaction between the (R)-2-aryl (3-pyridyl for 4d) substituent on the pyrrolidine and G2484 (G2505, Escherichia coli) of the Deinococcus radiodurans 50S ribosome (3.2Å resolution).

PubMed: 23414806
DOI: 10.1016/j.bmcl.2013.01.067

Experimental method

X-RAY DIFFRACTION (3.2 Å)