3u6k

From Proteopedia

Ef-tu (escherichia coli) in complex with nvp-ldk733

PDB ID 3u6k

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Structural highlights

3u6k is a 4 chain structure with sequence from Escherichia coli K-12 and Planobispora rosea. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 2.45Å
Ligands:	, , , , , , , ,
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

EFTU1_ECOLI This protein promotes the GTP-dependent binding of aminoacyl-tRNA to the A-site of ribosomes during protein biosynthesis.[HAMAP-Rule:MF_00118] May play an important regulatory role in cell growth and in the bacterial response to nutrient deprivation.[HAMAP-Rule:MF_00118]

Publication Abstract from PubMed

4-Aminothiazolyl analogues of the antibiotic natural product GE2270 A (1) were designed, synthesized, and optimized for their activity against Gram positive bacterial infections. Optimization efforts focused on improving the physicochemical properties (e.g., aqueous solubility and chemical stability) of the 4-aminothiazolyl natural product template while improving the in vitro and in vivo antibacterial activity. Structure-activity relationships were defined, and the solubility and efficacy profiles were improved over those of previous analogues and 1. These studies identified novel, potent, soluble, and efficacious elongation factor-Tu inhibitors, which bear cycloalkylcarboxylic acid side chains, and culminated in the selection of development candidates amide 48 and urethane 58.

Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: identification of the cycloalkylcarboxylic acids.,LaMarche MJ, Leeds JA, Amaral K, Brewer JT, Bushell SM, Dewhurst JM, Dzink-Fox J, Gangl E, Goldovitz J, Jain A, Mullin S, Neckermann G, Osborne C, Palestrant D, Patane MA, Rann EM, Sachdeva M, Shao J, Tiamfook S, Whitehead L, Yu D J Med Chem. 2011 Dec 8;54(23):8099-109. Epub 2011 Nov 1. PMID:21999529^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ LaMarche MJ, Leeds JA, Amaral K, Brewer JT, Bushell SM, Dewhurst JM, Dzink-Fox J, Gangl E, Goldovitz J, Jain A, Mullin S, Neckermann G, Osborne C, Palestrant D, Patane MA, Rann EM, Sachdeva M, Shao J, Tiamfook S, Whitehead L, Yu D. Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: identification of the cycloalkylcarboxylic acids. J Med Chem. 2011 Dec 8;54(23):8099-109. Epub 2011 Nov 1. PMID:21999529 doi:10.1021/jm200938f