1ork

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1ork, resolution 2.4Å

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TET REPRESSOR, CLASS D IN COMPLEX WITH 9-(N,N-DIMETHYLGLYCYLAMIDO)-6-DEMETHYL-6-DEOXY-TETRACYCLINE

Overview

The tetracycline analog 9-(N, N-dimethylglycylamido)-6-demethyl-6-deoxy-tetracycline (9glyTc) belongs to, a new group of tetracyclines called glycylcyclines. They are strong, antibiotics showing reduced sensitivity against the major tetracycline, resistance mechanisms. We have determined the crystal structure of 9glyTc, in complex with Tet repressor class D, TetR(D), at 2.4 A resolution., Sterical hindrance at the entrance of the tetracycline binding tunnel of, TetR by the bulky and charged glycyl amido substituent interferes with, conformational changes required for the mechanism of induction, and leads, to decreased induction efficiency as observed for point mutations of amino, acid residues located in the neighbourhood to the glycylamido moiety of, bound 9glyTc.

About this Structure

1ORK is a Single protein structure of sequence from Escherichia coli with MG and ATC as ligands. Structure known Active Site: TNE. Full crystallographic information is available from OCA.

Reference

Crystal structure of the tet repressor in complex with a novel tetracycline, 9-(N,N-dimethylglycylamido)- 6-demethyl-6-deoxy-tetracycline., Orth P, Schnappinger D, Sum PE, Ellestad GA, Hillen W, Saenger W, Hinrichs W, J Mol Biol. 1999 Jan 15;285(2):455-61. PMID:9878420

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