1ORK

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

Summary for 1ORK

• Entry DOI: 10.2210/pdb1ork/pdb
• Descriptor: TETRACYCLINE REPRESSOR, MAGNESIUM ION, 9-(N,N-DIMETHYLGLYCYLAMIDO)-6-DEOXY-6-DEMETHYL-TETRACYCLINE, ... (4 entities in total)
• Functional Keywords: transcription regulation
• Biological source: Escherichia coli
• Total number of polymer chains: 1
• Total formula weight: 23827.17

Authors

Orth, P.,Schnappinger, D.,Sum, P.-E.,Ellestad, G.A.,Hillen, W.,Saenger, W.,Hinrichs, W. (deposition date: 1998-05-21, release date: 1999-06-15, Last modification date: 2024-05-22)

Primary citation

Orth, P.,Schnappinger, D.,Sum, P.E.,Ellestad, G.A.,Hillen, W.,Saenger, W.,Hinrichs, W.
Crystal structure of the tet repressor in complex with a novel tetracycline, 9-(N,N-dimethylglycylamido)- 6-demethyl-6-deoxy-tetracycline.
J.Mol.Biol., 285:455-461, 1999

PubMed Abstract: 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.

PubMed: 9878420
DOI: 10.1006/jmbi.1998.2290

Experimental method

X-RAY DIFFRACTION (2.4 Å)