1ORK

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

1ORK の概要

• エントリーDOI: 10.2210/pdb1ork/pdb
• 分子名称: TETRACYCLINE REPRESSOR, MAGNESIUM ION, 9-(N,N-DIMETHYLGLYCYLAMIDO)-6-DEOXY-6-DEMETHYL-TETRACYCLINE, ... (4 entities in total)
• 機能のキーワード: transcription regulation
• 由来する生物種: Escherichia coli
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 23827.17

構造登録者

Orth, P.,Schnappinger, D.,Sum, P.-E.,Ellestad, G.A.,Hillen, W.,Saenger, W.,Hinrichs, W. (登録日: 1998-05-21, 公開日: 1999-06-15, 最終更新日: 2024-05-22)

主引用文献

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

実験手法

X-RAY DIFFRACTION (2.4 Å)