Crystal structure of the tet repressor in complex with a novel tetracycline, 9-(N,N-dimethylglycylamido)- 6-demethyl-6-deoxy-tetracycline. Academic Article uri icon

Overview

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.

publication date

  • January 15, 1999

Research

keywords

  • Repressor Proteins
  • Tetracyclines

Identity

Scopus Document Identifier

  • 0033555296

Digital Object Identifier (DOI)

  • 10.1006/jmbi.1998.2290

PubMed ID

  • 9878420

Additional Document Info

volume

  • 285

issue

  • 2