Structural Insights into the Mechanism of Carbapenemase Activity of the OXA-48 ?-Lactamase [electronic resource]

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Tác giả:

Ngôn ngữ: eng

Ký hiệu phân loại: 636.7 Dogs

Thông tin xuất bản: Oak Ridge, Tenn. : Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2019

Mô tả vật lý: Size: 14 p. : , digital, PDF file.

Bộ sưu tập: Metadata

ID: 259964

 Carbapenem-hydrolyzing class D carbapenemases (CHDLs) are enzymes that produce resistance to the last-resort carbapenem antibiotics, severely compromising the available therapeutic options for the treatment of life-threatening infections. A broad variety of CHDLs, including OXA-23, OXA-24/40, and OXA-58, circulate in <
 em>
 Acinetobacter baumannii<
 /em>
 , while the OXA-48 CHDL is predominant in <
 em>
 Enterobacteriaceae<
 /em>
 . Extensive structural studies of A. baumannii enzymes have provided important information regarding their interactions with carbapenems and significantly contributed to the understanding of the mechanism of their carbapenemase activity. However, the interactions between carbapenems and OXA-48 have not yet been elucidated. We determined the X-ray crystal structures of the acyl-enzyme complexes of OXA-48 with four carbapenems, imipenem, meropenem, ertapenem, and doripenem, and compared them with those of known carbapenem complexes of <
 em>
 A. baumannii<
 /em>
  CHDLs. In the <
 em>
 A. baumannii<
 /em>
  enzymes, acylation by carbapenems triggers significant displacement of one of two conserved hydrophobic surface residues, resulting in the formation of a channel for entry of the deacylating water into the active site. We show that such a channel preexists in apo?OXA-48 and that only minor displacement of the conserved hydrophobic surface residues occurs upon the formation of OXA-48 acyl-enzyme intermediates. We also demonstrate that the extensive hydrophobic interactions that occur between a conserved hydrophobic bridge of the <
 em>
 A. baumannii<
 /em>
  CHDLs and the carbapenem tails are lost in OXA-48 in the absence of an equivalent bridge structure. In conclusion, these data highlight significant differences between the interactions of carbapenems with OXA-48 and those with <
 em>
 A. baumannii<
 /em>
  enzymes and provide important insights into the mechanism of carbapenemase activity of the major <
 em>
 Enterobacteriaceae<
 /em>
  CHDL, OXA-48.
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