Structure-based mechanism of cysteinyl leukotriene receptor inhibition by antiasthmatic drugs [electronic resource]

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Tác giả:

Ngôn ngữ: eng

Ký hiệu phân loại: 616.24 *Diseases of lungs

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: Article No. eaax2518 : , digital, PDF file.

Bộ sưu tập: Metadata

ID: 259952

 The G protein?coupled cysteinyl leukotriene receptor CysLT<
 sub>
 1<
 /sub>
 R mediates inflammatory processes and plays a major role in numerous disorders, including asthma, allergic rhinitis, cardiovascular disease, and cancer. Selective CysLT<
 sub>
 1<
 /sub>
 R antagonists are widely prescribed as antiasthmatic drugs
  however, these drugs demonstrate low effectiveness in some patients and exhibit a variety of side effects. To gain deeper understanding into the functional mechanisms of CysLTRs, we determined the crystal structures of CysLT<
 sub>
 1<
 /sub>
 R bound to two chemically distinct antagonists, zafirlukast and pranlukast. The structures reveal unique ligand-binding modes and signaling mechanisms, including lateral ligand access to the orthosteric pocket between transmembrane helices TM4 and TM5, an atypical pattern of microswitches, and a distinct four-residue?coordinated sodium site. These results provide important insights and structural templates for rational discovery of safer and more effective drugs.
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