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High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors
Human haematopoietic prostaglandin D synthase (H-PGDS; EC 5.3.99.2) produces prostaglandin D(2), an allergic and inflammatory mediator, in mast cells and Th2 cells. H-PGDS has been crystallized with novel inhibitors with half-maximal inhibitory concentrations (IC(50)) in the low nanomolar range by t...
Autores principales: | , , , , , , , , , , , , |
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Formato: | Texto |
Lenguaje: | English |
Publicado: |
International Union of Crystallography
2010
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2898477/ https://www.ncbi.nlm.nih.gov/pubmed/20606289 http://dx.doi.org/10.1107/S1744309110020828 |
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author | Takahashi, Sachiko Tsurumura, Toshiharu Aritake, Kosuke Furubayashi, Naoki Sato, Masaru Yamanaka, Mari Hirota, Erika Sano, Satoshi Kobayashi, Tomoyuki Tanaka, Tetsuo Inaka, Koji Tanaka, Hiroaki Urade, Yoshihiro |
author_facet | Takahashi, Sachiko Tsurumura, Toshiharu Aritake, Kosuke Furubayashi, Naoki Sato, Masaru Yamanaka, Mari Hirota, Erika Sano, Satoshi Kobayashi, Tomoyuki Tanaka, Tetsuo Inaka, Koji Tanaka, Hiroaki Urade, Yoshihiro |
author_sort | Takahashi, Sachiko |
collection | PubMed |
description | Human haematopoietic prostaglandin D synthase (H-PGDS; EC 5.3.99.2) produces prostaglandin D(2), an allergic and inflammatory mediator, in mast cells and Th2 cells. H-PGDS has been crystallized with novel inhibitors with half-maximal inhibitory concentrations (IC(50)) in the low nanomolar range by the counter-diffusion method onboard the Russian Service Module on the International Space Station. The X-ray diffraction of a microgravity-grown crystal of H-PGDS complexed with an inhibitor with an IC(50) value of 50 nM extended to 1.1 Å resolution at 100 K using SPring-8 synchrotron radiation, which is one of the highest resolutions obtained to date for this protein. |
format | Text |
id | pubmed-2898477 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2010 |
publisher | International Union of Crystallography |
record_format | MEDLINE/PubMed |
spelling | pubmed-28984772010-07-13 High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors Takahashi, Sachiko Tsurumura, Toshiharu Aritake, Kosuke Furubayashi, Naoki Sato, Masaru Yamanaka, Mari Hirota, Erika Sano, Satoshi Kobayashi, Tomoyuki Tanaka, Tetsuo Inaka, Koji Tanaka, Hiroaki Urade, Yoshihiro Acta Crystallogr Sect F Struct Biol Cryst Commun Crystallization Communications Human haematopoietic prostaglandin D synthase (H-PGDS; EC 5.3.99.2) produces prostaglandin D(2), an allergic and inflammatory mediator, in mast cells and Th2 cells. H-PGDS has been crystallized with novel inhibitors with half-maximal inhibitory concentrations (IC(50)) in the low nanomolar range by the counter-diffusion method onboard the Russian Service Module on the International Space Station. The X-ray diffraction of a microgravity-grown crystal of H-PGDS complexed with an inhibitor with an IC(50) value of 50 nM extended to 1.1 Å resolution at 100 K using SPring-8 synchrotron radiation, which is one of the highest resolutions obtained to date for this protein. International Union of Crystallography 2010-06-24 /pmc/articles/PMC2898477/ /pubmed/20606289 http://dx.doi.org/10.1107/S1744309110020828 Text en © Takahashi et al. 2010 http://creativecommons.org/licenses/by/2.0/uk/ This is an open-access article distributed under the terms of the Creative Commons Attribution Licence, which permits unrestricted use, distribution, and reproduction in any medium, provided the original authors and source are cited. |
spellingShingle | Crystallization Communications Takahashi, Sachiko Tsurumura, Toshiharu Aritake, Kosuke Furubayashi, Naoki Sato, Masaru Yamanaka, Mari Hirota, Erika Sano, Satoshi Kobayashi, Tomoyuki Tanaka, Tetsuo Inaka, Koji Tanaka, Hiroaki Urade, Yoshihiro High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors |
title | High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors |
title_full | High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors |
title_fullStr | High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors |
title_full_unstemmed | High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors |
title_short | High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors |
title_sort | high-quality crystals of human haematopoietic prostaglandin d synthase with novel inhibitors |
topic | Crystallization Communications |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2898477/ https://www.ncbi.nlm.nih.gov/pubmed/20606289 http://dx.doi.org/10.1107/S1744309110020828 |
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