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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...

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Detalles Bibliográficos
Autores principales: 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
Formato: Texto
Lenguaje:English
Publicado: International Union of Crystallography 2010
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.
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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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