2013 Fiscal Year Final Research Report
Product release mechanism of Lipocalin-type Prostaglandin D synthase
| Project/Area Number |
24790055
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Physical pharmacy
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| Research Institution | Kinki University |
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Principal Investigator |
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| Project Period (FY) |
2012-04-01 – 2014-03-31
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| Keywords | リポカリン型プロスタグランジンD合成酵素 / プロスタグランジンD2 / NMR / ITC |
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| Research Abstract |
Lipocalin-type Prostaglandin D synthase (L-PGDS) catalyzes the isomerization of prostaglandin H2 (PGH2) to produce prostaglandin D2 (PGD2), which acts as a potent endogenous somnogen in the brain. A number of studies of L-PGDS, as a drug target for sleep disorders, have been reported in attempts to understand its catalytic mechanism, and several substrate recognition models of L-PGDS have been proposed. However, details of the mechanism by which L-PDGS recognizes its substrates and products are obscure, since essential information, such as its binding affinity and stoichiometry, of the interactions between L-PGDS and its substrates and products remains unclear. Therefore, we carried out ITC and NMR experiments to characterize the binding properties. The results of the ITC and NMR measurements revealed that both the substrate and the product bind to L-PGDS in a stoichiometry of 2 to 1 and two binding sites, namely a high and a low affinity binding site, are present.
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Research Products
(11 results)
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[Journal Article] Drug delivery system for poorly water-soluble compounds using lipocalin-type prostaglandin D synthase2012
Author(s)
Fukuhara A., Nakajima H., Miyamoto Y., Inoue K., Kume S., Lee Y.H., Noda M., Uchiyama S., Shimamoto S., Nishimura S., Ohkubo T., Goto Y., Takeuchi T., and Inui T
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Journal Title
J. Control. Release
Volume: 159(1)
Pages: 143-150
Peer Reviewed
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