1r35
From Proteopedia
(New page: 200px<br /><applet load="1r35" size="450" color="white" frame="true" align="right" spinBox="true" caption="1r35, resolution 2.30Å" /> '''MURINE INDUCIBLE NIT...) |
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| - | [[Image:1r35.jpg|left|200px]]<br /><applet load="1r35" size=" | + | [[Image:1r35.jpg|left|200px]]<br /><applet load="1r35" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1r35, resolution 2.30Å" /> | caption="1r35, resolution 2.30Å" /> | ||
'''MURINE INDUCIBLE NITRIC OXIDE SYNTHASE OXYGENASE DIMER, TETRAHYDROBIOPTERIN AND 4R-FLUORO-N6-ETHANIMIDOYL-L-LYSINE'''<br /> | '''MURINE INDUCIBLE NITRIC OXIDE SYNTHASE OXYGENASE DIMER, TETRAHYDROBIOPTERIN AND 4R-FLUORO-N6-ETHANIMIDOYL-L-LYSINE'''<br /> | ||
==Overview== | ==Overview== | ||
| - | In the literature, the introduction of fluorine into bioactive molecules | + | In the literature, the introduction of fluorine into bioactive molecules has been known to enhance the biological activity relative to the parent molecule. Described in this article is the synthesis of 4R-fluoro-L-NIL (12) and 4,4-difluoro-L-NIL (23) as part of our iNOS program. Both 12 and 23 were found to be selective iNOS inhibitors as shown in Table 2 below. Secondarily, methodology to synthesize orthogonally protected 4-fluoro-L-lysine and 4,4-difluoro-L-lysine has been developed. |
==About this Structure== | ==About this Structure== | ||
| - | 1R35 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with SO4, HEM, H4B and I58 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Nitric-oxide_synthase Nitric-oxide synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.13.39 1.14.13.39] Full crystallographic information is available from [http:// | + | 1R35 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with <scene name='pdbligand=SO4:'>SO4</scene>, <scene name='pdbligand=HEM:'>HEM</scene>, <scene name='pdbligand=H4B:'>H4B</scene> and <scene name='pdbligand=I58:'>I58</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Nitric-oxide_synthase Nitric-oxide synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.13.39 1.14.13.39] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1R35 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Nitric-oxide synthase]] | [[Category: Nitric-oxide synthase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Shieh, H | + | [[Category: Shieh, H S.]] |
| - | [[Category: Stallings, W | + | [[Category: Stallings, W C.]] |
| - | [[Category: Stevens, A | + | [[Category: Stevens, A M.]] |
[[Category: H4B]] | [[Category: H4B]] | ||
[[Category: HEM]] | [[Category: HEM]] | ||
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[[Category: tetrahydrobiopterin]] | [[Category: tetrahydrobiopterin]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:46:33 2008'' |
Revision as of 12:46, 21 February 2008
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MURINE INDUCIBLE NITRIC OXIDE SYNTHASE OXYGENASE DIMER, TETRAHYDROBIOPTERIN AND 4R-FLUORO-N6-ETHANIMIDOYL-L-LYSINE
Overview
In the literature, the introduction of fluorine into bioactive molecules has been known to enhance the biological activity relative to the parent molecule. Described in this article is the synthesis of 4R-fluoro-L-NIL (12) and 4,4-difluoro-L-NIL (23) as part of our iNOS program. Both 12 and 23 were found to be selective iNOS inhibitors as shown in Table 2 below. Secondarily, methodology to synthesize orthogonally protected 4-fluoro-L-lysine and 4,4-difluoro-L-lysine has been developed.
About this Structure
1R35 is a Single protein structure of sequence from Mus musculus with , , and as ligands. Active as Nitric-oxide synthase, with EC number 1.14.13.39 Full crystallographic information is available from OCA.
Reference
4-Fluorinated L-lysine analogs as selective i-NOS inhibitors: methodology for introducing fluorine into the lysine side chain., Hallinan EA, Kramer SW, Houdek SC, Moore WM, Jerome GM, Spangler DP, Stevens AM, Shieh HS, Manning PT, Pitzele BS, Org Biomol Chem. 2003 Oct 21;1(20):3527-34. PMID:14599013
Page seeded by OCA on Thu Feb 21 14:46:33 2008
Categories: Mus musculus | Nitric-oxide synthase | Single protein | Shieh, H S. | Stallings, W C. | Stevens, A M. | H4B | HEM | I58 | SO4 | Dimer | H4b | Heme | Intermediate | Nitric oxide monooxygenase | Pterin | Tetrahydrobiopterin
