1R35

MURINE INDUCIBLE NITRIC OXIDE SYNTHASE OXYGENASE DIMER, TETRAHYDROBIOPTERIN AND 4R-FLUORO-N6-ETHANIMIDOYL-L-LYSINE

1R35 の概要

• エントリーDOI: 10.2210/pdb1r35/pdb
• 分子名称: Nitric oxide synthase, inducible, SULFATE ION, PROTOPORPHYRIN IX CONTAINING FE, ... (6 entities in total)
• 機能のキーワード: nitric oxide monooxygenase, heme, dimer, intermediate, pterin, h4b, tetrahydrobiopterin, oxidoreductase
• 由来する生物種: Mus musculus (house mouse)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 102463.90

構造登録者

Shieh, H.S.,Stevens, A.M.,Stallings, W.C. (登録日: 2003-09-30, 公開日: 2004-10-05, 最終更新日: 2023-08-23)

主引用文献

Hallinan, E.A.,Kramer, S.W.,Houdek, S.C.,Moore, W.M.,Jerome, G.M.,Spangler, D.P.,Stevens, A.M.,Shieh, H.S.,Manning, P.T.,Pitzele, B.S.
4-Fluorinated L-lysine analogs as selective i-NOS inhibitors: methodology for introducing fluorine into the lysine side chain.
Org.Biomol.Chem., 1:3527-3534, 2003

PubMed Abstract: 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.

PubMed: 14599013
DOI: 10.1039/b307563j

実験手法

X-RAY DIFFRACTION (2.3 Å)