6VGI

Crystal Structures of FLAP bound to MK-866

Summary for 6VGI

• Entry DOI: 10.2210/pdb6vgi/pdb
• Descriptor: 5-lipoxygenase-activating protein, 3-[3-(tert-butylsulfanyl)-1-[(4-chlorophenyl)methyl]-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid, SULFATE ION, ... (4 entities in total)
• Functional Keywords: 5-lipoxygenase activating protein, flap, mk-866, membrane protein
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 6
• Total formula weight: 119275.96

Authors

Ho, J.D.,Lee, M.R.,Rauch, C.T.,Aznavour, K.,Park, J.S.,Luz, J.G.,Antonysamy, S.,Condon, B.,Maletic, M.,Zhang, A.,Hickey, M.J.,Hughes, N.E.,Chandrasekhar, S.,Sloan, A.V.,Gooding, K.,Harvey, A.,Yu, X.P.,Kahl, S.D.,Norman, B.H. (deposition date: 2020-01-08, release date: 2020-12-02, Last modification date: 2023-10-11)

Primary citation

Ho, J.D.,Lee, M.R.,Rauch, C.T.,Aznavour, K.,Park, J.S.,Luz, J.G.,Antonysamy, S.,Condon, B.,Maletic, M.,Zhang, A.,Hickey, M.J.,Hughes, N.E.,Chandrasekhar, S.,Sloan, A.V.,Gooding, K.,Harvey, A.,Yu, X.P.,Kahl, S.D.,Norman, B.H.
Structure-based, multi-targeted drug discovery approach to eicosanoid inhibition: Dual inhibitors of mPGES-1 and 5-lipoxygenase activating protein (FLAP).
Biochim Biophys Acta Gen Subj, 1865:129800-129800, 2020

PubMed Abstract: Due to the importance of both prostaglandins (PGs) and leukotrienes (LTs) as pro-inflammatory mediators, and the potential for eicosanoid shunting in the presence of pathway target inhibitors, we have investigated an approach to inhibiting the formation of both PGs and LTs as part of a multi-targeted drug discovery effort.

PubMed: 33246032
DOI: 10.1016/j.bbagen.2020.129800

Experimental method

X-RAY DIFFRACTION (2.61 Å)