5LZ5

Fragment-based inhibitors of Lipoprotein associated Phospholipase A2

Summary for 5LZ5

• Entry DOI: 10.2210/pdb5lz5/pdb
• Descriptor: Platelet-activating factor acetylhydrolase, CHLORIDE ION, 2-fluoranyl-5-[2-[(4~{S})-4-methyl-2-oxidanylidene-4-phenyl-pyrrolidin-1-yl]ethoxy]benzenecarbonitrile, ... (4 entities in total)
• Functional Keywords: lp-pla2 phospholipase, hydrolase, lipid metabolism, inhibitors, lp-pla2#4
• Biological source: Homo sapiens (Human)
• Cellular location: Secreted, extracellular space: Q13093
• Total number of polymer chains: 1
• Total formula weight: 44612.41

Authors

Woolford, A.J.A.,Day, P.J. (deposition date: 2016-09-29, release date: 2016-12-21)

• Primary citation: Woolford, A.J.,Day, P.J.,Beneton, V.,Berdini, V.,Coyle, J.E.,Dudit, Y.,Grondin, P.,Huet, P.,Lee, L.Y.,Manas, E.S.,McMenamin, R.L.,Murray, C.W.,Page, L.W.,Patel, V.K.,Potvain, F.,Rich, S.J.,Sang, Y.,Somers, D.O.,Trottet, L.,Wan, Z.,Zhang, X.; Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2).; J. Med. Chem., 59:10738-10749, 2016; PubMed: 27933945; DOI: 10.1021/acs.jmedchem.6b01427

Experimental method

X-RAY DIFFRACTION (2.05 Å)