5OW8
Indole-2 carboxamides as selective secreted phospholipase A2 type X (sPLA2-X) inhibitors
Summary for 5OW8
| Entry DOI | 10.2210/pdb5ow8/pdb |
| Descriptor | Group 10 secretory phospholipase A2, CALCIUM ION, DIMETHYL SULFOXIDE, ... (7 entities in total) |
| Functional Keywords | inhibitor, secreted, phospholipase, lipid binding protein |
| Biological source | Homo sapiens (Human) |
| Total number of polymer chains | 2 |
| Total formula weight | 29275.24 |
| Authors | Sandmark, J.S.,Roth, R.G.,Knerr, L.,Bodin, C.,Pettersen, D. (deposition date: 2017-08-31, release date: 2018-08-01, Last modification date: 2024-10-16) |
| Primary citation | Knerr, L.,Giordanetto, F.,Nordberg, P.,Pettersen, D.,Selmi, N.,Beisel, H.G.,de la Motte, H.,Olsson, T.,Perkins, T.D.J.,Herslof, M.,Mansson, A.,Dahlstrom, M.,Starke, I.,Broddefalk, J.,Saarinen, G.,Klingegard, F.,Hurt-Camejo, E.,Rosengren, B.,Brengdahl, J.,Jansen, F.,Rohman, M.,Sandmark, J.,Hallberg, K.,Akerud, T.,Roth, R.G.,Ahlqvist, M. Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2Type X (sPLA2-X) Inhibitors. Acs Med.Chem.Lett., 9:594-599, 2018 Cited by PubMed Abstract: In order to assess the potential of sPLA-X as a therapeutic target for atherosclerosis, novel sPLA inhibitors with improved type X selectivity are required. To achieve the objective of identifying such compounds, we embarked on a lead generation effort that resulted in the identification of a novel series of indole-2-carboxamides as selective sPLA2-X inhibitors with excellent potential for further optimization. PubMed: 30034585DOI: 10.1021/acsmedchemlett.7b00505 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.9 Å) |
Structure validation
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