| Structural highlights
5ow8 is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Method: | X-ray diffraction, Resolution 1.9Å |
| Ligands: | , , , , |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
PA2GX_HUMAN PA2 catalyzes the calcium-dependent hydrolysis of the 2-acyl groups in 3-sn-phosphoglycerides. Has a powerful potency for releasing arachidonic acid from cell membrane phospholipids. Prefers phosphatidylethanolamine and phosphatidylcholine liposomes to those of phosphatidylserine.
Publication Abstract from PubMed
In order to assess the potential of sPLA2-X as a therapeutic target for atherosclerosis, novel sPLA2 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.
Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors.,Knerr L, Giordanetto F, Nordberg P, Pettersen D, Selmi N, Beisel HG, de la Motte H, Olsson T, Perkins TDJ, 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 RG, Ahlqvist M ACS Med Chem Lett. 2018 Jun 23;9(7):594-599. doi: 10.1021/acsmedchemlett.7b00505., eCollection 2018 Jul 12. PMID:30034585[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Knerr L, Giordanetto F, Nordberg P, Pettersen D, Selmi N, Beisel HG, de la Motte H, Olsson T, Perkins TDJ, 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 RG, Ahlqvist M. Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors. ACS Med Chem Lett. 2018 Jun 23;9(7):594-599. doi: 10.1021/acsmedchemlett.7b00505., eCollection 2018 Jul 12. PMID:30034585 doi:http://dx.doi.org/10.1021/acsmedchemlett.7b00505
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