4AT5
CRYSTAL STRUCTURE OF TRKB KINASE DOMAIN IN COMPLEX WITH GW2580
Summary for 4AT5
| Entry DOI | 10.2210/pdb4at5/pdb |
| Related | 1HCF 1WWB 4ASZ 4AT3 4AT4 4F0I |
| Descriptor | BDNF/NT-3 GROWTH FACTORS RECEPTOR, 5-{3-methoxy-4-[(4-methoxybenzyl)oxy]benzyl}pyrimidine-2,4-diamine, GLYCEROL, ... (4 entities in total) |
| Functional Keywords | transferase |
| Biological source | HOMO SAPIENS (HUMAN) |
| Total number of polymer chains | 1 |
| Total formula weight | 34810.20 |
| Authors | Bertrand, T.,Kothe, M.,Liu, J.,Dupuy, A.,Rak, A.,Berne, P.F.,Davis, S.,Gladysheva, T.,Valtre, C.,Crenne, J.Y.,Mathieu, M. (deposition date: 2012-05-03, release date: 2012-08-22, Last modification date: 2023-12-20) |
| Primary citation | Bertrand, T.,Kothe, M.,Liu, J.,Dupuy, A.,Rak, A.,Berne, P.F.,Davis, S.,Gladysheva, T.,Valtre, C.,Crenne, J.Y.,Mathieu, M. The Crystal Structures of Trka and Trkb Suggest Key Regions for Achieving Selective Inhibition. J.Mol.Biol., 423:439-, 2012 Cited by PubMed Abstract: The Trk family of neurotrophin receptors, which includes the three highly homologous proteins TrkA, TrkB and TrkC, is strongly associated with central and peripheral nervous system processes. Trk proteins are also of interest in oncology, since Trk activation has been observed in several cancer types. While Trk kinases are attractive oncology targets, selectivity might be more of an issue than for other kinases due to potential CNS side effects if several Trk kinases are simultaneously targeted. In order to address this issue, we present here the first structures of human TrkA and TrkB kinase domains and three complexes between TrkB and Trk inhibitors. These structures reveal different conformations of the kinase domain and suggest new regions of selectivity among the Trk family. PubMed: 22902478DOI: 10.1016/J.JMB.2012.08.002 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.71 Å) |
Structure validation
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