4AT3

CRYSTAL STRUCTURE OF TRKB KINASE DOMAIN IN COMPLEX WITH CPD5N

4AT3 の概要

• エントリーDOI: 10.2210/pdb4at3/pdb
• 関連するPDBエントリー: 1HCF 1WWB 4ASZ 4AT4 4AT5 4F0I
• 分子名称: BDNF/NT-3 GROWTH FACTORS RECEPTOR, (5Z)-5-(carbamoylimino)-3-[(5R)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ylsulfanyl]-2,5-dihydroisothiazole-4-carboxamide (3 entities in total)
• 機能のキーワード: transferase
• 由来する生物種: HOMO SAPIENS (HUMAN)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 34714.17

構造登録者

Bertrand, T.,Kothe, M.,Liu, J.,Dupuy, A.,Rak, A.,Berne, P.F.,Davis, S.,Gladysheva, T.,Valtre, C.,Crenne, J.Y.,Mathieu, M. (登録日: 2012-05-03, 公開日: 2012-08-22, 最終更新日: 2023-12-20)

主引用文献

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

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: 22902478
DOI: 10.1016/J.JMB.2012.08.002

実験手法

X-RAY DIFFRACTION (1.77 Å)