作者: Morgan Huse , Ye-Guang Chen , Joan Massagué , John Kuriyan
DOI: 10.1016/S0092-8674(00)80555-3
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摘要: Activation of the type I TGFbeta receptor (TbetaR-I) requires phosphorylation a regulatory segment known as GS region, located upstream serine/threonine kinase domain in cytoplasmic portion receptor. The crystal structure fragment unphosphorylated TbetaR-I, containing both region and catalytic domain, has been determined complex with FK506-binding protein FKBP12. TbetaR-I adopts an inactive conformation that is maintained by region. FKBP12 binds to receptor, capping TbetaR-II sites further stabilizing TbetaR-I. Certain structural features at center are characteristic tyrosine kinases rather than Ser/Thr kinases.