Methods for designing inhibitors of serine/threonine-kinases and
tyrosine kinases
    1.
    发明授权
    Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases 失效
    设计丝氨酸/苏氨酸激酶和酪氨酸激酶抑制剂的方法

    公开(公告)号:US6162613A

    公开(公告)日:2000-12-19

    申请号:US25580

    申请日:1998-02-18

    CPC分类号: C12N9/1205 G01N2333/9121

    摘要: The invention relates to methods for designing inhibitors of serine/threonine kinases and tyrosine kinases, particularly MAP kinases, through the use of ATP-binding site mutants of those kinases. The methods of this invention take advantage of the fact that the mutant kinases are capable of binding inhibitory compounds of other kinases with greater affinity than the corresponding wild-type kinase. The invention further relates to the mutant kinases themselves and crystallizable co-complexes of the mutant kinase and the inhibitory compound.

    摘要翻译: 本发明涉及通过使用这些激酶的ATP结合位点突变体设计丝氨酸/苏氨酸激酶和酪氨酸激酶抑制剂,特别是MAP激酶的方法。 本发明的方法利用突变体激酶能够以比相应的野生型激酶更大的亲和力结合其它激酶的抑制性化合物的事实。 本发明还涉及突变型激酶本身和突变型激酶与抑制性化合物的可结晶共配合物。

    Methods for designing inhibitors of serine/threonine kinases and tyrosine kinases
    2.
    发明授权
    Methods for designing inhibitors of serine/threonine kinases and tyrosine kinases 失效
    设计丝氨酸/苏氨酸激酶和酪氨酸激酶抑制剂的方法

    公开(公告)号:US06849716B1

    公开(公告)日:2005-02-01

    申请号:US09642749

    申请日:2000-08-18

    CPC分类号: C12N9/1205 G01N2333/9121

    摘要: The invention relates to methods for designing inhibitors of serine/threonine kinases and tyrosine kinases, particularly MAP kinases, through the use of ATP-binding site mutants of those kinases. The methods of this invention take advantage of the fact that the mutant kinases are capable of binding inhibitory compounds of other kinases with greater affinity than the corresponding wild-type kinase. The invention further relates to the mutant kinases themselves and crystallizable co-complexes of the mutant kinase and the inhibitory compound.

    摘要翻译: 本发明涉及通过使用这些激酶的ATP结合位点突变体设计丝氨酸/苏氨酸激酶和酪氨酸激酶抑制剂,特别是MAP激酶的方法。 本发明的方法利用突变型激酶能够以比相应的野生型激酶更大的亲和力结合其它激酶的抑制性化合物的事实。 本发明还涉及突变型激酶本身和突变型激酶与抑制性化合物的可结晶共配合物。