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P38 and JNK MAPK inhibitors for treating and preventing degenerative diseases of the nervous system

机译:P38和JNK MAPK抑制剂用于治疗和预防神经系统退行性疾病

摘要

The present invention provides novel p38 and JNK mitogen activated protein (MAP) kinase allosteric inhibitors useful for the treatment and / or prevention of degenerative diseases of the nervous system. Accordingly, the present invention provides compounds used in methods for the treatment and / or prevention of the diseases as well as compounds used in general therapy. The compound comprises MAP kinase 14 (Uniprot accession number Q16539 or SEQ ID NO: 1) and / or MAP kinase 11 (Uniprot accession number Q15759 or SEQ ID NO: 2), that is, amino acids of MAPK14 (p38α) and MAPK11 (p38β), respectively. It binds to a region composed of amino acids at positions 170 to 199 of SEQ ID NOs: 1 and 2, which are sequences. Specific regions composed of amino acids 170-199 are disclosed as SEQ ID NO: 4 for MAP kinase 14 and SEQ ID NO: 5 for MAP kinase 11, which are considered novel inhibitory binding sites.
机译:本发明提供了用于治疗和/或预防神经系统退行性疾病的新颖的p38和JNK丝裂原活化蛋白(MAP)激酶变构抑制剂。因此,本发明提供了用于治疗和/或预防疾病的方法中的化合物以及用于一般疗法的化合物。该化合物包含MAP激酶14(Uniprot登录号Q16539或SEQ ID NO:1)和/或MAP激酶11(Uniprot登录号Q15759或SEQ ID NO:2),即MAPK14(p38α)和MAPK11( p38β)。它结合由SEQ ID NO:1和2的序列的170至199位氨基酸组成的区域。由氨基酸170-199组成的特定区域公开为MAP激酶14的SEQ ID NO:4和MAP激酶11的SEQ ID NO:5,它们被认为是新的抑制性结合位点。

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