PEPTIDE ANTAGONISTS OF THE CALCITONIN CGRP FAMILY OF PEPTIDE HORMONES AND THEIR USE

    公开(公告)号:US20170204155A1

    公开(公告)日:2017-07-20

    申请号:US15478053

    申请日:2017-04-03

    摘要: The embodiments provide a modified calcitonin gene-related peptide antagonist including an N-terminal fragment of modified calcitonin gene-related peptide or related protein family member where at least two residues of the N-terminal fragment are cysteine (Cys) and at least one amino acid comprises a non-threonine substitution of a threonine (Thr) residue; a central core where the central core comprises an a-helix; and a C-terminal fragment of modified calcitonin gene-related peptide or related protein family member comprising a C-terminal amide and where at least one amino acid of the C-terminal fragment is phenylalanine (Phe), proline (Pro), tyrosine (Tyr) or hydroxyproline (Hyp) or pharmaceutically acceptable salt thereof, as well as compositions, including pharmaceutical compositions, comprising a subject peptide. The embodiments further provide treatment methods, including methods of treating a migraine, the methods generally involving administering to an individual in need thereof an effective amount of a subject peptide or composition.

    PEPTIDE ANTAGONISTS OF THE CALCITONIN CGRP FAMILY OF PEPTIDE HORMONES AND THEIR USE
    6.
    发明申请
    PEPTIDE ANTAGONISTS OF THE CALCITONIN CGRP FAMILY OF PEPTIDE HORMONES AND THEIR USE 审中-公开
    肽激素CGRP家族肽肽拮抗剂及其使用

    公开(公告)号:US20160145315A1

    公开(公告)日:2016-05-26

    申请号:US14948032

    申请日:2015-11-20

    IPC分类号: C07K14/575

    摘要: The embodiments provide a modified calcitonin gene-related peptide antagonist including an N-terminal fragment of modified calcitonin gene-related peptide or related protein family member where at least two residues of the N-terminal fragment are cysteine (Cys) and at least one amino acid comprises a non-threonine substitution of a threonine (Thr) residue; a central core where the central core comprises an a-helix; and a C-terminal fragment of modified calcitonin gene-related peptide or related protein family member comprising a C-terminal amide and where at least one amino acid of the C-terminal fragment is phenylalanine (Phe), proline (Pro), tyrosine (Tyr) or hydroxyproline (Hyp) or pharmaceutically acceptable salt thereof, as well as compositions, including pharmaceutical compositions, comprising a subject peptide. The embodiments further provide treatment methods, including methods of treating a migraine, the methods generally involving administering to an individual in need thereof an effective amount of a subject peptide or composition.

    摘要翻译: 实施方案提供了修饰的降钙素基因相关肽拮抗剂,其包括修饰的降钙素基因相关肽或相关蛋白家族成员的N末端片段,其中N-末端片段的至少两个残基是半胱氨酸(Cys)和至少一个氨基 酸包括苏氨酸(Thr)残基的非苏氨酸取代; 中心芯,其中心芯包含α-螺旋; 和包含C-末端酰胺的修饰的降钙素基因相关肽或相关蛋白家族成员的C末端片段,其中C-末端片段的至少一个氨基酸是苯丙氨酸(Phe),脯氨酸(Pro),酪氨酸( Tyr)或羟脯氨酸(Hyp)或其药学上可接受的盐,以及包含受试肽的组合物,包括药物组合物。 实施方案进一步提供治疗方法,包括治疗偏头痛的方法,所述方法通常涉及向有需要的个体施用有效量的受试肽或组合物。