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    • 2. 发明申请
    • PEPTIDE ANTAGONISTS OF THE CALCITONIN CGRP FAMILY OF PEPTIDE HORMONES AND THEIR USE
    • 肽激素CGRP家族肽肽拮抗剂及其使用
    • US20140329752A1
    • 2014-11-06
    • US13821936
    • 2013-01-25
    • Christopher J. Soares
    • Christopher J. Soares
    • C07K14/575
    • C07K14/57527A61K38/00A61K38/225A61K38/23C07K14/585
    • 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 oc-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.
    • 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。