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Methods for improving the antagonistic/agonistic properties of peptidic antagonists/agonists of the corticotropin-releasing factor receptor (crfr)

机译:改善促肾上腺皮质激素释放因子受体(crfr)的肽类拮抗剂/激动剂的拮抗/激动特性的方法

摘要

The present invention relates to a method for improving the antagonistic/agonistic properties of peptidic antagonists/agonists of the corticotropin-releasing factor receptor (CRFR). Further, the present invention relates to an antagonist of the ligand of the corticotropin-releasing factor receptor (CRFR) comprising or alternatively consisting of the amino acid sequence of astressin wherein at least Ala at position 11 is replaced by another amino acid. Further, the present invention relates to an antibody directed against the agonist or antagonist of the present invention. Also described is an anti-idiotypic antibody which is directed against the antibody(ies) of the invention. The present invention also relates to a pharmaceutical or diagnostic composition comprising the antagonist, the agonist, the antibody(ies) and/or the anti-idiotypic antibody of the invention. Furthermore, the present invention relates to a kit comprising the agonist, the antagonist, the antibody(ies) and/or the anti-idiotypic antibody of the present invention. Also described is the use of the agonist, the antagonists, the antibody(ies) and/or the anti-idiotypic antibody of the invention for the preparation of a pharmaceutical composition for the treatment, diagnosis and/or prevention of corticotropin-releasing factor receptor-associated diseases. The present invention also relates to a method of refining the agonist and/or the antagonists of the present invention by means of peptidomimetics and synthesizing the refined compound. Furthermore, the present invention relates to a method of formulating the agonist/antagonist of the invention into a pharmaceutical composition.
机译:本发明涉及改善促肾上腺皮质激素释放因子受体(CRFR)的肽拮抗剂/激动剂的拮抗/激动特性的方法。此外,本发明涉及促肾上腺皮质激素释放因子受体(CRFR)的配体的拮抗剂,该拮抗剂包括或其中由应激素的氨基酸序列组成,其中至少11位的Ala被另一种氨基酸替代。此外,本发明涉及针对本发明的激动剂或拮抗剂的抗体。还描述了针对本发明的抗体的抗独特型抗体。本发明还涉及药物或诊断组合物,其包含本发明的拮抗剂,激动剂,一种或多种抗体和/或抗独特型抗体。此外,本发明涉及包含本发明的激动剂,拮抗剂,一种或多种抗体和/或抗独特型抗体的试剂盒。还描述了本发明的激动剂,拮抗剂,一种或多种抗体和/或抗独特型抗体在制备用于治疗,诊断和/或预防促肾上腺皮质激素释放因子受体的药物组合物中的用途。 -相关疾病。本发明还涉及通过拟肽模拟和合成精制化合物来精制本发明的激动剂和/或拮抗剂的方法。此外,本发明涉及将本发明的激动剂/拮抗剂配制为药物组合物的方法。

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