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PEPTIDE ANTAGONISTS OF VASOPRESSIN RECEPTOR 2
专利权人:
ЮНИВЕРСИТИ ОФ РЕГЕНСБУРГ (DE);САНТР НАСЬОНАЛЬ ДЕ ЛЯ РЕШЕРШ СЬЯНТИФИК (FR);КОММИССАРИАТ А Л'ЭНЕРЖИ АТОМИК Э О ЭНЕРЖИ АЛЬТЕРНАТИВ (FR);КОММИССАРИАТ А ЛЭНЕРЖИ АТОМИК Э О ЭНЕРЖИ АЛЬТЕРНАТИВ (FR);ЭНСТИТЮ НАСЬОНАЛЬ ДЕ ЛЯ САНТЕ Э ДЕ ЛЯ РЕШЕРШ МЕДИКАЛЬ (ЭНСЭРМ) (FR)
发明人:
ЖИЛЛЬ Николя (FR),СЕРВАН Дени (FR),КИНТОН Лоик (BE),РАЙНФРАНК Хелен (DE),ВИТЦГАЛЛЬ Ральф (DE),МУЙЛАК Бернар (FR),МЕНДР Кристиан (FR)
申请号:
RU2015114320
公开号:
RU2015114320A
申请日:
2013.09.17
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
1. An isolated protein having vasopressin receptor 2 (V2R) antagonistic activity, comprising an amino acid sequence that is at least 50% identical to residues 1-57 of SEQ ID NO: 1, and which contains: (i) an XXXXX motive at positions 15-18 SEQ ID NO: 1, where X is asparagine (N), X is glycine (G), X and X are hydrophobic amino acids, or X is methionine (M), X and X are phenylalanine (F), and X is isoleucine (I), and (ii) one to three disulfide bonds between two cysteine residues. 2. The protein of claim 1, wherein said protein contains a sequence selected from the group consisting of: amino acid sequences of SEQ ID NO: 1-5, a variant of any of SEQ ID NO: 1-3, containing an N-terminal deletion of one to four amino acid residues and / or a C-terminal deletion of one or two amino acid residues, and a variant of SEQ ID NO: 5 or 6, comprising an N-terminal deletion of one to thirty amino acid residues and / or a C-terminal deletion of one or two amino acid residues; or consists of the indicated sequence. 3. The use of the isolated protein of claim 1 in the treatment of diseases including the V2R pathway. 4. The use according to claim 3, wherein said diseases are selected from the group consisting of pathological conditions characterized by normovolemic or hypervolemic hyponatremia, nephrogenic syndrome of inadequate inhibition of urine output by the kidneys, congenital diabetes insipidus renal disease, polycystic kidney disease, malignant tumors, thrombosis and disease . The use of the isolated protein according to claim 1 for the diagnosis of in vivo pathology, including increasing or decreasing the level of expression of V2R. 6. The use of isolated protein1. Выделенный белок, обладающий антагонистической активностью в отношении рецептора 2 вазопрессина (V2R), содержащий аминокислотную последовательность, которая является по меньшей мере на 50% идентичной остаткам 1-57 SEQ ID NO: 1, и которая содержит:(i) мотив ХХХХв положениях 15-18 SEQ ID NO: 1, где Xпредставляет собо
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