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Glucagon superfamily peptides with activity in relation to G-protein-coupled receptors
专利权人:
ИНДИАНА ЮНИВЕРСИТИ РИСЕРЧ ЭНД ТЕКНОЛОДЖИ КОРПОРЕЙШН (US);МАРКАДИА БАЙОТЕК, ИНК. (US)
发明人:
ДИМАРЧИ Ричард Д. (US),ЧЖАН Ляньшань (US)
申请号:
RU2012153753/04
公开号:
RU2012153753A
申请日:
2011.05.10
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. A compound containing a Q-L-Y structure, where Q is a glucagon superfamily peptide; Y is a GPCR ligand that activates a G-protein coupled receptor with an EC of about 1 μM or less and has a molecular weight of up to about 1000 daltons; and L represents a linker group or bond. 2. The compound according to claim 1, where Q has at least 0.1% of the activity of the native GLP-1 relative to the GLP-1 receptor, Q has at least 0.1% of the activity of the native glucagon relative to the glucagon receptor, or Q has at least 0.1% of the activity of the native GIP relative to the GIP receptor, or a combination thereof. 3. The compound of claim 1, wherein Q has an EC relative to GLP-1 receptor within a 10-fold ECY relative to a G protein coupled receptor, Q has an EC relative to a glucagon receptor within a 10-fold ECY relative to a G protein coupler or Q coupled receptor has an EC relative to the GIP receptor within the 10-fold ECY relative to the receptor conjugated to the G-protein, or a combination thereof. The compound of claim 1, wherein Y is a GPCR ligand that acts on a G protein conjugated receptor selected from the group consisting of GPR30, GPR40, GPR119 and GPR120.5. The compound of claim 1, wherein Y is a GPCR ligand selected from the group consisting of steroids and their derivatives, free fatty acids and their derivatives, amides of free fatty acids and their derivatives, phospholipids and their derivatives, grifolic acid and its derivatives, diacetylfluroglucin and its derivatives, retinoic acid and its derivatives, 4-phenoxymethylpiperidine and its derivatives and thiazolidinedione derivatives. 6. The compound of claim 5, where1. Соединение, содержащее структуру Q-L-Y,где Q представляет собой пептид глюкагонового суперсемейства;Y представляет собой GPCR лиганд, который активирует рецептор, сопряженный с G-белком, с ЕСприблизительно 1 мкМ или менее и имеет молекулярную массу вплоть до приблизительно 1000 дальтон; иL представляет собой линкерную группу или связ
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