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Hydrophobic modified peptides and their use for specific targeting of the liver
专利权人:
Ruprecht-Karls-Universität Heidelberg
发明人:
MIER, Walter,URBAN, Stephan,MEHRLE, Stefan,HABERKORN, Uwe
申请号:
ES12704263
公开号:
ES2663368T3
申请日:
2012.02.10
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
Hydrophobic modified peptide of formula [X-P-Y-Ro] Ap in which P is a peptide having the amino acid sequence NPLGFXaaP, in which Xaa is an arbitrary amino acid, preferably F or L; X is an amino acid sequence comprising NX1SX2X3, which has a length of m>; = 5, 6, 7 or 8 amino acids, in which X1, X2 and X3 is an arbitrary amino acid and in which one or more of the amino acids carries one or more hydrophobic modifications selected from acylation, preferably with carboxylic acids, fatty acids, C8 to C22 fatty acids, amino acids with lipophilic side chains, and addition of hydrophobic fractions selected from cholesterol, cholesterol derivatives, phospholipids, glycolipids, glycerol esters , steroids, ceramides, isoprene derivatives, adamantane, farnesol, aliphatic groups, polyaromatic compounds; Y is an amino acid sequence having a length of n amino acids, in which n is 0 or at least 1, in which n is preferably 0 to 78; m + n>; = 11 R is a C-terminal modification of said hydrophobic modified peptide, which is preferably a fraction that protects against the degradation selected from amide, D-amino acid, modified amino acid, cyclic amino acid, albumin, natural and synthetic polymer, as PEG, glycine, or is 0 or at least 1, A is an anchor group, preferably selected from ester, ether, disulfide, amide, thiol, thioester; p is 0 or at least 1, in which one or more drugs (s) are coupled to one or more amino acid (s) of X.Péptido modificado hidrófobo de fórmula [X - P - Y - Ro] Ap en la que P es un péptido que tiene la secuencia de aminoácidos NPLGFXaaP, en la que Xaa es un aminoácido arbitrario, preferentemente F o L; X es una secuencia de aminoácidos que comprende NX1SX2X3, que tiene una longitud de m>;= 5, 6, 7 u 8 aminoácidos, en la que X1, X2 y X3 es un aminoácido arbitrario y en la que uno o más de los aminoácidos lleva una o más modificaciones hidrófobas seleccionadas entre acilación, preferentemente con ácidos carboxílicos, ácidos grasos, ácidos grasos de C8 a C22,
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