C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 17/06 (2006.01) A61K 38/00 (2006.01) A61K 38/17 (2006.01) A61K 47/48 (2006.01) C07C 323/58 (2006.01) C07D 213/70 (2006.01) C07D 213/71 (2006.01) C07H 21/00 (2006.01) C07K 5/037 (2006.01) C07K 5/065 (2006.01) C07K 5/078 (2006.01) C07K 5/087 (2006.01) C07K 5/097 (2006.01) C12N 9/08 (2006.01)
Patent
CA 2211442
Fatty acid derivatives of sulfhydryl-containing compounds (for example, sulfhydryl-containing peptides or proteins) comprising fatty acid-conjugated products with a disulfide linkage are employed for delivery of the compounds to mammalian cells. This modification markedly increases the absorption of the compounds by mammalian cells relative to the rate of absorption of the unconjugated compounds, as well as prolonging blood and tissue retention of the compounds. Moreover, the disulfide linkage in the conjugate is quite labile in the cells and thus facilitates intracellular release of the intact compounds from the fatty acid moieties.
On utilise des dérivés d'acide gras de composés contenant du sulfhydryle (par exemple, des peptides ou des protéines contenant du sulfhydryle), notamment des produits d'acide gras conjugués avec une liaison de bisulfure, pour administrer lesdits composés à des cellules de mammifères. Cette modification permet d'augmenter consdérablement l'absorption des composés par les cellules de mammifères en ce qui concerne le taux d'absorption des composés non conjugués, de même qu'elle prolonge la rétention des composés dans le sang et les tissus. En outre, la liaison de bisulfure dans le conjugué est assez labile dans les cellules, ce qui facilite la libération intracellulaires des composés intacts par les fractions d'acide gras.
Ekrami Hossein
Shen Wei-Chiang
Mbm & Co.
The University Of Southern California
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