A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 38/00 (2006.01) A61K 38/04 (2006.01)
Patent
CA 2594927
The present invention provides homing conjugates containing an antimicrobial peptide and a tumor homing molecule, wherein the tumor homing molecule comprises a dimer of two endothelium-homing peptide monomers, wherein the conjugate homes to and is internalized by a tumor cell type or tissue comprising angiogenic endothelial cells and exhibits high toxicity thereto, wherein the high toxicity is due to disruption of mitochondrial membranes, and wherein the antimicrobial peptide has low mammalian cell toxicity when not linked to said tumor homing molecule. The present invention is based, in part, on the discovery that dimerization of endothelium-homing peptide monomer confers greatly increased cytotoxic activity on the conjugate. Based on this discovery, the invention further provides methods of inducing selective toxicity in vivo in an angiogenic endothelial tissue or cell type as well as methods of treating an individual having cancer by administering an effective amount of a homing conjugate of the invention also are provided.
L'invention concerne des conjugués chercheurs qui contiennent un peptide antimicrobien et une molécule chercheuse de tumeur, laquelle comprend un dimère de deux monomères de peptide chercheur d'endothélium. Le conjugué cherche un type ou tissu de cellule tumorale comprenant des cellules endothéliales angiogéniques, qui l'internalise, et manifeste vis-à-vis de lui une toxicité élevée due à la rupture des membranes mitochondriales. Le peptide antimicrobien manifeste une faible toxicité aux cellules mammaliennes lorsqu'il n'est pas lié à la molécule chercheuse. L'invention s'inspire en partie de la découverte selon laquelle la dimérisation de monomère de peptide chercheur d'endothélium confère au conjugué une activité cytotoxique accrue, moyennant quoi on décrit des procédés induisant une toxicité sélective in vivo dans un tissu ou type de cellule endothélial angiogénique, et des procédés de traitement du cancer par administration d'une quantité efficace de conjugué chercheur.
Bredesen Dale E.
Ellerby Lisa
Ellerby Michael
Buck Institute
Smart & Biggar
LandOfFree
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