New angiogenesis inhibitors based on soluble cd44 receptor...

A - Human Necessities – 61 – K

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Details

A61K 38/00 (2006.01) A61K 38/17 (2006.01) C07K 14/705 (2006.01) G01N 33/566 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2458565

CD44, the receptor for hyaluronic acid, has complex functions in cellular physiology, cell migration and tumour metastasis. The inventors have previously found that human CD44 receptor overexpression in mouse fibrosarcoma cells inhibits subcutaneous tumour growth in mice [Kogerman et al., Oncogene 1997; 15:1407-16; Kogerman et al., Clin Exp Metastasis 1998; 16:83-93]. Here it is demonstrated that a tumour growth inhibitory effect of CD44 is caused by block of angiogenesis. Furthermore, the inventors have found that soluble recombinant CD44 hyaluronic acid binding domain (CD44HABD) inhibits angiogenesis in vivo in cLick and mouse and thereby inhibits human tumour growth of various origins. The anti-angiogenic effect of CD44-HABD is independent of hyaluronic acid (HA) binding, since non-HA-binding mutants of CD44HABD still maintain anti-angiogenic properties. The invention discloses soluble CD44 recombinant proteins as a novel class of angiogenesis inhibitors based on targeting of vascular cell surface receptor. A method of block of angiogenesis and treatment of human tumours using recombinant CD44 proteins as well as their analogues is disclosed. As a further embodiment of the invention, methods for screening for new drug targets using CD44 recombinant proteins and their analogues is presented.

CD44, récepteur d'acide hyaluronique, a des fonctions complexes en termes de physiologie cellulaire, de migration cellulaire et de métastase. Les inventeurs ont précédemment trouvé que la surexpression du récepteur CD44 humain dans les cellules de fibrosarcome de la souris inhibite la croissance tumorale sous-cutanée chez les souris [Kogerman et al., Oncogene 1997; 15:1407-16; Kogerman et al., Clin Exp Metastasis 1998; 16:83-93]. La présente invention démontre que CD44 a un effet inhibant la croissance tumorale, qui est dû au blocage de l'angiogénèse. En outre, les inventeurs ont trouvé que le domaine de liaison de l'acide hyaluronique du CD44 (CD44HABD) recombinant soluble inhibite l'angiogénèse in vivo chez le poussin et la souris et donc inhibe la croissance tumorale humaine d'origines diverses. L'effet anti-angiogénique du CD44-HABD est indépendant de la liaison de l'acide hyaluronique (HA). En effet, les mutants du CD44HABD n'assurant pas la liaison à HA, ils conservent encore des propriétés anti-angiogéniques. L'invention concerne des protéines recombinantes CD44 solubles comme nouvelle classe d'inhibiteurs d'angiogénèse basée sur le ciblage du récepteur de surface cellulaire vasculaire. L'invention concerne également un procédé de blocage de l'angiogénèse et de traitement de tumeurs humaines à l'aide de protéines CD44 recombinantes et de leurs analogues. L'invention concerne enfin, comme autre mode de réalisation, des procédés de criblage pour de nouvelles cibles de médicaments à l'aide de protéines recombinantes CD44 et de leurs analogues.

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