CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
发明人:
COURTY, JOSÉ,HOVANESSIAN, ARA,BRIAND, JEAN PAUL,GUICHARD, GILLES,HAMMA, YAMINA
申请号：
EP12185309.7
公开号：
EP2540737B1
申请日:
2007.04.27
申请国别(地区):
EP
年份:
2015
代理人:
摘要：
Use of a polyvalent synthetic ligand (I) to prepare a medicament to treat a disease involving a deregulation of cell proliferation and/or angiogenesis : Use of a polyvalent synthetic ligand (I) of formula [(X) n-Y 1-(Z) i-(Y 2)-(X) m] k-S 1 to prepare a medicament to treat a disease involving a deregulation of cell proliferation and/or angiogenesis. (I) has a support (S 1) on which at least three pseudopeptidic units are grafted, where the bond between Y 1 and Z represents a modified peptide bond, which is significantly more resistant to at least a protease as a standard peptide bond. X : amino acid Y 1, Y 2amino acid side chain having a basic side chain Z : proline (preferred) (optionally substituted OH, NH 2, 1-10C alkyl, 1-10C alkenyl, 1-10C alkynyl, 5-12C aryl, 5-14C aralkyl or 5-12C heteroaryl (optionally substituted by 1-6 groups e.g. halo, NO 2, OH, 1-4C alkyl, NH 2, CN, trihalomethyl, 1-4C acyloxy, 1-4C dialkylamino, guanidino or SH)), (un)natural N-alkyl amino acid, dialkyl amino acid, cyclic dialkyl amino acid or pipecolic acid or its derivative n, i : 0-1, preferably 1 m : 0-3 k : greater than or equal to 3, preferably 5-6 and S 1support. Provided that when Y 1 is arginine then Y 2 is lysine or vice versa. An independent claim is included for a screening process of inhibiting molecules that are involving cell proliferation and angiogenesis comprising placing cells expressing the nucleoline of surface with a molecule to be tested, and determining the ability of the molecule to be tested to be linked with RGG domain of the nucleoline. ACTIVITY : Angiogenesis inhibitor Cytostatic Antiinflammatory Respiratory-Gen. Immunosuppressive Antibacterial Cardiant Vulnerary Gastrointestinal-Gen. Dermatological Antiallergic. MECHANISM OF ACTION : None given.La présente invention concerne lutilisation dun composé synthétique multivalent comprenant un support sur lequel sont greffés au moins 3 motifs pseudopeptidiques, ledit composé étant de formule (I) :où chaque X repré
