Cancerforskningsfondet Af 1989

Boehringer Mannheim Gmbh

Cancerforskningsfonden Af 1989

Trt Innovations Aps

Cancerforskningsfonden Af 1989 (fonden Til Fremme Af Exsperimentel Cancerforskning)

Michael Ploug

Vincent Ellis

Ettore Appella

Charles Pyke

Eeva-Marjatta Salonen

Niels Behrendt

Keld Dano Slashed

Maria Teresa Masucci

Maria Vittoria Cubellis

Peter Kristensen

Ross W Stephens

Ann Louring Roldan

Antti Vaheri

Francesco Blasi

Hannele Tapiovaara

Ulrich Kohnert

Ulrich Weidle

Andreas Kjaer

Wolf-Dieter Schleuning

Arne Holm

Morten Persson

Ilse Bartke

Bernhard Konig

Ebbe Ro Slashednne

Keld Dan&oslash;

Claus Holst-Hansen

Ulrich Pessara

Leif Ro Lund

Ross Stephens

Ebbe R&oslash;nne

Jari Pollanen

Keld Danø

Wd Schleuning

Jari P&ouml;ll&auml;nen

Laszlo Patthy

Lisbeth Birk Mo Slashedller

Lisbeth Birk M&oslash;ller

Leif R&oslash;ge Lund

Søren Østergaard

L&aacute;szlo Patthy

There is provided a 177-Lu labelled peptide for site-specific targeting of the Urokinase Plasminogen Activator Receptor (uPAR) thereby enabling treatment of a cancer disease associated with high uPAR expression; e.g. treatment of colorectal cancer by administering to a patient an effective amount of the 177-Lu labelled peptide.

177-Lu labeled peptide for site-specific uPAR-targeting

A novel set of inhibitors of the binding interaction between human urokinase plasminogen activator (uPA) and its cell surface receptor (uPAR) has been developed. The inhibitors comprise of peptide fragments, monomeric or in multiple copies attached to a common scaffold, in which the amino acid sequence may include uncommon substituted amino acids to partially comprise of peptoid sequences. The present invention also relates to the use of such peptides in therapy, in particular for the treatment of cancer, having developed a modified non-human mammalian receptor to which the novel inhibitors are antagonistic.

Peptide antagonists of the human urokinase receptor and method for selecting them

Activation of plasminogen to plasmin is inhibited by preventing the binding of a receptor binding form of urokinase-type plasminogen activator to a urokinase-type plasminogen activator receptor in a mammal, thereby preventing the urokinase-type plasminogen activator from converting plasminogen into plasmin. DNA fragments which encode for soluble, active fragments of the urokinase-type plasminogen activator receptor are provided.

Urokinase-type plasminogen activator receptor

The invention relates to an antibody which inhibits the binding between u-PA and u-PAR to an extent of at least 90% in an assay as defined in the specification, or an active fragment or immunological equivalent of said antibody. Examples of such antibodies are deposited Jul. 7, 1994 at Deutsche Sammlung von Mikroorganismen und Zellkulturen (DSM) with accession numbers DSM ACC2178 and DSM ACC2179 under the terms and conditions of the Budapest Treaty. The invention furthermore relates to a method for detecting or quantifying u-PAR or a glycosylation variant of u-PAR in a sample by use of an antibody according to the invention. Furthermore, the invention relates to a method for the manufacture of a therapeutic agent for preventing or counteracting localized proteolytic activity using of an antibody of the invention as well as to use of an antibody according to the invention for the preparation of a diagnostic agent which is capable of targeting a diagnostic to a cell that contains a u-PAR on the surface.

Hydrophobic u-PAR binding site

Activation of plasminogen to plasma is inhibited by preventing the binding of a receptor binding form of urokinase-type plasminogen activator to a urokinase-type plasminogen activator receptor in a mammal, thereby preventing the urokinase-type plasminogen activator from converting plasminogen into plasmin. DNA fragments which encode for soluble, active fragments of the urokinase-type plasminogen activator are provided.

Vectors and methods for recombinant production of uPA-binding fragments

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Copenhagen, Denmark

Michael Ploug