US 7,531,502 B2
Diagnostic conjugate useful for intracellular imaging and for differentiating between tumor- and non-tumor cells
Klaus Braun, Sandhausen (Germany); Jürgen Debus, Stettfeld (Germany); Jürgen Jenne, Mannheim (Germany); Rudiger Pipkorn, Heidelberg (Germany); Ralf Rastert, Mosbach (Germany); Waldemar Waldeck, Laudenbach (Germany); Isabell Braun, Cölbe-Bürgeln (Germany); and Stefan Heckl, Heidelberg (Germany)
Assigned to Deutsches Krebsforschungszentrum Stiftung Des Offentlichen Rechts, (Germany)
Appl. No. 10/502,442
PCT Filed Jan. 22, 2003, PCT No. PCT/EP03/00609
§ 371(c)(1), (2), (4) Date Oct. 04, 2004,
PCT Pub. No. WO03/061712, PCT Pub. Date Jul. 31, 2003.
Claims priority of application No. 02001506 (EP), filed on Jan. 22, 2002.
Prior Publication US 2006/0019249 A1, Jan. 26, 2006
Int. Cl. A01N 37/18 (2006.01); A61K 38/16 (2006.01); A61K 38/00 (2006.01); A61K 38/04 (2006.01); C07K 7/00 (2006.01); C07K 17/00 (2006.01)
U.S. Cl. 514—2  [514/8; 514/12; 514/21; 530/324; 530/326] 16 Claims
 
1. A diagnostic conjugate having the structure: transmembrane module (TPU) coupled via a spacer to an address module (AS) coupled via a spacer to a signalling module (SM); wherein
the transmembrane module is a cell-penetrating human transmembrane peptide comprising the amino acid sequence KMTRQTWWHRIKHKC (SEQ ID NO: 2), MTRQTFWHRIKHKC (SEQ ID NO: 3) or KHKIRHWFTQRTMC (SEQ ID NO: 4),
the address module is a peptide nucleic acid (PNA) antisense to and hybridizing with a mRNA selected from the group consisting of c-myc-, c-ras-, hern-, sst1, or sst2-mRNA, and
the signalling module is a compound trapping Gadolinium.