Global Patent Index - EP 1242824 A2

EP 1242824 A2 2002-09-25 - SCREENING USING BIOLOGICAL TARGET MOLECULES WITH METAL-ION BINDING SITES

Title (en)

SCREENING USING BIOLOGICAL TARGET MOLECULES WITH METAL-ION BINDING SITES

Title (de)

SCREENINGVERFAHREN UNTER VERWENDUNG VON BIOLOGISCHEN ZIELMOLEKÜLEN MIT METALLIONEN-BINDUNGSSTELLEN

Title (fr)

DETECTION AU MOYEN DE MOLECULES CIBLES BIOLOGIQUES POSSEDANT DES SITES DE LIAISON D'IONS METALLIQUES

Publication

EP 1242824 A2 (EN)

Application

EP 00993741 A

Priority

  • DK PA199901879 A
  • DK PA199901880 A
  • DK PA200000705 A
  • EP 0013389 W
  • US 17540100 P
  • US 17599400 P
  • US 20299000 P

Abstract (en)

[origin: WO0150127A2] The present invention provides a molecular approach for rapidly and selectively identifying small organic molecule ligands, i.e. compounds, that are capable of interacting with and binding to specific sites on biological target molecules. The methods of the present invention are applicable to any biological target molecule that has or can be manipulated to have a metal-ion binding site. Biological target molecules are e.g. proteins, polypeptides, oligopeptides, nucleic acids, carbohydrates, nucleoproteins, glycoproteins, glycolipids, lipoproteins and derivatives thereof. More specifically, the biological target molecules include membrane receptors, signal transduction proteins, scaffolding proteins, nuclear receptors, steroid receptors, intracellular receptors, transcription factors, enzymes, allosteric enzyme regulatory proteins, growth factors, hormones, neuropeptides and immunoglobulins. A very interesting group of biological target molecules are membrane proteins such as, e.g., transmembrane protein (e.g. 7 TMs). The methods described herein make it possible to construct and screen libraries of compounds specifically directed against predetermined epitopes on the biological target molecules. The compounds are initially constructed to be bifunctional, i.e. having both a metal-ion binding moiety, which conveys them with the ability to bind to either a natural or an artificially constructed metal-ion binding site as well as a variable moiety, which is varied chemically to probe for interactions with specific parts of the biological target molecule located spatially adjacent to the metal-ion binding site. Compounds may subsequently be further modified to bind to the unmodified biological target molecule without help of the bridging metal-ion. The methods according to the invention may be performed easily and quickly and lead to unambiguous results. The compounds identified by the methods described herein may themselves be employed for various applications or may be further derivatised or modified to provide novel compounds.

IPC 1-7 (main, further and additional classification)

G01N 33/68; G01N 33/531; G01N 33/566

IPC 8 full level (invention and additional information)

G01N 33/531 (2006.01); G01N 33/566 (2006.01); G01N 33/68 (2006.01); C07B 61/00 (2006.01)

CPC (invention and additional information)

G01N 33/6803 (2013.01); G01N 33/531 (2013.01); G01N 33/566 (2013.01); C40B 40/00 (2013.01); G01N 2500/00 (2013.01)

Citation (search report)

See references of WO 0150127A3

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

EPO simple patent family

WO 0150127 A2 20010712; WO 0150127 A3 20020131; WO 0150127 A8 20040219; WO 0150127 A9 20020912; AU 2844901 A 20010716; CA 2395999 A1 20010712; EP 1242824 A2 20020925

INPADOC legal status


2005-06-08 [18W] APPLICATION WITHDRAWN

- Effective date: 20050415

2004-11-10 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20040923

2002-09-25 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20020624

2002-09-25 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A2

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

2002-09-25 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO:

- Free text: AL;LT;LV;MK;RO;SI