EP 0804460 A1 19971105 - CONFORMATIONALLY CONSTRAINED REVERSE-TURN LIBRARY AND METHODS RELATING THERETO
Title (en)
CONFORMATIONALLY CONSTRAINED REVERSE-TURN LIBRARY AND METHODS RELATING THERETO
Title (de)
KONFORMATIONSBESCHRÄNKTE BIBLIOTHEK MIT UMGEKEHRTER DIEHUNG UND DAZU BEZIEHENDE VERFAHREN
Title (fr)
BIBLIOTHEQUE DE SUBSTANCES MIMETIQUES DE RETOURNEMENT ASTREINTES A UNE CONFORMATION ET PROCEDES ASSOCIES
Publication
Application
Priority
- US 9600786 W 19960119
- US 37590495 A 19950120
Abstract (en)
[origin: WO9622304A1] Libraries of conformationally constrained-reverse turn mimetics, and methods of constructing the same are disclosed. The reverse-turn mimetics include beta-turn, gamma-turn and beta-bulge mimetics which mimic the biologically active conformation of a linear peptide. In a preferred embodiment, a template library is constructed based on the amino acid sequence of the linear peptide, and which contains a plurality of beta-turn, gamma-turn and beta-bulge mimetics of varying ring sizes. The template library is then screened in a suitable assay to identify a biologically active template library member. An optimized library is then constructed based on structure of the biologically active template member, and which includes substitutions to the amino acid sequence thereof. The optimized library is similarly screened to identify a biologically active reverse-turn mimetic. Methods relating to identifying library members which interact with biological targets of interest, and the use of such members as diagnostic, prophylactic and/or therapeutic agents are also disclosed.
IPC 1-7
IPC 8 full level
C07K 1/04 (2006.01); C07K 1/06 (2006.01); C07K 5/02 (2006.01); C07K 14/54 (2006.01); C07K 14/675 (2006.01)
CPC (source: EP)
C07K 1/047 (2013.01); C07K 5/02 (2013.01); C07K 5/021 (2013.01)
Citation (search report)
See references of WO 9622304A1
Designated contracting state (EPC)
CH DE FR GB IE IT LI
DOCDB simple family (publication)
WO 9622304 A1 19960725; AU 4761996 A 19960807; CA 2210349 A1 19960725; EP 0804460 A1 19971105; JP H10512570 A 19981202
DOCDB simple family (application)
US 9600786 W 19960119; AU 4761996 A 19960119; CA 2210349 A 19960119; EP 96903585 A 19960119; JP 52241396 A 19960119