EP 1758640 A2 20070307 - INHIBITION OF HIV-1 REPLICATION BY DISRUPTION OF THE PROCESSING OF THE VIRAL CAPSID-SPACER PEPTIDE 1 PROTEIN
Title (en)
INHIBITION OF HIV-1 REPLICATION BY DISRUPTION OF THE PROCESSING OF THE VIRAL CAPSID-SPACER PEPTIDE 1 PROTEIN
Title (de)
HIV-1-REPLIKATIONSHEMMUNG MITTELS UNTERBRECHUNG DER VERARBEITUNG DES VIRALEN CAPSID-SPACER PEPTID-1-PROTEINS
Title (fr)
INHIBITION DE LA REPLICATION DU VIH-1 PAR RUPTURE DE LA TRANSFORMATION DE LA PROTEINE PEPTIDE 1 ESPACEUR-CAPSIDE VIRALE
Publication
Application
Priority
- US 2005018331 W 20050524
- US 85163704 A 20040524
- US 65396105 P 20050217
Abstract (en)
[origin: WO2005113059A2] Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to Gag rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.
IPC 8 full level
A61K 31/00 (2006.01); A61K 31/56 (2006.01); A61K 38/16 (2006.01); A61K 45/06 (2006.01); A61M 37/00 (2006.01); A61P 31/18 (2006.01); C07K 14/16 (2006.01); C07K 16/10 (2006.01); C12N 5/10 (2006.01); C12N 7/00 (2006.01); C12N 15/48 (2006.01); C12N 15/86 (2006.01); G01N 33/569 (2006.01)
CPC (source: EP)
A61K 38/162 (2013.01); A61P 31/04 (2017.12); A61P 31/10 (2017.12); A61P 31/12 (2017.12); A61P 31/18 (2017.12); A61P 35/00 (2017.12); A61P 37/02 (2017.12); A61P 43/00 (2017.12); C07K 14/005 (2013.01); C07K 16/1054 (2013.01); C12N 7/00 (2013.01); G01N 33/56988 (2013.01); C12N 2740/16222 (2013.01); G01N 2500/02 (2013.01)
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU MC NL PL PT RO SE SI SK TR
Designated extension state (EPC)
AL BA HR LV MK YU
DOCDB simple family (publication)
WO 2005113059 A2 20051201; WO 2005113059 A3 20070215; AU 2005245506 A1 20051201; BR PI0511514 A 20080805; CA 2568248 A1 20051201; EP 1758640 A2 20070307; EP 1758640 A4 20090603; IL 179494 A0 20070515; JP 2008504808 A 20080221; MX PA06013698 A 20070815; NO 20065982 L 20070201
DOCDB simple family (application)
US 2005018331 W 20050524; AU 2005245506 A 20050524; BR PI0511514 A 20050524; CA 2568248 A 20050524; EP 05779995 A 20050524; IL 17949406 A 20061122; JP 2007515290 A 20050524; MX PA06013698 A 20050524; NO 20065982 A 20061222