TY - JOUR
T1 - Fragment-based design of ligands targeting a novel site on the integrase enzyme of human immunodeficiency virus 1
AU - Wielens, Jerome
AU - Headey, Stephen
AU - Deadman, John
AU - Rhodes, David
AU - Le, G
AU - Parker, Michael
AU - Chalmers, David
AU - Scanlon, Martin
PY - 2011
Y1 - 2011
N2 - The genome of the human immunodeficiency virus (HIV) encodes
three enzymes that are essential for viral replication. Of
these, the integrase (IN) enzyme remains significantly underexploited
as a therapeutic target although clinically, inhibition of
IN has been demonstrated to reduce viral load in HIV-1-infected
individuals.[1] During the HIV replication cycle, IN catalyzes
two reactions.[2] In the first, IN binds pro-viral cDNA in the
host-cell cytoplasm and catalyzes the removal of two conserved
nucleotides (GT) from the 3 -ends of the long terminal
repeat (LTR) strands. Following 3 processing, the pre-integration
complex (PIC) is transported into the nucleus where the
second reaction-strand- transfer-occurs.
AB - The genome of the human immunodeficiency virus (HIV) encodes
three enzymes that are essential for viral replication. Of
these, the integrase (IN) enzyme remains significantly underexploited
as a therapeutic target although clinically, inhibition of
IN has been demonstrated to reduce viral load in HIV-1-infected
individuals.[1] During the HIV replication cycle, IN catalyzes
two reactions.[2] In the first, IN binds pro-viral cDNA in the
host-cell cytoplasm and catalyzes the removal of two conserved
nucleotides (GT) from the 3 -ends of the long terminal
repeat (LTR) strands. Following 3 processing, the pre-integration
complex (PIC) is transported into the nucleus where the
second reaction-strand- transfer-occurs.
UR - http://onlinelibrary.wiley.com.ezproxy.lib.monash.edu.au/journal/10.1002/(ISSN)1860-7187;jsessionid=293951D97DCE016188FD353CFF6FA33A.d01t02
U2 - 10.1002/cmdc.201000483
DO - 10.1002/cmdc.201000483
M3 - Article
SN - 1860-7179
VL - 6
SP - 258
EP - 261
JO - ChemMedChem
JF - ChemMedChem
IS - 4
ER -