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2015 ; 5
(6
): 493-9
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Pharmacological intervention of HIV-1 maturation
#MMPMID26713265
Wang D
; Lu W
; Li F
Acta Pharm Sin B
2015[Nov]; 5
(6
): 493-9
PMID26713265
show ga
Despite significant advances in antiretroviral therapy, increasing drug
resistance and toxicities observed among many of the current approved human
immunodeficiency virus (HIV) drugs indicate a need for discovery and development
of potent and safe antivirals with a novel mechanism of action. Maturation
inhibitors (MIs) represent one such new class of HIV therapies. MIs inhibit a
late step in the HIV-1 Gag processing cascade, causing defective core
condensation and the release of non-infectious virus particles from infected
cells, thus blocking the spread of the infection to new cells. Clinical
proof-of-concept for the MIs was established with betulinic acid derived
bevirimat, the prototype HIV-1 MI. Despite the discontinuation of its further
clinical development in 2010 due to a lack of uniform patient response caused by
naturally occurring drug resistance Gag polymorphisms, several second-generation
MIs with improved activity against viruses exhibiting Gag polymorphism mediated
resistance have been recently discovered and are under clinical evaluation in
HIV/AID patients. In this review, current understanding of HIV-1 MIs is described
and recent progress made toward elucidating the mechanism of action, target
identification and development of second-generation MIs is reviewed.
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