Inhibition of HIV-1 by fusion inhibitors

D Eggink, B Berkhout… - Current pharmaceutical …, 2010 - ingentaconnect.com
The envelope glycoprotein complex (Env) is responsible for entry of the human
immunodeficiency virus type 1 (HIV-1) into cells by mediating attachment to target cells and …

Is there a future for antiviral fusion inhibitors?

B Berkhout, D Eggink, RW Sanders - Current opinion in virology, 2012 - Elsevier
Entry of human immunodeficiency virus type 1 (HIV-1) into cells is mediated by attachment of
the envelope glycoproteins, gp120 and gp41, to the CD4 receptor and a chemokine receptor …

Design of a Potent d-Peptide HIV-1 Entry Inhibitor with a Strong Barrier to Resistance

BD Welch, JN Francis, JS Redman, S Paul… - Journal of …, 2010 - Am Soc Microbiol
The HIV gp41 N-trimer pocket region is an ideal viral target because it is extracellular, highly
conserved, and essential for viral entry. Here, we report on the design of a pocket-specific d …

Potent HIV fusion inhibitors against Enfuvirtide-resistant HIV-1 strains

Y He, J Cheng, H Lu, J Li, J Hu, Z Qi… - Proceedings of the …, 2008 - National Acad Sciences
T20 (generic name: Enfuvirtide, brand name: Fuzeon) is the only FDA-approved HIV fusion
inhibitor that is being used for treatment of HIV/AIDS patients who have failed to respond to …

Identification of a critical motif for the human immunodeficiency virus type 1 (HIV-1) gp41 core structure: implications for designing novel anti-HIV fusion inhibitors

Y He, J Cheng, J Li, Z Qi, H Lu, M Dong… - Journal of …, 2008 - Am Soc Microbiol
Human immunodeficiency virus type 1 (HIV-1) entry into the host cell involves a cascade of
events and currently represents one of most attractive targets in the search for new antiviral …

Biophysical property and broad anti-HIV activity of albuvirtide, a 3-maleimimidopropionic acid-modified peptide fusion inhibitor

H Chong, X Yao, C Zhang, L Cai, S Cui, Y Wang… - PLoS One, 2012 - journals.plos.org
Albuvirtide (ABT) is a 3-maleimimidopropionic acid (MPA)-modified peptide HIV fusion
inhibitor that can irreversibly conjugate to serum albumin. Previous studies demonstrated its …

Broad antiviral activity and crystal structure of HIV-1 fusion inhibitor sifuvirtide

X Yao, H Chong, C Zhang, S Waltersperger… - Journal of Biological …, 2012 - ASBMB
Sifuvirtide (SFT) is an electrostatically constrained α-helical peptide fusion inhibitor showing
potent anti-HIV activity, good safety, and pharmacokinetic profiles, and it is currently under …

Resistance of human immunodeficiency virus type 1 to a third-generation fusion inhibitor requires multiple mutations in gp41 and is accompanied by a dramatic loss of …

D Eggink, I Bontjer, JPM Langedijk, B Berkhout… - Journal of …, 2011 - Am Soc Microbiol
ABSTRACT HIV-1 entry into target cells requires the fusion of viral and cellular membranes.
This process is an attractive target for therapeutic intervention, and a first-generation fusion …

HIV-1 gp41 fusion intermediate: a target for HIV therapeutics

C Pan, S Liu, S Jiang - Journal of the Formosan Medical Association, 2010 - Elsevier
Human immunodeficiency virus (HIV)-1 infection is initiated by the binding of gp120
envelope glyco-protein to its cell receptor (CD4) and a coreceptor (CXCR4 or CCR5) …

Detailed mechanistic insights into HIV-1 sensitivity to three generations of fusion inhibitors

D Eggink, JPM Langedijk, AMJJ Bonvin, Y Deng… - Journal of Biological …, 2009 - ASBMB
Peptides based on the second heptad repeat (HR2) of viral class I fusion proteins are
effective inhibitors of virus entry. One such fusion inhibitor has been approved for treatment …