« Previous
Next »
Journal of the Formosan Medical Association
Volume 109, Issue 2
, Pages 94-105
, February 2010
HIV-1 gp41 Fusion Intermediate: A Target for HIV Therapeutics
References
- . HIV-1 at age 25: some thoughts for Taiwan and China . J Formos Med Assoc . 2008;107:907–908
- Isolation of a T-lymphotropic retrovirus from a patient at risk for acquired immune deficiency syndrome (AIDS) . Science . 1983;220:868–871
- Frequent detection and isolation of cytopathic retroviruses (HTLV-III) from patients with AIDS and at risk for AIDS . Science . 1984;224:500–503
-
FDA-approved antiretrovial (ARV) drugs
.
Available at http://www.hivandhepatitis.com/hiv_and_aids/hiv_treat.html
[Date accessed: September 14, 2009]
- . Antiviral drugs in current clinical use . J Clin Virol . 2004;30:115–133
- Drug resistance mutations in HIV-1 . Top HIV Med . 2003;11:215–221
- The prevalence of antiretroviral drug resistance in the United States . AIDS . 2004;18:1393–1401
- . Adverse effects of antiretroviral therapy . Lancet . 2000;356:1423–1430
-
.
Evidence that a prominent cavity in the coiled coil of HIV type 1 gp41 is an attractive drug target
.
Proc Natl Acad Sci USA
. 1998;95:15613–15617
- . Peptide and non-peptide HIV fusion inhibitors . Curr Pharm Des . 2002;8:563–580
- Different from the HIV fusion inhibitor C34, the anti-HIV drug Fuzeon (T-20) inhibits HIV-1 entry by targeting multiple sites in gp41 and gp120 . J Biol Chem . 2005;280:11259–11273
- HIV gp41 C-terminal hep-tad repeat contains multifunctional domains: relation to mechanisms of action of anti-HIV peptides . J Biol Chem . 2007;282:9612–9620
- Rationally designed anti-HIV peptides containing multifunctional domains as molecule probes for studying the mechanisms of action of the first and second generation HIV fusion inhibitors . J Biol Chem . 2008;283:30376–30384
- . A trimeric structural domain of the HIV-1 transmembrane glycoprotein . Nat Struct Biol . 1995;2:1075–1082
- Inhibition of HIV-1 infectivity by the gp41 core: role of a conserved hydrophobic cavity in membrane fusion . J Virol . 1999;73:8578–8586
- The hydrophobic pocket contributes to the structural stability of the N-terminal coiled coil of HIV gp41 but is not required for six-helix bundle formation . Biochemistry . 2003;42:4945–4953
- Core structure of gp41 from the HIV envelope glycoprotein . Cell . 1997;89:263–273
- Atomic Structure of the Ectodomain from HIV-1 gp41 . Nature . 1997;387:426–428
- . HIV entry and its inhibition . Cell . 1998;93:681–684
-
.
Blocking viral entry: a complementary strategy for HIV therapy
.
Drug Discovery Today: Therapeutic Strategies
. 2004;1:497–503
-
.
HIV entry inhibitors targeting gp41: from polypeptides to small-molecule compounds
.
Curr Pharm Design
. 2007;13:143–162
- HIV-1 inhibition by a peptide . Nature . 1993;365:113
- Inhibition of HIV-1 infection by a fusion domain binding peptide from HIV-1 envelope glycoprotein gp41 . Biochem Biophys Res Commun . 1993;195:533–538
-
Peptides corresponding to a predictive alpha-helical domain of human immunodeficiency virus type 1 gp41 are potent inhibitors of virus infection
.
Proc Natl Acad Sci USA
. 1994;91:9770–9774
- . A trimeric structural subdomain of the HIV-1 transmembrane glycoprotein . J Biomol Struct Dyn . 1997;15:465–471
- . Subdomain folding and biological activity of the core structure from human immunodeficiency virus type 1 gp41: implications for viral membrane fusion . J Virol . 1999;73:4433–4438
-
Atomic structure of a thermostable subdomain of HIV-1 gp41
.
Proc Natl Acad Sci USA
. 1997;94:12303–12308
- Mode of action of an antiviral peptide from HIV-1. Inhibition at a post-lipid mixing stage . J Biol Chem . 2001;276:1391–1397
- C-terminal octylation rescues an inactive T20 mutant: implications for the mechanism of HIV/SIV-induced membrane fusion . J Biol Chem . 2003;278:21012–21017
- . Novel therapies based on mechanisms of HIV-1 cell entry . N Engl J Med . 2003;348:2228–2238
- Emergence of resistant human immunodeficiency virus type 1 in patients receiving fusion inhibitor (T-20) monotherapy . Antimicrob Agents Chemother . 2002;46:1896–1905
- Minimal variation in T-20 binding domain of different HIV-1 subtypes from antiretroviralnaive and -experienced patients . AIDS . 2002;16:1684–1686
- Rapid emergence of enfuvirtide resistance in HIV-1-infected patients: results of a clonal analysis . J Acquir Immune Defic Syndr . 2006;43:6–14
- Characterization of determinants of genotypic and phenotypic resistance to enfuvirtide in baseline and on-treatment HIV-1 isolates . AIDS . 2004;18:1787–1794
- The safety, plasma pharmacokinetics, and antiviral activity of subcutaneous enfuvirtide (T-20), a peptide inhibitor of gp41-mediated virus fusion, in HIV-infected adults . AIDS Res Hum Retroviruses . 2002;18:685–693
- Human immunodeficiency virus type 1 variants resistant to first- and secondversion fusion inhibitors and cytopathic in ex vivo human lymphoid tissue . J Virol . 2007;81:6563–6572
- Short-term safety and antiretroviral activity of T-1249, a second-generation fusion inhibitor of HIV . J Infect Dis . 2004;189:1075–1083
- Genotype and phenotype patterns of human immunodeficiency virus type 1 resistance to enfuvirtide during long-term treatment . Antimicrob Agents Chemother . 2004;48:3253–3259
- T-1249 retains potent antiretroviral activity in patients who had experienced virological failure while on an enfuvirtide-containing treatment regimen . J Infect Dis . 2005;191:1155–1163
- Evolution of Genotypic and Phenotypic Resistance during Chronic Treatment with the Fusion Inhibitor T-1249 . AIDS Res Hum retroviruses . 2007;23:1366–1373
-
Delmedico M, Bray B, Cammack N, et al. Next generation HIV peptide fusion inhibitor candidates achieve potent, durable suppression of virus replication in vitro and improved pharmacokinetic properties. In: 13th Conference on Retroviruses and Opportunistic Infections, 2006;5–8 [Abstract].
-
Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus
.
Proc Natl Acad Sci USA
. 2007;104:12772–12777
- Design and evaluation of sifuvirtide, a novel HIV-1 fusion inhibitor . J Biol Chem . 2008;283:11126–11134
-
FusoGen
.
Available at: http://www.fusogen.com
[Date accessed: September 14, 2009]
-
A synthetic peptide inhibitor of human immunodeficiency virus replication: correlation between solution structure and viral inhibition
.
Proc Natl Acad Sci USA
. 1992;89:10537–10541
- Identification of a critical motif for the HIV-1 gp41 core structure: implication for designing novel anti-HIV fusion inhibitors . J Virol . 2008;82:6349–6358
-
Potent HIV fusion inhibitors against Enfuvirtide-resistant HIV-1 strains
.
Proc Natl Acad Sci USA
. 2008;105:16332–16337
- Remodeling of gp41-C34 peptide leads to highly effective inhibitors of the fusion of HIV-1 with target cells . Angew Chem Int Ed Engl . 2002;41:2937–2940
-
Short constrained pep-tides that inhibit HIV-1 entry
.
Proc Natl Acad Sci USA
. 2002;99:14664–14669
- . Crystal structure of GCN4-pIQI, a trimeric coiled coil with buried polar residues . J Mol Biol . 1998;284:859–865
- Inhibiting HIV-1 entry: discovery of D-peptide inhibitors that target the gp41 coiled-coil pocket . Cell . 1999;99:103–115
-
Potent D-pep-tide inhibitors of HIV-1 entry
.
Proc Natl Acad Sci USA
. 2007;104:16828–16833
- Protein design of a bacte-rially expressed HIV-1 gp41 fusion inhibitor . Biochemistry . 2007;46:4360–4369
- Protection of macaques from vaginal SHIV challenge by vaginally delivered inhibitors of virus-cell fusion . Nature . 2005;438:99–102
- . Rational design of highly potent HIV-1 fusion inhibitory proteins: implication for developing antiviral therapeutics . Biochem Biophys Res Commun . 2005;332:831–836
- Recombinant protein of heptad-repeat HR212, a stable fusion inhibitor with potent anti-HIV action in vitro . Virology . 2008;377:80–87
- Covalent trimers of the internal N-terminal trimeric coiled-coil of gp41 and antibodies directed against them are potent inhibitors of HIV envelope-mediated cell fusion . J Biol Chem . 2003;278:20278–20285
- . Protein design of an HIV-1 entry inhibitor . Science . 2001;291:884–888
-
.
Targeting therapeutics to an exposed and conserved binding element of the HIV-1 fusion protein
.
Proc Natl Acad Sci USA
. 2003;100:5016–5021
- Discovery and optimization of a natural HIV-1 entry inhibitor targeting the gp41 fusion peptide . Cell . 2007;129:263–275
- . A conformation-specific monoclonal antibody reacting with fusion-active gp41 from the HIV-1 envelope glycoprotein . J Virol . 1998;72:10213–10217
- A screening assay for antiviral compounds targeted to the HIV-1 gp41 core structure using a conformation-specific monoclonal antibody . J Virol Methods . 1999;80:85–96
- . Structure-based identification of small molecule antiviral compounds targeted to the gp41 core structure of the human immunodecifiency virus type 1 . J Med Chem . 1999;42:3203–3209
- . A salt bridge between an N-terminal coiled coil of gp41 and an antiviral agent targeted to the gp41 core is important for anti-HIV-1 activity . Biochem Biophys Res Commun . 2000;270:153–157
- Conserved residue Lys574 in the cavity of HIV-1 gp41 coiled-coil domain is critical for six-helix bundle stability and virus entry . J Biol Chem . 2007;282:25631–25639
- Conserved salt-bridge between the N- and C-terminal heptad repeat regions of HIV-1 gp41 core structure is critical for virus entry and inhibition . J Virol . 2008;82:11129–11139
- N-substituted pyrrole derivatives as novel human immunodeficiency virus type 1 entry inhibitors that interfere with the gp41 six-helix bundle formation and block virus fusion . Antimicrob Agents Chemother . 2004;48:4349–4359
- Design, synthesis, and biological evaluation of N-carboxyphenylpyrrole derivatives as potent HIV fusion inhibitors targeting gp41 . J Med Chem . 2008;51:7843–7854
- Design, synthesis, and structure-activity relationship of a novel series of 2-Aryl 5-(4-oxo-3-phenethyl-2-thioxothiazolidin-ylidenemethyl)furans as HIV-1 entry inhibitors . J Med Chem . 2009;52:7631–7639
- Selection of gp41-mediated HIV-1 cell entry inhibitors from biased combinatorial libraries of non-natural binding elements . Nat Struct Biol . 1999;6:953–960
- Design of a protein surface antagonist based on alpha-helix mimicry: inhibition of gp41 assembly and viral fusion . Angew Chem Int Ed Engl . 2002;41:278–281
- Evaluation of “credit card” libraries for inhibition of HIV-1 gp41 fusogenic core formation . J Comb Chem . 2006;8:531–539
- A fluorescence assay for rapid detection of ligand binding affinity to HIV-1 gp41 . Biol Chem . 2006;387:477–483
- . A novel fluorescence intensity screening assay identifies new low molecular weight inhibitors of the gp41 coiled coil domain of HIV-1 . Antimicrob Agents Chemother . 2007;51:2388–2395
- . Therapy of HIV infections: problems and prospects . Bull N Y Acad Med . 1996;73:37–45
- Human immunodeficiency virus type 1 entry inhibitors PRO 542 and T-20 are potently synergistic in blocking virus-cell and cell-cell fusion . J Infect Dis . 2001;183:1121–1125
- Strong in vitro synergy between the fusion inhibitor T-20 and the CXCR4 blocker AMD-3100 . J Acquir Immune Defic Syndr . 2000;25:99–102
- Anti-human immunodeficiency virus interactions of SCH-C (SCH 351125), a CCR5 antagonist, with other antiretroviral agents in vitro . Antimicrob Agents Chemother . 2002;46:1336–1339
- Synergistic efficacy of combination of enfuvirtide and sifuvirtide, the first- and next-generation HIV-fusion inhibitors . AIDS . 2009;23:639–641
- Combinations of the first and next generation HIV fusion inhibitors exhibit highly potent synergistic effect against enfuvirtide-sensitive and resistant HIV-1 strains . J Virol . 2009;83:7862–7872
- . Determinants of human immunodeficiency virus type 1 resistance to gp41-derived inhibitory peptides . J Virol . 1998;72:986–993
- Selection of T1249-resistant Human Immunodeficiency Virus type 1 variants . J Virol . 2008;82:6678–6688
- . Resistance to enfuvirtide, the first HIV fusion inhibitor . J Antimicrob Chemother . 2004;54:333–340
- Role of the envelope genetic context in the development of enfu-virtide resistance in human immunodeficiency virus type 1-infected patients . J Virol . 2006;80:8807–8819
- Enfuvirtide: the first therapy to inhibit the entry of HIV-1 into host CD4 lymphocytes . Nat Rev Drug Discov . 2004;3:215–225
- Impact of human immunodeficiency virus type 1 gp41 amino acid substitutions selected during enfuvirtide treatment on gp41 binding and antiviral potency of enfuvirtide in vitro . J Virol . 2005;79:12447–12454
- Clinical resistance to enfuvirtide does not affect susceptibility of human immunodeficiency virus type 1 to other classes of entry inhibitors . J Virol . 2007;81:3240–3250
- . HR-2 mutations in human immunodeficiency virus type 1 gp41 restore fusion kinetics delayed by HR-1 mutations that cause clinical resistance to enfuvirtide . J Virol . 2009;83:2989–2995
- The LLSGIV stretch of the N-terminal region of HIV-1 gp41 is critical for binding to a model peptide, T20 . Protein Eng . 2003;16:311–317
PII: S0929-6646(10)60029-0
doi: 10.1016/S0929-6646(10)60029-0
© 2010 Formosan Medical Association & Elsevier. Published by Elsevier Inc. All rights reserved.
« Previous
Next »
Journal of the Formosan Medical Association
Volume 109, Issue 2
, Pages 94-105
, February 2010
