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Items: 20


Peptide triazole inactivators of HIV-1: how do they work and what is their potential?

Chaiken I, Rashad AA.

Future Med Chem. 2015;7(17):2305-10. doi: 10.4155/fmc.15.152. Epub 2015 Nov 24. No abstract available.


Disulfide Sensitivity in the Env Protein Underlies Lytic Inactivation of HIV-1 by Peptide Triazole Thiols.

Bailey LD, Kalyana Sundaram RV, Li H, Duffy C, Aneja R, Rosemary Bastian A, Holmes AP, Kamanna K, Rashad AA, Chaiken I.

ACS Chem Biol. 2015 Dec 18;10(12):2861-73. doi: 10.1021/acschembio.5b00381.


Macrocyclic Envelope Glycoprotein Antagonists that Irreversibly Inactivate HIV-1 before Host Cell Encounter.

Rashad AA, Kalyana Sundaram RV, Aneja R, Duffy C, Chaiken I.

J Med Chem. 2015 Sep 24;58(18):7603-8. doi: 10.1021/acs.jmedchem.5b00935. Epub 2015 Sep 11.


Peptide Triazole Inactivators of HIV-1 Utilize a Conserved Two-Cavity Binding Site at the Junction of the Inner and Outer Domains of Env gp120.

Aneja R, Rashad AA, Li H, Kalyana Sundaram RV, Duffy C, Bailey LD, Chaiken I.

J Med Chem. 2015 May 14;58(9):3843-58. doi: 10.1021/acs.jmedchem.5b00073. Epub 2015 Apr 28.


Discovery and optimization of novel small-molecule HIV-1 entry inhibitors using field-based virtual screening and bioisosteric replacement.

Tuyishime M, Danish M, Princiotto A, Mankowski MK, Lawrence R, Lombart HG, Esikov K, Berniac J, Liang K, Ji J, Ptak RG, Madani N, Cocklin S.

Bioorg Med Chem Lett. 2014 Dec 1;24(23):5439-45.


Mechanism of multivalent nanoparticle encounter with HIV-1 for potency enhancement of peptide triazole virus inactivation.

Rosemary Bastian A, Nangarlia A, Bailey LD, Holmes A, Kalyana Sundaram RV, Ang C, Moreira DR, Freedman K, Duffy C, Contarino M, Abrams C, Root M, Chaiken I.

J Biol Chem. 2015 Jan 2;290(1):529-43. doi: 10.1074/jbc.M114.608315. Epub 2014 Nov 4.


Covalent conjugation of a peptide triazole to HIV-1 gp120 enables intramolecular binding site occupancy.

Emileh A, Duffy C, Holmes AP, Rosemary Bastian A, Aneja R, Tuzer F, Rajagopal S, Li H, Abrams CF, Chaiken IM.

Biochemistry. 2014 Jun 3;53(21):3403-14. doi: 10.1021/bi500136f. Epub 2014 May 19.


A model of peptide triazole entry inhibitor binding to HIV-1 gp120 and the mechanism of bridging sheet disruption.

Emileh A, Tuzer F, Yeh H, Umashankara M, Moreira DR, Lalonde JM, Bewley CA, Abrams CF, Chaiken IM.

Biochemistry. 2013 Apr 2;52(13):2245-61. doi: 10.1021/bi400166b. Epub 2013 Mar 22.


Non-natural peptide triazole antagonists of HIV-1 envelope gp120.

Kamanna K, Aneja R, Duffy C, Kubinski P, Rodrigo Moreira D, Bailey LD, McFadden K, Schön A, Holmes A, Tuzer F, Contarino M, Freire E, Chaiken IM.

ChemMedChem. 2013 Feb;8(2):322-8. doi: 10.1002/cmdc.201200422. Epub 2012 Dec 13.


HIV-1 Env gp120 structural determinants for peptide triazole dual receptor site antagonism.

Tuzer F, Madani N, Kamanna K, Zentner I, LaLonde J, Holmes A, Upton E, Rajagopal S, McFadden K, Contarino M, Sodroski J, Chaiken I.

Proteins. 2013 Feb;81(2):271-90. doi: 10.1002/prot.24184. Epub 2012 Oct 26.


Phages and HIV-1: from display to interplay.

Delhalle S, Schmit JC, Chevigné A.

Int J Mol Sci. 2012;13(4):4727-94. doi: 10.3390/ijms13044727. Epub 2012 Apr 13. Review.


Antiviral breadth and combination potential of peptide triazole HIV-1 entry inhibitors.

McFadden K, Fletcher P, Rossi F, Kantharaju, Umashankara M, Pirrone V, Rajagopal S, Gopi H, Krebs FC, Martin-Garcia J, Shattock RJ, Chaiken I.

Antimicrob Agents Chemother. 2012 Feb;56(2):1073-80. doi: 10.1128/AAC.05555-11. Epub 2011 Nov 14.


Probing the HIV gp120 envelope glycoprotein conformation by NMR.

Celigoy J, Ramirez B, Tao L, Rong L, Yan L, Feng YR, Quinnan GV, Broder CC, Caffrey M.

J Biol Chem. 2011 Jul 8;286(27):23975-81. doi: 10.1074/jbc.M111.251025. Epub 2011 May 18.


Monoclonal antibody m18 paratope leading to dual receptor antagonism of HIV-1 gp120.

Gift SK, McFadden K, Zentner IJ, Rajagopal S, Zhang MY, Dimitrov DS, Chaiken IM.

Biochemistry. 2011 Apr 12;50(14):2769-79. doi: 10.1021/bi101161j. Epub 2011 Mar 18.


HIV envelope: challenges and opportunities for development of entry inhibitors.

Caffrey M.

Trends Microbiol. 2011 Apr;19(4):191-7. doi: 10.1016/j.tim.2011.02.001. Epub 2011 Mar 4. Review.


Conformational and structural features of HIV-1 gp120 underlying the dual receptor antagonism by cross-reactive neutralizing antibody m18.

Gift SK, Zentner IJ, Schön A, McFadden K, Umashankara M, Rajagopal S, Contarino M, Duffy C, Courter JR, Zhang MY, Gershoni JM, Cocklin S, Dimitrov DS, Smith AB 3rd, Freire E, Chaiken IM.

Biochemistry. 2011 Apr 12;50(14):2756-68. doi: 10.1021/bi101160r. Epub 2011 Mar 18.


The V1-V3 region of a brain-derived HIV-1 envelope glycoprotein determines macrophage tropism, low CD4 dependence, increased fusogenicity and altered sensitivity to entry inhibitors.

Rossi F, Querido B, Nimmagadda M, Cocklin S, Navas-Martín S, Martín-García J.

Retrovirology. 2008 Oct 6;5:89. doi: 10.1186/1742-4690-5-89.


Introducing metallocene into a triazole peptide conjugate reduces its off-rate and enhances its affinity and antiviral potency for HIV-1 gp120.

Gopi H, Cocklin S, Pirrone V, McFadden K, Tuzer F, Zentner I, Ajith S, Baxter S, Jawanda N, Krebs FC, Chaiken IM.

J Mol Recognit. 2009 Mar-Apr;22(2):169-74. doi: 10.1002/jmr.892.


Structural determinants for affinity enhancement of a dual antagonist peptide entry inhibitor of human immunodeficiency virus type-1.

Gopi H, Umashankara M, Pirrone V, LaLonde J, Madani N, Tuzer F, Baxter S, Zentner I, Cocklin S, Jawanda N, Miller SR, Schön A, Klein JC, Freire E, Krebs FC, Smith AB, Sodroski J, Chaiken I.

J Med Chem. 2008 May 8;51(9):2638-47. doi: 10.1021/jm070814r. Epub 2008 Apr 11.


Broad-spectrum anti-human immunodeficiency virus (HIV) potential of a peptide HIV type 1 entry inhibitor.

Cocklin S, Gopi H, Querido B, Nimmagadda M, Kuriakose S, Cicala C, Ajith S, Baxter S, Arthos J, Martín-García J, Chaiken IM.

J Virol. 2007 Apr;81(7):3645-8. Epub 2007 Jan 24.

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