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Saturation Mutagenesis of the HIV-1 Envelope CD4 Binding Loop Reveals Residues Controlling Distinct Trimer Conformations.

Duenas-Decamp M, Jiang L, Bolon D, Clapham PR.

PLoS Pathog. 2016 Nov 7;12(11):e1005988. doi: 10.1371/journal.ppat.1005988.


Design, synthesis and evaluation of small molecule CD4-mimics as entry inhibitors possessing broad spectrum anti-HIV-1 activity.

Curreli F, Belov DS, Ramesh RR, Patel N, Altieri A, Kurkin AV, Debnath AK.

Bioorg Med Chem. 2016 Nov 15;24(22):5988-6003. doi: 10.1016/j.bmc.2016.09.057.


Co-receptor Binding Site Antibodies Enable CD4-Mimetics to Expose Conserved Anti-cluster A ADCC Epitopes on HIV-1 Envelope Glycoproteins.

Richard J, Pacheco B, Gohain N, Veillette M, Ding S, Alsahafi N, Tolbert WD, Prévost J, Chapleau JP, Coutu M, Jia M, Brassard N, Park J, Courter JR, Melillo B, Martin L, Tremblay C, Hahn BH, Kaufmann DE, Wu X, Smith AB 3rd, Sodroski J, Pazgier M, Finzi A.

EBioMedicine. 2016 Oct;12:208-218. doi: 10.1016/j.ebiom.2016.09.004.


Antibodies Elicited by Multiple Envelope Glycoprotein Immunogens in Primates Neutralize Primary Human Immunodeficiency Viruses (HIV-1) Sensitized by CD4-Mimetic Compounds.

Madani N, Princiotto AM, Easterhoff D, Bradley T, Luo K, Williams WB, Liao HX, Moody MA, Phad GE, Vázquez Bernat N, Melillo B, Santra S, Smith AB 3rd, Karlsson Hedestam GB, Haynes B, Sodroski J.

J Virol. 2016 Apr 29;90(10):5031-46. doi: 10.1128/JVI.03211-15.


The Yin and Yang of ADCC-Mediating Antibodies.

Robert-Guroff M.

EBioMedicine. 2016 Jan 8;3:10-1. doi: 10.1016/j.ebiom.2016.01.003. No abstract available.


Small CD4 Mimetics Prevent HIV-1 Uninfected Bystander CD4 + T Cell Killing Mediated by Antibody-dependent Cell-mediated Cytotoxicity.

Richard J, Veillette M, Ding S, Zoubchenok D, Alsahafi N, Coutu M, Brassard N, Park J, Courter JR, Melillo B, Smith AB 3rd, Shaw GM, Hahn BH, Sodroski J, Kaufmann DE, Finzi A.

EBioMedicine. 2015 Dec 9;3:122-34. doi: 10.1016/j.ebiom.2015.12.004.


Molecular mechanism of respiratory syncytial virus fusion inhibitors.

Battles MB, Langedijk JP, Furmanova-Hollenstein P, Chaiwatpongsakorn S, Costello HM, Kwanten L, Vranckx L, Vink P, Jaensch S, Jonckers TH, Koul A, Arnoult E, Peeples ME, Roymans D, McLellan JS.

Nat Chem Biol. 2016 Feb;12(2):87-93. doi: 10.1038/nchembio.1982.


Functional Mimetics of the HIV-1 CCR5 Co-Receptor Displayed on the Surface of Magnetic Liposomes.

Kuzmina A, Vaknin K, Gdalevsky G, Vyazmensky M, Marks RS, Taube R, Engel S.

PLoS One. 2015 Dec 2;10(12):e0144043. doi: 10.1371/journal.pone.0144043. Erratum in: PLoS One. 2015;10(12):e0146309.


Synthesis, antiviral activity and resistance of a novel small molecule HIV-1 entry inhibitor.

Curreli F, Haque K, Xie L, Qiu Q, Xu J, Yong W, Tong X, Debnath AK.

Bioorg Med Chem. 2015 Dec 15;23(24):7618-28. doi: 10.1016/j.bmc.2015.11.006.


Development of Small-molecule HIV Entry Inhibitors Specifically Targeting gp120 or gp41.

Lu L, Yu F, Cai L, Debnath AK, Jiang S.

Curr Top Med Chem. 2016;16(10):1074-90. Review.


Structure-Based Design of a Small Molecule CD4-Antagonist with Broad Spectrum Anti-HIV-1 Activity.

Curreli F, Kwon YD, Zhang H, Scacalossi D, Belov DS, Tikhonov AA, Andreev IA, Altieri A, Kurkin AV, Kwong PD, Debnath AK.

J Med Chem. 2015 Sep 10;58(17):6909-27. doi: 10.1021/acs.jmedchem.5b00709.


CD4 mimetics sensitize HIV-1-infected cells to ADCC.

Richard J, Veillette M, Brassard N, Iyer SS, Roger M, Martin L, Pazgier M, Schön A, Freire E, Routy JP, Smith AB 3rd, Park J, Jones DM, Courter JR, Melillo BN, Kaufmann DE, Hahn BH, Permar SR, Haynes BF, Madani N, Sodroski JG, Finzi A.

Proc Natl Acad Sci U S A. 2015 May 19;112(20):E2687-94. doi: 10.1073/pnas.1506755112.


Characterization of HIV-1 entry inhibitors with broad activity against R5 and X4 viral strains.

Sironi F, Malnati M, Mongelli N, Cozzi P, Guzzo C, Ghezzi S, Martínez-Romero C, García-Sastre A, Lusso P, Jabes D, Biswas P.

J Transl Med. 2015 Apr 2;13:107. doi: 10.1186/s12967-015-0461-9.


HIV-1 gp120 as a therapeutic target: navigating a moving labyrinth.

Acharya P, Lusvarghi S, Bewley CA, Kwong PD.

Expert Opin Ther Targets. 2015 Jun;19(6):765-83. doi: 10.1517/14728222.2015.1010513. Review.


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.


A broad HIV-1 inhibitor blocks envelope glycoprotein transitions critical for entry.

Herschhorn A, Gu C, Espy N, Richard J, Finzi A, Sodroski JG.

Nat Chem Biol. 2014 Oct;10(10):845-52. doi: 10.1038/nchembio.1623.


Binding mode characterization of NBD series CD4-mimetic HIV-1 entry inhibitors by X-ray structure and resistance study.

Curreli F, Kwon YD, Zhang H, Yang Y, Scacalossi D, Kwong PD, Debnath AK.

Antimicrob Agents Chemother. 2014 Sep;58(9):5478-91. doi: 10.1128/AAC.03339-14.

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