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Items: 1 to 20 of 107


Chemical library screens targeting an HIV-1 accessory factor/host cell kinase complex identify novel antiretroviral compounds.

Emert-Sedlak L, Kodama T, Lerner EC, Dai W, Foster C, Day BW, Lazo JS, Smithgall TE.

ACS Chem Biol. 2009 Nov 20;4(11):939-47. doi: 10.1021/cb900195c.


Effector kinase coupling enables high-throughput screens for direct HIV-1 Nef antagonists with antiretroviral activity.

Emert-Sedlak LA, Narute P, Shu ST, Poe JA, Shi H, Yanamala N, Alvarado JJ, Lazo JS, Yeh JI, Johnston PA, Smithgall TE.

Chem Biol. 2013 Jan 24;20(1):82-91. doi: 10.1016/j.chembiol.2012.11.005.


Nef alleles from all major HIV-1 clades activate Src-family kinases and enhance HIV-1 replication in an inhibitor-sensitive manner.

Narute PS, Smithgall TE.

PLoS One. 2012;7(2):e32561. doi: 10.1371/journal.pone.0032561. Epub 2012 Feb 29.


Discovery of a diaminoquinoxaline benzenesulfonamide antagonist of HIV-1 Nef function using a yeast-based phenotypic screen.

Trible RP, Narute P, Emert-Sedlak LA, Alvarado JJ, Atkins K, Thomas L, Kodama T, Yanamala N, Korotchenko V, Day BW, Thomas G, Smithgall TE.

Retrovirology. 2013 Nov 14;10:135. doi: 10.1186/1742-4690-10-135.


Subtle Dynamic Changes Accompany Hck Activation by HIV-1 Nef and are Reversed by an Antiretroviral Kinase Inhibitor.

Wales TE, Hochrein JM, Morgan CR, Emert-Sedlak LA, Smithgall TE, Engen JR.

Biochemistry. 2015 Oct 20;54(41):6382-91. doi: 10.1021/acs.biochem.5b00875. Epub 2015 Oct 6.


The identification of a small molecule compound that reduces HIV-1 Nef-mediated viral infectivity enhancement.

Chutiwitoonchai N, Hiyoshi M, Mwimanzi P, Ueno T, Adachi A, Ode H, Sato H, Fackler OT, Okada S, Suzu S.

PLoS One. 2011;6(11):e27696. doi: 10.1371/journal.pone.0027696. Epub 2011 Nov 15.


Synthesis and structure-activity analysis of diphenylpyrazolodiazene inhibitors of the HIV-1 Nef virulence factor.

Iyer PC, Zhao J, Emert-Sedlak LA, Moore KK, Smithgall TE, Day BW.

Bioorg Med Chem Lett. 2014 Apr 1;24(7):1702-6. doi: 10.1016/j.bmcl.2014.02.045. Epub 2014 Feb 26.


Interaction with the Src homology (SH3-SH2) region of the Src-family kinase Hck structures the HIV-1 Nef dimer for kinase activation and effector recruitment.

Alvarado JJ, Tarafdar S, Yeh JI, Smithgall TE.

J Biol Chem. 2014 Oct 10;289(41):28539-53. doi: 10.1074/jbc.M114.600031. Epub 2014 Aug 13.


Synthesis and evaluation of orally active small molecule HIV-1 Nef antagonists.

Emert-Sedlak LA, Loughran HM, Shi H, Kulp JL 3rd, Shu ST, Zhao J, Day BW, Wrobel JE, Reitz AB, Smithgall TE.

Bioorg Med Chem Lett. 2016 Mar 1;26(5):1480-1484. doi: 10.1016/j.bmcl.2016.01.043. Epub 2016 Jan 21.


HIV-1 infection of T cells and macrophages are differentially modulated by virion-associated Hck: a Nef-dependent phenomenon.

Cornall A, Mak J, Greenway A, Tachedjian G.

Viruses. 2013 Sep 18;5(9):2235-52. doi: 10.3390/v5092235.


A mammalian two-hybrid screening system for inhibitors of interaction between HIV Nef and the cellular tyrosine kinase Hck.

Murakami Y, Fukazawa H, Kobatake T, Yamagoe S, Takebe Y, Tobiume M, Matsuda M, Uehara Y.

Antiviral Res. 2002 Jul;55(1):161-8.


Guanidine alkaloid analogs as inhibitors of HIV-1 Nef interactions with p53, actin, and p56lck.

Olszewski A, Sato K, Aron ZD, Cohen F, Harris A, McDougall BR, Robinson WE Jr, Overman LE, Weiss GA.

Proc Natl Acad Sci U S A. 2004 Sep 28;101(39):14079-84. Epub 2004 Sep 15.


HIV-1 Nef dimerization is required for Nef-mediated receptor downregulation and viral replication.

Poe JA, Smithgall TE.

J Mol Biol. 2009 Nov 27;394(2):329-42. doi: 10.1016/j.jmb.2009.09.047. Epub 2009 Sep 23.


Oligomerization is required for HIV-1 Nef-induced activation of the Src family protein-tyrosine kinase, Hck.

Ye H, Choi HJ, Poe J, Smithgall TE.

Biochemistry. 2004 Dec 21;43(50):15775-84.


Dys-regulated activation of a Src tyroine kinase Hck at the Golgi disturbs N-glycosylation of a cytokine receptor Fms.

Hassan R, Suzu S, Hiyoshi M, Takahashi-Makise N, Ueno T, Agatsuma T, Akari H, Komano J, Takebe Y, Motoyoshi K, Okada S.

J Cell Physiol. 2009 Nov;221(2):458-68. doi: 10.1002/jcp.21878.


Affinity of Src family kinase SH3 domains for HIV Nef in vitro does not predict kinase activation by Nef in vivo.

Briggs SD, Lerner EC, Smithgall TE.

Biochemistry. 2000 Jan 25;39(3):489-95.


Development and validation of a high-content bimolecular fluorescence complementation assay for small-molecule inhibitors of HIV-1 Nef dimerization.

Poe JA, Vollmer L, Vogt A, Smithgall TE.

J Biomol Screen. 2014 Apr;19(4):556-65. doi: 10.1177/1087057113513640. Epub 2013 Nov 26.


Identification of Binding Mode and Prospective Structural Features of Novel Nef Protein Inhibitors as Potential Anti-HIV Drugs.

Moonsamy S, Bhakat S, Ramesh M, Soliman ME.

Cell Biochem Biophys. 2017 Mar;75(1):49-64. doi: 10.1007/s12013-016-0774-1. Epub 2016 Dec 16.


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