Literature DB >> 24451644

Small molecule inhibitors of the HIV-1 virulence factor, Nef.

Thomas E Smithgall, Gary Thomas.   

Abstract

Although antiretroviral therapy has revolutionized the clinical management of AIDS, life-long treatment is required because these drugs do not eradicate HIV- infected cells. Chronic antiretroviral therapy may not protect AIDS patients from cognitive impairment, raising important quality of life issues. Because of the rise of HIV strains resistant to current drugs and uncertain vaccine prospects, an urgent need exists for the discovery and development of new therapeutic approaches. This review is focused on one such approach, which involves targeting HIV-1 Nef, a viral accessory protein essential for AIDS pathogenesis.

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Year:  2013        PMID: 24451644      PMCID: PMC3900877          DOI: 10.1016/j.ddtec.2013.07.002

Source DB:  PubMed          Journal:  Drug Discov Today Technol        ISSN: 1740-6749


  43 in total

1.  Mutation of a conserved residue (D123) required for oligomerization of human immunodeficiency virus type 1 Nef protein abolishes interaction with human thioesterase and results in impairment of Nef biological functions.

Authors:  L X Liu; N Heveker; O T Fackler; S Arold; S Le Gall; K Janvier; B M Peterlin; C Dumas; O Schwartz; S Benichou; R Benarous
Journal:  J Virol       Date:  2000-06       Impact factor: 5.103

2.  HIV-1 Nef downregulates MHC-I by a PACS-1- and PI3K-regulated ARF6 endocytic pathway.

Authors:  Anastassia D Blagoveshchenskaya; Laurel Thomas; Sylvain F Feliciangeli; Chien Hui Hung; Gary Thomas
Journal:  Cell       Date:  2002-12-13       Impact factor: 41.582

3.  A specific protein disorder catalyzer of HIV-1 Nef.

Authors:  Adrien Lugari; Sebastian Breuer; Thibault Coursindel; Sandrine Opi; Audrey Restouin; Xiaoli Shi; Alexis Nazabal; Bruce E Torbett; Jean Martinez; Yves Collette; Isabelle Parrot; Stefan T Arold; Xavier Morelli
Journal:  Bioorg Med Chem       Date:  2011-10-20       Impact factor: 3.641

4.  Protein protein interaction inhibition (2P2I) combining high throughput and virtual screening: Application to the HIV-1 Nef protein.

Authors:  Stéphane Betzi; Audrey Restouin; Sandrine Opi; Stefan T Arold; Isabelle Parrot; Françoise Guerlesquin; Xavier Morelli; Yves Collette
Journal:  Proc Natl Acad Sci U S A       Date:  2007-11-27       Impact factor: 11.205

5.  Brief report: absence of intact nef sequences in a long-term survivor with nonprogressive HIV-1 infection.

Authors:  F Kirchhoff; T C Greenough; D B Brettler; J L Sullivan; R C Desrosiers
Journal:  N Engl J Med       Date:  1995-01-26       Impact factor: 91.245

Review 6.  Nef: "necessary and enforcing factor" in HIV infection.

Authors:  Ajith M Joseph; Manish Kumar; Debashis Mitra
Journal:  Curr HIV Res       Date:  2005-01       Impact factor: 1.581

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

Authors:  Jerrod A Poe; Thomas E Smithgall
Journal:  J Mol Biol       Date:  2009-09-23       Impact factor: 5.469

Review 8.  Hematopoietic cell kinase (Hck) isoforms and phagocyte duties - from signaling and actin reorganization to migration and phagocytosis.

Authors:  Romain Guiet; Renaud Poincloux; Jerôme Castandet; Louis Marois; Arnaud Labrousse; Véronique Le Cabec; Isabelle Maridonneau-Parini
Journal:  Eur J Cell Biol       Date:  2008-06-05       Impact factor: 4.492

9.  Indolizine derivatives as HIV-1 VIF-ElonginC interaction inhibitors.

Authors:  Wenlin Huang; Tao Zuo; Xiao Luo; Hongwei Jin; Zhenming Liu; Zhenjun Yang; Xianghui Yu; Liangren Zhang; Lihe Zhang
Journal:  Chem Biol Drug Des       Date:  2013-06       Impact factor: 2.817

10.  Structural basis of evasion of cellular adaptive immunity by HIV-1 Nef.

Authors:  Xiaofei Jia; Rajendra Singh; Stefanie Homann; Haitao Yang; John Guatelli; Yong Xiong
Journal:  Nat Struct Mol Biol       Date:  2012-06-17       Impact factor: 15.369

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  20 in total

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

Authors:  Prema C Iyer; Jielu Zhao; Lori A Emert-Sedlak; Kerry K Moore; Thomas E Smithgall; Billy W Day
Journal:  Bioorg Med Chem Lett       Date:  2014-02-26       Impact factor: 2.823

Review 2.  New targets for HIV drug discovery.

Authors:  Ana C Puhl; Alfredo Garzino Demo; Vadim A Makarov; Sean Ekins
Journal:  Drug Discov Today       Date:  2019-03-15       Impact factor: 7.851

Review 3.  Structure, function, and inhibitor targeting of HIV-1 Nef-effector kinase complexes.

Authors:  Ryan P Staudt; John J Alvarado; Lori A Emert-Sedlak; Haibin Shi; Sherry T Shu; Thomas E Wales; John R Engen; Thomas E Smithgall
Journal:  J Biol Chem       Date:  2020-08-29       Impact factor: 5.157

4.  Remodeling of HIV-1 Nef Structure by Src-Family Kinase Binding.

Authors:  Jamie A Moroco; John Jeff Alvarado; Ryan P Staudt; Haibin Shi; Thomas E Wales; Thomas E Smithgall; John R Engen
Journal:  J Mol Biol       Date:  2017-12-16       Impact factor: 5.469

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

Authors:  Lori A Emert-Sedlak; H Marie Loughran; Haibin Shi; John L Kulp; Sherry T Shu; Jielu Zhao; Billy W Day; Jay E Wrobel; Allen B Reitz; Thomas E Smithgall
Journal:  Bioorg Med Chem Lett       Date:  2016-01-21       Impact factor: 2.823

Review 6.  Mechanisms of HIV-1 Control.

Authors:  Mary Soliman; Geetha Srikrishna; Ashwin Balagopal
Journal:  Curr HIV/AIDS Rep       Date:  2017-06       Impact factor: 5.071

7.  Cell-based Fluorescence Complementation Reveals a Role for HIV-1 Nef Protein Dimerization in AP-2 Adaptor Recruitment and CD4 Co-receptor Down-regulation.

Authors:  Sherry T Shu; Lori A Emert-Sedlak; Thomas E Smithgall
Journal:  J Biol Chem       Date:  2016-12-28       Impact factor: 5.157

8.  Inhibitors of HIV-1 Nef-Mediated Activation of the Myeloid Src-Family Kinase Hck Block HIV-1 Replication in Macrophages and Disrupt MHC-I Downregulation.

Authors:  Lori A Emert-Sedlak; Omar Moukha-Chafiq; Haibin Shi; Shoucheng Du; John J Alvarado; Vibha Pathak; Samuel G Tanner; Robert N Hunter; Miranda Nebane; Li Chen; Tatiana V Ilina; Rieko Ishima; Sixue Zhang; Yury V Kuzmichev; Elizabeth R Wonderlich; Susan M Schader; Corinne E Augelli-Szafran; Roger G Ptak; Thomas E Smithgall
Journal:  ACS Infect Dis       Date:  2022-01-05       Impact factor: 5.578

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

Authors:  Thomas E Wales; James M Hochrein; Christopher R Morgan; Lori A Emert-Sedlak; Thomas E Smithgall; John R Engen
Journal:  Biochemistry       Date:  2015-10-06       Impact factor: 3.162

Review 10.  Challenges and Opportunities for T-Cell-Mediated Strategies to Eliminate HIV Reservoirs.

Authors:  Mark A Brockman; R Brad Jones; Zabrina L Brumme
Journal:  Front Immunol       Date:  2015-10-02       Impact factor: 7.561

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