skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: Allosteric HIV Integrase Inhibitors Promote Formation of Inactive Branched Polymers via Homomeric Carboxy-Terminal Domain Interactions

Journal Article · · Structure

Research Organization:
Brookhaven National Laboratory (BNL), Upton, NY (United States)
Sponsoring Organization:
~OTHER
DOE Contract Number:
SC0012704
OSTI ID:
1783997
Report Number(s):
BNL-221528-2021-JACI
Journal Information:
Structure, Vol. 29, Issue 3
Country of Publication:
United States
Language:
English

References (88)

Identification of cellular factors binding to acetylated HIV-1 integrase journal December 2009
The TRIM Family Protein KAP1 Inhibits HIV-1 Integration journal June 2011
HIV-1 Antiretroviral Drug Therapy journal January 2012
Non-Catalytic Site HIV-1 Integrase Inhibitors Disrupt Core Maturation and Induce a Reverse Transcription Block in Target Cells journal September 2013
Small-Angle X-Ray-Scattering Investigation of Submicroscopic Porosity with Fractal Properties journal August 1984
A supramolecular assembly mediates lentiviral DNA integration journal January 2017
An Hsp60 related protein is associated with purified HIV and SIV journal February 1994
Three-dimensional Structure of HIV-1 Virus-like Particles by Electron Cryotomography journal February 2005
Characterization of the neutron detector upgrade to the GP-SANS and Bio-SANS instruments at HFIR
  • Berry, Kevin D.; Bailey, Katherine M.; Beal, Justin
  • Nuclear Instruments and Methods in Physics Research Section A: Accelerators, Spectrometers, Detectors and Associated Equipment, Vol. 693 https://doi.org/10.1016/j.nima.2012.06.052
journal November 2012
Association Equilibrium of the HIV-1 Capsid Protein in a Crowded Medium Reveals that Hexamerization during Capsid Assembly Requires a Functional C-Domain Dimerization Interface journal February 2013
Calculations and Publication-Quality Illustrations for Analytical Ultracentrifugation Data book January 2015
The stoichiometry of Gag protein in HIV-1 journal June 2004
F-actin and Microtubule Suspensions as Indeterminate Fluids journal March 1987
Solution structure of the His 12 → Cys mutant of the N-terminal zinc binding domain of HIV-1 integrase complexed to cadmium journal December 1998
Solution structure of the N-terminal zinc binding domain of HIV-1 integrase journal July 1997
Acetylation of HIV-1 integrase by p300 regulates viral integration journal August 2005
Rheology of Soft Materials journal August 2010
Crystal structure of the HIV-1 integrase catalytic core and C-terminal domains: A model for viral DNA binding journal July 2000
Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication journal May 2010
Current status and prospects of HIV treatment journal June 2016
Modulating Target Site Selection During Human Immunodeficiency Virus DNA Integration In Vitro with an Engineered Tethering Factor journal September 2006
A role for LEDGF/p75 in targeting HIV DNA integration journal November 2005
HIV DNA Integration journal May 2012
Effect of Macromolecular Crowding Agents on Human Immunodeficiency Virus Type 1 Capsid Protein Assembly In Vitro journal November 2005
Dynamic microtubules at the synapse journal August 2020
Oligomeric States of the HIV-1 Integrase As Measured by Time-Resolved Fluorescence Anisotropy journal August 2000
DNA binding induces dissociation of the multimeric form of HIV-1 integrase: A time-resolved fluorescence anisotropy study journal August 2001
LEDGINs inhibit late stage HIV-1 replication by modulating integrase multimerization in the virions journal May 2013
Role of metal ions in catalysis by HIV integrase analyzed using a quantitative PCR disintegration assay journal November 2006
The life science x-ray scattering beamline at NSLS-II
  • DiFabio, Jonathan; Chodankar, Shirish; Pjerov, Sal
  • PROCEEDINGS OF THE 12TH INTERNATIONAL CONFERENCE ON SYNCHROTRON RADIATION INSTRUMENTATION – SRI2015, AIP Conference Proceedings https://doi.org/10.1063/1.4952872
conference January 2016
Crystal Structure of the Catalytic Domain of HIV-1 Integrase: Similarity to Other Polynucleotidyl Transferases journal December 1994
Refined solution structure of the c-terminal DNA-binding domain of human immunovirus-1 integrase journal September 1999
Über die von der molekularkinetischen Theorie der Wärme geforderte Bewegung von in ruhenden Flüssigkeiten suspendierten Teilchen journal January 1905
The structural biology of HIV-1: mechanistic and therapeutic insights journal March 2012
Allosteric inhibition of HIV-1 integrase activity journal June 2013
Structure-based mutagenesis of the catalytic domain of human immunodeficiency virus type 1 integrase. journal January 1997
Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs journal June 2016
The Competitive Interplay between Allosteric HIV-1 Integrase Inhibitor BI/D and LEDGF/p75 during the Early Stage of HIV-1 Replication Adversely Affects Inhibitor Potency journal March 2016
The A128T Resistance Mutation Reveals Aberrant Protein Multimerization as the Primary Mechanism of Action of Allosteric HIV-1 Integrase Inhibitors journal April 2013
ATSAS 2.8 : a comprehensive data analysis suite for small-angle scattering from macromolecular solutions journal June 2017
Three new structures of the core domain of HIV-1 integrase: An active site that binds magnesium journal August 1998
Allosteric Inhibition of Human Immunodeficiency Virus Integrase: LATE BLOCK DURING VIRAL REPLICATION AND ABNORMAL MULTIMERIZATION INVOLVING SPECIFIC PROTEIN DOMAINS journal June 2014
Structural Properties of HIV Integrase·Lens Epithelium-derived Growth Factor Oligomers journal April 2010
Coiled-coil interactions mediate serine integrase directionality journal May 2017
Structural Basis for Inhibitor-Induced Aggregation of HIV Integrase journal December 2016
Structural Basis for Functional Tetramerization of Lentiviral Integrase journal July 2009
A Novel Co-Crystal Structure Affords the Design of Gain-of-Function Lentiviral Integrase Mutants in the Presence of Modified PSIP1/LEDGF/p75 journal January 2009
Structural and Functional Analyses of the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir (S/GSK1349572) journal June 2011
The Bio-SANS instrument at the High Flux Isotope Reactor of Oak Ridge National Laboratory journal June 2014
BioXTAS RAW : improvements to a free open-source program for small-angle X-ray scattering data reduction and analysis journal September 2017
VMD: Visual molecular dynamics journal February 1996
A Soluble Active Mutant of HIV-1 Integrase: INVOLVEMENT OF BOTH THE CORE AND CARBOXYL-TERMINAL DOMAINS IN MULTIMERIZATION journal March 1996
Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation journal April 2013
HIV-1 Integrase Binds the Viral RNA Genome and Is Essential during Virion Morphogenesis journal August 2016
HIV-1 Tat transcriptional activity is regulated by acetylation journal November 1999
Acetylation regulates Cyclophilin A catalysis, immunosuppression and HIV isomerization journal April 2010
Interaction of the HIV-1 Intasome with Transportin 3 Protein (TNPO3 or TRN-SR2) journal October 2012
Dual inhibition of HIV-1 replication by integrase-LEDGF allosteric inhibitors is predominant at the post-integration stage journal January 2013
The Conserved Set of Host Proteins Incorporated into HIV-1 Virions Suggests a Common Egress Pathway in Multiple Cell Types journal March 2013
Solution Structure of the DNA Binding Domain of HIV-1 Integrase journal August 1995
Genetic Analyses of Conserved Residues in the Carboxyl-Terminal Domain of Human Immunodeficiency Virus Type 1 Integrase journal August 2005
Structure-Based Mutational Analysis of the C-Terminal DNA-Binding Domain of Human Immunodeficiency Virus Type 1 Integrase: Critical Residues for Protein Oligomerization and DNA Binding journal June 1998
Allosteric HIV-1 Integrase Inhibitors Lead to Premature Degradation of the Viral RNA Genome and Integrase in Target Cells journal September 2017
Evolving factor analysis for the resolution of overlapping chromatographic peaks journal February 1987
The mechanism of retroviral integration from X-ray structures of its key intermediates journal November 2010
Structural basis for retroviral integration into nucleosomes journal June 2015
Human H4 tail stimulates HIV-1 integration through binding to the carboxy-terminal domain of integrase journal February 2019
Domain Movements upon Activation of Phenylalanine Hydroxylase Characterized by Crystallography and Chromatography-Coupled Small-Angle X-ray Scattering journal May 2016
Structural Analysis of a Mutant of the HIV-1 Integrase Zinc Finger Domain That Forms a Single Conformation journal April 2006
Functional Interactions of Human Immunodeficiency Virus Type 1 Integrase with Human and Yeast HSP60 journal December 2001
Cryo-EM structures and atomic model of the HIV-1 strand transfer complex intasome journal January 2017
Scalable molecular dynamics with NAMD journal January 2005
Effects of Macromolecular Crowding on the Inhibition of Virus Assembly and Virus-Cell Receptor Recognition journal February 2011
HIV-1 Integration in the Human Genome Favors Active Genes and Local Hotspots journal August 2002
Size-Distribution Analysis of Macromolecules by Sedimentation Velocity Ultracentrifugation and Lamm Equation Modeling journal March 2000
GNOM – a program package for small-angle scattering data processing journal October 1991
A New Class of Multimerization Selective Inhibitors of HIV-1 Integrase journal May 2014
LEDGF/p75 functions downstream from preintegration complex formation to effect gene-specific HIV-1 integration journal July 2007
CRYSOL – a Program to Evaluate X-ray Solution Scattering of Biological Macromolecules from Atomic Coordinates journal December 1995
Small-angle scattering by fractal systems journal December 1988
Interaction between Reverse Transcriptase and Integrase Is Required for Reverse Transcription during HIV-1 Replication journal September 2015
Sedimentation equilibrium analysis of protein interactions with global implicit mass conservation constraints and systematic noise decomposition journal March 2004
Structure of a two-domain fragment of HIV-1 integrase: implications for domain organization in the intact protein journal December 2001
Two-Stage PCR Protocol Allowing Introduction of Multiple Mutations, Deletions and Insertions Using QuikChange TM Site-Directed Mutagenesis journal April 1999
MULCh : modules for the analysis of small-angle neutron contrast variation data from biomolecular assemblies journal January 2008
Retroviral integration into nucleosomes through DNA looping and sliding along the histone octamer journal September 2019
Crystal structure of the Rous sarcoma virus intasome journal February 2016
Selective Histonedeacetylase Inhibitor M344 Intervenes in HIV-1 Latency through Increasing Histone Acetylation and Activation of NF-kappaB journal November 2012