List of works - Frauke Christ

2-hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4.

scientific article published on 27 November 2010

4-[1-(4-Fluorobenzyl)-4-hydroxy-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acid as a prototype to develop dual inhibitors of HIV-1 integration process

scientific article

A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition

scientific article published on 20 February 2014

A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series

scientific article published on 8 April 2008

A symmetric region of the HIV-1 integrase dimerization interface is essential for viral replication

scientific article

A versatile and practical synthesis toward the development of novel HIV-1 integrase inhibitors

scientific article published on 18 January 2011

Association of polymorphisms in the LEDGF/p75 gene (PSIP1) with susceptibility to HIV-1 infection and disease progression

scientific article published on September 2011

Cellular co-factors of HIV-1 integration

scientific article

Cellular cofactors of lentiviral integrase: from target validation to drug discovery

scientific article published on 7 August 2012

Characterization of rare lens epithelium-derived growth factor/p75 genetic variants identified in HIV-1 long-term nonprogressors

scientific article

Design and discovery of 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide inhibitors of HIV-1 integrase

scientific article published on 30 July 2014

Design of a novel cyclotide-based CXCR4 antagonist with anti-human immunodeficiency virus (HIV)-1 activity

scientific article

Design of cell-permeable stapled peptides as HIV-1 integrase inhibitors

scientific article published on 24 June 2013

Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain

scientific article

Development of a series of 3-hydroxyquinolin-2(1H)-ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity

scientific article published on 30 April 2012

Development of an AlphaScreen-based HIV-1 integrase dimerization assay for discovery of novel allosteric inhibitors

scientific article published on 14 February 2012

Differential interaction of HIV-1 integrase and JPO2 with the C terminus of LEDGF/p75.

scientific article

Diketoacid chelating ligands as dual inhibitors of HIV-1 integration process

scientific article published on 25 March 2014

Discovery of N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75.

scientific article published on 22 June 2015

Discovery of a novel 5-carbonyl-1H-imidazole-4-carboxamide class of inhibitors of the HIV-1 integrase-LEDGF/p75 interaction

scientific article published on 2 August 2013

Discovery of novel inhibitors of LEDGF/p75-IN protein-protein interactions

scientific article published on 20 December 2012

Discovery of small molecule HIV-1 integrase dimerization inhibitors

scientific article published on 21 March 2012

Docking studies on a new human immunodeficiency virus integrase-Mg-DNA complex: phenyl ring exploration and synthesis of 1H-benzylindole derivatives through fluorine substitutions

scientific article

Dynamic Oligomerization of Integrase Orchestrates HIV Nuclear Entry

scientific article published on 10 November 2016

Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors

scientific article

Fragment hopping approach directed at design of HIV IN-LEDGF/p75 interaction inhibitors

scientific article

Fragment-based discovery of 8-hydroxyquinoline inhibitors of the HIV-1 integrase-lens epithelium-derived growth factor/p75 (IN-LEDGF/p75) interaction

scientific article published on 18 March 2013

HIV-1 integrase inhibition: looking at cofactor interactions

scientific article published on 15 December 2015

HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation

scientific article

Host factors for retroviral integration site selection

scientific article published on 31 December 2014

Identification of residues in the C-terminal domain of HIV-1 integrase that mediate binding to the transportin-SR2 protein

scientific article

Identification of the LEDGF/p75 binding site in HIV-1 integrase

scientific article

Impact of LEDGIN treatment during virus production on residual HIV-1 transcription

article

In search of second-generation HIV integrase inhibitors: targeting integration beyond strand transfer

scientific article published on October 2009

In search of small molecules blocking interactions between HIV proteins and intracellular cofactors

scientific article published on 16 October 2008

In vitro DNA tethering of HIV-1 integrase by the transcriptional coactivator LEDGF/p75.

scientific article

Inhibitors of the integrase-transportin-SR2 interaction block HIV nuclear import

scientific article published on 12 January 2018

Inhibitory profile of a LEDGF/p75 peptide against HIV-1 integrase: insight into integrase-DNA complex formation and catalysis

scientific article published on 10 March 2008

Insight into HIV-2 latency may disclose strategies for a cure for HIV-1 infection

scientific article published on January 2017

Integrase mutants defective for interaction with LEDGF/p75 are impaired in chromosome tethering and HIV-1 replication

scientific article published on 25 April 2005

Interaction of the HIV-1 intasome with transportin 3 protein (TNPO3 or TRN-SR2)

scientific article

Interplay between HIV entry and transportin-SR2 dependency

scientific article

Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors

scientific article

Kuwanon-L as a New Allosteric HIV-1 Integrase Inhibitor: Molecular Modeling and Biological Evaluation

scientific article published on 11 September 2015

LEDGF/p75-independent HIV-1 replication demonstrates a role for HRP-2 and remains sensitive to inhibition by LEDGINs

scientific article

LEDGIN-mediated Inhibition of Integrase-LEDGF/p75 Interaction Reduces Reactivation of Residual Latent HIV

scientific article published on 13 May 2016

LEDGINs inhibit late stage HIV-1 replication by modulating integrase multimerization in the virions

scientific article published on 30 May 2013

LEDGINs, non-catalytic site inhibitors of HIV-1 integrase: a patent review (2006 - 2014).

scientific article published on 25 March 2014

Lens epithelium-derived growth factor/p75 interacts with the transposase-derived DDE domain of PogZ.

scientific article

Lentiviral nuclear import: a complex interplay between virus and host

scientific article

Lessons Learned: HIV Points the Way Towards Precision Treatment of Mixed-Lineage Leukemia

scientific article

Magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function

scientific article published on 2 March 2011

New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action

scientific article published on 22 June 2010

New scaffolds of natural origin as Integrase-LEDGF/p75 interaction inhibitors: virtual screening and activity assays

scientific article published on 9 August 2013

Nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity

scientific article published on 11 January 2012

Optimization of rhodanine scaffold for the development of protein-protein interaction inhibitors

scientific article published on 2 May 2015

Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodeficiency virus replication

scientific article

Pharmacophore-based discovery of small-molecule inhibitors of protein-protein interactions between HIV-1 integrase and cellular cofactor LEDGF/p75.

scientific article published in August 2009

Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors

scientific article published on 9 June 2008

Protein-protein and protein-chromatin interactions of LEDGF/p75 as novel drug targets

scientific article published in June 2017

Rational Design, Synthesis and Evaluation of Coumarin Derivatives as Protein-protein Interaction Inhibitors

scientific article published on 25 July 2016

Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication

scientific article

Single-cell imaging of HIV-1 provirus (SCIP).

scientific article published on 19 March 2013

Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor

scientific article published on 17 September 2010

Small-molecule inhibitors of the LEDGF/p75 binding site of integrase block HIV replication and modulate integrase multimerization

scientific article

Structure of transportin SR2, a karyopherin involved in human disease, in complex with Ran

scientific article

Synthesis and biological evaluation of novel antiviral agents as protein-protein interaction inhibitors

scientific article published on 16 July 2013

Synthesis of new pyridazine derivatives as potential anti-HIV-1 agents

article

Targeting Virus-host Interactions of HIV Replication

scientific article published on September 2015

Targeting the HIV integration process in antiviral therapy

scientific article published on December 2008

The LEDGF/p75 integrase interaction, a novel target for anti-HIV therapy ⬇️

scientific article published on January 5, 2013

The interaction of LEDGF/p75 with integrase is lentivirus-specific and promotes DNA binding

scientific article

The stress oncoprotein LEDGF/p75 interacts with the methyl CpG binding protein MeCP2 and influences its transcriptional activity

scientific article published on 24 January 2012

Transient and stable knockdown of the integrase cofactor LEDGF/p75 reveals its role in the replication cycle of human immunodeficiency virus

scientific article

Transportin-SR2 imports HIV into the nucleus

scientific article

Virus evolution reveals an exclusive role for LEDGF/p75 in chromosomal tethering of HIV.

scientific article

List of works by Frauke Christ

2-hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4.

4-[1-(4-Fluorobenzyl)-4-hydroxy-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acid as a prototype to develop dual inhibitors of HIV-1 integration process

A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition

A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series

A symmetric region of the HIV-1 integrase dimerization interface is essential for viral replication

A versatile and practical synthesis toward the development of novel HIV-1 integrase inhibitors

Association of polymorphisms in the LEDGF/p75 gene (PSIP1) with susceptibility to HIV-1 infection and disease progression

Cellular co-factors of HIV-1 integration

Cellular cofactors of lentiviral integrase: from target validation to drug discovery

Characterization of rare lens epithelium-derived growth factor/p75 genetic variants identified in HIV-1 long-term nonprogressors

Design and discovery of 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide inhibitors of HIV-1 integrase

Design of a novel cyclotide-based CXCR4 antagonist with anti-human immunodeficiency virus (HIV)-1 activity

Design of cell-permeable stapled peptides as HIV-1 integrase inhibitors

Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain

Development of a series of 3-hydroxyquinolin-2(1H)-ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity

Development of an AlphaScreen-based HIV-1 integrase dimerization assay for discovery of novel allosteric inhibitors

Differential interaction of HIV-1 integrase and JPO2 with the C terminus of LEDGF/p75.

Diketoacid chelating ligands as dual inhibitors of HIV-1 integration process

Discovery of N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75.

Discovery of a novel 5-carbonyl-1H-imidazole-4-carboxamide class of inhibitors of the HIV-1 integrase-LEDGF/p75 interaction

Discovery of novel inhibitors of LEDGF/p75-IN protein-protein interactions

Discovery of small molecule HIV-1 integrase dimerization inhibitors

Docking studies on a new human immunodeficiency virus integrase-Mg-DNA complex: phenyl ring exploration and synthesis of 1H-benzylindole derivatives through fluorine substitutions

Dynamic Oligomerization of Integrase Orchestrates HIV Nuclear Entry

Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors

Fragment hopping approach directed at design of HIV IN-LEDGF/p75 interaction inhibitors

Fragment-based discovery of 8-hydroxyquinoline inhibitors of the HIV-1 integrase-lens epithelium-derived growth factor/p75 (IN-LEDGF/p75) interaction

HIV-1 integrase inhibition: looking at cofactor interactions

HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation

Host factors for retroviral integration site selection

Identification of residues in the C-terminal domain of HIV-1 integrase that mediate binding to the transportin-SR2 protein

Identification of the LEDGF/p75 binding site in HIV-1 integrase

Impact of LEDGIN treatment during virus production on residual HIV-1 transcription

In search of second-generation HIV integrase inhibitors: targeting integration beyond strand transfer

In search of small molecules blocking interactions between HIV proteins and intracellular cofactors

In vitro DNA tethering of HIV-1 integrase by the transcriptional coactivator LEDGF/p75.

Inhibitors of the integrase-transportin-SR2 interaction block HIV nuclear import

Inhibitory profile of a LEDGF/p75 peptide against HIV-1 integrase: insight into integrase-DNA complex formation and catalysis

Insight into HIV-2 latency may disclose strategies for a cure for HIV-1 infection

Integrase mutants defective for interaction with LEDGF/p75 are impaired in chromosome tethering and HIV-1 replication

Interaction of the HIV-1 intasome with transportin 3 protein (TNPO3 or TRN-SR2)

Interplay between HIV entry and transportin-SR2 dependency

Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors

Kuwanon-L as a New Allosteric HIV-1 Integrase Inhibitor: Molecular Modeling and Biological Evaluation

LEDGF/p75-independent HIV-1 replication demonstrates a role for HRP-2 and remains sensitive to inhibition by LEDGINs

LEDGIN-mediated Inhibition of Integrase-LEDGF/p75 Interaction Reduces Reactivation of Residual Latent HIV

LEDGINs inhibit late stage HIV-1 replication by modulating integrase multimerization in the virions

LEDGINs, non-catalytic site inhibitors of HIV-1 integrase: a patent review (2006 - 2014).

Lens epithelium-derived growth factor/p75 interacts with the transposase-derived DDE domain of PogZ.

Lentiviral nuclear import: a complex interplay between virus and host

Lessons Learned: HIV Points the Way Towards Precision Treatment of Mixed-Lineage Leukemia

Magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function

New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action

New scaffolds of natural origin as Integrase-LEDGF/p75 interaction inhibitors: virtual screening and activity assays

Nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity

Optimization of rhodanine scaffold for the development of protein-protein interaction inhibitors

Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodeficiency virus replication

Pharmacophore-based discovery of small-molecule inhibitors of protein-protein interactions between HIV-1 integrase and cellular cofactor LEDGF/p75.

Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors

Protein-protein and protein-chromatin interactions of LEDGF/p75 as novel drug targets

Rational Design, Synthesis and Evaluation of Coumarin Derivatives as Protein-protein Interaction Inhibitors

Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication

Single-cell imaging of HIV-1 provirus (SCIP).

Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor

Small-molecule inhibitors of the LEDGF/p75 binding site of integrase block HIV replication and modulate integrase multimerization

Structure of transportin SR2, a karyopherin involved in human disease, in complex with Ran

Synthesis and biological evaluation of novel antiviral agents as protein-protein interaction inhibitors

Synthesis of new pyridazine derivatives as potential anti-HIV-1 agents

Targeting Virus-host Interactions of HIV Replication

Targeting the HIV integration process in antiviral therapy

The LEDGF/p75 integrase interaction, a novel target for anti-HIV therapy ⬇️

The interaction of LEDGF/p75 with integrase is lentivirus-specific and promotes DNA binding

The stress oncoprotein LEDGF/p75 interacts with the methyl CpG binding protein MeCP2 and influences its transcriptional activity

Transient and stable knockdown of the integrase cofactor LEDGF/p75 reveals its role in the replication cycle of human immunodeficiency virus

Transportin-SR2 imports HIV into the nucleus

Virus evolution reveals an exclusive role for LEDGF/p75 in chromosomal tethering of HIV.