Atom-based 3D-QSAR, molecular docking, DFT, and simulation studies of acylhydrazone, hydrazine, and diazene derivatives as IN-LEDGF/p75 inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Structural Chemistry"
DOI: 10.1007/s11224-020-01628-3
Abstract: Since HIV-1 integrase makes use of host genome machinery to accomplish the replication process, where LEDGF/p75 (a cellular cofactor) executes in the lentiviral integration process by interacting with integrase. Thus, the integrase-LEDGF/p75 interaction has become… read more here.
Keywords: hydrazine diazene; atom based; diazene derivatives; ledgf p75 ... See more keywords
Molecular Mechanism of LEDGF/p75 Dimerization.
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DOI: 10.1016/j.str.2020.08.012
Abstract: Dimerization of many eukaryotic transcription regulatory factors is critical for their function. Regulatory role of an epigenetic reader lens epithelium-derived growth factor/p75 (LEDGF/p75) requires at least two copies of this protein to overcome the nucleosome-induced… read more here.
Keywords: dimerization; ledgf p75; p75 dimerization; mechanism ... See more keywords
Targeted editing of the PSIP1 gene encoding LEDGF/p75 protects cells against HIV infection
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DOI: 10.1038/s41598-019-38718-0
Abstract: To fulfill a productive infection cycle the human immunodeficiency virus (HIV) relies on host-cell factors. Interference with these co-factors holds great promise in protecting cells against HIV infection. LEDGF/p75, encoded by the PSIP1 gene, is… read more here.
Keywords: ledgf p75; hiv infection; p75; cells hiv ... See more keywords
Evaluation of a flavonoid library for inhibition of interaction of HIV-1 integrase with human LEDGF/p75 towards a structure–activity relationship
Sign Up to like & getrecommendations! Published in 2022 at "Annals of Medicine"
DOI: 10.1080/07853890.2022.2081869
Abstract: Abstract Background: Proteinśprotein interaction (PPI) between lens epithelium-derived growth factor (LEDGF/p75) and human immunodeficiency virus (HIV) integrase (IN) becomes an attractive target for anti-HIV drug development. Methods: The blockade of this interaction by small molecules… read more here.
Keywords: p75 interaction; interaction; hiv integrase; ledgf p75 ... See more keywords
Quinoline-based Protein-protein Interaction Inhibitors of LEDGF/p75 and HIV Integrase: An In Silico Study.
Sign Up to like & getrecommendations! Published in 2018 at "Current topics in medicinal chemistry"
DOI: 10.2174/1568026619666190208164801
Abstract: The failure of the Integrase Strand Transfer Inhibitors (INSTIs) due to the mutations occurring at the catalytic site of HIV integrase (IN) has led to the design of allosteric integrase inhibitors (ALLINIs). Lens epithelium derived… read more here.
Keywords: protein; interaction inhibitors; protein protein; ledgf p75 ... See more keywords
LEDGF/p75 Is Required for an Efficient DNA Damage Response
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DOI: 10.3390/ijms22115866
Abstract: Lens epithelium-derived growth factor splice variant of 75 kDa (LEDGF/p75) plays an important role in cancer, but its DNA-damage repair (DDR)-related implications are still not completely understood. Different LEDGF model cell lines were generated: a… read more here.
Keywords: ledgf; ledgf p75; dna damage; ddr ... See more keywords
Allosteric Integrase Inhibitor Influences on HIV-1 Integration and Roles of LEDGF/p75 and HDGFL2 Host Factors
Sign Up to like & getrecommendations! Published in 2022 at "Viruses"
DOI: 10.3390/v14091883
Abstract: Allosteric integrase (IN) inhibitors (ALLINIs), which are promising preclinical compounds that engage the lens epithelium-derived growth factor (LEDGF)/p75 binding site on IN, can inhibit different aspects of human immunodeficiency virus 1 (HIV-1) replication. During the… read more here.
Keywords: allosteric integrase; hdgfl2; integration; roles ledgf ... See more keywords