The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.
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DOI: 10.1021/acs.jmedchem.2c00879
Abstract: GSK3640254 is an HIV-1 maturation inhibitor (MI) that exhibits significantly improved antiviral activity toward a range of clinically relevant polymorphic variants with reduced sensitivity toward the second-generation MI GSK3532795 (BMS-955176). The key structural difference between… read more here.
Keywords: generation; gsk3640254; inhibitor; hiv maturation ... See more keywords
Synthesis, Structure-Activity Relationships, and In Vivo Evaluation of Novel C-17 Amine Derivatives Based on GSK3640254 as HIV-1 Maturation Inhibitors with Broad Spectrum Activity.
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DOI: 10.1021/acs.jmedchem.2c01618
Abstract: An investigation of the structure-activity relationships of a series of HIV-1 maturation inhibitors (MIs) based on GSK3640254 (4) was conducted by incorporating novel C-17 amine substituents to reduce the overall basicity of the resultant analogues.… read more here.
Keywords: maturation inhibitors; structure activity; based gsk3640254; activity ... See more keywords
Structural changes in HIV maturation
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DOI: 10.1126/science.373.6555.637-h
Abstract: Structural Biology Nascent HIV particles assemble at the plasma membrane of an infected cell and bud into a membrane-enveloped, immature virion. Assembly and budding are driven by a polyprotein called Gag, which consists of a… read more here.
Keywords: structural changes; hiv maturation; science; biology ... See more keywords
QSAR-Based Design of The More Potent Betulinic Acid Derivatives as HIV Maturation Inhibitor
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DOI: 10.12982/cmujns.2021.010
Abstract: In this study, we make QSAR models from 29 of BA derivatives’ HIV maturation inhibition activities against their 3D descriptors. The best model involve 5 descriptors as follows: 1/log EC50 = -462.275 + (69.213 ×… read more here.
Keywords: hiv maturation; derivatives hiv; acid; qsar based ... See more keywords