Related Experiment Video
Updated: Mar 30, 2026
11:10
Genotypic Inference of HIV-1 Tropism Using Population-based Sequencing of V3
Published on: December 27, 2010
12.9K
Core chemotype diversification in the HIV-1 entry inhibitor class using field-based bioisosteric replacement
Marina Tuyishime1, Rae Lawrence2, Simon Cocklin1
1Department of Biochemistry & Molecular Biology, Drexel University College of Medicine, Rooms 10302-10306, 245 N. 15th Street, Philadelphia, PA 19102, USA.
Bioorganic & Medicinal Chemistry Letters
|November 5, 2015
Summary
New HIV-1 entry inhibitors were developed using bioisosteric replacements. Field-based analysis revealed 3D structure-activity relationships to guide future drug development for HIV-1 replication inhibition.
Area of Science:
- Medicinal Chemistry
- Virology
- Drug Discovery
Background:
- Human immunodeficiency virus type 1 (HIV-1) replication remains a target for therapeutic intervention.
- Inhibiting HIV-1 entry into host cells is a promising strategy for developing new antiviral treatments.
Purpose of the Study:
- To expand the range of chemical structures (chemotypes) for HIV-1 entry inhibitors.
- To establish three-dimensional structure-activity relationships (3D-SAR) for guiding further optimization of these inhibitors.
Main Methods:
- Employed field-based bioisosteric replacements to generate novel compound structures.
- Utilized field-based disparity analysis to investigate the relationship between compound structure and inhibitory activity.
Main Results:
- Successfully extended the diversity of chemotypes within the HIV-1 entry inhibitor class.
- Derived crucial 3D structure-activity relationships based on the analyzed compounds.
Conclusions:
- The developed compounds and identified 3D-SAR provide a foundation for advancing HIV-1 entry inhibitors.
- These findings contribute to the ongoing effort to discover clinically useful drugs against HIV-1 replication.
Related Concept Videos
01:10Retrovirus Life Cycles
50.6K
Retroviruses have a single-stranded RNA genome that undergoes a special form of replication. Once the retrovirus has entered the host cell, an enzyme called reverse transcriptase synthesizes double-stranded DNA from the retroviral RNA genome. This DNA copy of the genome is then integrated into the host’s genome inside the nucleus via an enzyme called integrase. Consequently, the retroviral genome is transcribed into RNA whenever the host’s genome is transcribed, allowing the...
50.6K
02:53Conservative Site-specific Recombination and Phase Variation
7.3K
Because the DNA segments are cut and reorganized in a direction-specific manner, site-specific recombination has emerged as an efficient genetic engineering technique. Flippase and Cyclization recombinases or Flp and Cre, respectively, are two members of the tyrosine recombinase family derived from bacteriophages, that are used to mediate site-specific DNA insertions, deletions, and targeted expression of proteins in mammalian cell lines.
The recognition sites for Cre recombinase called LoxP...
The recognition sites for Cre recombinase called LoxP...
7.3K
01:28Diversity of Antigen Receptors
2.1K
Antigen receptors are essential components of the immune system crucial in defending the body against foreign invaders. These receptors are present on the surface of B and T cells, enabling them to recognize antigens and mount an appropriate immune response.
Before encountering any antigen, lymphocytes express these receptors. On B cells, the antigen receptor is a membrane-bound antibody molecule called BCR; on T cells, it is a T cell receptor or TCR. B and T cell receptors are composed of two...
Before encountering any antigen, lymphocytes express these receptors. On B cells, the antigen receptor is a membrane-bound antibody molecule called BCR; on T cells, it is a T cell receptor or TCR. B and T cell receptors are composed of two...
2.1K