Combination antiretroviral therapy (cART) has been demonstrated to effectively inhibit the ongoing replication of human immunodeficiency virus type 1 (HIV-1), and significantly improve health outcomes in patients of acquired immunodeficiency syndrome (AIDS). There are approximately 50 approved HIV drugs currently on the market that can be used as part of a personalized treatment plan, and they form seven major drug classes based on viral targets and active substances. Different drugs act at different stages of the HIV life cycle, for example, some of them prevent the virus from entering immune system cells and some are able to block the enzymes that HIV needs to replicate-reverse transcriptase, protease and integrase. The advanced cART approach incorporates several drugs with different activities into the HIV treatment regimen to prevent the patient's infection and its progression to AIDS. Over the years, this multidrug strategy has become highly effective and available, successfully improving the quality of life of HIV-positive individuals.
BOC Sciences has delivered its anti-HIV screening library which is helpful for antiretroviral study.
Figure 1. The screening system used for the detection of the anti-HIV gene A human leukocyte cDNA library. (Strul, A.; Arber, N. 2002)
Anti-HIV Screening Library Design
- HIV Focused Library
Aiming to cover over 16,800 drug-like screening compounds with potential antiretroviral activity, we employ a 2D fingerprint similarity approach to design this library
- The reference compound set is selected from a large number of commercial databases
- The carefully selected molecules constitute target-specific HIV inhibitors such as: targeting HIV-associated proteins, cell lines or whole viruses
- Compounds are selected by applying a 75% similarity cut-off (Tanimoto)
- Among the selected compounds, the following potential inhibitors of HIV-specific molecular targets are present:
- Aberrant vpr protein
- HIV1 protease
- Anti-repression transactivator
- HIV1 reverse transcriptase
- Envelope glycoprotein gp160
- HIV1 Tat protein
- Envelope polyprotein GP160
- HIV1 enhancer-binding protein 1
- HIV1 integrase
- HIV Protease Library
HIV protease is an enzyme that participates in the infection process by splitting proteins into smaller units and using them to produce the mature protein components of infectious HIV virus particles. Inhibition of HIV protease can disrupt the ability of the retrovirus to replicate and infect other cells
At BOC Sciences, 2D similarity search (Tanimoto's 75% similarity cut-off) is used to select small molecule compounds for potential HIV protease inhibitors
- HIV Reverse Transcriptase Library
Retrovir uses HIV reverse transcriptase for self-replication, and this enzyme enables to catalyze the conversion of single-stranded viral RNA into proviral DNA, which further infects host cell DNA. Inhibition of HIV reverse transcriptase is one of the important method used to hinder the virus replication. Corresponding targeted drugs will exclude the reverse transcriptase from the infection process by blocking or altering its structure
BOC Sciences HIV reverse transcriptase library includes 2,100 compounds identified by 2D similarity search, demonstrating it has potential as HIV reverse transcriptase inhibitors
Anti-HIV Screening Library Characteristics
- No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
- Bioactivity and safety confirmed by preclinical studies and clinical trials
- Structural diversity, medicinal activity, and cellular penetration
- Structural document, IC50, and other chemical and biological data are provided
- All compounds are continually updated
- Compound cherry-picking service is provided
What We Deliver
- Delivered within 2 weeks in any customer-preferred format
- Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
- All compounds have a minimum purity of 90% assessed by 1H NMR and HPLC
- Analytical data is provided
BOC Sciences provides professional, rapid and high-quality services of Anti-HIV Screening Library design at competitive prices for global customers. Personalized and customized services of Anti-HIV Screening Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!
Reference
- Strul, A.; Arber, N. Strul H, Arber NFecal occult blood test for colorectal cancer screening. Annals of Oncology. 2002. 13(1): 51-56.
