Protease Inhibitors for the Treatment of HIV/AIDS: Recent Advances and Future Challenges.

@article{Voshavar2019ProteaseIF,
  title={Protease Inhibitors for the Treatment of HIV/AIDS: Recent Advances and Future Challenges.},
  author={Chandrashekhar Voshavar},
  journal={Current topics in medicinal chemistry},
  year={2019}
}
Acquired Immunodeficiency Syndrome (AIDS) is a chronic disease characterized by multiple life-threatening illnesses caused by a retro-virus, Human Immunodeficiency Virus (HIV). HIV infection slowly destroys the immune system and increasing the risk of various other infections and diseases. Although there is no immediate cure for HIV infection/AIDS, several drugs targeting various cruxes of HIV infection are used to slow down the progress of the disease and to boost the immune system. One of the… 
View on PubMed
doi.org
33 Citations
Highly Influential Citations
3
Background Citations
12
Methods Citations
2

33 Citations

Recent Developments in the Medicinal Chemistry for New Small-Molecule Therapeutics to Treat HIV-AIDS.

The advancement of antiretroviral therapy over the years, their limitations and development of novel drug formulations or regimen to address the limitations has been outlined in details.

The anti-HIV potential of imidazole, oxazole and thiazole hybrids: A mini-review

Current scenario on non-nucleoside reverse transcriptase inhibitors (2018-present)

Pharmacokinetic Parameters of HIV‐1 Protease Inhibitors

The pharmacokinetic properties of current PIs, the changes when pharmacological boosters are used and also lists the major mutations to help understanding of how long the continuous treatment can ensure a low viral load in patients are summarized.

Modern Solutions in the Treatment of HIV: From Antiretroviral Drug Therapy to Human Genome Editing

Due to its simplicity, convenience, efficiency and cost-effectiveness, CRISPR/Cas has found application in a short period of time in a wide variety of fields of fundamental and applied medicine and biotechnology.

Off-Target-Based Design of Selective HIV-1 PROTEASE Inhibitors

A new mixed-hierarchical, ligand-structure-based protocol, centered on an on/off-target approach, to identify the new selective inhibitors of HIV-1 PR, could represent a reliable help in the research of new selective targeted small molecules, permitting to design new agents without undesirable interactions.

Adaptive Mutation in the Main Protease Cleavage Site of Feline Coronavirus Renders the Virus More Resistant to Main Protease Inhibitors

The research explains the evolutionary characteristics of coronaviruses under antiviral drugs, which is helpful for a more comprehensive understanding of the molecular basis of virus resistance and provides important basic data for the effective prevention and control of CoVs.

Single-Agent and Fixed-Dose Combination HIV-1 Protease Inhibitor Drugs in Fission Yeast (Schizosaccharomyces pombe)

Results of this study show that fission yeast is a reliable cell-based system for the discovery and testing of HIV PIs and further demonstrate the need for new PI drugs against viral multi-PI resistance.

Development of A Fission Yeast Cell-based Platform for High Throughput Screening of HIV-1 Protease Inhibitors.

A fission yeast cell-based HTS platform that is suitable for high throughput screening (HTS) of small molecules against HIV-1 protease (PR) and to exclude all hidden nmt1 inhibitors is successfully developed.

Molecular Mechanisms of HIV Protease Inhibitors Against HPV-Associated Cervical Cancer: Restoration of TP53 Tumour Suppressor Activities

The role players, such as HPV oncoproteins involved cervical cancer development and how they are targeted in HIV protease inhibitors-induced p53 restoration in cervical cancer are evaluated.

References

SHOWING 1-10 OF 278 REFERENCES

HAART in HIV/AIDS Treatments: Future Trends.

The major progresses and drawbacks of HIV/AIDS chemotherapy (HAART) to HIV/ AIDS patients have been discussed and future trends (updating pathogenesis study, next generations of drug developments, new drug target discovery, different scientific disciplinary and so on) are highlighted.

HIV-1 protease: mechanism and drug discovery.

In this review, studies conducted in the last two decades on the mechanism of HIV PR and the impact of their conclusions on the drug discovery processes are summarized.

The Continuing Evolution of HIV-1 Therapy: Identification and Development of Novel Antiretroviral Agents Targeting Viral and Cellular Targets

The difficult treatment regimens, the presence of class-specific drug toxicities, and the emergence of drug-resistant virus isolates highlight the fact that improvements in therapeutic regimens and the identification of new and novel viral and cellular targets for therapy are still necessary.

HIV-1 antiretroviral drug therapy.

  • E. ArtsD. Hazuda
  • Biology, Medicine
    Cold Spring Harbor perspectives in medicine
  • 2012
The basic principles of antiretroviral drug therapy, the mode of drug action, and the factors leading to treatment failure are reviewed (i.e., drug resistance).

Atazanavir: a novel HIV-1 protease inhibitor

  • P. Piliero
  • Biology, Chemistry
    Expert opinion on investigational drugs
  • 2002
Atazanavir (formerly BMS-232632), a novel azapeptide protease inhibitor, is a potent protease inhibition that is not associated with significant dyslipidaemia as seen with other protease inhibitors.

HIV drug resistance and viral fitness.

Antiretroviral drugs

The clinical effectiveness of antiretroviral therapy has improved markedly over the last few years. Since 1996 in the developed world there have been dramatic falls in the incidence of new AIDS cases…

Resilience to resistance of HIV-1 protease inhibitors: profile of darunavir.

Darunavir has a higher genetic barrier to the development of resistance and better clinical efficacy against multidrug-resistant HIV relative to current protease inhibitors and is an important new therapeutic option for HIV-infected patients.

Targeting the HIV-protease in AIDS therapy: a current clinical perspective.

In vivo emergence of HIV-1 variants resistant to multiple protease inhibitors

Five resistant variants isolated from patients undergoing therapy with the protease inhibitor MK-639 exhibited cross-resistance to all members of a panel of six structurally diverse protease inhibitors, suggesting that com-bination therapy with multiple protease inhibition may not prevent loss of antiviral activity resulting from resistance selection.
...