Article
Biochemistry & Molecular Biology
Sunday N. Okafor, Pavimol Angsantikul, Hashim Ahmed
Summary: This research utilized computational tools to screen a large compound library and identified potential HIV-1 protease inhibitors. Two optimized molecules showed promising activity and should be further investigated in vitro and in clinical trials.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Pharmacology & Pharmacy
Matthew Weichseldorfer, Marvin Reitz, Olga S. Latinovic
Summary: Combined antiretroviral therapy (cART) is widely recommended for controlling HIV-1 replication and improving the quality of life of infected individuals. However, latent infected cells remain a major barrier to treatment efficacy in the long term.
Article
Biochemistry & Molecular Biology
Roberto Arrigoni, Luigi Santacroce, Andrea Ballini, Luigi Leonardo Palese
Summary: The availability of drugs capable of blocking microorganism replication is a major accomplishment in medicine, but the increasing number of resistant strains poses a significant challenge for infectious disease treatment. Therefore, the search for new potential ligands for pathogens' life cycle is a crucial research area today.
Article
Biochemistry & Molecular Biology
Sunday N. Okafor, Abigail Meyer, Jay Gadsden, Fadi Ahmed, Lilian Guzman, Hashim Ahmed, Jose A. Fernandez Romero, Pavimol Angsantikul
Summary: This study screened FDA-approved and investigational drugs for their potential as HIV-1 protease inhibitors. The findings revealed that CBR003PS and CBR013PS exhibited significant binding affinity to the HIV-1 protease with high stability, showing potential for repurposing as HIV-1 protease inhibitors.
Review
Pharmacology & Pharmacy
Violet Dismas Kajogoo, Mary Gorret Atim, Demeke Amare, Melka Geleta, Yilkal Muchie, Hanna Amanuel Tesfahunei, Willyhelmina Olomi, Joan Acam, Tsegahun Manyazewal
Summary: This study analyzed the impact of Protease Inhibitors (PIs) on insulin sensitivity and the onset of diabetes mellitus (DM) in HIV patients. The results showed that among PIs, atazanavir, fosamprenavir, and darunavir did not demonstrate significant changes in insulin sensitivity.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Urology & Nephrology
Zunaid Barday, Kathryn Manning, Robert Freercks, Laurie Bertels, Nicola Wearne, Elmi Muller
Summary: Managing the interaction between ART and CNI immunosuppression in HIV-positive kidney transplant recipients is challenging. This study retrospectively analyzed ART regimen switches in 53 patients and found that PI-based regimen may be associated with increased rejection rates.
KIDNEY INTERNATIONAL REPORTS
(2022)
Article
Infectious Diseases
Leonardo Calza, Isabella Bon, Marina Tadolini, Marco Borderi, Vincenzo Colangeli, Lorenzo Badia, Gabriella Verucchi, Giada Rossini, Caterina Vocale, Paolo Gaibani, Pierluigi Viale, Luciano Attard
Summary: The study reported a case series of 26 HIV-infected patients with COVID-19 diagnosed at S.Orsola Hospital in Italy. Among them, 19 were male, with a median age of 54 years, and 73% had one or more comorbidities. Only 5 patients with interstitial pneumonia were hospitalized, and there were no ICU admissions or deaths.
Review
Pharmacology & Pharmacy
Srinivas Reddy Jitta, Salwa, Navya Ajitkumar Bhaskaran, Shirleen Miriam Marques, Lalit Kumar
Summary: This article reviews the adverse effects of Ritonavir and recent approaches in the development of nanoformulations. It also discusses the patents filed on Ritonavir. While most research focuses on enhancing the solubility and oral bioavailability of the drug, researchers should also consider toxicity evaluation during formulation development.
EXPERT OPINION ON DRUG DELIVERY
(2022)
Article
Chemistry, Medicinal
Gordon J. Lockbaum, Linah N. Rusere, Mina Henes, Klajdi Kosovrasti, Desaboini Nageswara Rao, Ean Spielvogel, Sook-Kyung Lee, Ellen A. Nalivaika, Ronald Swanstrom, Nese Kurt Yilmaz, Celia A. Schiffer, Akbar Ali
Summary: Protease inhibitors are powerful antivirals against HIV-1, but their effectiveness is reduced against resistant variants. Enhancing resistance profiles is crucial for developing more robust inhibitors, which could be promising for simplified next-generation antiretroviral therapies.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Infectious Diseases
Frank Mulindwa, Barbara Castelnuovo, Bruce Kirenga, Dennis Kalibbala, Priscilla Haguma, Martin Muddu, Fred C. Semitala
Summary: Despite the low utilization of double dose LPV/r in HIV patients on rifampicin-based TB treatment in Uganda's public HIV clinics, it does not seem to impact patient survival and viral suppression.
BMC INFECTIOUS DISEASES
(2021)
Article
Oncology
Soyeong Park, Andrew Auyeung, Denis L. Lee, Paul F. Lambert, Evie H. Carchman, Nathan M. Sherer
Summary: High-risk strains of human papillomavirus (HPV), such as HPV16, cause various cancers, including cervical cancer, which is a major cause of death for women globally. Anti-HPV vaccines are available but do not treat existing infections. Current treatments for HPV-associated cancers have side effects on healthy tissues, prompting the need for better targeted therapies. The study found that HIV protease inhibitors can selectively deplete HPV16 oncoproteins, suggesting their potential for treating HPV16-driven cancers.
Article
Biochemistry & Molecular Biology
Kolin M. Clark, Josh G. Kim, Qiankun Wang, Hongbo Gao, Rachel M. Presti, Liang Shan
Summary: The sensitization of the CARD8 inflammasome to non-nucleoside reverse transcriptase inhibitors (NNRTIs) can be achieved through chemical inhibition of the negative regulator DPP9. The DPP9 inhibitor Val-boroPro (VbP) can kill HIV-1-infected cells without NNRTIs and synergize with NNRTIs to promote clearance of infected cells. This offers a promising strategy for enhancing NNRTI efficacy in eliminating HIV-1 reservoirs.
NATURE CHEMICAL BIOLOGY
(2023)
Review
Cell Biology
Athanasios-Dimitrios Bakasis, Theodoros Androutsakos
Summary: Since the introduction of ART in 1996, the lifespan of PLWH has increased and the major causes of mortality have shifted towards cardiovascular and liver diseases. HIV itself and various liver diseases may contribute to liver damage and subsequent LF in PLWH. Among ART drug classes, nucleoside reverse transcriptase inhibitors, especially didanosine and zidovudine, appear to pose the greatest risk for LF.
Review
Virology
Irene T. Weber, Yuan-Fang Wang, Robert W. Harrison
Summary: The HIV protease is a key target for antiviral therapy, but drug resistance poses a growing threat. Dr. Stephen Oroszlan's contributions to understanding the function of the HIV protease and the development of clinical inhibitors are highlighted. Drug-resistant protease variants serve as valuable models for studying resistance mechanisms and evolution.
Article
Multidisciplinary Sciences
Min Hi Park, Jeffrey L. Suhalim, Firas Elmastour, Santu K. Singha, Tadashi Imafuku, Ramanathan Venkatnarayan, Anette Christ, Alena Grebe, Sarah A. Oppelt, Dmitri Sviridov, Michael Bukrinsky, Eicke Latz, Eric O. Potma, Michael L. Fitzgerald
Summary: This study used non-linear optical microscopy to investigate plaque crystal structure and composition in SIV-infected macaques, revealing a cholesterol ester dominated composition. The findings help clarify the evolution of plaque core lipid and its role in systemic inflammation.