[HTML][HTML] Block-and-lock: new horizons for a cure for HIV-1

I Moranguinho, ST Valente - Viruses, 2020 - mdpi.com
HIV-1/AIDS remains a global public health problem. The world health organization (WHO)
reported at the end of 2019 that 38 million people were living with HIV-1 worldwide, of which …

Shock and kill within the CNS: A promising HIV eradication approach?

MM Nühn, SBH Gumbs, NVEJ Buchholtz… - Journal of Leukocyte …, 2022 - academic.oup.com
The most studied HIV eradication approach is the “shock and kill” strategy, which aims to
reactivate the latent reservoir by latency reversing agents (LRAs) and allowing elimination of …

HIV-1 transcriptional modulation: Novel host factors and prospective therapeutic strategies

QMR Gibaut, LP Mori, ST Valente - Current Opinion in HIV and …, 2023 - journals.lww.com
The HIV-1 latent reservoir is established early after infection, persists during antiretroviral
therapy, and is the source of viral rebound after treatment interruption. An HIV cure requires …

[HTML][HTML] Inhibition of the TRIM24 bromodomain reactivates latent HIV-1

RM Horvath, ZL Brumme, I Sadowski - Scientific Reports, 2023 - nature.com
Expression of the HIV-1 genome by RNA Polymerase II is regulated at multiple steps, as are
most cellular genes, including recruitment of general transcription factors and control of …

An evaluation on the role of non-coding RNA in HIV transcription and latency: a review

PW Ramirez, C Pantoja… - HIV/AIDS-Research and …, 2023 - Taylor & Francis
The existence of latent cellular reservoirs is recognized as the major barrier to an HIV cure.
Reactivating and eliminating “shock and kill” or permanently silencing “block and lock” the …

Total synthesis and biological evaluation of the potent HIV latency-reversing agent Ansellone A and its analogues

M Yanagihara, K Murai, N Kishimoto, T Abe… - Organic …, 2021 - ACS Publications
The total synthesis and biological evaluation of the marine sesterterpenoid ansellone A (1),
an HIV latency-reversing agent, and its analogues are reported. The key to the success of …

[HTML][HTML] Developments in Exploring Fungal Secondary Metabolites as Antiviral Compounds and Advances in HIV-1 Inhibitor Screening Assays

B Nzimande, JP Makhwitine, NP Mkhwanazi, SI Ndlovu - Viruses, 2023 - mdpi.com
The emergence of drug-resistant Human Immunodeficiency Virus-1 strains against anti-HIV
therapies in the clinical pipeline, and the persistence of HIV in cellular reservoirs remains a …

Synthesis and Biological Evaluation of Simplified Ansellone Analogues with Lipophilic Side Chains as HIV Latency‐Reversing Agents

M Yanagihara, N Kishimoto, K Nakahara… - … A European Journal, 2023 - Wiley Online Library
Structurally simplified analogues of ansellone A, in which the decalin skeleton is replaced
with a lipophilic chain, were prepared and their HIV latency‐reversing activities biologically …

Total Synthesis of Ansellone G and Phorbadione

M Yanagihara, K Nakahara, N Kishimoto… - The Journal of …, 2022 - ACS Publications
The first total synthesis of marine sesterterpenoid ansellone G (2) was accomplished. This
strategy utilizes the Prins cyclization reaction of a chloro-substituted homoallyl alcohol to …

Small molecule inhibitors of transcriptional cyclin-dependent kinases impose HIV-1 latency, presenting “block and lock” treatment strategies

RM Horvath, ZL Brumme… - Antimicrobial Agents and …, 2024 - Am Soc Microbiol
Current antiretroviral therapy for HIV-1 infection does not represent a cure for infection as
viral rebound inevitably occurs following discontinuation of treatment. The “block and lock” …