Medicinal chemistry strategies for discovering antivirals effective against drug-resistant viruses

Y Ma, E Frutos-Beltrán, D Kang… - Chemical Society …, 2021 - pubs.rsc.org
During the last forty years we have witnessed impressive advances in the field of antiviral
drug discovery culminating with the introduction of therapies able to stop human …

Restriction factors: from intrinsic viral restriction to shaping cellular immunity against HIV-1

M Colomer-Lluch, A Ruiz, A Moris… - Frontiers in …, 2018 - frontiersin.org
Antiviral restriction factors are host cellular proteins that constitute a first line of defense
blocking viral replication and propagation. In addition to interfering at critical steps of the …

Clinical targeting of HIV capsid protein with a long-acting small molecule

JO Link, MS Rhee, WC Tse, J Zheng, JR Somoza… - Nature, 2020 - nature.com
Oral antiretroviral agents provide life-saving treatments for millions of people living with HIV,
and can prevent new infections via pre-exposure prophylaxis,,,–. However, some people …

A highly potent long-acting small-molecule HIV-1 capsid inhibitor with efficacy in a humanized mouse model

SR Yant, A Mulato, D Hansen, WC Tse… - Nature medicine, 2019 - nature.com
People living with HIV (PLWH) have expressed concern about the life-long burden and
stigma associated with taking pills daily and can experience medication fatigue that might …

The capsid lattice engages a bipartite NUP153 motif to mediate nuclear entry of HIV-1 cores

Q Shen, S Kumari, C Xu, S Jang, J Shi… - Proceedings of the …, 2023 - National Acad Sciences
Increasing evidence has suggested that the HIV-1 capsid enters the nucleus in a largely
assembled, intact form. However, not much is known about how the cone-shaped capsid …

New approved drugs appearing in the pharmaceutical market in 2022 featuring fragments of tailor-made amino acids and fluorine

N Wang, H Mei, G Dhawan, W Zhang, J Han… - Molecules, 2023 - mdpi.com
The strategic fluorination of oxidatively vulnerable sites in bioactive compounds is a
relatively recent, widely used approach allowing us to modulate the stability, bio-absorption …

LILAC pilot study: effects of metformin on mTOR activation and HIV reservoir persistence during antiretroviral therapy

D Planas, A Pagliuzza, R Ponte, A Fert… - …, 2021 - thelancet.com
Background Chronic inflammation and residual HIV transcription persist in people living with
HIV (PLWH) receiving antiretroviral therapy (ART), thus increasing the risk of developing …

Ebselen, a small-molecule capsid inhibitor of HIV-1 replication

S Thenin-Houssier, IMS De Vera… - Antimicrobial agents …, 2016 - Am Soc Microbiol
The human immunodeficiency virus type 1 (HIV-1) capsid plays crucial roles in HIV-1
replication and thus represents an excellent drug target. We developed a high-throughput …

HIV-1 capsid variability: viral exploitation and evasion of capsid-binding molecules

A Saito, M Yamashita - Retrovirology, 2021 - Springer
The HIV-1 capsid, a conical shell encasing viral nucleoprotein complexes, is involved in
multiple post-entry processes during viral replication. Many host factors can directly bind to …

Design, synthesis, and mechanism study of benzenesulfonamide-containing phenylalanine derivatives as novel HIV-1 capsid inhibitors with improved antiviral …

L Sun, A Dick, ME Meuser, T Huang… - Journal of medicinal …, 2020 - ACS Publications
The HIV-1 CA protein has gained remarkable attention as a promising therapeutic target for
the development of new antivirals, due to its pivotal roles in HIV-1 replication (structural and …