The discovery and design of novel HIV-1 capsid modulators and future perspectives

D Ding, S Xu, X Zhang, X Jiang, S Cocklin… - Expert opinion on …, 2023 - Taylor & Francis
Introduction Although combination antiretroviral therapy (cART) has achieved significant
success in treating HIV, the emergence of multidrug-resistant viruses and cumulative …

Targeting the virus capsid as a tool to fight RNA viruses

L Hozáková, B Vokatá, T Ruml, P Ulbrich - Viruses, 2022 - mdpi.com
Several strategies have been developed to fight viral infections, not only in humans but also
in animals and plants. Some of them are based on the development of efficient vaccines, to …

Discovery of novel 1, 2, 4‐triazole phenylalanine derivatives targeting an unexplored region within the interprotomer pocket of the HIV capsid protein

X Jiang, PP Sharma, B Rathi, X Ji, L Hu… - Journal of medical …, 2022 - Wiley Online Library
Human immunodeficiency virus (HIV) capsid (CA) protein is a promising target for
developing novel anti‐HIV drugs. Starting from highly anticipated CA inhibitors PF‐74, we …

Nickel-Catalyzed Radical Heck-Type C(sp3)–C(sp2) Coupling Cascades Enabled by Bromoalkane-Directed 1,4-Aryl Shift: Access to Olefinated Arylalanines

J Liu, Y Hong, YL Liu, JY Tan, HM Liu, GL Dai… - Organic …, 2022 - ACS Publications
A bromoalkane-directed radical 1, 4-aryl shift strategy for nickel-catalyzed reductive Heck-
type C (sp3)–C (sp2) coupling cascades of α-amino-β-bromocarboxylic acid esters with α …

Discovery, Crystallographic Studies, and Mechanistic Investigations of Novel Phenylalanine Derivatives Bearing a Quinazolin-4-one Scaffold as Potent HIV Capsid …

S Xu, L Sun, M Barnett, X Zhang, D Ding… - Journal of medicinal …, 2023 - ACS Publications
Optimization of compound 11L led to the identification of novel HIV capsid modulators,
quinazolin-4-one-bearing phenylalanine derivatives, displaying potent antiviral activities …

Discovery and mechanistic investigation of piperazinone phenylalanine derivatives with terminal indole or benzene ring as novel HIV-1 capsid modulators

S Xu, L Sun, WA Zalloum, T Huang, X Zhang, D Ding… - Molecules, 2022 - mdpi.com
HIV-1 capsid (CA) performs multiple roles in the viral life cycle and is a promising target for
antiviral development. In this work, we describe the design, synthesis, assessment of …

Low-molecular-weight anti-HIV-1 agents targeting HIV-1 capsid proteins

T Kobayakawa, M Yokoyama, K Tsuji, M Fujino… - RSC …, 2023 - pubs.rsc.org
The HIV-1 capsid is a shell that encapsulates viral RNA, and forms a conical structure by
assembling oligomers of capsid (CA) proteins. Since the CA proteins are highly conserved …

Design, synthesis, and mechanistic study of 2-pyridone-bearing phenylalanine derivatives as novel HIV capsid modulators

X Zhang, L Sun, S Xu, X Shao, Z Li, D Ding, X Jiang… - Molecules, 2022 - mdpi.com
The AIDS pandemic is still of importance. HIV-1 and HIV-2 are the causative agents of this
pandemic, and in the absence of a viable vaccine, drugs are continually required to provide …

Design, synthesis, and mechanistic study of 2-piperazineone-bearing peptidomimetics as novel HIV capsid modulators

X Zhang, L Sun, S Xu, T Huang, F Zhao… - RSC medicinal …, 2023 - pubs.rsc.org
HIV-1 capsid (CA) is an attractive target for its indispensable roles in the viral life cycle. We
report the design, synthesis, and mechanistic study of a novel series of 2-piperazineone …

HIV-1 capsid inhibitors: A sword to destroy the virus

X Zhang, S Xu, L Sun, D Ding, Y Tao… - Future Medicinal …, 2022 - Taylor & Francis
Conclusion HIV-1 CA has become a hot research target due to its special structure and
function. The recent success of LEN in clinical trials has made medicinal chemists realize …