A5022097807- Viral-associated cancers and disorders
- Antimicrobial Peptides and Activities
- Cytomegalovirus and herpesvirus research
- Bacterial biofilms and quorum sensing
- Biochemical and Structural Characterization
- Lymphoma Diagnosis and Treatment
- Herpesvirus Infections and Treatments
- HIV/AIDS drug development and treatment
- Antibiotic Resistance in Bacteria
- HIV Research and Treatment
Helmholtz Institute for Pharmaceutical Research Saarland
2020-2023
Saarland University
2020-2023
German Center for Infection Research
2020-2023
Helmholtz Centre for Infection Research
2020-2021
Abstract Pseudomonas aeruginosa (PA) infections can be notoriously difficult to treat and are often accompanied by the development of antimicrobial resistance (AMR). Quorum sensing inhibitors (QSI) acting on PqsR (MvfR) – a crucial transcriptional regulator serving major functions in PA virulence enhance antibiotic efficacy eventually prevent AMR. An integrated drug discovery campaign including design, medicinal chemistry‐driven hit‐to‐lead optimization in‐depth biological profiling new QSI...
Kaposi's sarcoma-associated herpesvirus (KSHV) can establish latent lifelong infections in infected individuals. During viral latency, the latency-associated nuclear antigen (LANA) mediates replication of genome dividing cells and tethers them to mitotic chromosomes, thus ensuring their partitioning into daughter during mitosis. This study aims inhibit by targeting LANA-DNA interaction using small molecular entities. Drawing from first-generation inhibitors growth vectors identified through...
The Latency-associated nuclear antigen (LANA) plays a central role for the latent persistence of Kaposi's Sarcoma Herpesvirus (KSHV) in human host and helps to establish lifelong infections. Herein, we report our efforts towards hit-to-lead generation starting from previously discovered LANA-DNA inhibitor. By tethering viral genome nucleosomes, LANA ensures segregation DNA during mitosis. is also required replication episome S phase cell cycle. We aim inhibit interaction between prevent KSHV...
The Kaposi sarcoma-associated herpesvirus (KSHV) is an oncogenic human herpesviruses that responsible for cancer, especially in immunosuppressed people, such as patients with AIDS. So far, there are no KSHV-specifc antiviral agents available. In this review, we provide overview on one particular target-centered approach toward novel anti-KSHV drugs focusing interfering the molecular functions of latency-associated nuclear antigen (LANA). This review focuses attempts to interfere LANA-DNA...
In article number 2004369, Martin Empting and colleagues describe a new generation of dual-loaded nanoparticles enabling efficient eradication Pseudomonas aeruginosa biofilms. The squalene-based nanocarrier facilitates co-delivery novel pathogenspecific Quorum Sensing Inhibitor (QSI) together with the standard-of-care antibiotic tobramycin. QSI itself shows high anti-virulence efficacy, favorable DMPK no overt safety pharmacology. When applied as nanoparticle formulation potentiates biofilm...