Zebrafish disease models in drug discovery: from preclinical modelling to clinical trials

EE Patton, LI Zon, DM Langenau - Nature Reviews Drug Discovery, 2021 - nature.com
Numerous drug treatments that have recently entered the clinic or clinical trials have their
genesis in zebrafish. Zebrafish are well established for their contribution to developmental …

Imidazoles as potential anticancer agents: An update on recent studies

P Sharma, C LaRosa, J Antwi, R Govindarajan… - Molecules, 2021 - mdpi.com
Nitrogen-containing heterocyclic rings are common structural components of marketed
drugs. Among these heterocycles, imidazole/fused imidazole rings are present in a wide …

Polypharmacology by design: a medicinal chemist's perspective on multitargeting compounds

E Proschak, H Stark, D Merk - Journal of medicinal chemistry, 2018 - ACS Publications
Multitargeting compounds comprising activity on more than a single biological target have
gained remarkable relevance in drug discovery owing to the complexity of multifactorial …

Dual inhibitors of human DNA topoisomerase II and other cancer-related targets

Z Skok, N Zidar, D Kikelj, J Ilaš - Journal of medicinal chemistry, 2019 - ACS Publications
Human DNA topoisomerase II is an important target in anticancer therapy. Despite the
clinical success of drugs that target topoisomerase II, the development of resistant cancer …

Anticancer thiosemicarbazones: chemical properties, interaction with iron metabolism, and resistance development

FS PapeVeronika, A EnyedyÉva… - Antioxidants & redox …, 2019 - liebertpub.com
Significance: During the past decades, thiosemicarbazones were clinically developed for a
variety of diseases, including tuberculosis, viral infections, malaria, and cancer. With regard …

The kinase polypharmacology landscape of clinical PARP inhibitors

AA Antolin, M Ameratunga, U Banerji, PA Clarke… - Scientific reports, 2020 - nature.com
Polypharmacology plays an important role in defining response and adverse effects of
drugs. For some mechanisms, experimentally map** polypharmacology is commonplace …

The BCL-2 inhibitor APG-2575 resets tumor-associated macrophages toward the M1 phenotype, promoting a favorable response to anti-PD-1 therapy via NLRP3 …

F Luo, H Li, W Ma, J Cao, Q Chen, F Lu, M Qiu… - Cellular & Molecular …, 2024 - nature.com
The main challenges in the use of immune checkpoint inhibitors (ICIs) are ascribed to the
immunosuppressive tumor microenvironment and the lack of sufficient infiltration of activated …

Polypharmacological approaches for CNS diseases: focus on endocannabinoid degradation inhibition

A Papa, S Pasquini, C Contri, S Gemma, G Campiani… - Cells, 2022 - mdpi.com
Polypharmacology breaks up the classical paradigm of “one-drug, one target, one disease”
electing multitarget compounds as potential therapeutic tools suitable for the treatment of …

Turning liabilities into opportunities: Off-target based drug repurposing in cancer

V Palve, Y Liao, LLR Rix, U Rix - Seminars in cancer biology, 2021 - Elsevier
Targeted drugs and precision medicine have transformed the landscape of cancer therapy
and significantly improved patient outcomes in many cases. However, as therapies are …

Structural and Molecular Insight into Piperazine and Piperidine Derivatives as Histamine H3 and Sigma-1 Receptor Antagonists with Promising Antinociceptive …

K Szczepańska, S Podlewska, M Dichiara… - ACS chemical …, 2021 - ACS Publications
In an attempt to extend recent studies showing that some clinically evaluated histamine H3
receptor (H3R) antagonists possess nanomolar affinity at sigma-1 receptors (σ1R), we …