A5065601408- Click Chemistry and Applications
- Cancer, Stress, Anesthesia, and Immune Response
- Adenosine and Purinergic Signaling
- Viral-associated cancers and disorders
- Receptor Mechanisms and Signaling
- Pharmacological Receptor Mechanisms and Effects
- Nanoplatforms for cancer theranostics
- Corneal Surgery and Treatments
- Glaucoma and retinal disorders
- Corneal surgery and disorders
- Protein Degradation and Inhibitors
- Estrogen and related hormone effects
- T-cell and Retrovirus Studies
- Neuropeptides and Animal Physiology
Institute of Molecular and Translational Medicine
2024
Palacký University Olomouc
2022-2024
Abstract INTRODUCTION: The molecular hybridization of three pharmacophores—benzothiazole, cyclobut-2-ene-1, 2-dione, and hydrazone—has led to the development novel compounds with diverse biological activities, including anticancer, anti-inflammatory, antiviral properties. Among these, certain derivatives demonstrated potent selective anticancer activity, particularly in CCRF-CEM HCT116 cell lines. Some also emitted green fluorescence, enabling organelle-specific imaging by fluorescence...
Abstract Introduction: The A3 adenosine receptor (A3AR) is a promising cancer therapy targeted due to its role in tumor progression, immune regulation, and apoptosis. Its selective expression tumors like the liver pancreas makes it ideal for therapies with minimal off-target effects. However, live-cell imaging techniques study A3AR, including expression, membrane localization, interactions AR modulators, are limited. Here, we present CELT-228, an A3AR-specific fluorescent probe, as tool...
Estradiol dimers (EDs) possess significant anticancer activity by targeting tubulin dynamics. In this study, we synthesised 12 EDs variants via copper-catalysed azide-alkyne cycloaddition (CuAAC) reaction, focusing on structural modifications within the aromatic bridge connecting two estradiol moieties. vitro testing of these revealed a marked improvement in selectivity towards cancerous cells, particularly for ED1–8. The most active compounds, ED3 (IC50 = 0.38 μM CCRF-CEM) and ED5 0.71...
Several series of 2,6‐disubstituted 7‐deazapurine ribonucleosides were synthesized to investigate their biological activities. The key‐intermediate chloronucleosides prepared by an anion‐base glycosylation with 2‐amino‐6‐chloro‐7‐deazapurine. target compounds obtained diazotation, either Suzuki and Sonogashira reactions in the case 2‐arylethynyl‐6‐hetaryl nucleosides or two consecutive 2,6‐diaryl nucleosides. sequence diazotation first reaction is flexible can be changed depending on...
Abstract Introduction: Colorectal cancer (CRC) stands as a prominent contributor to global cancer-related mortality. Post-surgical management of CRC patients often involves the administration opioid analgesics. These analgesics operate through and cannabinoid receptors, pathways implicated in tumor progression metastasis, potentially impacting patient survival adversely. This investigation delves into influence piritramide morphine on dissemination, encompassing vitro vivo assessments,...
The global shortage of corneal endothelial graft tissue necessitates the exploration alternative therapeutic strategies. Rho-associated protein kinase inhibitors (ROCKi), recognized for their regenerative potential in cardiology, oncology, and neurology, have shown promise regeneration. This study investigates repurposing additional ROCKi compounds. Through screening a self-assembled library on B4G12 cells, we evaluated dose-dependent effects proliferation, migration, toxicity using...
Abstract Introduction: Adenosine receptors belong to G protein-coupled (GPCRs). There are four types of adenosine (A1, A2A, A2B, and A3). These play roles in several pathological conditions. It has been proven that the A3 receptor (A3AR) is expressed at high densities various tumor cells. Activation this leads, some cases, growth cell proliferation and, other activation apoptotic pathways mediation antiproliferative effects. Therefore A3AR a promising therapeutic target anticancer therapy....
Abstract Introduction: G protein-coupled receptors (GPCRs) are among the most druggable targets. Adenosine (ARs) belong to class A GPCRs. The role of adenosine and ARs in tumorigenesis is increasingly appreciated. Moreover, novel studies also point out pro-tumor anti-tumor effects modulating ARs. Besides A2AR A2BR immune-oncology, A3R was shown be overexpressed tumor tissue play an important cancer. Especially agonists decrease proliferation, induce cell cycle arrest cytotoxicity selectively...