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Chempluschem 2021 Mar 30;86(4):662-673. Epub 2021 Mar 30.

Westfälische Wilhelms-Universität Münster, Institut für Anorganische und Analytische Chemie, Corrensstr. 30, 48149, Münster, Germany.

Guanine quadruplexes are tetra-stranded nucleic acid structures currently raising significant interest in the context of the development of potential anticancer therapeutics with a new mode of action. They are composed of planar guanine tetrads, allowing a high-affinity targeting by using molecules with a large π surface. However, the extreme topological versatility of guanine quadruplexes impedes a straightforward targeting of particular preselected guanine-rich sequences. Read More

Chemistry 2021 Apr 20. Epub 2021 Apr 20.

The University of Texas at Austin, Chemistry, UNITED STATES.

Targeting of low-oxygen (hypoxic) environments found in many tumors using redox-active metal complexes is a strategy that can enhance efficacy and reduce side effects of chemotherapies. We have developed a series of Cu(II) complexes with tridentate pyridine aminophenolate-based ligands for preferential activation in the reduction window provided by hypoxic tissues. Furthermore, ligand functionalization with a CF3 pendant group provides a 19F spectroscopic handle for magnetic resonance studies of redox processes at the metal centre and behaviour in cellular environments. Read More

Biochem Pharmacol 2021 Apr 16:114565. Epub 2021 Apr 16.

KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute, Laboratory of Virology and Chemotherapy, Herestraat 49, 3000 Leuven, Belgium. Electronic address:

The human CC chemokine receptor 8 (CCR8) is a promising drug target for cancer immunotherapy and autoimmune disease. Besides human and viral chemokines, previous studies revealed diverse classes of CCR8-targeting small molecules. We characterized a selection of these CCR8 ligands (hCCL1, vCCL1, ZK756326, AZ6; CCR8 agonists and a naphthalene-sulfonamide-based CCR8 antagonist), in in vitro cell-based assays (hCCL1 binding, calcium mobilization, cellular impedance, cell migration, β-arrestin 1/2 recruitment), and used pharmacological tools to determine G protein-dependent and -independent signaling pathways elicited by these ligands. Read More

J Tradit Complement Med 2021 Apr 12. Epub 2021 Apr 12.

Department of Chemistry, Sardar Vallabhbhai National Institute of Technology (SVNIT), Surat, 395007, Gujarat, India.

Background And Aim: The year 2020 begins with the outbreak of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) that cause the disease COVID-19, and continue till today. As of March 23, 2021, the outbreak has infected 124,313,054 worldwide with a total death of 2,735,707. The use of traditional medicines as an adjuvant therapy with western drugs can lower the fatality rate due to the COVID-19. Read More

Mol Ther Nucleic Acids 2021 Jun 13;24:426-435. Epub 2021 Mar 13.

Center for RNA Nanobiotechnology and Nanomedicine, The Ohio State University, Columbus, OH 43210, USA.

Immunotherapy has become a revolutionary subject in cancer therapy during the past few years. Immune checkpoint-targeting antibodies (Abs) could boost anticancer immune responses. However, certain protein-based immunotherapies revealed side effects and unfavorable biodistribution, so effective non-protein options with lower side effects are highly sought after. Read More