adenosine-5--(n-ethylcarboxamide) and Neoplasms

In the past few decades, the development of heat shock protein 90 (Hsp90) inhibitors for cancer treatment has not stopped. About twenty compounds have been evaluated in the clinical trials, but the FDA approved none of them because of toxic effects and/or not enough efficacies. Insufficient isoform selectivity has been considered as one of the reasons for these failures recently. Therefore, developing isoform-selective Hsp90 inhibitors could probably make great progress in searching for therapeutic agents for cancer as well as many other diseases. Here, we summarized classic pan-inhibitors of Hsp90 based on the classification of binding sites and illustrated design strategies applied in the drug discovery. We summed up current isoform-specific Hsp90 inhibitors including their discovery processes and potential indications.

Topics: Antineoplastic Agents; Binding Sites; HSP90 Heat-Shock Proteins; Humans; Neoplasms; Protein Isoforms

In recent years, the adenosine A

Topics: Adenosine; Adenosine A2 Receptor Antagonists; Adenosine-5'-(N-ethylcarboxamide); Immunotherapy; Neoplasms; Receptor, Adenosine A2A

The adenosine A

Topics: Adenosine; Adenosine-5'-(N-ethylcarboxamide); HEK293 Cells; Humans; Ligands; Mutation; Neoplasms; Receptor, Adenosine A2A; Tumor Microenvironment

In cancer, G protein-coupled receptors (GPCRs) are involved in tumor progression and metastasis. In this study we particularly examined one GPCR, the adenosine A

Topics: Adenosine A2 Receptor Agonists; Adenosine-5'-(N-ethylcarboxamide); Aminopyridines; Computational Biology; Humans; Models, Molecular; Mutation; Neoplasms; Receptor, Adenosine A2B; Saccharomyces cerevisiae

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain cancer. However, the complete repertoire of signaling pathways that governs the proliferation and self-renewal of NSCs, which we refer to as the 'ground state', remains largely uncharacterized. Although the candidate gene approach has uncovered vital pathways in NSC biology, so far only a few highly studied pathways have been investigated. Based on the intimate relationship between NSC self-renewal and neurosphere proliferation, we undertook a chemical genetic screen for inhibitors of neurosphere proliferation in order to probe the operational circuitry of the NSC. The screen recovered small molecules known to affect neurotransmission pathways previously thought to operate primarily in the mature central nervous system; these compounds also had potent inhibitory effects on cultures enriched for brain cancer stem cells. These results suggest that clinically approved neuromodulators may remodel the mature central nervous system and find application in the treatment of brain cancer.

Topics: Animals; Cell Survival; Cells, Cultured; Mice; Molecular Structure; Neoplasms; Neurons; Pharmaceutical Preparations; Sensitivity and Specificity; Stem Cells