Benzenesulfonamide Analogs: Synthesis, Anti-GBM Activity and Pharmacoprofiling

Article Medicine, Research & Experimental

GPR17 signaling activation by CHBC agonist induced cell death via modulation of MAPK pathway in glioblastoma

Phung Nguyen et al.

Summary: The study demonstrates that CHBC induces G2/M cell cycle arrest and apoptosis by disrupting MAPK signaling in human glioblastoma cells. CHBC could potentially be a class of compounds for treating glioblastoma.

LIFE SCIENCES (2022)

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Article Pharmacology & Pharmacy

Why 90 % of clinical drug development fails and how to improve it?

Duxin Sun et al.

Summary: Despite the implementation of many successful strategies, the majority of clinical drug development fails. This study suggests that current drug optimization strategies overlook tissue exposure/selectivity, leading to misleading drug candidate selection and impacting clinical efficacy/toxicity balance. The proposed structure-tissue exposure/selectivity-activity relationship (STAR) classification system aims to improve drug optimization and enhance the success rate of clinical drug development.

ACTA PHARMACEUTICA SINICA B (2022)

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Article Chemistry, Multidisciplinary

Chalcogen and Hydrogen Bonds at the Periphery of Arylhydrazone Metal Complexes

Atash Gurbanov et al.

Summary: Ligands with intramolecular RAHB and RAChB were used to form Cu(II), Ag(I), and Cd(II) metal complexes. Despite not directly involving these interactions, both interactions underwent significant changes upon ligand binding to the metal.

CRYSTAL GROWTH & DESIGN (2022)

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Article Biochemistry & Molecular Biology

Transcriptomic analysis of glioblastoma multiforme providing new insights into GPR17 signaling communication

Gnanavel Mutharasu et al.

Summary: In this study, the differential expressions of around 170 genes along with GPR17 have been identified through RNA-Seq analysis of 169 GBM samples. The coordinated expression patterns between these genes and GPR17 were analyzed using gene ontology and protein-protein interaction data. Crucial signaling components and genes related to tumor progression, including GPR17, have been discovered, with GPR17 significantly interacting with about 30 different pathways. Molecular docking experiments showed effective recognition and binding of GPR17 to PX, SH3, and Ig-like domains as well as Gi protein. These findings provide insights into the mechanistic interaction of GPR17 and its potential role in regulating complex GBM signaling networks. Overall, GPR17 mediated signaling networks could serve as a therapeutic target for GBM.

JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS (2022)

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Article Biochemistry & Molecular Biology

TheAutoDocksuite at 30

David S. Goodsell et al.

Summary: The AutoDock suite offers a comprehensive toolset for computational ligand docking and drug design, with specialized tools available for challenging systems. All methods in the suite are freely available, leading to the rapid growth of user and developer communities.

PROTEIN SCIENCE (2021)

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Article Chemistry, Medicinal

Synthesis and Preclinical Validation of Novel Indole Derivatives as a GPR17 Agonist for Glioblastoma Treatment

Phung Nguyen et al.

Summary: The discovery of a novel indoline-derived phenolic Mannich base as an activator of GPR17 shows potential for developing chemotherapeutic agents against GBM. The compound inhibits cAMP and Ca2+ to induce cytotoxic effects on GBM cells, presenting a possible innovative treatment for GBM.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Biochemistry & Molecular Biology